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The interaction of flavonoids, alkaloids, and terpenoids with the major drug transporters in the organic anion transporting polypeptide and organic anion transporter families

delete2026-07-25
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Z
Zichong Li
X
Xuyang Wang
C
Chaomin Pan
洪梅 (Mei Hong) *
DOI:10.1016/j.apsb.2026.07.032delete
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Abstract

Abstract

En 中文
Natural compounds are ubiquitously found in the plant kingdom and are well-known for their beneficial effects on human health. The easy accessibility and the relatively affordable price make them popular choices for self-medication and/or as part of a healthy daily diet. While it has long been established that natural compounds can influence the function of drug transporters, information about these interactions is often scattered and fragmented. To more systematically and comprehensively summarize the available information in the related field, we categorized the natural products that affect uptake transporters in the organic anion transporting polypeptide (OATP) and organic anion transporter (OAT) families into three groups: flavonoids, alkaloids, and terpenoids. By providing the half-maximal inhibitory concentration (IC50) and/or inhibition constant (Ki) of the specific substrates and comparing them to the maximum plasma concentrations (Cmax) of natural products, the likelihood of drug–drug interactions (DDIs) at these transporters is proposed. Moreover, information regarding mechanistic studies, which is essential for understanding the molecular mechanisms of natural product–transporter interactions but is currently quite limited, is included. We also suggested potential indirect DDIs posed by natural compounds that are mediated by nuclear receptors and protein kinases, which may affect expression and post-translational modification of OATPs and OATs.
Keywords:
OATPs
OATs
Drug–drug interaction
Flavonoids
Alkaloids
Terpenoids
Nuclear receptors
Protein kinases
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Journal

Acta Pharmaceutica Sinica B cover
Acta Pharmaceutica Sinica B
IF:
14.6
Papers:
2.6K
Citations:
2.1W

Organization

S
South China Agricultural University
Scholars:
3.0W
Papers: 1.5W
Citations: 2.6W
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