Metabolic Insights into Coumarins from Angelica Dahurica Radix: Underlying Mechanisms of Herb-Drug Interactions.
- 1School of Chinese Materia Medica, Chongqing College of Traditional Chinese Medicine, Chongqing, 402760, People's Republic of China.
Abstract
Angelica dahurica Radix (AD), a traditional Chinese medicine, is widely used and has a diverse array of pharmacological activities. The main chemical components of AD are coumarins. AD and its main components are often used in combination with other drugs and have anti-inflammatory, antibacterial, antitumor, and whitening effects. With the increasing use of AD-containing formulations in clinical applications, herb-drug interactions (HDIs) have increased. A comprehensive narrative review is performed based on multiple databases, including Web of Science, ScienceDirect, PubMed, Elsevier, CNKI, and Scopus, from 1988 to 2026, using the keywords "Angelica dahurica Radix", "coumarins", "cytochrome P450 enzymes (CYPs)", UDP-glucuronosyltransferases (UGTs), and "transporter". Only fully published peer-reviewed articles satisfying our predefined inclusion criteria were ultimately included. This study aimed to explore whether AD, a key regulator of pharmacokinetic drug interactions, affects the expression and activity of CYPs, UGTs, and P-glycoprotein (P-gp). This study mainly included drug-metabolizing enzymes (DMEs) and transport proteins. Recent studies have indicated that AD and its main components (linear and angular furanocoumarins) exert multiple regulatory effects on CYP1A2, CYP2D6, CYP3A4, and P-gp. Collectively, the results of clinical trials of human volunteers, in vitro liver microsome assays, and rodent pharmacokinetic experiments collectively demonstrate that AD and its main coumarin constituents lead to complex inhibitory and inductive regulation of key DMEs and transporters, altering the absorption, metabolism and elimination of coadministered drugs and triggering HDIs. This study may provide a comprehensive reference for safe and rational clinical combined medication with AD preparations.
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BibTeX
@article{rao2026metabolic,
title = {{Metabolic Insights into Coumarins from Angelica Dahurica Radix: Underlying Mechanisms of Herb-Drug Interactions.}},
author = {Jinqiu Rao and Shasha Qin and Yafei Yang and Jiaying Zhao and Chunyu Li and Lingli Mou and Fan Wang and Weiguo Cao},
journal = {Drug design, development and therapy},
year = {2026},
month = oct,
doi = {10.2147/dddt.s624447},
url = {https://europepmc.org/article/MED/42928897},
note = {CC BY-NC},
}
RIS
TY - JOUR
TI - Metabolic Insights into Coumarins from Angelica Dahurica Radix: Underlying Mechanisms of Herb-Drug Interactions.
AU - Jinqiu Rao
AU - Shasha Qin
AU - Yafei Yang
AU - Jiaying Zhao
AU - Chunyu Li
AU - Lingli Mou
AU - Fan Wang
AU - Weiguo Cao
PY - 2026
DA - 2026/10/21
JO - Drug design, development and therapy
DO - 10.2147/dddt.s624447
UR - https://europepmc.org/article/MED/42928897
AB - Angelica dahurica Radix (AD), a traditional Chinese medicine, is widely used and has a diverse array of pharmacological activities. The main chemical components of AD are coumarins. AD and its main components are often used in combination with other drugs and have anti-inflammatory, antibacterial, antitumor, and whitening effects. With the increasing use of AD-containing formulations in clinical applications, herb-drug interactions (HDIs) have increased. A comprehensive narrative review is performed based on multiple databases, including Web of Science, ScienceDirect, PubMed, Elsevier, CNKI, and Scopus, from 1988 to 2026, using the keywords "Angelica dahurica Radix", "coumarins", "cytochrome P450 enzymes (CYPs)", UDP-glucuronosyltransferases (UGTs), and "transporter". Only fully published peer-reviewed articles satisfying our predefined inclusion criteria were ultimately included. This study aimed to explore whether AD, a key regulator of pharmacokinetic drug interactions, affects the expression and activity of CYPs, UGTs, and P-glycoprotein (P-gp). This study mainly included drug-metabolizing enzymes (DMEs) and transport proteins. Recent studies have indicated that AD and its main components (linear and angular furanocoumarins) exert multiple regulatory effects on CYP1A2, CYP2D6, CYP3A4, and P-gp. Collectively, the results of clinical trials of human volunteers, in vitro liver microsome assays, and rodent pharmacokinetic experiments collectively demonstrate that AD and its main coumarin constituents lead to complex inhibitory and inductive regulation of key DMEs and transporters, altering the absorption, metabolism and elimination of coadministered drugs and triggering HDIs. This study may provide a comprehensive reference for safe and rational clinical combined medication with AD preparations.
SN - 1177-8881
ER -