Drug intelligence / Profile preview

worenine

Development stage
Preclinical
Modality
Small Molecules
Administration
Topical, Intraperitoneal, In Vitro
01

Overview

Worenine is a bioactive isoquinoline alkaloid primarily isolated from the traditional Chinese medicinal herb *Coptis chinensis* (Coptidis Rhizoma). It has demonstrated significant anti-tumor activity across various cancers, including triple-negative breast cancer, non-small cell lung cancer, and colorectal cancer, often by reversing the Warburg effect and inhibiting HIF-1α signaling. Additionally, worenine acts as an inhibitor of T-lymphokine-activated killer cell-originated protein kinase (TOPK) and c-Jun N-terminal kinase 2 (JNK2), showing potential in treating inflammatory conditions like psoriasis and solar ultraviolet-induced sunburn. While it exhibits therapeutic potential, studies have also noted its potential for hepatotoxicity mediated by organic cation transporter 1 (OCT1) uptake and cytochrome P450-driven metabolic activation.

Other names
worenine chloride
02

Targets

HIF1A (Hypoxia-inducible factor 1-alpha)

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