Drug intelligence / Profile preview

rhapontigenin

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Rhapontigenin is a naturally occurring stilbenol, structurally related to resveratrol, found in plants such as Rheum undulatum (rhubarb) and Gnetum hainanense. It is characterized chemically as trans-stilbene substituted with hydroxy groups at positions 3 and 5 on one phenyl ring, and a hydroxy group at position 3 plus a methoxy group at position 4 on the other phenyl ring. Rhapontigenin exhibits multiple biological activities including inhibition of cytochrome P450 enzymes (notably CYP1A1), antineoplastic (anticancer), antioxidant, antiviral, antifungal, antibacterial, antilipemic (lipid-lowering), cardioprotective effects, angiogenesis inhibition, melanin synthesis inhibition, radical scavenging activity and quorum sensing inhibition. It has been studied for its cytotoxic effects against cancer cells—particularly colon cancer—and for its potential use in improving cardiovascular health due to its structural similarity to phytoestrogens like resveratrol and diethylstilbestrol. Its mechanism of action includes selective inactivation of cytochrome P450 enzymes; it may also act as a phytoestrogen due to structural similarities with estrogenic compounds[1][2][3][4][10].

Other names
protigeninpontigeninrhapontin genin
02

Targets

CYP1B1 (Cytochrome P450 1B1)CYP1A1 (Cytochrome P450 1A1)CYP1A2 (Cytochrome P450 1A2)

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