Insights into oral bioavailability enhancement of therapeutic herbal constituents by cytochrome P450 3A inhibition.
Drug Metab Rev
; 53(4): 491-507, 2021 11.
Article
em En
| MEDLINE
| ID: mdl-33905669
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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Preparações de Plantas
/
Citocromo P-450 CYP3A
/
Inibidores do Citocromo P-450 CYP3A
Limite:
Humans
Idioma:
En
Revista:
Drug Metab Rev
Ano de publicação:
2021
Tipo de documento:
Article
País de afiliação:
China