| Research Title |
Bovine serum albumin enhances CYP1A2-mediated phenacetin O-deethylation formation by binding to polyunsaturated fatty acids |
| Date of Distribution |
18 March 2011 |
| Conference |
| Title of the Conference |
การประชุมวิชาการประจำปีสมาคมเภสัชวิทยาแห่งประเทศไทย ครั้งที่ 33 |
| Organiser |
สมาคมเภสัชวิทยาแห่งประเทศไทย |
| Conference Place |
ณ ห้องประกายเพชร โรงแรมไดมอนด์พลาซ่า |
| Province/State |
อ.หาดใหญ่ จ.สงขลา |
| Conference Date |
17 March 2011 |
| To |
19 March 2011 |
| Proceeding Paper |
| Volume |
33 |
| Issue |
- |
| Page |
60 |
| Editors/edition/publisher |
Laddawal Phivthong-ngam |
| Abstract |
The addition of bovine serum albumin (BSA) to incubations has been shown to enhance activities of certain cytochrome P450 (CYP) activities including 2C8 and 2C9 mainly via a reduction of the Km values without an effect on Vmax. It has been demonstrated that the intrinsic clearances of CYP2C8 and CYP2C9 substrates that were calculated from microsomal incubations in the presence of BSA improved the prediction of in vivo hepatic clearance. This effect arises from albumin binding to inhibitory polyunsaturated fatty acids (PUFAs) released during the course of incubation. The universality of the BSA effect on other CYP isoforms, however, is currently unknown. Since CYP1A2 is one of the enzymes responsible for the metabolism of several drugs, it is therefore interesting to elucidate the effect of BSA on the in vitro kinetics of CYP1A2-catalysed phenacetin O-deethylation. In the absence and presence of BSA (2% w/v), data for phenacetin O-deethylation formation by human liver microsomes (HLM) and recombinant CYP1A2 (rCYP1A2) respective exhibited two enzymes and single enzyme Michaelis-Menten kinetics. BSA statistically decreased mean Km for phenacetin O-deethylation by HLM and rCYP1A2 with a minor effect on mean Vmax, resulting in statistically increment of intrinsic clearance. A mixture of oleic, linoleic, and arachidonic acid caused an increase in Km without an effect on Vmax for phenacetin O-deethylation by rCYP1A2. The addition of 2% BSA to the incubation reversed this inhibitory effect of fatty acid mixture.
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| Author |
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| Peer Review Status |
มีผู้ประเมินอิสระ |
| Level of Conference |
ชาติ |
| 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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Publication
Journal Publication
ไทย