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Objective: The main objective of this work is to synthesize thiobarbituric acid based bis-Schiff base derivatives and to evaluate their ability to inhibit urease enzyme and DPPH free radical scavenging potential. Methods: Thiobarbituric acid derived bis-Schiff bases (IIIa–IIIi) were synthesized by treating 2,4-dihydroxybenzaldehyde and the starting moiety 1,3-diethyl-2-thiobarbituric acid in ethanol through refluxed followed by treating chloro ethyl acetate in DMF solvent. Subsequently, hydrazine hydrate was added to compound (II), yielding bis-hydrazide in better yield, which was further reacted via refluxed with benzaldehydes in ethanol, catalyzed by acetic acid to yield compounds (IIIa–IIIi) in excellent yields. Results: The resulting compounds were tested to inhibit urease enzyme and DPPH free radical scavenging activity. Among the series, compound (IIId) (IC50 = 16.11 ± 0.92 µM), (IIIc) (IC50 = 19.11 ± 0.55 µM), and (IIIf) (IC50 = 21.01 ± 1.42 µM) were found as promising lead urease inhibitors, stronger than the standard thiourea (IC50 = 21.15 ± 0.32 µM). Moreover, compound (IIIa) (IC50 = 40.21 ± 0.12 µM) was found as the excellent antioxidant agent comparing it with the standard ascorbic acid. Molecular docking study was performed to analyze the most potent compounds against urease enzyme. The results also shows that all compounds had good ADME properties there was no violation found in compounds ranges all are under druglikness criteria. Additional research combining in vivo, toxicological, and computational analyses can offer thorough understandings of the effectiveness, safety, and fundamental mechanisms of action of these potentially beneficial antioxidant substances. Conclusions: These compounds showed tremendous potential as DPPH free radical scavengers and urease enzyme inhibitors. Compound (IIId) demonstrated the greatest suppression of urease enzyme activity, however compound (IIIa) displayed superior antioxidant effects. Additional research, incorporating in vivo, toxicological, and computational examinations, is necessary to thoroughly assess the effectiveness, safety, and fundamental mechanisms of action of these intriguing antioxidant molecules. [ABSTRACT FROM AUTHOR]

Galium species are used worldwide for their antioxidant, antibacterial, antifungal, and antiparasitic properties. Although this plant has demonstrated its antitumor properties on various types of cancer, its biological activity on cutaneous melanoma has not been established so far. Therefore, the present study was designed to investigate the phytochemical profile of two extracts of G. verum L. herba (ethanolic and ethyl acetate) as well as the biological profile (antioxidant, antimicrobial, and antitumor effects) on human skin cancer. The extracts showed similar FT-IR phenolic profiles (high chlorogenic acid, isoquercitrin, quercitrin, and rutin), with high antioxidant capacity (EC50 of ethyl acetate phase (0.074 ± 0.01 mg/mL) > ethanol phase (0.136 ± 0.03 mg/mL)). Both extracts showed antimicrobial activity, especially against Gram-positive Streptococcus pyogenes and Staphylococcus aureus bacilli strains, the ethyl acetate phase being more active. Regarding the in vitro antitumor test, the results revealed a dose-dependent cytotoxic effect against A375 melanoma cell lines, more pronounced in the case of the ethyl acetate phase. In addition, the ethyl acetate phase stimulated the proliferation of human keratinocytes (HaCaT), while this effect was not evident in the case of the ethanolic phase at 24 h post-stimulation. Consequently, G. verum l. could be considered a promising phytocompound for the antitumor approach of cutaneous melanoma. [ABSTRACT FROM AUTHOR]

Endophytic fungi in medicinal plants have the capacity to produce bioactive compounds whose features have great identity or similarity with the phytohosts. Since Asclepias curassavica has been known to possess a broad range of biological activities, we sought to obtain the active endophytic fungi from this plant. We performed the study followed the idea of “ethnic drug-endophytic fungi-active ingredients”, and thereafter we examined the bioactivities of fungal metabolites from 168 strains of endophytic fungi isolated from A. curassavica. To evaluate the biological activities of anti-tumor, anti-inflammatory, anti-α-glucosidase and anti-oxidant in these fungi, the ethyl acetate extracts from fermentation broth of endophytic fungi were first determined using the methods of SRB, Griess, PNPG and DPPH, respectively. Furthermore, we identified the bioactive fungal strains with conserved ITS sequencing. The results were as follows:(1) A total of 22 in 168 isolated strains had variable biological activities. Nine strains had obvious anti-tumor effect with the IC50 values of 0.1-40 μg·mL-1. Further, the strain MJF-53 displayed prominent inhibitory effects on the release of both NO and IL-1β in Raw264.7 cell line by LPS- induction under the concentration of 2.5 μg·mL-1. There were seven strains showing α-glucosidase inhibitory activity with the IC50 values ranging from 1.0 to 4.0 mg·mL-1, especially, the inhibitory activities of MYF-16 and MYF-55 were close to acarbose; 19 endophytic fungi had different degrees of DPPH free radical scavenging activities, among which MYF-9, MYF-19 and MJF-84 showed moderate anti-oxidant activities with IC50 values of 13.562, 17.776 and 12.395 μg·mL-1 respectively.(2)The ITS identification showed that the 22 active strains were mainly distribute in six genera: Alternaria sp., Colletotrichum sp., Fusarium sp., Diaporthe sp., Talaromyces sp. and Neofusicoccum sp. This study indicates that the bioactivities of the endophytic fungi from A. curassavica are diverse, which lays a foundation for exploring new potential natural anti-tumor, anti-inflammatory, hypoglycemic and anti-oxidant compounds from the endophytic fungi of A. curassavica. [ABSTRACT FROM AUTHOR]

Neptunia oleracea Lour. is a tropical plant cultivated in Southeast Asia. It is consumed as vegetable and traditional herb for the treatment of several disorders. The objective of the present work was to isolate the phenolic compounds from N. oleracea, followed by their bioactivity evaluation and quantitative analysis. The ethyl acetate (EtOAc) and methanol (MeOH) fractions of N. oleracea were subjected to various chromatographic techniques to isolate the phenolic compounds. The isolated phenolic compounds were characterised by several spectroscopic methods, including mass spectrometry (MS) and nuclear magnetic resonance (NMR). Then, these compounds were subjected to DPPH free radical scavenging as α-glucosidase inhibitory assays for the evaluation of their activities. Their contents in the fractions were analysed via high performance liquid chromatography (HPLC) quantitative analysis. Five phenolic compounds including quercetin-3-O-β-D-xylopyranoside (1), quercetin-3-O-α-Larabinopyranoside (2), quercetin-3-O-α-L-rhamnoside (3), methylgallate (4) and rutin (5) were isolated from N. oleracea for the first time. Evaluation on the DPPH free radical scavenging and α-glucosidase inhibitory activities of these compounds showed that methylgallate (4) was the most potent antioxidant and α-glucosidase inhibitors among them, with IC50 values of 17.25 and 50.76 μM, respectively. The HPLC quantitative analysis revealed the high content of the quercetin derivatives (compounds 1, 2 and 3) in the EtOAc fraction (ranging from 125.68 to 157.55 μg/mg) and methylgallate (4) in the MeOH fraction (75.25 μg/mg). Comparison of the bioactivities of the isolated phenolic compounds with the fractions indicated their significant contribution for the DPPH free radical scavenging of N. oleracea; while they might be working synergistically for the α-glucosidase inhibitory activity. The results of the present work could help to validate the contribution of phenolic compounds for the studied bioactivities of N.oleracea. [ABSTRACT FROM AUTHOR]