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Zeitschrift

Zeitschrift für Naturforschung C

A Journal of Biosciences

Editor-in-Chief: Jürgen Seibel
Wissenschaftlicher Beirat: Achim Aigner , Wilhelm Boland , Uwe Bornscheuer und Klaus Hoffmann

Sprache: Englisch

Erstveröffentlichung: 20. Februar 1973

Erscheinungsweise: 12 Hefte pro Jahr

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Über diese Zeitschrift

Objective

A Journal of Biosciences: Zeitschrift für Naturforschung C (ZNC) is an international scientific journal and a community resource for the emerging field of natural and natural-like products.

The journal publishes original research on the isolation (including structure elucidation), bio-chemical synthesis and bioactivities of natural products, their biochemistry, pharmacology, biotechnology, and their biological activity and innovative developed computational methods for predicting the structure and/or function of natural products.

A Journal of Biosciences: Zeitschrift für Naturforschung C (ZNC) welcomes research papers in fields on the chemistry-biology boundary which address scientific ideas and approaches to generate and understand natural compounds on a molecular level and/or use them to stimulate and manipulate biological processes.

Topics

Bio-chemical synthesis and bioactivities of natural products
Isolation (including structure elucidation)
Biochemistry
Biotechnology
Pharmacology
Chemistry
Biology

Article formats

Original research articles, rapid communications, letters and review articles

Please have a look at the call for papers for two upcoming Special Issues:

Ihre Vorteile

Zeitschrift für Naturforschung C – A Journal of Biosciences is proud to announce a new feature, the Editor’s Choice free access article. To download the featured article free of charge, please click the link below.

Vol. 76, Iss. 3-4: Design and synthesis of novel n-butyphthalide derivatives as promising botanical fungicides by Zhongfu Luo, Yu Deng, Bilan Luo, Yong Li, Qing Lan, Judi Fan, Wei Xue, Lei Tang and Lingling Fan

Vol. 76, Iss. 3-4: Synergistic antibacterial combination of Lavandula latifolia Medik. essential oil with camphor by Nursenem Karaca, Görkem Şener, Betül Demirci and Fatih Demirci

Vol. 76, Iss. 1-2: Gas chromatography coupled to mass spectrometry (GC-MS) characterization and evaluation of antibacterial bioactivities of the essential oils from Piper arboreum Aubl., Piper aduncum L. e Piper gaudichaudianum Kunth by Ana Cristina A. da Silva, Edinardo F. F. Matias, Janaína E. Rocha, Ana Carolina Justino de Araújo, Thiago S. de Freitas, Fábia F. Campina, Maria do S. Costa, Luiz E. Silva, Wanderlei do Amaral, Beatriz Helena L. N. S. Maia, Aurea P. Ferriani, Camila F. Bezerra, Marcello Iriti and Henrique D. M. Coutinho

Vol. 76, Iss. 1-2: Ethyl acetate extract from Cistus x incanus L. leaves enriched in myricetin and quercetin derivatives, inhibits inflammatory mediators and activates Nrf2/HO-1 pathway in LPS-stimulated RAW 264.7 macrophages by Mario D’Ambrosio, Elisabetta Bigagli, Lorenzo Cinci, Antonella Gori, Cecilia Brunetti, Francesco Ferrini and Cristina Luceri

Vol. 75, Iss. 11-12: Modulation of antibiotic resistance by the essential oil of Ocimum gratissimum L. in association with light-emitting diodes (LED) lights by Maria Karollyna do N. Silva Leandro, Janaína E. Rocha, Camila F. Bezerra, Priscilla R. Freitas, Jessica Horana F. Feitosa, Viviane B. Bezerra, Rizelle de O. Barros, Livia Maria G. Leandro, José Junior dos S. Aguiar, Paulo S. Pereira, Marcela Christofoli, Jaime Ribeiro-Filho, Marcello Iriti, Henrique Douglas M. Coutinho and Edinardo Fagner F. Matias

Vol. 78, Iss. 3-4: Special Issue on Organic Chemistry and Medicinal Applications

Vol. 75, Iss. 7-8: Special Issue on Essential Oils

Vol. 74, Iss. 9-10: Special Section on Chemistry of Social Insects

Vol. 74, Iss. 3-4: Special Issue on Chemo-enzymatic cascade reactions

Vol. 72, Iss. 9-10: Special Issue on Insect Biotechnology

Vol. 72, Iss. 7-8: The Special Section is dedicated to the memory of Professor Lothar Jaenicke

Vol. 71, Iss. 9-10: The issue is dedicated to the memory of Professor Peter Böger

Your Benefits

International outreach of A Journal of Biosciences: Zeitschrift für Naturforschung C (ZNC)
Cross-disciplinary contributions from chemistry-biology boundary
Authoritative and recognized reviewers

Geschichte

Alfred Klemm, then working at the Kaiser Wilhelm Institute of Chemistry in Tailfingen, founded the Zeitschrift fuer Naturforschung together with Hans Friedrich-Freksa in 1946. In 1947 the Zeitschrift fuer Naturforschung was divided into two parts which were devoted to the physical sciences (Section A) and the chemical and biological sciences including biophysics (Section B). It was then only in 1973, that Section C was established for the biological sciences while Section B concentrated on chemistry. In Zeitschrift fuer Naturforschung C – A Journal of Biosciences, as it is fully referred to now, research papers are presented in fields on the chemistry-biology boundary which address scientific ideas and approaches to generate and understand natural compounds on a molecular level and/or use them to stimulate and manipulate biological processes.

Other publications in the field

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Equisarmine, a new steroidal glycoalkaloid, from sterile stems of Equisetum arvense

30. September 2025

Atsumi Shimada, Hiroshi Ueno, Kohei Kawabata, Masanori Inagaki

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Glutaminase is an important target that is often over expressed in neurodegenerative and lifestyle related diseases but few effective inhibitors of this enzyme have yet reached clinical trials. To select plants with high glutaminase inhibitory activities, this study was to compare glutaminase inhibitory activities of 20 plant extracts and investigate the isolation, structural elucidation and the inhibitory activity of an active compound from the selected extract of Equisetum arvense L. (horsetail). Equisarmine ( 1 ), a new steroidal glycoalkaloid, was elucidated by analyzing its nuclear magnetic resonance (NMR) and electrospray ionization mass spectrometry (ESI-MS) spectral data. The half maximal inhibitory concentration (IC 50 ) values of 1 and 6-diazo-5-oxo-L-norleucine (DON) as control were 0.72 mM and 0.27 mM, respectively. The results suggest that the extract from horsetail shows the strongest biological activity among 20 tested plant extracts, and that 1 may serve as a lead compound for the prevention and treatment of neurodegenerative and lifestyle-related diseases by targeting glutaminase. This is the first report on the structure and glutaminase inhibitory activity of 1 .
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Oroxylum indicum root bark extract mitigates hepato-renal damage induced by acetaminophen and cisplatin

25. September 2025

Seema Menon, Lincy Lawrence, Vipin P. Sivaram, Jose Padikkala, Shaji E. Mathew, Arunaksharan Narayanankutty

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Oroxylum indicum is an important Ayurvedic plant from the “Dasamoola” group, traditionally used as a detoxifying agent. This study evaluates the protective effects of the root bark methanol extract of O . indicum (ORX) against acetaminophen-induced hepatotoxicity and cisplatin-induced nephrotoxicity in rats. The doses of ORX used in the study were selected based on the previous toxicity analysis (200 mg/kg and 400 mg/kg doses). Acetaminophen administration increased serum liver function markers (AST, ALT, ALP, bilirubin), while ORX and silymarin treatments significantly reduced these levels ( p < 0.01). ORX administration also reversed the acetaminophen-induced depletion in hepatic redox balance as indicated in terms of SOD, GPx, GSH and lipid peroxidation. Corroborating these, the changes in the hepatic normal architecture induced by acetaminophen were also reversed by the pre-treatment with ORX. Similarly, the cisplatin administration resulted in strong myelosuppression and nephrotoxicity. In cisplatin-exposed rats, renal oxidative stress markers worsened, and serum renal function parameters were elevated. On the contrary, the pre-treatment with ORX alleviated the cisplatin-induced myelosuppression and redox imbalance in the renal tissues; further, it also restored the renal histology to near normal. Overall, O . indicum root bark extract effectively mitigated drug-induced liver and kidney damage, likely through redox balance restoration.
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Cytotoxic isoflavones from the stem bark of Protea gaguedi

18. September 2025

Diriba Borena Hunde, Dereilo Bekere Belitibo, Chaltu File, Zelalem Abdissa, Andrianambinina Andriamarolahy Razakarivony, Marcel Frese, Norbert Sewald, Negera Abdissa

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Protea gaguedi is widely used in Ethiopia for the treatments of diarrhea, tumor, urological diseases, and menorrhagia. Despite its extensive use by traditional healers, the pharmacological properties and chemical composition of this medicinal plant remain largely unexplored. Anticipated by these claims, the chromatographic separation of CH 2 Cl 2 /CH 3 OH (1:1) stem bark extract of P. gaguedi led to the isolation of a new isoflavone ( 1 ) together with five known compounds: jamaicin ( 2 ), 5-methoxydurmillone ( 3 ), dipteryxine ( 4 ), 4′- O -geranylisoliquiritigenin ( 5 ), and stigmasterol ( 6 ), whose structures were determined using IR, UV, MS, and NMR and comparison with literature data. The cytotoxic effects of the isolated compounds were evaluated using human cervical carcinoma cell line, KB-3-1. Compounds 1 , 2 , and 3 demonstrated remarkable cytotoxicity with IC 50 values of 24.6 nM, 3.09 µM, and 21.70 µM, respectively, while the other compounds demonstrated negligible or no inhibitory activities against the tested strain. Following the high cytotoxicity of compound 1 against KB-3-1, its activity against the multidrug-resistant subclone KB-V1 was also evaluated and revealing an IC 50 of 17.5 nM. In silico molecular docking analyses were performed for these active compounds and revealed relative binding energies (−10.0, −9.4, −9.5 kJ/mol for compounds 1 , 2 and 3 , respectively) against the ternary target protein complex HPV16 E6/E6AP/p53 (PDB ID: 4XR8). ADME analysis also revealed good cytotoxicity candidacy of these compounds, provided that in vivo activities have been performed for further confirmation.
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Exploring the potency of 6-bromo-3-methylquinoline analogues as prostaglandin F2α inhibitors

17. September 2025

Kaushik Sarkar, Sandhya Yadav, Ammena Y. Binsaleh, Nawal Al-Hoshani, Rajesh Kumar Das

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Prostaglandin F2α (PGF2α) is associated with preterm labor and preterm birth. PGF2α inhibitors have thus proven to be a promising target in the development of lead compounds to prevent preterm birth. In this work, Quantitative Structural Activity Relationship (QSAR) was implemented on a dataset of 77 compounds of 6-bromo-3-methylquinoline analogues using statistical approach and random selection in the QSARINS software. The Genetic Algorithm-Multiple Linear Regression (GA-MLR) approach was used to predict the best model ( R 2 = 0.8943 and Q 2 LOO = 0.8836). The inclusion of descriptors FNSA-2 and WV.mass resulted in a well‐fitted and highly predictable model. Artificial neural network (ANN) analysis was also carried out to validate the model effectiveness. Twenty eight new molecules with better predicted biological activity (pIC50) were designed. The binding energy from the docking study of seven compounds have shown higher binding activity than P10 into prostaglandin F synthase protein (PDB ID: 2F38). The stability of protein–ligand complex was further validated by 100 ns molecular dynamics simulation and MM-PBSA binding free energy. DFT and ADME-toxicity analysis also confirmed their drug-likeness properties. Collectively, our findings highlight novel quinoline derivatives as promising lead candidates, warranting further validation through collaborative in vitro and in vivo studies.
Open Access
Exploring the chemical composition and anti-cancer potential of Matricaria recutita L. essential oil

15. September 2025

Serkan Yilmaz, Hafize Fidan, Mine Çağlayan, Stanko Stankov, Selma Yazar, Albena Stoyanova

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This study aims to investigate the chemical composition and assess the anti-cancer potential of Matricaria recutita L. essential oil against various cancer cell lines. The chemical profile of the essential oil was determined through gas chromatography-mass spectrometry (GC-MS), identifying major constituents such as (Z)- β -farnesene, α -bisabolol oxides, and chamazulene. The anti-cancer activity was evaluated using in vitro cytotoxicity assays (MTT assay) on human lung adenocarcinoma (A549), human hepatocellular carcinoma (HepG2), human breast adenocarcinoma (MDA-MB-231), and mouse fibroblast (L929) cell lines. The experiments were performed in triplicate, and data were analyzed using ANOVA to determine statistical significance. The main constituents of the essential oil included (Z)- β -farnesene (33.90 %), α -bisabolol oxide B (11.60 %), and others. The oil demonstrated considerable cytotoxic effects across all tested cancer cell lines, with IC 50 values indicating strong anti-proliferative activity, particularly at higher concentrations and longer exposure times. The results showed dose-dependent reductions in cell viability, with significant decreases in cell proliferation observed especially at concentrations over 7.81 μg/mL. These findings support its potential as a natural, complementary agent in cancer therapy, warranting further in vivo studies for clinical application.
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Unrevealing the potential of fibrous biomaterials in cartilage tissue engineering: a review

15. September 2025

Sachin S. Mali, Dipak S. Thorat, Anil Kumar Singh, Prajakta R. Patil, Snehal S. Patil, Akshay Kundale, Yogesh V. Ushir, Durgacharan A. Bhagwat, Sheeba Shafi, Sudarshan Singh

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Fibrous biomaterials have showed considerable potential in cartilage tissue engineering due to their ability to imitate the structure and characteristics of the original extracellular matrix. Sustainable biomaterials such as chitosan, silk fibroin, and collagen can be produced into a variety of shapes, including hydrogels, scaffolds, and electrospun nanofibers, to develop an optimal milieu for chondrocyte adhesion, proliferation, and cartilage matrix deposition. In recent years, various studies showed that biomaterials-based fiber mats obtained through electrospinning as scaffolds exhibit remarkable chondrocyte growth support. These fiber mats promote high chondrocyte viability and cell proliferation, particularly when thin neutralized fibers are utilized. The biomimetic attributes of these biomaterials obtained from renewable resources such as plants, animals, and microbes have intrinsic benefits such as biocompatibility, microstructure resemblance to the original extracellular matrix, and adjustable mechanical properties. However, there are still hurdles in optimizing scaffold–cell interactions, controlled degradation, stress response, and flexibility for successful clinical translation. As a result, fibrous biomaterials exhibit significant potential for cartilage tissue engineering by promoting chondrocyte adhesion, proliferation, and cartilage matrix deposition. Nonetheless, additional study is required to solve the obstacles and optimize these materials for successful clinical applications.
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Integrated experimental and In silico evaluation of the antioxidant, antibacterial, antiviral, and antiproliferative activities of Boswellia neglecta S. Moore stem extract and its bioactive constituents

12. September 2025

Gashaw Nigussie, Aman Dekebo, Markos Abebe, Asfaw Meressa, Temesgen Negassa, Menberework Chanyalew, Maria A. Niukalova, Vladimir V. Zarubaev, Abiy Abebe, Rajalakshmanan Eswaramoorthy, Ahmed A. Hussein, Mo Hunsen, Milkyas Endale

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Boswellia neglecta has been traditionally used to treat leukemia, cancer, and skin diseases. In this study, seven compounds ( 1 – 7 ) were isolated from the stem methanol extract and identified for the first time from this species using NMR spectroscopy. GC-MS analysis revealed 17 compounds, with olean-12-en-3-one (32.59 %), oleic acid (13.79 %), and β -amyrin (10.66 %) as major constituents. Among the isolated compounds 7 showed the strongest antibacterial activity against Pseudomonas aeruginosa (MIC = 0.23 ± 0.11 mg/mL). Compounds 3 – 7 demonstrated promising antioxidant activity (IC 50 = 1.29–7.05 μg/mL) compared with ascorbic acid (IC 50 = 0.86 μg/mL). The methanol extract also exhibited significant cytotoxicity against MCF-7 breast cancer cells (27.25 % viability at 200 μg/mL) and antiviral activity against influenza A (H1N1) (IC 50 = 1.5 μg/mL, SI = 21). Molecular docking revealed that compound 7 had strong binding affinity against P. aeruginosa DNA gyrase (−10.8 kcal/mol), surpassing ciprofloxacin (−6.9 kcal/mol). Compounds 3 – 7 also had stronger affinities (−5.1 to −6.5 kcal/mol) against human peroxiredoxin 5 and (−6.0 to −10.3 kcal/mol) against myeloperoxidase compared to ascorbic acid (−4.7 and −6.0 kcal/mol). These findings highlight the plant’s therapeutic potential, warranting further in vivo , preclinical, clinical, and mechanistic investigations.
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Plant-derived secondary metabolites for malaria treatment: extraction, mechanisms, and therapeutic potential

10. September 2025

Addisu Tamir Wassie, Ibrahim Nasser Ahmed, Rakesh Kumar Bachheti, Mesfin Getachew Tadesse, Aselefech Sorsa Wotango, Archana Bachheti, Yilma Hunde Gonfa, Ayalew Hussen Assen

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Medicinal plants have long been used as a primary healthcare resource for treating malaria and other diseases globally. Malaria, caused by Plasmodium species, remains a serious health threat, with the World Health Organization reporting that over 40 % of the global population lives in malaria-endemic regions. The rise of drug-resistant strains has further complicated treatment efforts, necessitating the search for new therapeutic agents. This review emphasizes the antimalarial potential of plant-derived secondary metabolites, which exhibit diverse pharmacological activities. Several compounds, such as ceramicine R (IC 50 = 2.80 μM), knipholone clooxanthrone (IC 50 = 14.58 μM for D6 and 9.42 μM for W2), joziknipholone A (IC 50 = 0.17 μM), joziknipholone B (IC 50 = 0.26 μM), and cajachalcone (IC 50 = 7.4 μM), have shown potent activity against Plasmodium falciparum . Data were collected from Web of Science, PubMed, Scopus, Google Scholar, and Science Direct. A total of 34 medicinal plants were identified, along with details on extraction techniques and factors influencing metabolite efficacy. Key secondary metabolites include alkaloids, flavonoids, terpenoids, and their derivatives (e.g., quinine, artemisinin, quercetin, chalcones). This review highlights their mechanisms of action and their promise as templates for developing novel drugs to combat both drug-sensitive and drug-resistant malaria strains.
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Utilizing olive leaves as a rich source of multifunctional bioactive compounds to fight oxidative stress, Alzheimer’s disease, diabetes, and cancer using in vitro, in silico, and bioinformatics techniques

9. September 2025

Gunes Ak, Nilofar Nilofar, Nadire Pelin Bahadirli, Agnese Santanatoglia, Giovanni Caprioli, Gianni Sagratini, Ismail Koyuncu, Idris Kirhan, Jasmina Glamočlija, Dejan Stojković, Abdullahi Ibrahim Uba, Savaş Kaya, Mikhail M. Maslov, Sakina Yagi, Gokhan Zengin

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Olive leaves are of significant interest in traditional medicine and in the development of functional nutraceuticals. In this study, the leaves of four olive varieties (Halhali, arbequina, gemlik, karamani) were utilized to examine and compare the chemical composition and biological activities, particularly their role in enzyme inhibition, cancer prevention, and apoptosis induction. Results showed that among the tested varieties analyzed, Gemlik (77.79 mg gallic acid equivalent (GAE)/g) and halhali (76.03 mg GAE/g) exhibited the phenolic contents while arbequina had the highest flavonoid content (36.51 mg rutin equivalent (RE)/g). Similarly, these two varieties of extracts recorded strong antioxidant activity in several assays. Gemlik (2.70 mg galantamine equivalent (GALAE)/g) and arbequina (2.59 mg GALAE/g) demonstrated the highest acetylcholinesterase (AChE) inhibition. The results of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide)) assay showed arbequina provided the highest cytotoxic effect against HeLa cells (IC 50 value: 60.59 μg/ml) and annexin-V/PI staining confirmed the inducing of apoptosis by arbequina in HeLa cells. In conclusion, the studied olive varieties of leaf extracts appeared to have more potential as a health supplement rich in natural antioxidants and merit further intensive study.
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Synergistic role of microbiologically synthesized nanoparticles and PGPR in sustainable agriculture: a critical review

26. August 2025

Priyvart Choudhary, Nishesh Sharma, Vinay Kumar Pandey, Aum Garg, Jerin James, Sarvesh Rustagi

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In recent years, agriculture has undergone transformative innovations to enhance crop productivity, resilience, and nutritional value. With increasing concerns over food security, environmental degradation, and soil health, there is growing emphasis on sustainable agricultural practices. Among these strategies, the use of plant growth-promoting rhizobacteria (PGPR) have emerged as promising solutions. Advances in nanobiotechnology have led to the development of various metal-based nanoparticles (NPs), such as silver (Ag NPs), zinc oxide (ZnO NPs), titanium dioxide (TiO 2 NPs), carbon nanotubes (CNTs), and quantum dots (QDs). These nanomaterials have the potential to enhance plant biomass and crop yield in both laboratory and field settings. PGPR have gained attention for their ability to improve crop productivity through mechanisms such as nitrogen fixation, phosphate solubilization, siderophore and phytohormone production, and the induction of systemic resistance. The synergistic use of nanotechnology and PGPR represents a revolutionary platform for sustainable agriculture. This integrated approach offers practical solutions to critical agricultural challenges such as low productivity, soil degradation, and environmental sustainability. This review highlights how the combination of synergistic utilization of nanotechnology and PGPR can be developed as a winning strategy for sustainable agriculture to solve the current challenges of food security, soil degradation, and environmental sustainability.
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Studies on the pharmacological potential of starfish Luidia maculata using acute oral toxicity, in vivo anti-nociceptive, locomotor, and in vitro cytotoxic activities

15. August 2025

Suguna Anbukkarasu, Prabhu Kolandhasamy, Bragadeeswaran Subramanian, Ramachandran Vinayagam

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In the present study, starfish ( Luidia maculata ) specimens were collected from bycatch trash fish at a fish landing center, and their pharmacological and cytotoxic potentials were evaluated through acute oral toxicity, in vivo anti-nociceptive and locomotor assays, as well as in vitro cytotoxicity assay. The crude ethanol extract from starfish L. maculata was purified by liquid–liquid partition chromatography using cyclohexane and n-butanol was used to determine the acute oral toxicity (LD 50 ) and a histopathological examination of the rat. In acute oral toxicity studies, an LD 50 value of 33.33 % of mortality was observed at 2000 mg/kg per oral dosage of the extract. Oral administration extract (2000 mg/kg) revealed significant histopathological alterations in tissues when compared to the control rats. Both in thermal and chemical-induced analgesic methods, administered extract (400 mg/kg bw) showed the maximum analgesic activity. In the tail flick method, the high dose of the extract significantly elevated the pain threshold throughout the observation period, with all groups showing increased pain tolerance over time. In locomotor activity, the highest percentage reduction (91.16 %) was observed in group IV animals after 90 min of administration, which showed the potent CNS depressant activity of the extract. The extract exhibited significant cytotoxicity against MCF-7 cells with a low IC 50 of 6.51 µg. Hence, the result of the present study showed the anti-nociceptive, CNS depressant cytotoxic properties of starfish L. maculata.
Open Access
Protective effect of (±)-gossypol through modulation of VEGF and apoptosis in mice bearing Ehrlich’s solid carcinoma

15. August 2025

Gönül Ulus, Çinel Köksal Karayıldırım, Gürkan Yigitturk, Ayse Tansu Koparal, Altug Yavasoglu, Nefise Ulku Karabay Yavasoglu

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This study aimed to demonstrate the protective effect of the racemic form of gossypol ((±)-gossypol) on Ehrlich’s solid carcinoma (ESC) model as a syngeneic breast cancer model. In the study, solid tumors developed in 100 % of BALB/c mice in the tumor control group, no tumor development was observed in the group treated with (±)-gossypol prior to tumor cell implantation, and tumor formation was determined as 28.6 % in the post-implantation gossypol treatment group. (±)-Gossypol treatment significantly reduced VEGF expression, indicating a potent anti-angiogenic effect. In the tumor control group, VEGF expression was observed to be markedly intense and extensively distributed across the tumor tissue. Conversely, in the post-implantation gossypol treatment group, VEGF expression was assessed to be significantly lower in comparison to the tumor control group. Administration of (±)-gossypol (40 mg/kg/day ip) for five consecutive days was well tolerated, with no observable signs of systemic toxicity, such as >5 % weight loss or behavioral abnormalities on mice. These findings revealed that (±)-gossypol, in addition to its tumor suppressive effect, can inhibit pro-angiogenic effects of Ehrlich’s ascites carcinoma (EAC) cells and have a protective effect in breast cancer.
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Design, synthesis, investigation, and biological activity assessments of n-allyl-2-(benzylidene) hydrazine-1-carbothioamide derivatives as monoamine oxidase-b inhibitor agents

15. August 2025

Sazan Haji Ali, Derya Osmaniye, Begüm Nurpelin Sağlık Özkan, Serkan Levent, Yusuf Özkay, Zafer Asım Kaplancıklı

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Parkinson’s disease (PD) is a progressive neurodegenerative disease characterized by tremor and bradykinesia and is a common neurologic ailment. There are a number of other extrapyramidal conditions that can make the diagnosis challenging. Unlike other neurodegenerative diseases, idiopathic PD has effective treatments that mitigate symptoms. Inspired by the existing findings related to the hypothesis such as activated monoamine oxidase (MAO) enzyme, we have developed a series of new molecules that serve as inhibitors for MAO-B enzyme. In this investigation, a range of nitrogen-containing heterocyclic as thiosemicarbazone derivatives, are explored to showcase their functionality as inhibitors of MAO-B enzymes. This study characterizes and validates their potential as new agents for addressing PD. The produced compounds were assessed for their biological activity and cytotoxicity using nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS) spectroscopy. The biological activity and cytotoxicity studies were performed for the synthesized molecules as h MAO-B inhibitors. Among the designed compounds, 3g demonstrated the best MAO-B inhibitory activity and optimal docking poses and stability in the molecular dynamic’s studies. Based on the data obtained, molecule 3g was a candidate for further investigations. Theoretical pharmacokinetic and drug ability studies showed favorable properties to the candidate compound 3g among other synthesized molecules.
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Synthesis and antibacterial activity of 8-nitro-7-(aryl/alkyl) and tetracyclic fluoroquinolones encompassing thiophene, furan, and related congeners

1. August 2025

Ala’a A. Al-Akhras, Jalal A. Zahra, Mustafa M. El-Abadelah, Shaima’ K. Alsawalha, Salma A. Musameh, Marwan Abu-Halaweh, Monther A. Khanfar

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This work outlines the synthesis of six novel 8-nitro-7-(aryl/hetaryl)fluoroquinolones and five (aryl/hetaryl)tetracyclic fluoroquinolones; 4-oxo-4,11-dihydro-1 H -pyrido[2,3- a ]carbazole-3-carboxylic acids ( 10b , 11b ) and 4-oxo-4,10-dihydro-1 H -thieno/furo[4,5]pyrrolo[3,2- h ]quinoline-3-carboxylic acids ( 3b – 5b ). The tetracyclic fluoroquinolone compounds were synthesized using a Suzuki–Miyaura cross-coupling acylation reaction of ethyl 7-chloro-1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylate, followed by a microwave-assisted phosphite-mediated Cadogan reaction. The antibacterial activity of the compounds was evaluated against a range of Gram-negative bacteria, including Salmonella typhimurium, Pseudomonas aeruginosa, Escherichia coli, Acinetobacter baumannii, and Klebsiella aerogenes , as well as Gram-positive bacteria, including Listeria monocytogenes, Enterococcus faecalis, Streptococcus agalactiae, Staphylococcus aureus, and Staphylococcus epidermidis . The results demonstrated significant antibacterial activity against most of the tested strains. The lowest minimum inhibitory concentration (MIC) values observed were 7.7 μg/mL for compound 4b against S. agalactiae and compound 9b against S. aureus . These values are comparable to Streptomycin, which exhibited an MIC greater than 3.8 μg/mL for all tested pathogens.
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Exploring the inhibitory potentials of metal-doped graphene in combating biofilm formation: a review

1. August 2025

Kunal Biswas, Devadass Jessy Mercy, Agnishwar Girigoswami, Koyeli Girigoswami

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The emergence of anti-microbial resistance (AMR) has become a pressing need for the design of novel and potential anti-microbial and anti-biofilm agents. Nano-scaled materials have been designed in the research domain to curb the populous spread of microbial biofilms. In the context of nano-scaled materials, metal nanoparticles are of unique importance and have been studied in detail for the treatment of biofilm propagation and menace. The crucial aspects of metal nanoparticles and their complexation with graphene have been extensively understood at the molecular level in this review article. The molecular interplay between the various external stimuli, like pH, temperature, sound, mechanical stimuli, and different external factors, on biofilm regulation has been studied and accentuated in the paper. The effect of such external factors succumbing to the biofilm-producing microbes, to the potential inhibitory activities of such novel nano-composites has been unraveled in the present review. Understanding the methodology behind nanoscaled treatments and their molecular mechanisms could pave the way for novel biofilm targeting strategies.
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Unveiling of the novel benzothiazole derived thiazolidinone derivatives: in vitro and in silico insights to design a promising agent for anti-Alzheimer’s disease

24. Juni 2025

Yousaf Khan, Anila Mukhtiar, Hina Sarfraz, Shoaib Khan, Rafaqat Hussain, Mujeeb Ul Naeem, Abdul Sattar, Tariq Aziz, Zia Ur Rehman Panezai, Thamer H. Albekairi, Farwa Jabbir

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The present investigation explained various heterocyclic moieties particularly the thiazolidinone scaffold ( 1–16 ) which were synthesized from benzothiazole as promising anti-Alzheimer agent. In this, we have unveiled the synthetic path for generation of thiazolidinone scaffolds which was initiated benzothiazole having 2-amine moiety. These synthesized scaffolds were then inveterate through several analytical techniques including high-resolution electron impact mass spectrometry (HREI-MS), proton nuclear magnetic resonance ( 1 H NMR), and carbon-13 nuclear magnetic resonance ( 13 C NMR). The anti-Alzheimer potential of these compounds was evaluated through molecular docking studies to examine their interactions with target proteins. Additionally, ADMET analysis was performed to assess drug-likeness and pharmacokinetic properties. Among the synthesized analogs, scaffold- 3 emerged as the most promising inhibitor compared to other derivatives in the series. This study highlights the potential of thiazolidinone derivatives in the development of novel anti-Alzheimer drugs and underscores the need for further optimization to enhance their therapeutic efficacy.
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Moringa oleifera: a multifunctional botanical resource for sustainable agriculture, nutrition, and therapeutic applications, a review

11. Juni 2025

Anila Mukhtiar, Yousaf Khan, Hina Sarfraz, Aisha Usman, Marouan Kouki, Umair Mukhtiar

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Moringa oleifera , widely recognized as the “miracle tree,” has garnered significant scientific interest due to its exceptional nutritional, medicinal, and industrial properties. This study provides a comprehensive evaluation of its potential as a sustainable feed additive, antimicrobial agent, functional food ingredient, and a bioresource for agricultural and industrial advancements. Enriched with high-quality proteins, essential amino acids, vitamins, minerals, antioxidants, and bioactive compounds, M. oleifera exhibits remarkable benefits in aquaculture, livestock production, and human nutrition. Its potent immunomodulatory, antifungal, antidiabetic, and antimicrobial properties further underscore its therapeutic significance in disease prevention and health promotion. Additionally, its ecological advantages, including soil enrichment, natural pest control, and wastewater purification, highlight its pivotal role in fostering environmental sustainability. A comprehensive investigation over the past five years has consistently validated its effective insecticidal efficacy, further expanding its agricultural applications. The efficacy of M. oleifera bioactive compounds is profoundly influenced by extraction methodologies. Advanced techniques such as ultrasound-assisted extraction (UAE), microwave-assisted extraction (MAE), supercritical fluid extraction (SFE), and enzymatic-assisted extraction (EAE) significantly enhance the yield, purity, and bioavailability of phytochemicals, optimizing their pharmacological and industrial applications. The selection of an appropriate extraction strategy is crucial to preserving bioactivity and ensuring maximum efficacy in pharmaceutical, nutraceutical, and functional food formulations. Despite its vast potential, challenges such as the presence of anti-nutritional factors, variations in nutrient composition due to differing cultivation and processing methods, and the absence of standardized dosage guidelines require further investigation. Future research should focus on optimizing inclusion levels in animal and human diets, elucidating molecular mechanisms of action, and advancing green extraction technologies to enhance its efficacy and sustainability. This study highlights the multifaceted applications of M. oleifera across diverse sectors and its potential to revolutionize sustainable agriculture, healthcare, and environmental conservation. Addressing existing challenges through cutting-edge research and technological innovation will unlock its full potential as a key natural resource for enhancing global food security, promoting sustainable development, and pioneering pharmaceutical breakthroughs. By integrating information from recent five-year literature from 2019 to 2024, this work offers a roadmap for future study, addressing significant challenges and outlining prospective avenues for the development of novel therapeutic and pest control approaches exploiting M. oleifera .
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Synthesis of benzimidazole-based hydrazones as potential anticarbonic anhydrase agents: a theoretical and experimental investigations

9. Juni 2025

Abdul Shakoor, Aftab Alam, Faheem Jan, Saeed Ullah, Mumtaz Ali, Mahboob Ali, Abid Ali, Abdullah F. AlAsmari, Fawaz Alasmari, Ajmal Khan, Ahmed Al-Harrasi, Momin Khan

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In this research, a series of new hydrazone-Schiff bases of benzimidazole were synthesized in good yields through three step reactions, and the structures were confirmed by means of modern spectroscopic techniques (HR-ESI-MS, 1 H-, and 13 C NMR). These compounds have been assessed for their in vitro carbonic anhydrase (CA) inhibitory activity, 12 derivatives showed potent inhibition (IC 50 = 13.29 ± 0.46 to 30.74 ± 1.28 µM) comparing to the acetazolamide as a standard (IC 50 = 18.20 ± 0.43 µM). Molecular docking studies exposed vital binding interactions and robust affinities with the CA active site. Electronic properties and structural stability were examined through DFT (B3LYP/6–311++G(d,p)), and intramolecular interactions were evaluated by means of DFT-D3 and reduced density gradient analysis. Furthermore, TD-DFT (CAM-B3LYP/6–311++G(d,p)) calculations provided insights into the electronic transitions and reactivity parameters like electron affinity, electronegativity, ionization energy, and chemical hardness, offering a deeper understanding of the compounds’ inhibitory mechanisms.
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Chemometric study of the effects of the geographical origin and the collection period on the chemical compositions and the antimicrobial activities of Pituranthos tortuosus essential oils

6. Juni 2025

Zina Benissa, Fatma Chtourou, Françoise Dumas, Sylvie Bouttier, Mohamed Bouaziz, Sami Zouari

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The present study aims to analyze the chemometric variation of the chemical composition of the aerial part’s essential oils of Pituranthos tortuosus , collected from different regions from Tunisia (Majoura and Sened (Gafsa), Sbeitla (Kasserine), and Eljem (Mahdia)) during the period from February to June and to assess their antimicrobial activity. The different samples of the aerial parts of P. tortuosus were hydrodistillated during 4 h. The obtained essential oils were analyzed by GC/FID and GC/MS techniques. The antimicrobial activity of these essential oils samples was evaluated in vitro using Petri dishes against Staphylococcus aureus subsp . aureus , Pseudomonas aeruginosa , Escherichia coli , and Candida albicans . The obtained results showed that the yields of all essential oils were ranging from 0.42 to 0.77 %. They differ significantly ( p ≤ 0.01) with the regions of collection. The chromatographic analysis of these essential oils displayed different chemical compositions leading to the identification of eight chemotypes. The majority of their chemical compounds differ significantly with the collection regions ( p ≤ 0.05). The studied antimicrobial effects of the essential oils revealed significant differences ( p ≤ 0.02) with the collection region. All the essential oils displayed an important antimicrobial effect against S. aureus and C. albicans .
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In vitro antibacterial, DPPH radical scavenging activities, and in silico studies of isolated compounds from Rubus apetalus leaves extract

6. Juni 2025

Tolessa Duguma, Yadessa Melaku, Akalu Terfa, Kebede Shenkute, Taye B. Demissie, Nayang Kgakatsi, Mo Hunsen

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Rubus apetalus Poir. is a medicinal plant used in Ethiopia to treat different diseases. This study aimed to isolate phytochemicals from the leave s and evaluate their antibacterial and DPPH scavenging activities using in vitro and in silico studies. The GC-MS study resulted in the identification of 16 compounds. Palmitic acid ( 9 ), palmityl alcohol ( 17 ), β -sitosterol ( 18 ), tiliroside ( 19 ), and astragalin ( 20 ) were isolated using chromatographic techniques and characterized using NMR data. The inhibition zones (IZs) of 100 mg/mL extracts and 5 mg/mL isolated compounds ranged from 9.33 ± 0.47 to 15.07 ± 0.74 mm against all bacteria. Compound 18 showed better activity against Staphylococcus aureus and Streptococcus pyogenes . Compound 19 exhibited better activity against Escherichia coli and Pseudomonas aeruginosa . The activity of compound 19 was supported by molecular docking studies against E . coli DNA gyrase B (−8.0 kcal/mol) and Pseudomonas quinolone signal A (PqsA, −9.5 kcal/mol) for E . coli and P . aeruginosa , respectively. At 62.5 mg/mL, combined fractions 16–21 and compound 19 showed the lowest (54.5 %) and the highest (89.8 %) DPPH scavenging activity, respectively. The in silico studies indicated that none of the isolated compounds is fatal if swallowed. Therefore, these findings support the traditional use of the plant to treat various bacterial diseases.
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From current landscape to future horizon in stem cell therapy for tissue regeneration and wound healing: bridging the gap

23. Mai 2025

Kashvy R. Morakhia, Aayushi C. Shah, Mannat P. Patel, Jainam K. Shah, Rajanikant Patel, Mehul R. Chorawala

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Stem cell therapy has emerged as a groundbreaking approach in regenerative medicine, offering immense potential for tissue regeneration and wound healing. Stem cells, with their ability to self-renew and differentiate into specialized cell types, provide innovative therapeutic strategies for variety of medical conditions. Key stem cell types, including embryonic, induced pluripotent, and adult stem cells such as mesenchymal and hematopoietic stem cells, play pivotal roles in regenerative processes and wound repair. In tissue regeneration, stem cells replenish damaged or necrotic cells by differentiating into specialized cell types like bone, muscle, or nerve cells, thus restoring the structural and functional integrity of tissues. In wound healing, stem cells stimulate angiogenesis, generate new skin cells, and modulate immune responses to enhance repair. This multifaceted therapeutic potential has paved the way for clinical applications in cardiovascular, neurological, musculoskeletal, and autoimmune disorders, as well as skin and burn injuries. This review highlights recent advancements in stem cell therapy, exploring its clinical applications and addressing challenges such as immune rejection, ethical concerns, scalability, and the need for long-term clinical trials. The article underscores the importance of continued research to fully realize the transformative potential of stem cell therapy in modern medicine.
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Sphingolipids in medicinal mushrooms: structural insights, biological activities, and therapeutic potential

1. Mai 2025

Yhiya Amen, Ahmed Othman, Kuniyoshi Shimizu

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Edible mushrooms are well-known for their nutritional value, serving as rich sources of bioactive nutrients, mainly proteins, carbohydrates, lipids, vitamins, and minerals that are vital for human health. Lipids, integral to biological functions such as cellular structure and energy storage, play crucial roles in mushrooms’ bioactivity. Sphingolipids, an important class of lipids, serve not only as structural elements in cell membranes but also act as bioactive molecules, playing key roles in cancer prevention, skin health, and infection control. Recent studies highlight their unique presence in mushrooms. Despite their relatively low abundance, sphingolipids in mushrooms are pivotal in cellular processes and offer therapeutic potential. Advances in analytical techniques have facilitated the characterization of these compounds. This review explores the structural profiles, biological activities, and therapeutic applications of sphingolipids in medicinal mushrooms, highlighting their potential in the development of functional foods and novel therapeutic agents.
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Chemical composition, anticholinesterase activity and cytotoxicity of the essential oil of Luvunga scandens (Roxb.) Wight from Malaysia

30. April 2025

Abubakar Siddiq Salihu, Wan Mohd Nuzul Hakimi Wan Salleh, Nurunajah Ab Ghani, Arwa R. Althaher, Salam Ahmed Abed

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Luvunga scandens (Roxb.) Wight is identified as one of the vital folk medicinal plants in Malaysia. Despite its traditional use, the essential oil composition and bioactivities of L. scandens remain largely unexplored. This study investigates the essential oil composition, anticholinesterase activity, and cytotoxicity of L. scandens leaves. After the essential oil was extracted using hydrodistillation, GC-FID and GC-MS were used for analysis, identifying 35 components, representing 93.8 % of the total oil. The major components included germacrene D (17.8 %), γ -elemene (15.6 %), β -gurjunene (10.8 %), α -cadinol (5.3 %), α -humulene (4.9 %), and alloaromadendrene (4.5 %). With IC 50 values of 78.5 and 95.2 μg/mL, the essential oil showed moderate inhibition of butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). The cytotoxicity was evaluated using an MTT assay. The essential oil exhibited cytotoxicity against three cancer cell lines; HepG2, MCF7, and A549 with IC 50 values of 70.2, 52.8, and 65.5 μg/mL, respectively. These findings provide new insights into the potential therapeutic applications of L. scandens essential oil, particularly in neurodegenerative diseases and cancer therapy.
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Native/modified dextran-based nanogel in delivering drug and management of ocular complications: a review

29. April 2025

Biswajit Basu, Suraj Mallick, Suman Dhauria, Pooja V Nagime, Sudarshan Singh

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Ocular nanogels have emerged as a promising therapeutic approach, and nanotechnology has speed up the growth of the pharmaceutical and medical technology sectors. The physiological and anatomical barriers of the eye limit the use of traditional ocular preparations, which leads to low drug bioavailability and a brief retention period. This presents a serious problem for patients, doctors, and chemists. Nevertheless, nanogels can encapsulate medications within three-dimensional crosslinked polymeric networks and provide controlled and prolonged drug delivery by using particular structural layouts and unique preparation techniques, improving therapeutic efficacy and patient compliance. Dextran and its variants, a naturally occurring polysaccharide, have drawn a lot of interest in developing delivery systems for use in pharmaceutical and medical applications. Many dextran-based delivery systems with customized geometries and features have been fabricated recently, such as hydrogels, nanogels, magnetic nanoparticles, nanoemulsions, self-assembled micelles and nanoparticles, and microparticles. The review presents advancement and therapeutic potential of dextran-based nanogels for the treatment of various eye conditions, such as cataract, conjunctivitis, glaucoma, dry eye syndrome, age-related macular degeneration, and corneal ulcers. Moreover, the process for development and assessing these nanomedicines, emphasizing their safety and effectiveness as established by preclinical, toxicological, clinical assessments, and patent updates, has been elaborated.
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Biotransformation of vinblastine into vincristine using a fungal endophyte Fusarium equiseti along with the assessment of its antiangiogenic properties

24. März 2025

Gauri Srivastava, Ruchika Mittal, Nidhi Srivastava, Sarita Srivastava, Deepak Ganjewala

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This study focuses on the microbial biotransformation of vinblastine to vincristine, a compound with enhanced anticancer efficacy compared to vinblastine utilizing a fungal endophyte Fusarium equiseti , isolated from Catharanthus roseus . Additionally, the antiangiogenic properties of the resulting vincristine were evaluated in vivo using the chick chorioallantoic membrane assay. The biotransformation was conducted in liquid medium containing vinblastine (0.6–2.4 mM), and F. equiseti spore suspension (50–150 µL) by incubating at 30 °C, pH 5.6, and 200 rpm for eight days. After the reaction was over, products were extracted using methanol and analyzed by LC-MS/MS. The results confirmed the production of vincristine from vinblastine in different sets of biotransformation reactions. In biotransformation reaction-1, which comprised of vinblastine (0.6 mM) and fungal inoculum 150 µL (82 × 10 4  spores/mL), 92 % of vinblastine was converted into vincristine on 8th day of incubation. The vincristine produced demonstrated significant antiangiogenetic properties in the chick chorioallantoic membrane assay in a dose-dependent manner. The antiangiogenic properties of vincristine produced was comparable to standard vincristine. Hence, the study revealed that F. equiseti present a viable alternative to produce vincristine from vinblastine. To our knowledge, this is the first report on F. equiseti highlighting its vinblastine biotransformation potential.
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Insight the confirmation of benzothiazolidinone-derived thiadiazole scaffolds as promising antiurease and anti-Alzheimer agents: synthesis, in vitro, and in silico investigations

21. März 2025

Shoaib Khan, Tayyiaba Iqbal, Tayyaba Zahoor, Rafaqat Hussain, Mohammad Shahidul Islam, Kholood A. Dahlous

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Alzheimer’s disease is a serious neurological disorder, and traditional therapies for Alzheimer’s, like radiation and surgical procedures, as well as chemotherapeutics, are usually linked with multiple negative consequences. Finding a novel therapeutic anti-Alzheimer agent with high efficacy and minimal side effects, we have designed and synthesized benzothiazolidinone-derived thiadiazole-based Schiff base derivatives ( 1–15 ). Biological assessment of these compounds was carried out against acetylcholinesterase and butyrylcholinesterase, and all the derivatives showed varying degrees of inhibitory activity. Analog 8 (IC 50 = 3.60 ± 0.20 and 4.10 ± 0.20 μM for acetylcholinesterase and butyrylcholinesterase, respectively) demonstrated spellbinding efficacy in contrast to standard donepezil (IC 50 = 50 ± 0.10 and 8.10 ± 0.20 μM ). The surpassing inhibition of analog 8 is due to highly reactive CF 3 moiety at the para -position, inhibiting the enzymes via strong hydrogen bond. Analog 7 with IC 50 value of 5.70 ± 0.10 and 6.20 ± 0.40 μM was also found with strong therapeutic potential than standard drug. The strong inhibition potential of lead compounds was also evaluated under enzyme kinetics and spellbinding potential was observed. Biological effectiveness of potent compounds was validated by visualizing the binding interactions via in silico molecular docking study and prediction of drug-likeness via ADME analysis. All the synthesized compounds were analyzed for their structural confirmation via 1 HNMR, 13 CNMR, and HREI-MS.
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Potential of curcumin and its derivatives, modern insights on the anticancer properties: a comprehensive overview

21. März 2025

Rafi Ullah, Muhammad Siraj, Javed Iqbal, Banzeer Ahsan Abbasi

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Globally, cancer is the top cause of mortality, placing a heavy load on the medical system. One of the first known secondary metabolites is curcumin, a bioactive substance. This study aims to emphasize the chemopreventive and chemotherapeutic properties of curcumin and its derivatives, therefore, offering important insights for the possible creation of certain supplemental medications for the treatment of different cancers. Electronic Google databases, including Google scholar, ResearchGate, PubMed/Medline, and ScienceDirect, were searched to gather pertinent data about the chemopreventive and chemotherapeutic effects of curcumin and its derivatives. Various studies have revealed a diverse array of significant biological effects. The majority of investigations pertaining to the potential anticancer effects and associated processes are currently in the experimental preclinical stage and lack sufficient clinical trial data to validate their findings. Clinical research is further needed to clarify the molecular processes and specific targeted action of curcumin and its derivatives, as well as their potential for toxicity and side effects in humans, in order to open up new therapeutic avenues for treating cancer.
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New hydrazone derivatives: synthesis, characterization, carbonic anhydrase I-II enzyme inhibition, anticancer activity and in silico studies

14. März 2025

Ulviye Acar Cevik, Hakan Ünver, Hayrani Eren Bostancı, Burak Tüzün, Nurten İrem Gedik, Ümit M. Kocyigit

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A new series of hydrazone derivatives ( 1a-1l ) were prepared from a condensation reaction between different hydrazide derivatives and 3-formylbenzoic acid. Through the use of several spectral techniques, such as 1 H-NMR, 13 C-NMR, and elemental analysis, the structures of the compounds were clarified. The crystal structure of compound 1d was obtained by single-crystal X-ray crystallography. They were found to have inhibitory effects on the anticancer potentials and human carbonic anhydrase isoforms I and II. Compound 1d was found to be the strongest inhibitor, with IC 50 values of 0.133 µM against hCA I. Also, compound 1l showed the highest inhibitory activity with IC 50 values of 3.244 µM against hCA II. Moreover, their cytotoxic effects on rat glioma cell and colon adeno carcinoma cell lines were evaluated. According to the cytotoxicity results, compounds 1j and 1l exhibited the highest cytotoxicity on the HT29 cell, while compounds 1e , 1g, and 1l showed the strongest cytotoxic effect on C6 cell line. Compound 1l , which carries the methoxy substituent at the 3 rd position on the phenyl ring, was effective against both cancer cells and showed the highest inhibitory effect on hCA II. The ADME/T properties and molecular docking of the molecules with the highest activity were examined.
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Unveiling the essential oil composition and bioactivities of Piper frustratum Boerl.

14. März 2025

Syarifah Nadhirah Wan Idrus, Wan Mohd Nuzul Hakimi Wan Salleh, Abubakar Siddiq Salihu, Mohd Hafiz Arzmi, Carlos L. Cespedes-Acuña

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This study aimed to investigate the chemical composition, and anticholinesterase and anti-tyrosinase activities of the essential oil extracted from the leaves of Piper frustratum Boerl., growing in Malaysia. Nineteen chemical components were identified using gas chromatography-flame ionization detection (GC-FID) and gas chromatography-mass spectrometry (GC-MS), accounting for 99.6 % of the essential oil. The identified major components include β-caryophyllene (12.6 %), β-asarone (10.7 %), myristicin (10.4 %), α-copaene (9.6 %), methyl eugenol (7.2 %), and β-cubebene (6.5 %). Anticholinesterase activity was assessed using the Ellman’s method, while anti-tyrosinase activity was evaluated against mushroom tyrosinase. The essential oil demonstrated moderate inhibitory activity against acetylcholinesterase (IC 50 value of 84.2 μg/mL), butyrylcholinesterase (IC 50 value of 98.5 μg/mL), and tyrosinase (IC 50 value of 95.4 μg/mL) enzymes. This study is the first to report the chemical composition and bioactivities of the essential oil obtained from P. frustratum , which may have implications on the characterization, pharmaceutical, and therapeutic applications of Piper essential oils.
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Design and synthesis of 3-(azepan-1-ylsulfonyl)-N-aryl benzamide derivatives as potent carbonic anhydrase IX inhibitors with anticancer activities

3. März 2025

Mohammad A. Khanfar, Mohammad Saleh

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Carbonic anhydrase IX (CAIX) is known to be overexpressed in various tumors and plays a significant role in tumor development and progression. A series of 3-sulfonamide benzoate derivatives with a 7-membered azepane ring were synthesized and evaluated for their CAIX inhibitory activities. Most of the synthesized compounds successfully inhibited CAIX activities, exhibiting IC 50 values in the low nanomolar range. The most potent CAIX inhibitor was compound 26 , with an IC 50 of 19 nM. A structure-activity relationship analysis of the synthesized compounds was conducted, and molecular docking revealed strong coordination with the catalytic Zn 2+ metal, hydrophobic interactions of the azepane ring with a hydrophobic pocket, and π-stacking interactions of the aryl ring with an aromatic surface. The three most active analogues ( 8 , 16 , and 26 ) were further tested for their antiproliferative activities in the NCI-60 human tumor cell lines screen. Notably, compound 16 (CAIX, IC 50 = 310 nM) demonstrated potent growth inhibitory effects against several cancer cell lines.
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Design and synthesis of new 1,3,4-thiadiazoles as antimicrobial and antibiofilm agents

3. März 2025

Betül Kaya, Ulviye Acar Çevik, Pervin Soyer, Mehmet Taha Yıldız, Yusuf Özkay, Zafer Asım Kaplancıklı

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This study assessed the in vitro antibacterial and antibiofilm properties of new 1,3,4-thiadiazole derivatives. 1 H NMR and 13 C NMR analyses were employed to confirm the structure of the synthesized compounds, the characterization is followed by assessments of their efficacy against Bacillus subtilis NRRL B478, Staphylococcus aureus ATCC 29213, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, as well as for antifungal activity against Candida albicans ATCC 90028 and Candida krusei ATCC 6258, using the broth microdilution method. Notably, among the tested compounds, compound 4a exhibited the highest antimicrobial activity, with a minimal inhibitory concentration of 125 μg/mL against P. aeruginosa ATCC 27853 and significant antibiofilm activity, achieving 94 %, 98 % and 100 % biofilm inhibition at 250, 500 and 1,000 μg/mL, respectively. Besides, compound 4h achieved 81 %, 89 % and 98 % S. aureus ATCC 29213 biofilm inhibition at 250, 500 and 1,000 μg/mL, respectively, and displayed potent antibacterial activity against this bacterium. Finally, the theoretical ADME properties of the compounds 4a - 4h were analyzed by calculations. This study has consolidated a base for the development of new antibacterial and antibiofilm agents and advanced our understanding of their potential mode of action against biofilm-associated infections.
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Enhancing vaginal drug delivery: the nanoemulsion gel strategy

27. Februar 2025

Biswajit Basu, Dipanjana Ash, Ayon Dutta, Rajdip Goswami, Swarnali Dutta, Kevin Garala, Gehan M. Elossaily, Devesh U. Kapoor, Bhupendra G. Prajapati

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In the 21st century, 75 % of women encounter vaginal malfunctions (cervicitis, mucoid ectopy, aerobic vaginitis, candidiasis, bacterial vaginosis, degenerated vaginitis, desquamative chronic vaginitis, and sexually transmitted infections) that clinically manifest as irritation, awkwardness, irregular bleeding, or evacuation. Vaginal drug delivery, an approach to treat the aforementioned diseases, primarily focuses on vaginal epithelium thickness, cyclic changes, vaginal secretions, mucus and enzymatic activity, pH, local microflora, and the presence of efflux transporters for their fabrication. There has been a growing interest in nanoemulsion gel for drug delivery to the vagina in comparison to conventional vaginal delivery systems (rings and gels). This review provides an in-depth examination of nanoemulsion gel formulation, highlighting key considerations such as the choice of vehicles, gel-forming agents, and permeation enhancers. It further explores formulation techniques, stability issues, and novel approaches like mucoadhesive and controlled-release systems. The biocompatibility and safety of nanoemulsion gels are also critically assessed, along with regulatory aspects. The paper underscores the growing significance of these formulations in the management of various vaginal conditions, including infections, hormonal therapies, and contraceptive applications. As nanoemulsion gels continue to evolve, their role in optimizing vaginal drug delivery systems offers considerable potential for improving therapeutic outcomes and patient compliance.
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Emerging silk sericin-based formulation fortified with therapeutics in the management of diabetic wound and skin tissue regeneration

21. Februar 2025

Biswajit Basu, Monosiz Rahaman, Sourav Ghosh, Swarnali Dutta, Ashwini Kumar, Swarupananda Mukherjee, Sudarshan Singh

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Sericin, a protein extracted from the cocoons of silkworms, has recently become an attractive biomaterial due to its potential as a good candidate for wound healing especially wounds seen in diabetic and immune-compromised patients. This review discusses the special biological nature of sericin such as its water-solubility and inherent moisturizing properties, antimicrobial, and antioxidant activities, which can act synergistically to foster ideal conditions for wound healing. The incorporation of sericin into composite wound dressings along with other natural and synthetic polymers was found to improve the mechanical properties, biocompatibility, and overall therapeutic performance. Moreover, the review draws attention toward sericin-based materials in diabetic wound healing with a focus on promoting rapid tissue regeneration and cell proliferation and enhancing clinical outcomes that conventional therapeutics cannot serve. The review also discusses the challenges associated with the production and application of sericin-based wound dressings and outlines the prospects for this emerging field. As research continues to advance, silk sericin holds the potential to revolutionize wound care, offering innovative solutions for the effective and holistic management of complex wounds.
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Exploring the therapeutic potential of leriodenine and nuciferine from Nelumbo nucifera for renal fibrosis: an In-silico analysis

11. Februar 2025

Rushendran Rapuru, Rukaiah Fatma Begum, S. Ankul Singh, Chitra Vellapandian, Nemat Ali, Abdullah F. AlAsmari, Bhupendra G. Prajapati

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A major problem in chronic kidney illnesses is renal fibrosis. This research investigates the therapeutic potential of compounds derived from Nelumbo nucifera (Lotus). Comprehensive screening identified these compounds, which exhibit promising binding affinities with key targets associated with renal fibrosis. Leriodenine and Nuciferine demonstrate substantial potential by modulating critical targets such as PTGS2, JUN, EGFR, STAT3, mTOR, and AKT1. The identified biomolecule-target-pathway network highlights the intricate interactions underlying the therapeutic effects of lotus seed compounds in renal fibrosis. Strong binding affinities with PTGS2-PDBID:5F19, Leriodenine −8.99 kcal/mol and Nuciferine −9.33 kcal/mol, and JUN-PDBID:1S9K, Leriodenine −7.95 kcal/mol and Nuciferine −7.05 kcal/mol are shown by molecular docking investigations, indicating their potential as fibrotic process inhibitors. During 10 ns of molecular docking simulations, these compounds demonstrated robust hydrogen-bonding connections within the protein’s active site, leading to a possible alteration in the conformation of the ligand-binding site. The research establishes the foundation for future experimental validation, clinical trials, to bridge the translational gap. The research combines target prediction, protein–protein interaction studies, and biomolecular screening to clarify the molecular pathways behind renal fibrosis. We also carried out Insilico molecular docking and carried out molecular dynamics simulation of the best compound identified to obtain more precise results.
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Antidiabetic activities of aerial part of Asparagus racemosus Willd. extract: an in vitro, in vivo, and in silico approach

10. Februar 2025

Priya Das, Ankrita Thapa, Suraj Mistri, Gouhar Jahan Ashraf, Sourav Sarkar, Debabrata Modak, Soumen Bhattacharjee, Ravi Kumar Singh, Tarun Kumar Dua, Paramita Paul, Gouranga Nandi, Ranabir Sahu

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Asparagus racemosus Willd., a significant medicinal plant in India’s Darjeeling Himalayan region. The current study aims to assess the antidiabetic efficacy of the aerial part of Asparagus racemosus Willd. utilizing a streptozotocin-nicotinamide-induced diabetic rat model. The methanolic extract of plant (ARME) was evaluated for in vitro antidiabetic activity through α-glucosidase and α-amylase enzyme suppression assay and assessed in vivo in a streptozotocin-induced rat model. A 21-day chronic multiple-dose study of ARME was examined. STZ-induced diabetic rats were treated with metformin (70 mg/kg) and ARME at concentrations of 200 and 400 mg/kg. It was discovered that ARME inhibited the activities of α-amylase and α-glucosidase and showed potent therapeutic effects on the rat’s model. ARME helps raise body weight, hemoglobin, and other blood counts and normalizes the serum parameters in the diabetic group. In addition, liver tissues’ abnormal levels of the antioxidant enzymes glutathione and lipid peroxides were returned to those of control animals. HPTLC study revealed the presence of stigmasterol, which showed a strong affinity for the proteins linked to diabetes mellitus through in silico study. As a result of these findings, ARME inhibits the activity of digestive enzymes and has antioxidant and antihyperglycemic effects in STZ-nicotinamide-induced diabetic rats.
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Cutting-edge developments in agro-waste derived carbon nanomaterials and their multifaceted applications in agriculture: enhancing crop imaging, nutrient efficiency, and plant health

10. Februar 2025

Tanima Bhattacharya, Tanmoy Das, Subham Preetam, Hitesh Chopra

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The rising global population is a contributing factor to the exponential rise of agricultural output. Agro-wastes are now recognized as a substitute substance to produce sustainable, affordable, and renewable bio-based products. Abundant farm products due to a lack of processing capacity or storage room are frequently lost. A substantial amount biopolymer is present in agricultural residues. It’s interesting that nanotechnology has the potential to more easily convert agricultural wastes into valuable and affordable products, eliminating the need to use toxic chemicals, which can lead to a variety of health and environmental problems. Recently, there has been a rise in interest in environmentally beneficial carbon nanomaterial (CNM) manufacturing methods that make use of agricultural waste extracts. Therefore, the goal of this review is to look into the various agro-waste sources, synthesis techniques of CNMs, characterization methods, surface functionalization chemistry, mechanistic approach and potential applications in imaging crops, nutrient utilization, and upgradation of crop health.
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Biogenic selenium nanoparticles: a comprehensive update on the multifaceted application, stability, biocompatibility, risk, and opportunity

10. Februar 2025

Pooja V. Nagime, Vinay Kumar Pandey, Charu Rajpal, Titilope John Jayeoye, Ashwini Kumar, Vijay R. Chidrawar, Sudarshan Singh

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Biogenic selenium nanoparticles (SeNPs) have emerged as promising area of research due to their unique properties and potential multifaceted applications. The biosynthesis of SeNPs through biological methods, such as using microorganism, plant extracts, etc., offers a safe, eco-friendly, and biocompatible approach, compared to traditional chemical synthesis. Recent several studies demonstrated that multifaceted application of SeNPs includes a broad area such as antibacterial, anticancer, antioxidant, antiviral, anti-inflammatory, antidiabetic, and excellent wound healing activity. On the other hand, SeNPs have also shown promising application in sensing of inorganic toxic metals, electrochemistry, agro-industries, aqua-cultures, and in fabrication of solar panels. Additionally, SeNPs capability to enhance the efficacy of traditional antibiotics and act as effective agents against multidrug-resistant pathogens has shown their potential in addressing critical health challenges. Although, the SeNPs exhibit wide applicability, the potential toxicity of Se, particularly in its various oxidative states, necessitates careful assessment of the environmental and health impacts associated with their use. Therefore, understanding the balance between their beneficial properties and potential risks is crucial for its safe applications. This review focuses exclusively on SeNPs synthesized via eco-friendly process, excluding research utilizing other synthesis processes. Moreover, this review aims to offer an overview of the diverse applications, potential risks, stability requirement, and cytocompatibility requirement, and multifaceted opportunities associated with SeNPs. Ultimately, the review bridges a gap in knowledge by providing an updated details of multifaceted applications of SeNPs.

Special Issue: CAZymes Structural and functional aspects of Glycoside Hydrolases and Glycosyl Transferases; Editors: Maria-Ortiz Soto and Jürgen Seibel

Special Issue: Chitin Structures and Pathways as Targets for Biopesticides and Drugs; Guest Editor: Klaus H. Hoffmann

Special Issue: Organic Chemistry and Medicinal Applications This issue is dedicated to the memory of Professor Wolfgang Voelter; Guest Editors: Raid Abdel-Jalil and Raphael Stoll

Special Issue: Essential oils; Editor: Klaus H. Hoffmann

Special Section: Chemistry of Social Insects / Special Section Editor: Wilhelm Boland

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Special Issue: Chemo-enzymatic cascade reactions / Editor: Uwe T. Bornscheuer

Special Issue: Insect Biotechnology / Editor: Klaus H. Hoffmann

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The Special Section is dedicated to the memory of Professor Lothar Jaenicke / Editor: Wilhelm Boland

This issue is dedicated to the memory of Professor Peter Böger / Editors: Nikolaus Amrhein, Gerhard Sandmann

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Prof Dr. Jürgen Seibel, Institute of Organic Chemistry, University of Würzburg, Germany

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Prof Dr. Achim Aigner, Rudolf Boehm-Institute for Pharmacology and Toxicology, Clinical Pharmacology, Leipzig University, Germany
Prof Dr. Wilhelm Boland, Department of Bioorganic Chemistry, Max Planck Institute for Chemical Ecology, Germany
Prof Dr. Uwe T. Bornscheuer, Department of Biotechnology & Enzyme Catalysis, Institute of Biochemistry, University of Greifswald, Germany
Prof Dr. Klaus H. Hoffmann, Department of Animal Ecology I, University of Bayreuth Animal Ecology I, Germany

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Prof Dr. David B. Berkowitz, Department of Chemistry, University of Nebraska, USA
Prof Dr. Birgit Dräger, Department of Pharmaceutical Biology and Pharmacology, Institute of Pharmacy, Faculty of Natural Sciences i, Martin Luther University Halle-Wittenberg, Germany
Prof Dr. Marcia González-Teuber, Departamento de Química Ambiental, Facultad de Ciencias, Universidad Católica de La Santísima and Departamento de Genética Molecular y Microbiología, Facultad de Ciencias Biológicas, Pontificia Universidad Católica de Chile, Chile
Prof Dr. Srivatsan Seergazhi Gopalan, Department of Chemistry, Indian Institute of Science Education and Research, Pune, India 　
Prof Dr. Jikai Liu, School of Pharmaceutical Sciences, South-Central University for Nationalities, China
Prof Dr. Till Opatz, Johannes Gutenberg University Mainz, Department of Chemistry, Germany
Prof Dr. Esther S. Rösch, Faculty of Engineering, Baden-Württemberg Cooperative State University Karlsruhe, Germany
Prof Dr. Klaus-Dieter Spindler, Institute for General Zoology and Endocrinology, Ulm University, Germany
Prof Dr. Dieter Strack, Institut für Pharmazeutische Biologie, Technische Universität Braunschweig, Germany

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1865-7125

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0939-5075

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Erstveröffentlichung:

20. Februar 1973

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eISSN: 1865-7125

ISSN: 0939-5075

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