文献类型：期刊文章

作　　者：吴妮[1] 徐嵬[1] 张友波[1] 杨秀伟[1]

机构地区：[1]北京大学医学部天然药物及仿生药物国家重点实验室.药学院天然药物学系,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》

基　　金：National Natural Science Foundation of China(Grant No.30973863.81161120429);National Key Technology R&D Program of China(Grant No.2011BAI07B08)

年　　份：2014

卷　　号：23

期　　号：4

起止页码：241-245

语　　种：中文

收录情况：CAB、CAS、CSCD、CSCD2013_2014、DOAJ、EMBASE、IC、JST、SCOPUS、ZGKJHX、普通刊

摘　　要：Malabaricone C （1）, isolated from the seeds ofMyristicafragrans Houtt., belongs to a kind of diarylnonanoid compounds that are only found in Myristicaceae till now. In this study, biotransformation of 1 was investigated using rat hepatic microsomes for the first time and the main biotransformation product was elucidated as malabaricone B （2） according to the spectroscopic data. Further evaluation on human gastric cancer cell lines showed that the cytotoxic effects of malabaricone C and its metabolite malabaricone B were comparable to those of vinorelbine, with the values of IC50 of （42.62±3.10） and （19.80±1.70） μg/mL on NCI-N87, and （22.94±1.33） and （19.60±2.21） μg/mL on MGC803, respectively. Statistical analysis revealed that malabaricone B had significantly stronger cytotoxicity than the parent compound （P〈0.01 on NCI-N87 and P〈0.05 on MGC803）, which may indicate a bioactivation of malabaricone C by hepatic microsomes. These results suggest that malabaricone C has a simple biotransformation pathway by hepatic microsomes and provide valuable information for further investigation on both the parent compound and its biotransformation product as anti-gastric cancer agents or lead compounds.

关 键 词：Malabaricone C  Malabaricone B  Myristicafragrans  BIOTRANSFORMATION Rat hepatic microsomes  Human gastric cancer NCI-N87  Human gastric cancer MGC803  

分 类 号：R284[中药学类]