| Title |
Reductive metabolism of oxymatrine is catalyzed by microsomal CYP3A4
|
|---|---|
| Published in |
Drug Design, Development and Therapy, October 2015
|
| DOI | 10.2147/dddt.s92276 |
| Pubmed ID | |
| Authors |
Wenqin Liu, Jian Shi, Lijun Zhu, Lingna Dong, Feifei Luo, Min Zhao, Ying Wang, Ming Hu, Linlin Lu, Zhongqiu Liu |
| Abstract |
Oxymatrine (OMT) is a pharmacologically active primary quinolizidine alkaloid with various beneficial and toxic effects. It is confirmed that, after oral administration, OMT could be transformed to the more toxic metabolite matrine (MT), and this process may be through the reduction reaction, but the study on the characteristics of this transformation is limited. The aim of this study was to investigate the characteristics of this transformation of OMT in the human liver microsomes (HLMs) and human intestinal microsomes (HIMs) and the cytochrome P450 (CYP) isoforms involved in this transformation. The current studies demonstrated that OMT could be metabolized to MT rapidly in HLMs and HIMs and CYP3A4 greatly contributed to this transformation. All HLMs, HIMs, and CYP3A4 isoform mediated reduction reaction followed typical biphasic kinetic model, and K m, V max, and CL were significant higher in HLMs than those in HIMs. Importantly, different oxygen contents could significantly affect the metabolism of OMT, and with the oxygen content decreased, the formation of metabolite was increased, suggesting this transformation was very likely a reduction reaction. Results of this in vitro study elucidated the metabolic pathways and characteristics of metabolism of OMT to MT and would provide a theoretical basis and guidance for the safe application of OMT. |
Mendeley readers
The data shown below were compiled from readership statistics for 14 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 14 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Bachelor | 4 | 29% |
| Researcher | 2 | 14% |
| Student > Master | 2 | 14% |
| Other | 1 | 7% |
| Student > Ph. D. Student | 1 | 7% |
| Other | 0 | 0% |
| Unknown | 4 | 29% |
| Readers by discipline | Count | As % |
|---|---|---|
| Biochemistry, Genetics and Molecular Biology | 4 | 29% |
| Agricultural and Biological Sciences | 3 | 21% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 14% |
| Computer Science | 1 | 7% |
| Unknown | 4 | 29% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 03 November 2015.
All research outputs
#22,758,309
of 25,371,288 outputs
Outputs from Drug Design, Development and Therapy
#1,754
of 2,268 outputs
Outputs of similar age
#245,761
of 286,873 outputs
Outputs of similar age from Drug Design, Development and Therapy
#86
of 110 outputs
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