Oleandomycin glycosyltransferase variant P67T/S132F/A242V（ASP） was used to convert 10-hydroxycamptothecin into camptothecin-10-O-glucoside, which was confirmed by spectral analysis. Compared to the previously report...Oleandomycin glycosyltransferase variant P67T/S132F/A242V（ASP） was used to convert 10-hydroxycamptothecin into camptothecin-10-O-glucoside, which was confirmed by spectral analysis. Compared to the previously reported results, the present study reached the conversion rate up to 80% through the optimization of reaction conditions. In addition, compared with 10-hydroxycamptotheein（HCPT）, camptothecin-10-O-glucoside inhibited the proliferation of Huh7 cells in a concentration-dependent manner and showed stronger antineoplastic effect but lower toxicity. Furthermore, camptothecin-10-O-glucoside induced more apoptotic cells as compared with the parent compound.展开更多
基金Supported by the National Natural Science Foundation of China（No. 81573315）, the Natural Science Foundation of Guangdong Province, China（No.2015A030313313）, the Guangzhou Industry University Collaborative Innovation Major Projects, China （No.201508030016） and the Natural Science Foundation of Hainan Province, China（No. 817307）.
文摘Oleandomycin glycosyltransferase variant P67T/S132F/A242V（ASP） was used to convert 10-hydroxycamptothecin into camptothecin-10-O-glucoside, which was confirmed by spectral analysis. Compared to the previously reported results, the present study reached the conversion rate up to 80% through the optimization of reaction conditions. In addition, compared with 10-hydroxycamptotheein（HCPT）, camptothecin-10-O-glucoside inhibited the proliferation of Huh7 cells in a concentration-dependent manner and showed stronger antineoplastic effect but lower toxicity. Furthermore, camptothecin-10-O-glucoside induced more apoptotic cells as compared with the parent compound.
