![](/images/graphics-bg.png)
Monoester-Diterpene Aconitum Alkaloid Metabolism in Human Liver Microsomes : Predominant Role of CYP3A4 and CYP3A5
Joint Authors
Dong, Ling-Na
Zeng, Shan
Ye, Ling
Liu, Zhong-Qiu
Peng, Xiao-Juan
Chen, Wei-Ying
Shi, Jian
Yan, Tong-Meng
Yang, Xiao-Shan
Lu, Lin-lin
Source
Evidence-Based Complementary and Alternative Medicine
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-24, 24 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-06-23
Country of Publication
Egypt
No. of Pages
24
Main Subjects
Abstract EN
Aconitum, widely used to treat rheumatoid arthritis for thousands of years, is a toxic herb that can frequently cause fatal cardiac poisoning.
Aconitum toxicity could be decreased by properly hydrolyzing diester-diterpene alkaloids into monoester-diterpene alkaloids.
Monoester-diterpene alkaloids, including benzoylaconine (BAC), benzoylmesaconine (BMA), and benzoylhypaconine (BHA), are the primary active and toxic constituents of processed Aconitum.
Cytochrome P450 (CYP) enzymes protect the human body by functioning as the defense line that limits the invasion of toxicants.
Our purposes were to identify the CYP metabolites of BAC, BMA, and BHA in human liver microsomes and to distinguish which isozymes are responsible for their metabolism through the use of chemical inhibitors, monoclonal antibodies, and cDNA-expressed CYP enzyme.
High-resolution mass spectrometry was used to characterize the metabolites.
A total of 7, 8, and 9 metabolites were detected for BAC, BMA, and BHA, respectively.
The main metabolic pathways were demethylation, dehydrogenation, demethylation-dehydrogenation, hydroxylation and didemethylation, which produced less toxic metabolites by decomposing the group responsible for the toxicity of the parent compound.
Taken together, the results of the chemical inhibitors, monoclonal antibodies, and cDNA-expressed CYP enzymes experiments demonstrated that CYP3A4 and CYP3A5 have essential functions in the metabolism of BAC, BMA, and BHA.
American Psychological Association (APA)
Ye, Ling& Yang, Xiao-Shan& Lu, Lin-lin& Chen, Wei-Ying& Zeng, Shan& Yan, Tong-Meng…[et al.]. 2013. Monoester-Diterpene Aconitum Alkaloid Metabolism in Human Liver Microsomes : Predominant Role of CYP3A4 and CYP3A5. Evidence-Based Complementary and Alternative Medicine،Vol. 2013, no. 2013, pp.1-24.
https://search.emarefa.net/detail/BIM-509982
Modern Language Association (MLA)
Ye, Ling…[et al.]. Monoester-Diterpene Aconitum Alkaloid Metabolism in Human Liver Microsomes : Predominant Role of CYP3A4 and CYP3A5. Evidence-Based Complementary and Alternative Medicine No. 2013 (2013), pp.1-24.
https://search.emarefa.net/detail/BIM-509982
American Medical Association (AMA)
Ye, Ling& Yang, Xiao-Shan& Lu, Lin-lin& Chen, Wei-Ying& Zeng, Shan& Yan, Tong-Meng…[et al.]. Monoester-Diterpene Aconitum Alkaloid Metabolism in Human Liver Microsomes : Predominant Role of CYP3A4 and CYP3A5. Evidence-Based Complementary and Alternative Medicine. 2013. Vol. 2013, no. 2013, pp.1-24.
https://search.emarefa.net/detail/BIM-509982
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-509982