Development of noninvasive drug metabolizing enzyme activity estimate method for side effect reduction of the drugs
| Project/Area Number |
25670077
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Medical pharmacy
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| Research Institution | Osaka Kyoiku University |
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Principal Investigator |
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| Project Period (FY) |
2013-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2015: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2014: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2013: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Keywords | ステロイド代謝 / 薬物代謝 / CYP3A4 / リアーゼ活性 / ヒト・ＣＹＰ / 薬物代謝酵素 / 水酸化活性 / CYP / コルチソール / リアーぜ活性 |
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| Outline of Final Research Achievements |
Fourteen CYPs which are drug metabolizing enzymes in human liver were reacted to more than eight kinds of adrenal steroids and their metabolites were identified. As a result, only CYP3A4 showed a various metabolite on HPLC chart. Production of androstendion from 17alpha-hydroxyprogesterone and 11-deoxycortisol by CYP3A4 was confirmed by GC-MS. It was revealed that CYP3A4 can catalyze side chain cleavage reaction (Lyase activity) to the steroids. 6beta-Hydoxy metabolite which were main metabolite from 11-deoxycortisol was identified. Then, Km and Vmax of 6beta-hydroxylase activity and Lyase activity against 11-deoxycortisol were determined and compared.
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Report
(4 results)
Research Products
(1 results)
