Drug intelligence / Profile preview

ginkgetin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intraperitoneal (preclinical Models)
01

Overview

Ginkgetin is a natural biflavonoid compound isolated from Ginkgo biloba and other plants, characterized as a 7,4'-dimethyl ether derivative of amentoflavone. It exhibits multiple biological activities including anti-inflammatory, antioxidant, neuroprotective, antineoplastic, and anti-viral effects. Mechanistically, ginkgetin inhibits several molecular targets: it acts as a direct inhibitor of cyclooxygenase 2 (COX-2) and arachidonate 5-lipoxygenase (5-LOX), suppresses inflammatory mediators (such as through the PI3K/NF-κB/TLR-4 pathway), inhibits cellular signal transducer and activator of transcription 3 (STAT3) signaling, and directly binds to the STING protein to inhibit cGAS-STING-mediated signaling. In preclinical models, ginkgetin reduced neuroinflammation, apoptosis, and Aβ accumulation in neurodegeneration, and demonstrated efficacy in models of stroke, Alzheimer's disease, osteoarthritis, and aging-related disorders[1][2][3][4][5][7][9].

Other names
ginkgetin7,4'-dimethylamentoflavoneamentoflavone 7,4'-dimethyl ether4',5,5'',7-tetrahydroxy-4''',7''-dimethoxy-8,3'''-biflavone5,7-dihydroxy-8-[5-(5-hydroxy-7-methoxy-4-oxochromen-2-yl)-2-methoxyphenyl]-2-(4-hydroxyphenyl)chromen-4-oneCHEBI:5353HY5EZW8269HY-5EZW8269HY 5EZW8269
02

Targets

ALOX5 (Arachidonate 5-lipoxygenase)STAT3 (Signal Transducer and Activator of Transcription 3)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)NF-κB

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