In Vitro Anticancer Properties of Novel Bis-Triazoles

Here, we describe the anticancer activity of our novel bis-triazoles MS47 and MS49, developed previously as G-quadruplex stabilizers, focusing specifically upon the human melanoma MDA-MB-435 cell line. At the National Cancer Institute (NCI), USA, bis-triazole MS47 (NCS 778438) was evaluated against a panel of sixty human cancer cell lines, and showed selective, distinct multi-log differential patterns of activity, with GI50 and LC50 values in the sub-micromolar range against human cancer cells. MS47 showed highly selective cytotoxicity towards human melanoma, ovarian, CNS and colon cancer cell lines; in contrast, the leukemia cell lines interestingly showed resistance to MS47 cytotoxic activity. Further studies revealed the potent cell growth inhibiting properties of MS47 and MS49 against the human melanoma MDA-MB-435 cell line, as verified by MTT assays; both ligands were more potent against cancer cells than MRC-5 fetal lung fibroblasts (SI > 9). Melanoma colony formation was significantly suppressed by MS47 and MS49, and time- and dose-dependent apoptosis induction was also observed. Furthermore, MS47 significantly arrested melanoma cells at the G0/G1 cell cycle phase. While the expression levels of Hsp90 protein in melanoma cells were significantly decreased by MS49, corroborating its binding to the G4-DNA promoter of the Hsp90 gene. Both ligands failed to induce senescence in the human melanoma cells after 72 h of treatment, corroborating their weak stabilization of the telomeric G4-DNA

Phytochemical screening and evaluation of cytotoxic and hypoglycemic properties of Mangifera indica peels

Objective: To investigate the presence of different phytoconstituents in Mangifera indica (M. indica) peel and evaluate its cytotoxicity to Artemia salina and hypoglycemic potential in Swiss albino mice. Methods: The methanolic extract of M. indica peel was used to determine the presence of phytoconstituents. Brine shrimp lethality bioassay method was followed to determine the cytotoxic potential of plant extract. In the case of hypoglycemic activity, oral administration of extract at 200 and 400 mg/kg and standard glibenclamide at 10 mg/kg was done, followed by determining the percentage of reduction of plasma glucose from the initial level. Results: The methanolic extract of M. indica peel showed the presence of flavonoid, saponin, steroid, tannins, terpenoids, glycosides and alkaloids. In brine shrimp lethality bioassay, the LC50 of the extract and standard vincristine sulfate was found to be 2.04 and 0.41 μg/mL, respectively. After 90 and 150 min, the methanolic extract at 200 and 400 mg/kg showed prominent plasma glucose reduction of 13.95%, 22.48% and 14.16%, 26.18% respectively compared to standard glibenclamide showing 14.90% and 20.67% plasma glucose reduction. Conclusions: This current research affirms prominent cytotoxic and moderate hypoglycemic potential of M. indica peel. Further bioactivity guided isolation of phytoconstituents and investigation on higher animals can lead to development of new drug molecules