【作者】 周应军； 申璀； 曾光尧； 张钰； 谭健兵； 谭桂山；

【Author】 Zhou Ying-jun~* Shen Cui Zeng Guang-yao Huang Ming-ju Tan Jian-bing Tan Gui-shan (School of Pharmaceutical Sciences,Central South University,Changsha 410013)

【机构】 中南大学药学院；

【摘要】 目的:研究 VBE-1在大鼠体内的代谢途径。方法:大鼠灌胃给予 VBE-1(100mg/kg),收集24小时大鼠的尿液和粪便,HPLC 分析检测,各种柱色谱法分离纯化代谢产物,理化与波谱方法鉴定各代谢物结构。结果:从大鼠的尿液和粪便中分离鉴定了三个代谢产物,代谢产物的体外抗肿瘤活性与 VBE-1的体外抗肿瘤活性相比,活性大大降低。结论:VBE-1 主要转化的特点为醛基被还原为羟甲基,4′位酚羟基被葡萄糖醛酸化。VBE-1的体内生物转化过程为代谢失活过程。更多还原

【Abstract】 OBJECTIVE:To investigate the metabolic pathway of VBE-1 in rats.METHODS:After oral dose of VBE-1 (100 mg/kg) to rats,urine and feces were collected for 24 h.The metabolites of VBE-1 in rats were analyzed by HPLC and purified by a series of column chromatography.Their structures were elucidated by chemical and spectroscopic analysis.RESULTS:Three metabolites were isolated from urine and feces of rats. Their structures were: 6-hydroxy-4-(4- β -D -glucuronyloxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-3,4-dihydro-2-naphthaldehyde (M-1),6-hydroxy-4-(4- β -D -glucuronyloxy-3-methoxyphenyl)- 7-methoxy- 3, 4-dihydro-2, 3-naphthahnedimethanol (M-2) and 6-hydroxy-4-(4-hydroxy-3-methoxyphenyl)-7-methoxy-3,4-dihydro-2,3-naphthalenedimethanol (M-3).CONCLUSION:In the proposed mechanism,aldehyde group was reduced to hydroxymethyl group and the C-4’ hydroxyl was attacked by glucuronic acid,to form the glucuronate compound.It may be the main metabolic pathway of VBE-1 in rats.The polarity of the glucuronate metaholite increased greatly and could be easily eliminated from body.The metabolism of VBE-1 in rats is inactivation.更多还原