Protective effect of Vitex altissima L.f. bark extract on cisplatin-induced renal injury in Wistar rats

Cisplatin (CP) is a commonly used chemotherapeutic drug. The major limiting factor in the use of CP is the side effects in normal tissues, including the kidney. Since ancient times, medicinal plants are rich sources of various bioactive constituents used to treat multiple ailments, including drug toxicities. The present work is a preliminary study to explore the renoprotective actions of methanolic extract of Vitex altissima L.f. bark (Va) against CP-induced renal damage in Wistar rats. Va was found to have potent radical scavenging activity than metal ion reducing power properties, compared with ascorbic acid. Further, Va was evaluated for nephroprotective activity in rats induced by CP (8 mg/kg; intraperitoneal) on the 7th day. The animals were grouped (n = 6) and treated with Va (100 and 200 mg/kg) orally for 14 days. The outcomes of the study found that CP significantly (P < 0.001) altered the oxidative stress markers (MDA, SOD and CAT), serum urea and creatinine levels. The administration of Va significantly halted the toxic condition and maintained it towards normal levels. The higher dose of Va significantly (P < 0.001) raised the SOD and CAT levels and halted the MDA levels than the low dose. Also, a higher dose of Va maintained the normal integrity of the histopathological studies of kidneys than a low dose. The present study demonstrates that V. altissima can attenuate the oxidative stress induced by CP by enhancing the endogenous antioxidant levels and depleting the lipid peroxidation levels

Isolation, characterization, and biological evaluation of flavonols and 1,2-diphenylethanes from Bauhinia vahlii

312-319In this study, three known flavonols, namely kaempferol (1), ombuin (2), and quercetin (3), and three known 1,2-diphenylethanes, namely 5-(2-hydroxyphenethyl)-3-methoxy-2-methylphenol (4), 2-(3,5-dimethoxyphenethyl) phenol (5) and 2-(2-hydroxyphenethyl)-4,6-dimethoxyphenol (6) from the methanolic extract (ME) of Bauhinia vahlii were identified and sucessfully isolated. They were also evaluated for in vitro antioxidant, anti-inflammatory, anti-gout and anticancer effects. Compound 3 (26.00±2.17 µg/mL) showed an almost equivalent IC50 value of standard drug (25.55±2.80 µg/mL) against superoxide free radicals. Moreover, compound 3 showed significant inhibition of COXs and 5-LOX enzymes, while compounds 1, 2, 4 and 5 exhibited good inhibition of XO enzymes. Except for compound 5, all compounds showed a significant reduction of cell growth lysis of MCF-7, DLD-1, HeLa, and A549. Besides, all the metabolites and ME showed a very weak degree of specificity against NHME, indicates less toxicity to normal cells. The results suggest that B. vahlii can be a favourable natural source for the treatment of oxidative stress, inflammation, gout and cancer, and these actions are linked to the natural active compounds 1, 3, 4 and 6

Isolation, characterization, and biological evaluation of flavonols and 1,2-diphenylethanes from Bauhinia vahlii

In this study, three known flavonols, namely kaempferol (1), ombuin (2), and quercetin (3), and three known 1,2-diphenylethanes, namely 5-(2-hydroxyphenethyl)-3-methoxy-2-methylphenol (4), 2-(3,5-dimethoxyphenethyl) phenol (5) and 2-(2-hydroxyphenethyl)-4,6-dimethoxyphenol (6) from the methanolic extract (ME) of Bauhinia vahlii were identified and sucessfully isolated. They were also evaluated for in vitro antioxidant, anti-inflammatory, anti-gout and anticancer effects. Compound 3 (26.00±2.17 µg/mL) showed an almost equivalent IC50 value of standard drug (25.55±2.80 µg/mL) against superoxide free radicals. Moreover, compound 3 showed significant inhibition of COXs and 5-LOX enzymes, while compounds 1, 2, 4 and 5 exhibited good inhibition of XO enzymes. Except for compound 5, all compounds showed a significant reduction of cell growth lysis of MCF-7, DLD-1, HeLa, and A549. Besides, all the metabolites and ME showed a very weak degree of specificity against NHME, indicates less toxicity to normal cells. The results suggest that B. vahlii can be a favourable natural source for the treatment of oxidative stress, inflammation, gout and cancer, and these actions are linked to the natural active compounds 1, 3, 4 and 6

A comparative study on synthesis of some novel α,β-unsaturated carbonyl derivatives and their antioxidant potential

Free radicals are constantly formed in human system either as accidental products during metabolism or deliberately during the process of phagocytosis or due to environmental pollutants, ionizing radiations, ozone, heavy metal poisoning, etc. It is found from literature survey that chalcones (α,β-unsaturated carbonyl derivatives) exhibit great antioxidant activity. Hence, the synthesis of some new chalcone derivatives was undertaken and were synthesized by two methods namely, conventional and microwave irradiation methods. The synthesized chalcone derivatives were tested for their in vitro antioxidant activity by using NBT-superoxide free-radical scavenging activity and DPPH radical scavenging activity. The potency of the chalcone derivatives was estimated by IC50 values and they have shown promising antioxidant activity. Among all the chalcones synthesized, derivative 3e showed maximum superoxide inhibition as per NBT method and all the derivatives have shown different percentage inhibitions at different concentrations as per  DPPH method. The compounds were characterized by 1H NMR and IR spectral analysis

In silico molecular docking studies of di hydro pyrimidinones as MTB thymidylate kinase inhibitors

Tuberculosis is the one of the leading cause of death. Efforts are needed to develop new anti-tuberculosis medicines with alternative scaffolds because the current antibiotics are increasingly becoming ineffective against M. tuberculosis. In this study, 21 novel di hydro pyrimidinone derivatives were designed and synthesized to arrive at potentially effective anti-tubercular agents. Molecular docking studies were conducted on Mtb thymidylate kinase of Mycobacterium tuberculosis H37Rv (PDB ID 5NQ5). The enzyme active sites were docked with the title compounds after they were energy-minimized. According to their docking scores and binding energies, the ligands were ordered. The molecular docking results for the title compounds with Mycobacterium TB thymidylate kinase are very promising. Thymidylate kinase appears to be inhibited by 17c and 20c, according to the study

Microwave-assisted synthesis, structural activity relationship and biological activity of some new quinoxaline Schiff base derivatives as highly potent spirochete bactericidal agents

The main aim of this work was to synthesise a new (E)-3-(4-or3-Aminophenylimino) quinoxaline-2(3H)-one oxime Schiff base derivatives and evaluate the anti-leptospiral activity against Leptospira icterohaemorrhagiae. The mentioned derivatives were prepared by performing microwave-assisted condensation reactions of (E)-3-(4-or3-Aminophenyl imino)quinoxaline-2(3H)-one and aromatic aldehydes. The structures of these interesting compounds were characterised by FT-IR, 1H NMR and mass spectroscopy. Furthermore, these compounds were screened for spirocidal activity against Leptospira icterohaemorrhagiae by using in vitro and in vivo method. The anti-leptospiral activity result reveals that most of the compounds were exhibiting considerable activity against Leptospira icterohaemorrhagiae. Compound 6c demonstrated remarkable activity at low concentration against the Leptospira icterohaemorrhagiae as compared to the standard drugs

Synthesis, spectroscopic characterization, X-ray crystallography, structural activity relationship and antimicrobial activity of some novel 4-(5-(10-(3-N, N-dimethylamino)propyl)-10H-phenothiazine-3-yl)-1, 3, 4-thiadiazole-2-yl) Azo dye/Schiff base derivatives

In the present investigation, a series of novel 4 (5-(10-(3-(N,N-dimethylamino)propyl)-10H-phenothiazine-3-yl)-1,3,4-thiadiazo-2-yl) Azo dye/Schiff base derivatives (5a-e & 6a-j) were synthesised by performing diazotization followed by coupling reaction between 4-(5-(10-(3-(N,N-dimethylamino)propyl)-10H-phenothiazine-3yl)-1,3,4-thiadiazole-2-amine, sodium nitrite, Con HCl and the different coupling reagent/condensation reaction of 4-(5-(10-(3-(N,N-dimethylamino)propyl)-10H-phenothiazine-3yl)-1,3,4-thiadiazole-2-amine and different aromatic aldehyde. The structures of these compounds were confirmed by FT-IR, 1H NMR, Mass spectroscopy and elemental analysis. In vitro antibacterial and antifungal activities of these compounds were screened against the different strains such as P. Aeruginosa (ATCC-2853), E. Coli (ATCC-25922), S. Epidermidis (ATCC-155), A. Fumigatus (ATCC-46645), S. Aureus (ATCC-9144), A. Niger (ATCC-9029) by disc diffusion and minimum inhibitory concentrations (MIC) method. The results revealed that compound N-(4-chlorobenzylidene)-5-(10-(3-(N,N-dimethylamino)propyl)-10H-phenothiazine-3yl)-1,3,4-thiadiazole-2-amine (6d) showed promising anti-microbial activity against various pathogenic microorganisms as compared to the antibiotics Ciprofloxacin and Fluconazole

Synthesis and spectroscopic characterisation of novel bioactive molecule of 3-(2-substituted)-1H-indol-3-yl)-1-(thiophen-2yl)prop-2-en-1-one chalcone derivatives as effective anti-oxidant and anti-microbial agents

The chief purpose of this work was to synthesise and find out the anti-oxidant and anti-microbial activities of novel 3-(2-substituted)-1H-indol-3-yl)-1-(thiophen-2yl)prop-2-en-1-one chalcone derivatives. These derivatives were prepared by performing Claisen–Schmidt condensation reaction of 1-(thiophen-2yl)ethanone and 2 substituted 1H-indole-3-carbaldehyde with constant stirring (approximately for 3 hours) in the presence of ethanol and potassium hydroxide. The newly synthesised compounds' anti-oxidant and anti-microbial activities have been identified by using DPPH radical scavenging assay, zone of inhibition and minimum inhibitory concentration. Most of the prepared compounds had shown excellent anti-oxidant and anti-microbial activities as compared to the standard drugs like Ascorbic acid, Ciprofloxacin and Fluconazole. Among the synthesised compounds, compounds 4e, 4h and 4a showed remarkable activity at low concentration. Therefore, these compounds deserve further research