Drug intelligence / Profile preview

rhaponticin

Development stage
Preclinical
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Rhaponticin is a natural stilbene glycoside compound primarily found in species of the Rheum genus (rhubarb), such as Rheum undulatum. It is structurally related to stilbenes and consists of a glucoside moiety attached to a methoxystilbene backbone. Rhaponticin exhibits diverse pharmacological activities, including anti-inflammatory, antioxidant, antitumor (antineoplastic), antilipemic, neuroprotective, anti-allergic, anti-fibrotic, and hypoglycemic effects[1][2][5]. Mechanistically, it has been shown to inhibit fatty acid synthase (EC 2.3.1.85), suppress osteoclast formation by targeting RANKL-induced ROS and NFATc1 pathways (including MAPK and NF-kB signaling), induce apoptosis in cancer cells by inhibiting angiogenesis and cell migration/invasion processes[1][5]. Rhaponticin also modulates AMP activated protein kinase (AMPK) activation and transforming growth factor beta/Smad pathway activity[5]. It is under investigation for potential use in chronic diseases such as osteoporosis (by inhibiting bone resorption), diabetes mellitus (anti-diabetic effect), cancer prevention/treatment, inflammatory disorders, fibrosis-related conditions, metabolic syndrome components like hyperlipidemia/hyperglycemia[1][2][5].

Other names
trans-rhaponticin3,3',5-trihydroxy-4'-methoxystilbene 3-O-beta-D-glucoside3-hydroxy-5-[E)-2-(3-hydroxy-4-methoxyphenyl)vinyl]phenyl beta-D-glucopyranoside
02

Targets

FASN (Fatty acid synthase)

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