地黄活性成分梓醇在大鼠体内的代谢变化研究

Metabolic Change of Catalpol in Rehmannia Glutinosa Libosch in Rats

目的观察大鼠口服地黄水提液后其主要成分梓醇在体内的代谢变化,初步探讨梓醇在体内的可能代谢途径和变化规律。方法 SD大鼠灌胃给予地黄水提液,分别给药后在不同时间点取血浆,采用HPLC-MS检测血浆中梓醇及其代谢物的变化。结果大鼠口服地黄煎液后,梓醇在大鼠体内主要有1个异构体和5个代谢转化产物:异构体、甲基化物、羟基化物、糖基化物、脱氧羟基化物和脱氧羟基化甲基化物。且梓醇及其代谢物均在给药后45 min达到最高值,随后呈下降趋势。结论地黄梓醇在体内可能代谢途径分析研究,可为地黄及含有梓醇的药物的体内外代谢分析和进一步与药效结合、作用机理研究提供参考。

Objective： To observe the metabolic changes of Catalpol in Rehmannia glutinosa Libosch in rats,and preliminarily investigate the possible metabolic pathways and changing rules of Catalpol in vivo. Methods：Water extraction was used to prepare Rehmannia glutinosa Libosch water extraction. Lavage method was used to give medicine. The plasma was taken at different time points after administration;HPLC-MS was used to detect metabolic change of catalpol. Results： There were six converted products： Isomer,Methylation,Hydrogenation,Glucose,Hydrogenation＋Loss of O,Methylation＋Hydrogenation＋Loss of 2 O. Catalpol and its metabolites reached the highest value within 45 minutes after administration,and then showed a downward trend. Conclusion： The analysis and research on the possible metabolic pathways of Catalpol in vivo can provide reference for the analysis of the metabolism in vivo and in vitro of rehmannia and the drugs containing Catalpol and the mechanism of the combination of drug effect.