Drug intelligence / Profile preview

fangchinoline

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intraperitoneal (in Animal Studies), Topical (experimental), In Vitro (cell Culture)
01

Overview

Fangchinoline is a **bisbenzylisoquinoline alkaloid** isolated primarily from the plant Stephania tetrandra. It demonstrates a wide range of biological activities, notably antineoplastic (anticancer), anti-inflammatory, antioxidant, anti-HIV-1, and neuroprotective effects. Its mechanism of action varies by indication and context but includes: - Suppressing homologous recombination (HR)-directed DNA repair by binding to far upstream element binding protein 2 (FUBP2) and downregulating HR factors such as BRCA1 and RAD51 in conjunctival melanoma, thereby enhancing sensitivity to DNA-damaging drugs like cisplatin and doxorubicin[1]. - Inducing apoptosis in gallbladder cancer cells by inhibiting the PI3K/Akt/XIAP pathway[3]. - Suppressing Focal adhesion kinase (FAK)-mediated signaling pathway in tumor cells, particularly those highly expressing FAK[5]. - Exerting inhibitory effects on cell proliferation in a range of cancers, including bladder, prostate, breast, gastric, hepatocellular carcinoma, melanoma, and colorectal cancer[4][16][18]. - Promoting autophagy and inhibiting apoptosis in osteoporosis models, with effects on gene expression of RANKL, ATG-5, RUNX-2, Beclin-1, and BMP2[6]. Experimental data suggest it is typically administered intraperitoneally in animal models, and in vitro studies use a variety of cell lines and solvent preparations.

Other names
Hanfangchin B7-O-DemethyltetrandrineTetrandrine BFangchinoline-RM12-O-Methylatherospermoline
02

Targets

PI3K (Phosphoinositide-3-kinase regulatory subunit 6)KHSRP (KH-type splicing regulatory protein)AKT (RAC-alpha serine/threonine-protein kinase)BRCA1 (Breast cancer type 1 susceptibility protein)RAD51 (RAD51 Recombinase)

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