Band 77, Heft 7-8

In the current study, five different plants, Syzygium Cumini , Fagonia cretica , Acacia modesta , Withania coagulans , and Olea europaea aqueous extracts were prepared and applied against the anticancer and antibacterial activities. It was observed that O. Europaea extract shows the highest anticancer activity with cell viability of 21.5%. All the five plants extract was also used against the inhibition of Bacillus subtilis where O. Europaea extract shows a promising inhibitory activity of 3.2 cm followed by W. coagulans . Furthermore, W. coagulans was subjected to the process of column chromatography as a result a withanolide was isolated. The fast atom bombardment mass spectrometry (FAB-MS) and high resolution fast atom bombardment (HRFAB-MS) [M + 1] indicated molecular weight at m/z 453 and molecular formula C 28 H 37 O 5 . The UV–Vis. spectrum shows absorbance at 210 nm suggesting the presence of conjugated system, and Fourier-transform infrared spectroscopy (FTIR) was recorded to explore the functional groups. Similarly, 1D and 2D NMR spectroscopy techniques such as 1 H, 13 C NMR, correlation spectroscopy (COSY-45°), heteronuclear single quantum correlation (HSQC), heteronuclear multiple bond correlation (HMBC) and Nuclear Overhauser effect Spectroscopy (NOESY) techniques was carried out to determine the unknown natural product. The collective data of all these techniques established the structure of the unknown compound and recognized as a withanolide.

Further investigation of the residual bioactive compounds produced by the soft coral Sarcophyton glaucom -derived Penicillium sp. MMA afforded five new compounds assigned as 9-methoxy-penicyrone A ( 1 ), 9-methoxy-penicyrone B ( 2 ), 3-hydroxy-2,2,4-trimethyl-pentyl ester ( 3 ), 3-hydroxy-1-isopropyl-2,2-dimethyl-propyl ester ( 4 ), and 3-isobutyryloxy-2,2,4-trimethyl-pentyl linoleate ( 5 ). Additional six known compounds were isolated: penicyrones A–B ( 6 , 7 ), 4-(2-hydroxy-3-butynoxy)benzoic acid ( 8 ), cyclopenol ( 9 ), aspermytin A ( 10 ), and aurantiomide A ( 11 ). Structures of the new compounds ( 1–5 ) were identified by 1D ( 1 H & 13 C) and 2 D ( 1 H– 1 H COSY, HMBC and NOESY) NMR and HRESI-MS spectroscopic data. Biologically, the antimicrobial activities of the obtained compounds were studied as well.

Novel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory and cytotoxic properties. 4-(2-chloroacetyl)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one were reacted with α-hydroxy aldehyde or α-hydroxy ketone derivatives to obtain nine novel pyrazolone derivatives. Structures were successfully elucidated by 1 H NMR, 13 C NMR, IR and HRMS. Enzyme inhibitory activity was measured on cyclooxygenases (COXs) as considered to address anti-inflammatory activity. Compound 2 showed the highest activity on both COX-1 and COX-2 subtypes with 12.0 μM and 8.0 μM IC 50 , respectively. This activity was found close to indomethacin COX-2 inhibition measured as 7.4 μM IC 50 . Rest of the compounds ( 1 , 3 – 9 ) showed 10.4–28.1 μM IC 50 on COX-2 and 17.0–35.6 μM IC 50 on COX-1 (Compound 1 has no activity on COX-1). Tested compounds ( 1–9 ) showed activity on NO production. Only compound was the 4 , which showed a low inhibition on IL-6 levels. Cell viability was up to 60% at 100 μM for all compounds ( 1 – 9 ) on RAW 264.7 and NIH3T3 cell lines, thus compounds were reported to be noncytotoxic.

Exposure to ultraviolet (UV) radiation is the main reason behind extrinsic skin aging. Changes due to chronic UV exposure are called photoaging. Natural products are effective ingredients against UV-mediated skin damage. Present study investigated the anti-photoaging properties of  Camellia japonica flowers which possess various bioactivities. To enrich the extracts of C. japonica flowers, pectinase and beta-glucosidase treatment was employed. Anti-photoaging effect was screened using the changes in MMP-1 and collagen levels in UVA-irradiated human HaCaT keratinocytes. The crude extract of C. japonica flowers (CE) was shown to decrease the UVA-induced MMP-1 secretion while attenuating the collagen levels. Pectinase and beta-glucosidase treated CE (ECE) showed increased anti-photoaging effects against UVA-induced changes in MMP-1 and collagen production. Camellenodiol (CMD), a known triterpenoid from C. japonica , isolated as the active ingredient of ECE and its anti-photoaging effect was screened. Results showed that CMD ameliorated the UVA-induced deterioration in collagen levels by suppressing MMP-1 production in transcriptional level. CMD treatment downregulated the phosphorylation of p38, ERK, and JNK MAPKs along their downstream effectors, c-Fos, and c-Jun. In conclusion, enzyme-assisted extraction of C. japonica flowers was suggested to enhance the anti-photoaging properties suggestively through high bioactive content such as CMD.

Point of care testing (PoCT) devices permit precise and rapid detection of disease-related biomarkers contributing to an early disease diagnosis and administration of an appropriate treatment. The enzyme myeloperoxidase (MPO) is a relevant biomarker for infection and inflammation events assessment; however its direct electrochemical quantification is hindered by the limited accessibility to the iron atom in its active center. Herein, such hindrance of the MPO biomolecule is overcome using the redox mediator 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS). The charge involved in the electrochemical reduction of the MPO-oxidized ABTS is correlated with the concentration of MPO. The use of ABTS allowed for the electrochemical assessment of a wide range of MPO concentrations (10–1000 nM) including those reported for wound infections, chronic obstructive pulmonary disease and early adverse cardiac events. The developed electroanalytical approach is rapid and inexpensive, and thus suitable for implementation in PoCT devices.

Scopoletin, also known as 6-methoxy-7 hydroxycoumarin, is one of the naturally occurring coumarin commonly found in many edible plants and plays an important role in human health. Despite the various potential pharmacological properties, the biosynthesis process, method of extraction, and mechanism of action on this compound have not been documented well. In this current review, the biosynthesis pathway, distribution of scopoletin in the plant kingdom, and extraction techniques are elaborated. The in vitro , in vivo , and in silico pharmacological studies are also discussed on antioxidant, antimicrobial, anticancer, anti-inflammation, and neuroprotective aspects of scopoletin. This study may help to understand the benefit of scopoletin containing plants and would be beneficial for the prevention and treatment of diseases.

Although Z -2-oxo-4-methyl-3-pentene-1,5-dioic acid ( Z -OMPD) has been identified as a major dicarboxylic acid in tulip tissues, its biosynthetic pathway has not been elucidated. Herein, Z -OMPD was isolated from tulip leaves and chemically synthesized. Comparisons of these samples revealed that Z -OMPD exists as a tautomeric mixture at physiological pH. As a regioisomer of Z -OMPD, we enzymatically and chemically prepared 4-methylene-2-oxo-glutaric acid (4-MEOG) for the first time. Using these compounds as standards, the occurrence of Z -OMPD and 4-MEOG in various tissues of the tulip cultivar “Murasakizuisho” was evaluated directly and by 2,4-dinitrophenylhydrazone derivatization. Z -OMPD was found to be abundant in the aerial tissues, whereas 4-MEOG was almost absent from all tissues. Stability analyses of Z -OMPD and 4-MEOG revealed that no double bond isomerization occurred at physiological pH, suggesting that enzyme systems are responsible for Z -OMPD biosynthesis in tulip tissues.

Matricaria aurea (Loefl.) Schultz Bip. (Asteraceae), known as golden chamomile, has been traditionally used for the treatment of various diseases. In this study, total phenolic, flavonoid, and tannin contents of total extract and different fractions of this plant were determined. The antioxidant, cytotoxic, and antimicrobial activities were also evaluated. Moreover, the phenolic profiles of selected fractions were determined by HPLC and LC-MS/MS analysis. Results demonstrated total phenolic contents of 37.8–57.2 mg GAE/g and total flavonoid contents of 3.0–111.2 mg QE/g. The ethyl acetate and methanol fractions (EF and MF) had the highest concentrations of phenolic, tannin, and flavonoid compounds. In both DPPH radical scavenging assay and phosphomolybdenum reduction assay, EF showed the best antioxidant activity, followed by MF. EF and MF indicated also the best antibacterial activities against Bacillus subtilis (MIC 1.56 and 12.5 mg ml −1 ) and Staphylococcus aureus (MIC 0.78 and 12.5 mg ml −1 ). Hexane fraction (HF) had no antibacterial effect. None of the samples had antifungal effect. MTT (3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay revealed for EF and HF the highest antiproliferative activities (IC 50 values ranged from 111.8 to 294.6 μg ml −1 ). The presence of chlorogenic acid, ferulic acid, and luteolin-7-O-glucoside in MF, and p-coumaric acid in EF was confirmed and quantified.

Nanostructures have distinctive chemical and physical features owing to their surface area and nanoscale size. In this study, silver nanoparticles were synthesized using curcumin, a medicinally valuable natural product. The structure of curcumin-mediated silver nanoparticles (c-AgNPs) was identified by extensive spectroscopic techniques. The maximum absorption was observed at 430 nm in UV–Vis spectrum. The crystal structure of c-AgNPs was identified by XRD. The morphology of the structure was determined by SEM image. The particle size was found as 51.13 nm. The functional groups of curcumin and c-AgNPs were established by FTIR spectroscopy. Cytotoxic activity of c-AgNPs was carried out using A549, DLD-1, and L929 with MTT assay. c-AgNPs revealed excellent activity on DLD-1 cell lines and A549 cell lines at 1.0 mg/mL concentration with the lethal effect of 80%. However, nanoparticles did not show the considerable effect on L929. Moreover, they induced apoptosis. Consequently, c-AgNPs are a promising material for anticancer drugs candidate.

Since the identification of the genomic sequence of SARS-CoV-2, an unprecedented effort is being made until this date for the development of a safe and effective vaccine by pharma companies and laboratories worldwide. To attain herd immunity and quite possibly recover from this pandemic, which has claimed the life of about 4.23 million people, an exceptional effort has been made by the scientific community for the development of a vaccine. Various vaccines have been developed based on different platforms and each of them seems to possess its own merits and demerits based on its safety, immunogenicity, the durability of immunity, dosing schedule, technological platform, and ease of manufacture and transport. Based on these parameters this review aims to critically assess the efficacy of Covaxin and compare it with other vaccines in the WHO EUL list and perform a comparative analysis of COVID-19 vaccines which are in phase 3 and phase 4 of clinical trials. This will help us determine where COVAXIN stands against other vaccines and vaccine candidates based on these parameters which will ultimately help us determine the best vaccine that could potentially eradicate the COVID-19 pandemic.