Drug intelligence / Profile preview

epiberberine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Epiberberine is a natural protoberberine alkaloid found as a main active constituent of the traditional Chinese medicinal herb Rhizoma Coptidis (Huanglian) and related plants including Corydalis ternata and Coptis deltoidea[1][5][8]. Epiberberine exhibits a range of pharmacological activities including antihyperglycemic, antihyperlipidemic, anti-inflammatory, antioxidant, anti-Alzheimer, and antitumor properties[1][3][4][6][7]. Recent studies show it acts as an inhibitor of urease and cytochrome P450 enzymes, regulates human organic cation transporters (OCT1, OCT2, OCT3), and can interact strongly with DNA (notably human telomeric G-quadruplexes) potentially impacting oncogenic processes[1][7][10]. In cancer biology, epiberberine downregulates the JNK pathway and metalloproteinase 13 (MMP-13), inhibiting metastasis and invasion in head and neck squamous cell carcinoma and suppresses osteoclastogenesis in breast cancer-induced bone metastasis[3][4][6]. Toxicity studies indicate epiberberine is relatively safe compared to related alkaloids[1]. It is proposed as a lead compound for the development of agents against metabolic syndrome, cardiovascular and neurodegenerative diseases, and certain cancers[1][6].

Other names
epiberberine ionepiberberine cationdehydrosinactinesiberianepiberberine chloride11,12-dihydro-8,9-dimethoxybenzo[a]-1,3-benzodioxolo[4,5-g]quinolizinium8,9-dimethoxy-11,12-dihydro-[1,3]dioxolo[4,5-h]isoquinolino[2,1-b]isoquinolin-13-ium
02

Targets

CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)OCT3 (Organic cation transporter 3)

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