Biological active compounds from Coscinium fenestratum (Gaertn.) Colebr

Abstract

This work is the first report concerning the investigation of biological active compounds from stems of Coscinium fenestratum (Gaertn.) Colebr. (Menispermaceae). It was found that ethanolic extract exhibited strong anticancer activity against cell lines (KB, BC-1 and NCI- H187) and displayed moderate activity against antifungal Candida albicans. In addition, it showed actively against antimalarial and exhibited low cytotoxicity against brine shrimp Artemia salina Linn. And vero cells in a preliminary screening test. The separation was performed by column chromatography and on the basis of spectroscopic techniques resulted in the isolation of a mixture of steroids (stigmastan-3,5,22-triene, stigmastan-3, 5 diene, β-sitosterol, campesterol and srigmasterol), berberine, jatrorrhizine, a long chain ester, a mixture of containing oleanolic acid, 8-oxotetrahydrothalifendine, 8-oxoberberine and a mixture of steroidal glycoside (srigmastery1-3-O-β-D-glucopyranoside and β–sitosteryl-3-O-β–D-glucopyranoside), calonysterone and ajugasterone D. Calonysterone and ajugasteron D have not been reported as the constituents, presented impressive anticancer activity against KB, BC-1 and NCI- H187 with IC₅₀ values of 0.48, 0.95 and 0.30 µg/mL, respectively. This compound showed antimalarial activity with EC₅₀ value of 0.11 µg/mL and displayed non-toxic activity against vero cells with IC₅₀ value of more than 50 µg/mL. In addition, this compound exhibited moderate antifungal activity against Candida albicans with IC₅₀ value 13.0 µg/mL and exhibited actively against antituberculosis activity with MIC values of 100 µg/mL. Jatrorrhizine showed strong anticancer activity against NCI-H187 with IC₅₀ values of 0.08 µg/mL and exhibited antituberculosis activity with MIC value of 200 µg/mL. In addition, it displayed non-toxicity against vero cells. SAR study of berberine and its salts revealed that some salts of berberine showed more potent activity than original compound for some biological assays.