RESUMEN
Objective: To design novel series of 1,3,4 thiadiazoles and to evaluate their anti-mycobacterial potency via In silico modeling.Methods: In silico modeling comprising of Lipinski rule evaluation, ADMET prediction, Molecular docking and Simulation studies aimed to identify potent 1,3,4 thiadiazoles.Results: The various physiochemical parameters and molecular descriptors of the proposed 1,3,4 thiadiazoles were predicted. And they exhibited good binding score compared with standard drug INH. The simulation studies showed minimal fluctuation of the ligand receptor complexes.Conclusion: The MD simulation and binding affinity of designed 1,3,4 thiadiazoles proved their efficiency as InhA inhibitors. The potency of the selected derivatives can be confirmed by further in vitro and in vivo experiments.
RESUMEN
The present study was aimed at investigating the in vivo hypouricaemic activity of the various fractions of the hydromethanolic extract of the leaves of Erythrina stricta roxb (papilionacea) using oxonate-induced hyperuricaemic mice. The leaves of this species was used in traditional medicinal system for the treatment of gout, rheumatism, jaundice, bronchitis, fever, skin eruptions, wounds, etc. The pet-ether, chloroform, ethyl acetate and residual fractions at a dose of 200 mg/kg b.w. orally, were tested for their ability to reduce the serum urate level and inhibitory actions on the XO/XDH enzyme activities in the mouse liver and intestine. Potassium oxonate (280 mg/kg, i.p.), an uricase inhibitor was used to induce hyperuricaemia. Allopurinol (10 mg/kg, p.o.) was used as the positive control. The pet-ether, chloroform and ethyl acetate fractions when administered to hyperuricaemic mice produced a significant reduction in serum urate levels. In addition, these fractions elicited significant inhibitory actions on the XO/XDH enzyme activities in the mouse liver. The hypouricaemic activity may be due to the inhibition of XO/XDH enzymes. The effect of the fractions was less potent than allopurinol. The activity produced by the residual fraction was insignificant (P>0.05). Phytochemical screening of the leaves of Erythrina stricta revealed the presence of tannins, flavonoids, alkaloids and terpenoids. The presence of phytochemical constituents may be partly responsible for the beneficial effect of the fractions on hyperuricaemia and gout. These results suggest that the leaves of Erythrina stricta could be used as a potential source to treat gout and other inflammatory disorders.
RESUMEN
Drug Use Evaluation of Antibiotics was studied in medical inpatients after regulation of its use. The total quantity of antibiotics consumed were analyzed using Defined Daily Doses(DDDs) technique. Significant differences were observed in DDDs before and after the regulation. The study proved that evaluation of antibiotic utilization improved the appropriate and effective use of antibiotics and is economical to the patient.