Dihydroxybergamottin caproate as a potent and stable CYP3A4 inhibitor |
| |
| Authors: | Ohta Tomihisa Nagahashi Minoru Hosoi Shinzo Tsukamoto Sachiko |
| |
| Affiliation: | Faculty of Pharmaceutical Sciences, Kanazawa University, Takara-machi, 920-0934, Kanazawa, Japan. ohta@dbs.p.kanazawa-u.ac.jp |
| |
| Abstract: | We investigated the inhibitory activity of the furanocoumarin derivatives from grapefruit juice to the drug metabolizing enzyme, cytochrome P450 (CYP) 3A4. Although two known furanocoumarin dimers GF-I-1 (1) and GF-I-4 (2) showed potent CYP3A4 inhibition with IC50 value of 0.07 microM, a semi-synthetic dihydroxybergamottin caproate (11), which was more stable and more simple than the dimers, exhibited comparable activity against CYP3A4. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
