Effect of alcoholic extract of roots of Dichrostachys cinerea Wight & Arn. against cisplatin-induced nephrotoxicity in rats

12-18The alcoholic extract of roots of Dichrostachys cinerea Wight & Arn. (200 and 400 mg/kg, p.o.) was studied for its protective effect against cisplatin-induced renal injury in rats. Cisplatin (6mg/kg, i.p.) significantly elevated serum markers level, increased urinary protein excretion, reduced urine to serum creatinine ratio and creatinine clearance. In curative regimen, the alcoholic extract exhibited dose dependent protection. Animals which received prophylactic treatment also showed partial protection against cisplatin-induced effects. Histopathological studies substantiated the above results. Further, the alcoholic extract showed marked nitric oxide scavenging effect and reducing power suggesting an antioxidant property. A triterpenoid, fatty acid and a steroid were isolated from the n-hexane, ethyl acetate fractions of alcoholic extract. The results suggested that the roots of D. cinerea showed protective effect against cisplatin-induced nephrotoxicity which may probably be mediated by its antioxidant property

Design, Synthesis and Evaluation of Functionalized Azaglycinamides as Cytotoxic and Antinociceptive Agents: Functionalized Azaglycinamides as Cytotoxic and Antinociceptive Agents

Aza analogs of peptides are used in the treatment of cancer and neurodegenerative disorders. The clinical approval of goserelin for the treatment of prostate cancer proves the therapeutic potentiality of azaglycine residue. With this background, a novel approach to functionalizing the azaglycine moiety aimed at compounds possessing C-functionalization with active five membered heterocycles (pyrrole, imidazole, etc thiazolidine-2, 4-dione) and N-functionalization with acyl chains on azaglycine moiety were synthesized. The compounds were evaluated for in vitro MAGL inhibition and cytotoxicity against MCF-7 cell lines. The biological activities were corroborated with molecular docking studies with Cathepsin B and MAGL enzymes. The compounds with prominent in vitro and in silico potential against MAGL were evaluated for antinociceptive activity. This privileged N- and C-functionalization approach in the synthesis of azaglycinyl analogs demonstrated that N-oleoyl and C-thiazolidine-2,4-dione functionalized azaglycinamide derivative 1q, was found to possess moderate cytotoxic and MAGL inhibitory profile. The active compounds were well accommodated in the binding sites of these targets with good electrostatic complementarity. The N-oleoyl and C-thiazolidine-2, 4-dione functionalized azaglycine can be envisaged as a novel molecule with potential anticancer and antinociceptive activities

Effect of ethanolic extract of <i>Phyla nodiflora</i> (Linn.) Greene against calculi producing diet induced urolithiasis

314-321Urolithiasis in its different forms is a frequently encountered urological disorder. For many years it has been at the forefront of urology. In the present study ethanolic extract of whole plant of Phyla nodiflora (Linn.) Greene was studied for its antiurolithiatic activity against most common type of renal stones i.e. calcium oxalate type. Calcium oxalate urolithiasis was induced by administration of Gentamycin and calculi producing diet (5% ammonium oxalate in standard rat pellet feed). The extract was also assessed for effect on in vivo antioxidant parameters like lipid peroxidation, reduced glutathione, catalase in hyperoxaluric kidney and in vitro scavenging of nitric oxide and 2-diphenyl-2-picryl hydrazyl free radicals. Ethanolic extract of P. nodiflora exhibited significant effect in preventing calcium oxalate stone formation and also in dissolving the pre-formed calcium oxalate stones in the kidney along with significant effect on both in vitro and in vivo antioxidant parameters. The present study clearly demonstrates the antiurolithiatic activity of P. nodiflora supporting the traditional claim