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Publication
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| Research Title |
Inhibition and Mechanism-Based Inactivation of Human CYP3A4 by Phyllanthus amarus |
| Date of Distribution |
10 May 2009 |
| Conference |
| Title of the Conference |
The 3rd Asian Pacific Regional ISSX Meeting: Understanding Xenobiotics for Better Drug Development and Therapy |
| Organiser |
International Society for the Study of Xenobiotics (ISSX) |
| Conference Place |
The Imperial Queen’s Park Hotel |
| Province/State |
Bangkok, Thailand |
| Conference Date |
10 May 2009 |
| To |
12 May 2009 |
| Proceeding Paper |
| Volume |
41 |
| Issue |
2 |
| Page |
39 |
| Editors/edition/publisher |
Jack A. Hinson |
| Abstract |
Phyllanthus amarus (P. amarus) has long been used as medicinal plant in several countries around the world, including Thailand, for the treatment of jaundice, hepatitis, diabetes and other diseases. It has been reported that alcoholic and aqueous extract of P. amarus could inhibit certain drug metabolizing enzymes both in vivo as well as in vitro. Since CYP3A4 is the major enzyme that responsible for the metabolism of a number of drugs, therefore the inhibitory effects of P. amarus extractions and its 2 major lignans; phyllanthin and hypophyllanthin were determined in the present study using human hepatic microsomal testosterone 6b-hydroxylase as a selective CYP3A4 marker. The ethanolic and aqueous extracts of P. amarus inhibited CYP3A4 activity in a dose-dependent manner with IC50 values of 1.26 ± 2.29 mg/ml and 65.57 ± 4.93 mg/ml, respectively. Furthermore, the soxhlet extractions of P. amarus by hexane, dichloromethane and methanol showed IC50 values of 0.39 ± 0.15 mg/ml, 11.6 ± 4.3 mg/ml and >100 mg/ml, respectively. Phyllanthin and hypophyllanthin which extracted from the hexane fraction showed time–dependent inhibition on CYP3A4. Mechanism-based inhibition kinetics of these lignans were also determined. |
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| Peer Review Status |
มีผู้ประเมินอิสระ |
| Level of Conference |
นานาชาติ |
| Type of Proceeding |
Abstract |
| Type of Presentation |
Poster |
| Part of thesis |
true |
| Presentation awarding |
false |
| Attach file |
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| Citation |
0
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Journal Publication
ไทย