首页> 外文会议>American Society for Mass Spectrometry Conference on Mass Spectrometry and Allied Topics >Mass spectrometric identification and characterization of cytochrome P4502D6 inhibitors from black cohosh (Actaea racemosa L.)
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Mass spectrometric identification and characterization of cytochrome P4502D6 inhibitors from black cohosh (Actaea racemosa L.)

机译:黑色宿源(Actaea Haremosa L.)细胞色素P4502D6抑制剂的质谱鉴定及表征。

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Black cohosh contains compounds that can inhibit cytochrome P4502D6. Mass spectrometric dereplication of the active fraction led to identification of two protopine-type alkaloids, protopine and allocryptopine, as potent inhibitors of CYP2D6. This is the first report that black cohosh contains protopine class of alkaloids. Both compounds were competitive inhibitors of CYP2D6 with Ki values of 72 nM and 110 nM for protopine and allocryptopine, respectively. The levels of these compounds in the crude black cohosh extract were low indicating that clinically relevant inhibition of CYP2D6 is unlikely to be observed. However, given the high activity of these compounds, extracts prepared by other procedures should be evaluated for content of these alkaloids to determine their potential to interact with drugs that are metabolized by CYP2D6.
机译:黑色Cohosh含有可以抑制细胞色素P4502D6的化合物。具有活性级分的质谱绝明,导致鉴定两种突出型生物碱,刺激素和Allocryptopine,作为CYP2D6的有效抑制剂。这是第一份报告,黑色·科学含有癌症类别的生物碱类。两种化合物分别是CYP2D6的竞争性抑制剂,其分别具有72nm和110nm的Ki值,分别用于原卟啉和Allocryptopine。粗黑色旋疗提取物中这些化合物的水平低表明,不太可能观察到CYP2D6的临床相关抑制。然而,考虑到这些化合物的高活性,应评估其他方法制备的提取物用于这些生物碱的含量,以确定它们与CYP2D6代谢的药物相互作用的潜力。

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