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灵芝酸A代谢产物及其代谢动力学

Ganoderic Acid A Metabolites and Their Metabolic Kinetics.

作者信息

Cao Fang-Rui, Feng Li, Ye Lin-Hu, Wang Li-Sha, Xiao Bing-Xin, Tao Xue, Chang Qi

机构信息

Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College Beijing, China.

出版信息

Front Pharmacol. 2017 Mar 7;8:101. doi: 10.3389/fphar.2017.00101. eCollection 2017.

DOI:10.3389/fphar.2017.00101
PMID:28326038
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5339268/
Abstract

Ganoderic acid A (GAA), a representative active triterpenoid from , has been reported to exhibit antinociceptive, antioxidative, cytotoxic, hepatoprotective and anticancer activities. The present study aims (1) to identify GAA metabolites, by analyzing the bile, plasma and urine after intravenous administration to rats (20 mg/kg), and by incubating with rat liver microsomes (RLMs) and human liver microsomes (HLMs); (2) to investigate the metabolic kinetics of main GAA metabolites. Using HPLC-DAD-MS/MS techniques, a total of 37 metabolites were tentatively characterized from samples based on their fragmentation behaviors. The metabolites detected in samples were similar to those found . GAA underwent extensive phase I and II metabolism. The main metabolic soft spots of GAA were 3, 7, 11, 15, 23-carbonyl groups (or hydroxyl groups) and 12, 20, 28 (29)-carbon atoms. Ganoderic acid C (GAC) and 7β,15-dihydroxy-3,11,23-trioxo-lanost-26-oic acid were two main reduction metabolites of GAA, and their kinetics followed classical hyperbolic kinetics. The specific isoenzyme responsible for the biotransformation of the two metabolites in RLMs and HLMs was CYP3A. This is the first report on the comprehensive metabolism of GAA, as well as the metabolic kinetics of its main metabolites.

摘要

灵芝酸A（GAA）是灵芝中的一种代表性活性三萜类化合物，据报道具有抗伤害感受、抗氧化、细胞毒性、肝脏保护和抗癌活性。本研究旨在：（1）通过分析大鼠静脉注射（20mg/kg）后胆汁、血浆和尿液以及与大鼠肝微粒体（RLMs）和人肝微粒体（HLMs）孵育来鉴定GAA代谢产物；（2）研究主要GAA代谢产物的代谢动力学。使用HPLC-DAD-MS/MS技术，基于其裂解行为从样品中初步鉴定出总共37种代谢产物。在样品中检测到的代谢产物与在其他地方发现的相似。GAA经历了广泛的I相和II相代谢。GAA的主要代谢软点是3、7、11、15、23位羰基（或羟基）以及12、20、28（29）位碳原子。灵芝酸C（GAC）和7β,15-二羟基-3,11,23-三氧代羊毛甾-26-酸是GAA的两种主要还原代谢产物，它们的动力学遵循经典的双曲线动力学。在RLMs和HLMs中负责这两种代谢产物生物转化的特定同工酶是CYP3A。这是关于GAA全面代谢及其主要代谢产物代谢动力学的首次报道。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/6aa18e4f86c5/fphar-08-00101-g0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/3374c502546f/fphar-08-00101-g0001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/2e4344d2a6c4/fphar-08-00101-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/32a4a59f9dc8/fphar-08-00101-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/56a573626a60/fphar-08-00101-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/8ca4afc535c6/fphar-08-00101-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/6aa18e4f86c5/fphar-08-00101-g0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/3374c502546f/fphar-08-00101-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/88967c232347/fphar-08-00101-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/2e4344d2a6c4/fphar-08-00101-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/32a4a59f9dc8/fphar-08-00101-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/56a573626a60/fphar-08-00101-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/8ca4afc535c6/fphar-08-00101-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41a2/5339268/6aa18e4f86c5/fphar-08-00101-g0007.jpg

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