Drug intelligence / Profile preview

berberine + evodiamine

Development stage
Preclinical
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Berberine + evodiamine is a combination of two natural alkaloids, berberine (from Coptis chinensis/Rhizoma Coptidis) and evodiamine (from Evodia rutaecarpa/Fructus Evodiae), used primarily in traditional Chinese medicine. This combination has demonstrated synergistic effects in preclinical studies for metabolic disorders such as obesity and non-alcoholic fatty liver disease (NAFLD), as well as anticancer activity against various cancer cell lines. Mechanistically, the combination enhances adipose tissue browning and activates the FGF21/PGC-1α signaling pathway, leading to improved lipid metabolism, reduced hepatic steatosis, better glucose tolerance, and modulation of adipocytokines. In cancer models, it induces cell cycle arrest and apoptosis while attenuating drug resistance mechanisms such as P-glycoprotein overexpression. The pair also exerts epigenetic effects by influencing DNA methyltransferases (DNMTs) and microRNAs involved in tumor progression[1][2][3][4][5].

02

Targets

FGF21 (Fibroblast growth factor 21)DNMT3A (DNA methyltransferase 3 alpha)PPARGC1A (Peroxisome proliferator–activated receptor gamma coactivator 1-alpha)ABCB1 (P-glycoprotein)PRDM16 (PR domain zinc finger protein 16)DNMT1 (DNA (cytosine-5)-methyltransferase 1)UCP1 (Uncoupling protein 1)CIDEA (Cell death-inducing DFFA-like effector A)

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