Click-chemistry-inspired synthesis of new series of 1,2,3-triazole fused chromene with glucose triazole conjugates: Antibacterial activity assessment with molecular docking evaluation.

A series of new 1,2,3-triazole fused chromene based glucose triazole conjugates were synthesized from chromene fused 1,2,3-triazolyl extended alkyne and 2,3,4,6-tetra-O-acetyl-ß-d-glucopyranosyl azide in good to excellent yield by a copper catalyzed azide-alkyne cycloaddition (CuAAC) reaction. The major advantages include mild reaction conditions, high yield, good substrate scope, and shorter reaction time. The antibacterial efficacy of the compounds were assessed in vitro against human pathogenic Gram-negative E. coli and Gram-positive S. aureus bacteria. Compound 24j was found to be the most potent molecule with zone of inhibition (ZI) of 17 mm and minimum inhibitory concentration (MIC) of 25 µg mL-1 in E. coli and ZI of 16 mm and MIC of 25 µg mL-1 in S. aureus. Also, it significantly inhibited E. coli DNA-gyrase in silico with a binding affinity of -9.4 kcal/mol. Among all the synthesized compounds, 24i, 24d, 24e and 24f showed significant antibacterial activity against both strains and inhibited DNA-gyrase in silico with good binding affinities. Hence, these 1,2,3-triazole fused chromene based glucose triazole conjugates may evolve to be powerful antibacterial agents in recent future, according to structure-activity relationships based on strong antibacterial properties and molecular docking studies.

Hypoxia: A cause of acute renal failure and alteration of gastrointestinal microbial ecology.

Oxygen is very important to the existence of life. Oxygen deficiency, defined as hypoxia, elicits adaptive responses in cells and tissues. Lower oxygen concentration can cause the alteration of renal function, affects the maintenance of a balance of the body fluids, electrolytes, pH, and blood pressure homeostasis. Impaired fluid regulation could, in addition, contribute to the precipitation of pulmonary edema and exacerbate hypoxemia which may accelerate the progression of chronic kidney disease. In this context, the present study attempted to evaluate the association of renal injury and oxidative stress at different atmospheric pressures (1829, 3657, and 5486 m). Limited fecal analysis of experimental animals was also done to evaluate the impact of hypobaric hypoxia on the composition of dominant gastrointestinal microbiota. The study was performed on 24 male Wister strain rats and divided into four groups (C, HA-I, HA-II, and HA-III), and exposure was carried out for seven days period. In hypoxic exposure rats, plasma urea, creatinine, electrolytes and malonaldehyde level elevated and catalase and superoxide dismutase level diminished significantly compared to the controls. Increase in blood uremia profile, toxicity markers, and lipid peroxidation marker enzymes indicated that hypoxia causes renal failure. Histological structures of the kidney of group HA-II and HA-III animals showed severe disorganization of glomerulus and dilation of renal tubules. These results indicate nephrotoxicity or acute renal failure can occur at hypobaric hypoxia and it also affected the gut microbial population. This alteration was observed significantly above 3000 m.

Therapeutic potential of different commercially available synbiotic on acetaminophen-induced uremic rats.

BACKGROUND: Currently kidney disease appears a foremost problem across the world. Acetaminophen is a commonly used antipyretic agent, which in high doses, causes uremia and used for experimentally induction of kidney disease. Bacteriotherapy affords a promising approach to mitigate uremic toxins by ingestion of urease positive bacteria, probiotics and symbiotic able to catabolize uremic solutes within the gut. The present study evaluates the effect of seven commercial symbiotic on kidney disease. METHODS: Fifty-four albino male rats were randomly divided into nine groups. Control group (Group-I) received distilled water interperitoneally for 7 days. Positive control group (Group-II) received 500 mg/kg acetaminophen interperitoneally for 7 days. Commercially available seven symbiotic combinations at a dose of 10(9)cells/day for 3 weeks was administered to the tested groups (Group III-IX) after receiving 500 mg/kg/day acetaminophen interperitoneally for 7 days. Blood, kidney, liver and stool samples were collected after scarification for biochemical tests and DNA fragmentation assay of kidney tissue, kidney histological studies. Limited fecal analysis was conducted. RESULT: Blood urea nitrogen and toxicity indicators were increased, and antioxidant enzymes were decreased in Group-II. Blood urea nitrogen, toxicity indicators, glomerular necrosis, DNA damage of kidney tissue were reduced, and antioxidant enzymes were increased significantly in the treated Groups IV and IX (p < 0.05) in response to Group-II. Number of pathogenic bacteria decreased in synbiotic treated groups than Group I and II. CONCLUSION: The study demonstrated that some of commercial symbiotic combination can reduce the sever effect of kidney disease.

Analysis of phytochemical profile of Terminalia arjuna bark extract with antioxidative and antimicrobial properties.

OBJECTIVE: To investigate phytochemical screening, antimicrobial activity and qualitative thin layer chromatographic separation of flavonoid components, antioxidant activity and total flavonoid compound of Terminalia arjuna. METHODS: For phytochemical screening, some common and available standard tests were done. Antimicrobial bioassay was done through agar well diffusion method. Detection of antioxidant activity and flavonoid compounds were done through thin layer chromatography. Total antioxidant activity was measured by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) in colorimetric method. Aluminum chloride colorimetric method was used for total flavonoid determination. RESULTS: Phytochemical screening showed the active compounds presence in high concentration, such as phytosterol, lactones, flavonoids, phenolic compounds and tannins and glycosides. The antimicrobial activity of extract showed that greater inhibition zone against Gram negative bacteria than Gram positive bacteria. This methanolic extract showed a promising antioxidant activity, as absorption of DPPH redicles decreased in DPPH free radical scavenging assay. Flavonoids components having antioxidant property present in the methanol extract at a level of 199.00 mg quercetin equivalent/g of dried methanol extract in colorimetric method. CONCLUSIONS: The Terminalia arjuna bark extract revealed the presence of bio-active constituents which are known to exhibit medicinal as well as physiological activities.

Analysis of phytochemical profile of Terminalia arjuna bark extract with antioxidative and antimicrobial properties

Objective: To investigate phytochemical screening, antimicrobial activity and qualitative thin layer chromatographic separation of flavonoid components, antioxidant activity and total flavonoid compound of Terminalia arjuna. Methods:For phytochemical screening, some common and available standard tests were done. Antimicrobial bioassay was done through agar well diffusion method. Detection of antioxidant activity and flavonoid compounds were done through thin layer chromatography. Total antioxidant activity was measured by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) in colorimetric method. Aluminum chloride colorimetric method was used for total flavonoid determination. Results:Phytochemical screening showed the active compounds presence in high concentration, such as phytosterol, lactones, flavonoids, phenolic compounds and tannins and glycosides. The antimicrobial activity of extract showed that greater inhibition zone against Gram negative bacteria than Gram positive bacteria. This methanolic extract showed a promising antioxidant activity, as absorption of DPPH redicles decreased in DPPH free radical scavenging assay. Flavonoids components having antioxidant property present in the methanol extract at a level of 199.00 mg quercetin equivalent/g of dried methanol extract in colorimetric method. Conclusions: The Terminalia arjuna bark extract revealed the presence of bio-active constituents which are known to exhibit medicinal as well as physiological activities.