Drug intelligence / Profile preview

demethylzeylasteral

Development stage
Preclinical
Lead developer
Zhongshan Hospital, Fudan University
Modality
Classical Binding Small Molecules → Small Molecules
Administration
In Vitro
01

Overview

Demethylzeylasteral is a pentacyclic triterpenoid compound (molecular formula C29H36O6, CAS 107316-88-1) isolated from the roots of Tripterygium wilfordii (thunder god vine), a traditional medicinal plant of East Asia. It exhibits broad pharmacological activities, including anti-tumor, anti-inflammatory, immunosuppressive, and anti-atherosclerotic effects. Mechanistically, demethylzeylasteral induces cell cycle arrest (notably at the S phase) and apoptosis in diverse cancer cell types by modulating the expression of cell cycle regulators (such as downregulating MCL1, leading to CDK2 degradation), promoting ROS-mediated endoplasmic reticulum stress, inhibiting autophagic flux, and blocking signaling pathways including TGF-β and JAK-STAT. It demonstrates enhanced chemosensitivity when used in combination with cytotoxic agents such as 5-fluorouracil or cisplatin. Its targets include immunological and cancer-related pathways, highlighting its potential as an investigational anti-cancer and immune-modulating small molecule[2][5][6][7][8][9].

Other names
(9beta,13alpha,14beta,20alpha)-2,3-Dihydroxy-9,13-dimethyl-6,23-dioxo-24,25,26-trinoroleana-1,3,5(10),7-tetraen-29-oic acid
02

Targets

CDK2 (Cyclin-dependent kinase 2)MCL1 (Myeloid cell leukemia sequence 1)

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