Drug intelligence / Profile preview

pectolinarigenin

Development stage
Preclinical
Lead developer
Wuhan University
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

Pectolinarigenin is a natural flavonoid compound primarily isolated from the medicinal herb *Linaria vulgaris* and other plants such as *Cirsium chanroenicum* and citrus fruits. It is currently being investigated for its potent anti-tumor activities across various malignancies, including bladder, gastric, and hepatocellular cancers. Its primary mechanism of action involves acting as a DNA topoisomerase II alpha (TOP2A) poison, which stabilizes TOP2A-DNA cleavage complexes, leading to double-strand DNA breaks and subsequent G2/M phase cell cycle arrest via the p53 pathway. Additionally, pectolinarigenin inhibits late-stage autophagic flux, preventing the degradation of autophagosomes and thereby sensitizing cancer cells to DNA damage-induced apoptosis. Beyond its oncology applications, it has demonstrated anti-inflammatory properties through the dual inhibition of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX).

Other names
pectolinarigenin5,7-dihydroxy-6-methoxy-2-(4-methoxyphenyl)chromen-4-one
02

Targets

ALOX12 (Arachidonate 12-lipoxygenase, 12S type)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)TOP2A (DNA topoisomerase II)NeuraminidasePI3K (Phosphoinositide-3-kinase regulatory subunit 6)STAT3 (Signal Transducer and Activator of Transcription 3)

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