Drug intelligence / Profile preview

hirsuteine

Development stage
Preclinical
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
01

Overview

Hirsuteine is a tetracyclic indole alkaloid primarily isolated from plants of the Uncaria genus, such as Uncaria rhynchophylla and Uncaria sinensis. It is known for its antagonistic activity at nicotinic acetylcholine receptors, where it acts as a noncompetitive antagonist. Hirsuteine has demonstrated various biological activities in vitro and in vivo, including inhibition of nicotine-mediated dopamine release by blocking ion channels associated with these receptors. Preclinical studies have shown that hirsuteine exhibits antiproliferative and pro-apoptotic effects against several cancer cell lines (including breast cancer, lung cancer, and colorectal cancer), often through mechanisms involving cell cycle arrest (notably G0/G1 phase), induction of apoptosis via the Bax/Bcl‑2 pathway or caspase activation, autophagy induction, and modulation of p53 signaling pathways. Hirsuteine is not an approved pharmaceutical drug but is studied for its potential anticancer properties[1][2][3][5][6][7][8][9][10].

Other names
hirsuteine3-Epicorynantheinedelta18-Hirsutinedelta-18-Hirsutinedelta 18-Hirsutine18,19-Didehydrohirsutine
02

Targets

BCL-2 (BCL-2 family)TP53 (Cellular Tumor Antigen p53 R175H)Nicotinic Acetylcholine Receptor

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