Drug intelligence / Profile preview

coptisine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Coptisine is a natural protoberberine alkaloid primarily extracted from the medicinal plant *Coptis chinensis* (Rhizoma Coptidis) and *Chelidonium majus*. It is chemically related to berberine and has been extensively studied for its diverse pharmacological activities, including anti-inflammatory, antimicrobial, and antineoplastic properties. Research indicates that coptisine exerts anti-tumor effects by modulating several key intracellular signaling pathways; notably, it has been shown to block the progression of bladder cancer by inhibiting the **PI3K/AKT pathway**, which reduces cell proliferation and induces apoptosis. Beyond oncology, coptisine is investigated for its potential in treating metabolic disorders such as diabetes and hyperlipidemia, often through the activation of **AMP-activated protein kinase (AMPK)**. It also shows inhibitory activity against monoamine oxidase and topoisomerases.

Other names
coptisine chloridebis(methylenedioxy)protoberberine6,7-dihydro-bis[1,3]benzodioxolo[5,6-a:4',5'-g]quinolizinium
02

Targets

AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)AMPK (Adenosine monophosphate–activated protein kinase)TOP (DNA topoisomerases)MAOA (Monoamine oxidase A)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)DNAKRAS rG4 (KRAS RNA G-quadruplex)GSK3 (Glycogen synthase kinase 3 beta)mTOR (Mammalian target of rapamycin kinase)

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