KMID : 1098420160240010007
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Korean Journal of Medicinal Crop Science 2016 Volume.24 No. 1 p.7 ~ p.13
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Effects of 6-Shogaol, A Major Component of Zingiber officinale Roscoe, on Human Cytochrome P450 Enzymes in vitro
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Kim Jin
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Abstract
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Background : Ginger has been extensively used in foods and traditional medicines in Asian countries. Despite its frequent consumption in daily life, the mechanism of potential interactions between ginger components-drug has not been examined. To elucidate the mechanism of governing the effects of 6-shogaol, a primary constituent of dried ginger, on human cytochrome P450 (CYP) isoenzymes an incubation studies were carried out using pooled human liver microsome (HLM).
Methods and Results : CYP isoenzyme specific substrate was incubated with multiple concentrations of inhibitor, HLM and cofactors. 6-shogaol showed a potent inhibitory effect on CYP2C9, CYP1A2 and CYP2C19 with half maximal inhibitory concentration (IC50) values of 29.20, 20.68 and 18.78 ¥ìM respectively. To estimate the value of the inhibition constant (Ki) and the mode of inhibition, an incubation study with varying concentrations of each CYP isoenzyme-specific probe was performed. 6-shogaol inhibited CYP2C9 and CYP2C19 noncompetitively (Ki = 29.02 and 19.26 ¥ìM respectively), in contrast, the inhibition of CYP1A2 was best explained by competitive inhibition (Ki = 6.33 ¥ìM).
Conclusions : These findings suggest that 6-shogaol may possess inhibitory effects on metabolic activities mediated by CYP1A2, CYP2C9 and CYP2C19 in humans.
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KEYWORD
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Zingiber officinale, Cytochrome P450, Inhibition Constant, 6-Shogaol
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