The modern therapeutic approaches of antiepileptic agents against epileptic patients are showing many side effects, dose related effects and chronic toxicity. The aim of our present work is to evaluate anticonvulsant activity of isatin derivatives (Ia-Ij) to reduce the side-effects and increase the percentage protection from various stages of convulsions. No animals showed toxic effects even up to 2000mg/kg. It is evident that Ib, Ie, Ih, Ii and Ij showed anticonvulsant effect at the dose levels of 10 and 100mg/kg in MES test and except Ij all other derivatives exhibited antiepileptic effect at 10 and 100mg/kg in PTZ induced convulsions test. The isatin derivatives (Ib, Ie, Ih and Ii) which proved antiepileptic effect in both MES and PTZ induced convulsion models are selected and GABA levels in brain were estimated. They showed significant increase of GABA levels in brain.
Isatin and its derivatives is versatile lead molecule for potential bioactive agents and shows wide spectrum of activities. In this study, we evaluated antioxidant, antimicrobial and cytotoxic activity of isatin-3-[N2-(2-benzalaminothiazol-4-yl)] hydrazone derivatives using well defined models. Antioxidant activity of the isatin derivatives (Va-Vj) was evaluated by using the 1, 1-diphenyl-2-picryl hydrazine radicals scavenging assay. The antimicrobial activity is evaluated by cup plate method and anticancer activity is evaluated by MTT assay against HBL-100 & HeLa cell lines. Compound Vh (R = 5-Cl, R1 = OH & R2 = OCH3) showed good antioxidant activity with the IC50 of 8.09 M. In addition Ve and Vi have showned most active antibacterial activity against Bacillus subtilis, Staphylococcus aureus and Escherichia coli with a Zone of Inhibition (mm) 20, 16, 18 and 14, 12, 15 on respective organism at 100 g/disc. The compound Vi have produced a good antifungal activity against Aspergillus niger and Clostridium vericulata with the zone of inhibition values of 9 and 8 mm respectively. These isatin derivatives also among the test compounds, compound Vd (R = 5-Cl, R1 = OH & R2 = OCH3) and compound Vh (R = 5-Cl, R1 = OH & R2 = OCH3) have shown nearly equal cytotoxic activity with IC50 values of 246.53 mM and 247.29 mM against HBL-100 cell lines and HeLa cell lines respectively. From the results, isatin derivatives showed powerful antioxidant activity, antimicrobial and anticancer activity may be due to the halogens substituted at 5th position of isatin. The standard drugs used were ampicillin, clotrimazole, cisplatin and ascorbic acid for antibacterial, antifungal, anticancer and antioxidant respectively.
Cisplatin (CP), a platinum compound, is one of the most active cytotoxic drugs used for cancer treatment. Nephrotoxicity is severe dose limiting side effect of this drug. Abnormal production of reactive oxygen species (ROSs) leading to oxidative stress has been implicated in kidney toxicity by Cisplatin. Here the study was aimed to evaluate nephroprotective effect of ethanolic extract of Terminalia arjuna bark (EETAB) at the doses (200 & 400 mg/kg, body weight) against Cisplatin (7.5 mg/kg, i.p) induced nephrotoxicity in rats. The evaluation was done by measuring % change in body weight, renal function tests such as Blood Urea Nitrogen (BUN), Serum Creatinine (Cr), Serum Total Protein (TP) and also Kidney SOD (Superoxide dismutase),CAT (Catalase), GSH (Reduced glutathione) and MDA (Malondialdehyde) levels altered by Cisplatin administration. Rats treated with EETAB2 (400mg/kg) significantly (P<0.001) reduced the elevated levels of BUN, Cr, TP, MDA and significantly (P<0.001) increased the levels of SOD, GSH, and CAT by restoring kidney architecture. In conclusion EETAB2 (400mg/kg) attractively showed the protection against Cisplatin nephrotoxicity.
Keywords: Cisplatin, Nephrotoxicity, Terminalaia arjuna, Reactive oxygen species, Renal function tests.
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