Insights into oral bioavailability enhancement of therapeutic herbal constituents by cytochrome P450 3A inhibition

Insights into oral bioavailability enhancement of therapeutic herbal constituents by cytochrome P450 3A inhibition
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通过细胞色素 P450 3A 抑制增强治疗性草药成分的口服生物利用度的见解

DOI:
10.1080/03602532.2021.1917598
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发表时间:
2021-04
影响因子:
5.9
通讯作者:
Qi Wang
Qi Wang
中科院分区:
医学2区
文献类型:
--
作者:
Junmei Chen;Jinman Liu;Yueyue Huang;Ruoyu Li;Cuiru Ma;Beiping Zhang;Fanchang Wu;Wenqian Yu;Xue Zuo;Yong Liang;Qi Wang

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摘要 草本植物通常具有复杂的成分和多样的机制。其中,体内暴露量相对较高的生物活性成分可能表现出治疗功效。另一方面,它们的生物利用度可能受到不同生物活性成分的协同效应的影响。细胞色素 P450 3A (CYP3A) 是最丰富的 CYP 酶之一,负责 50% 已批准药物的代谢。近年来,许多治疗性草药成分已被确定为 CYP3A 底物。更明显的是,源自草药配方的 CYP3A 抑制在提高治疗成分的口服生物利用度方面发挥着关键作用。 CYP3A 抑制可能是中药方协同作用的机制。在这篇综述中,我们探讨了CYP3A的多样性,总结了具有CYP3A抑制作用的草药单体,并评估了草药介导的CYP3A抑制作用,从而为CYP3A抑制介导的口服草药生物利用度的机制提供了新的见解。
Abstract Herbal plants typically have complex compositions and diverse mechanisms. Among them, bioactive constituents with relatively high exposure in vivo are likely to exhibit therapeutic efficacy. On the other hand, their bioavailability may be influenced by the synergistic effects of different bioactive components. Cytochrome P450 3A (CYP3A) is one of the most abundant CYP enzymes, responsible for the metabolism of 50% of approved drugs. In recent years, many therapeutic herbal constituents have been identified as CYP3A substrates. It is more evident that CYP3A inhibition derived from the herbal formula plays a critical role in improving the oral bioavailability of therapeutic constituents. CYP3A inhibition may be the mechanism of the synergism of herbal formula. In this review, we explored the multiplicity of CYP3A, summarized herbal monomers with CYP3A inhibitory effects, and evaluated herb-mediated CYP3A inhibition, thereby providing new insights into the mechanisms of CYP3A inhibition-mediated oral herb bioavailability.
DOI: --
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