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Synthesis of Camptothecin-10-O-glucoside Using an Engineered Oleandomycin Glucosyltransferase
Authors:ZHU Xuelin  YE Qinmei  WEN Chao  CHEN Liping  LIANG Guangping  ZENG Ting  ZHANG Dongmei  JIANG Renwang
Institution:Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drugs Research, Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, P. R. China
Abstract:Oleandomycin glycosyltransferase variant P67T/S132F/A242V(ASP) was used to convert 10-hydroxy-camptothecin 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-hydroxycamptothecin(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.
Keywords:Camptothecin-10-O-glucoside  10-Hydroxycamptothecin  Glycosylation  Glucosyltransferase  Antineoplastic  
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