Science and Technology Innovation Center, Guangzhou University of Chinese Medicine, Guangzhou, China.
Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, Guangzhou, China.
Drug Metab Rev. 2021 Nov;53(4):491-507. doi: 10.1080/03602532.2021.1917598. Epub 2021 Apr 27.
Herbal plants typically have complex compositions and diverse mechanisms. Among them, bioactive constituents with relatively high exposure 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.
草药植物通常具有复杂的成分和多样的作用机制。其中，相对高暴露量的生物活性成分可能表现出治疗效果。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作用的影响。细胞色素 P450 3A（CYP3A）是最丰富的 CYP 酶之一，负责代谢 50%已批准药物的代谢。近年来，许多治疗性草药成分被鉴定为 CYP3A 底物。更明显的是，草药配方中源自 CYP3A 的抑制作用在提高治疗性成分的口服生物利用度方面起着关键作用。CYP3A 抑制可能是草药配方协同作用的机制。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。
