Côté Cynthia S, Kor Christine, Cohen Jon, Auclair Karine
Department of Chemistry, McGill University, 801 Sherbrooke Street West, Montréal, Que., Canada H3A 2K6.
Biochem Biophys Res Commun. 2004 Sep 10;322(1):147-52. doi: 10.1016/j.bbrc.2004.07.093.
For centuries the South Pacific islanders have consumed kava (Piper methysticum) as a ceremonial intoxicating beverage. More recently, caplets of kava extracts have been commercialized for their anxiolytic and antidepressant activities. Several cases of hepatotoxicity have been reported following consumption of the commercial preparation whereas no serious health effects had been documented for the traditional beverage. A detailed comparison of commercial kava extracts (prepared in acetone, ethanol or methanol) and traditional kava (aqueous) reveals significant differences in the ratio of the major kavalactones. To show that these variations could lead to differences in biological activity, the extracts were compared for their inhibition of the major drug metabolizing P450 enzymes. In all cases (CYP3A4, CYP1A2, CYP2C9, and CYP2C19), the inhibition was more pronounced for the commercial preparation. Our results suggest that the variations in health effects reported for the kava extracts may result from the different preparation protocols used.
几个世纪以来，南太平洋岛民一直将卡瓦（胡椒科植物卡瓦）作为一种仪式性的致醉饮品。最近，卡瓦提取物胶囊因其抗焦虑和抗抑郁活性而实现了商业化。食用这种商业制剂后已报告了几例肝毒性病例，而传统饮品并未记录有严重的健康影响。对商业卡瓦提取物（用丙酮、乙醇或甲醇制备）和传统卡瓦（水性）进行的详细比较显示，主要卡瓦内酯的比例存在显著差异。为了表明这些差异可能导致生物活性的不同，对提取物抑制主要药物代谢P450酶的能力进行了比较。在所有情况下（CYP3A4、CYP1A2、CYP2C9和CYP2C19），商业制剂的抑制作用更为明显。我们的结果表明，所报告的卡瓦提取物健康影响的差异可能源于所使用的不同制备方法。
