体内的影响白毛茛,卡瓦胡椒,黑升麻,和缬草对人类细胞色素P450 1 a2, 2 d6 2 e1, 3 a4/5表型。

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Gurley BJ,加德纳科幻,哈伯德,威廉姆斯DK,贵族WB,汗IA,沙

体内的影响白毛茛,卡瓦胡椒,黑升麻,和缬草对人类细胞色素P450 1 a2, 2 d6 2 e1, 3 a4/5表型。

77年5月,中国新药杂志。2005(5):415 - 26所示。doi: 10.1016 / j.clpt.2005.01.009。

PubMed ID

15900287 (在PubMed

]

文摘

目的:Phytochemical-mediated调制的细胞色素P450 (CYP)活动可能构成许多herb-drug交互。单个时间点表型代谢比率是用来确定长期补充白毛茛(黄连碱黄花),黑升麻(升racemosa)、卡瓦胡椒(Piper methysticum),或缬草(缬草officinalis)提取影响CYP1A2, CYP2D6、CYP2E1,或者CYP3A4/5活动。方法:12个健康志愿者(6女性)被随机分配接受白毛茛,黑升麻,卡瓦胡椒,或缬草为28天。对于每一个主题,一个30天的洗脱期之间插入每个补充阶段。探针药物鸡尾酒的咪达唑仑和咖啡因,24小时后由chlorzoxazone和debrisoquin(客栈,debrisoquine),之前管理(基线)和结束时的补充。Presupplementation和postsupplementation表型特征测量测定CYP3A4/5, CYP1A2、CYP2E1,并通过使用1-hydroxymidazolam /咪达唑仑CYP2D6血清比率(小时样本),paraxanthine /咖啡因血清比率(6小时样本),6-hydroxychlorzoxazone / chlorzoxazone血清比率(2小时样品),和debrisoquin尿复苏比率(8个小时的集合),分别。所谓的“积极”的内容为每个补充确定植物化学物质。结果:比较presupplementation和postsupplementation表型比例意味着显示显著抑制CYP2D6(大约40%)(差异,-0.228;95%可信区间(CI), -0.268 - -0.188)和CYP3A4/5(差异,-1.501;95%可信区间,-1.840至-1.163)白毛茛的活动。 Kava produced significant reductions (approximately 40%) in CYP2E1 only (difference, -0.192; 95% CI, -0.325 to -0.060). Black cohosh also exhibited statistically significant inhibition of CYP2D6 (difference, -0.046; 95% CI, -0.085 to -0.007), but the magnitude of the effect (approximately 7%) did not appear to be clinically relevant. No significant changes in phenotypic ratios were observed for valerian. CONCLUSIONS: Botanical supplements containing goldenseal strongly inhibited CYP2D6 and CYP3A4/5 activity in vivo, whereas kava inhibited CYP2E1 and black cohosh weakly inhibited CYP2D6. Accordingly, serious adverse interactions may result from the concomitant ingestion of goldenseal supplements and drugs that are CYP2D6 and CYP3A4/5 substrates. Kava kava and black cohosh may interact with CYP2E1 and CYP2D6 substrates, respectively. Valerian appears to be less likely to produce CYP-mediated herb-drug interactions.

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药物酶

药物	酶	类	生物	药理作用	行动
黑升麻	细胞色素P450 1 a2	蛋白质	人类	没有	抑制剂	细节