Band 80, Heft 11-12

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.