| In vitro: |
| J Ethnopharmacol. 2015 May 26;166:66-73. | | Inhibitory effects of cytochrome P450 enzymes CYP1A2, CYP2A6, CYP2E1 and CYP3A4 by extracts and alkaloids of Gelsemium elegans roots.[Pubmed: 25764964] |
METHODS AND RESULTS:
Four extracts (petroleum ether, dichloromethane, EtOAc and aqueous) of GE and two commercially available alkaloids (koumine and Humantenmine) were screened for their CYP isoforms inhibitory activity. In the case of alkaloids, koumine exhibited significant inhibitory effects on CYP2E1 while Humantenmine showed more potent inhibition on CYP2E1 and CYP2A6 (IC50 of 47.44, 18.34 and 45.87µg/ml, Ki of 31.20, 35.06 and 52.06µg/ml, respectively). Because of their relatively high Ki values, the active constituents in GE dichloromethane extract were analyzed. The UPLC-DAD-ESI-MS/MS data showed that GE dichloromethane extract contains 6 kinds of indole alkaloids (koumine, Humantenmine, humantenine, humantenirine, N-methoxytaberpsychine, and sempervirine). As for CYP1A2 and CYP3A4, the negligible inhibitions were observed.
CONCLUSIONS:
G. elegans extracts inhibited several CYP450 enzyme activities with varying potency. Strong inhibition was observed in CYP2E1 and CYP2A6 isoforms by GE dichloromethane extract, koumine and Humantenmine, inferring the involvement of alkaloids chemical constituents from GE dichloromethane extract in the effect. |
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