Drug intelligence / Profile preview

piceatannol

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Piceatannol is a naturally occurring polyphenolic stilbenoid and phenol found in various fruits and vegetables such as grapes and passion fruit. It is also a metabolite of resveratrol formed via cytochrome P450-mediated hydroxylation[7][1]. Piceatannol acts as a protein kinase inhibitor—most notably inhibiting the tyrosine kinase Syk—and has demonstrated antineoplastic (anticancer), anti-inflammatory, antiangiogenic (inhibiting VEGF-mediated signaling), hypoglycemic (blood sugar-lowering), and geroprotective properties[1][6][5]. Mechanistically it inhibits Syk-dependent signaling pathways in immune cells and blocks VEGF-induced angiogenesis by interfering with VEGF binding to its receptors[6][5]. It also activates SIRT1 deacetylase activity[5]. While preclinical studies suggest potential for treating metabolic diseases (such as obesity-related disorders), cancer, cardiovascular disease (including atherosclerosis), and angiogenesis-related conditions, clinical development remains limited to experimental or early-stage research[3][6].

Other names
3-hydroxyresveratol3,3',4,5'-tetrahydroxystilbene3,5,3',4'-tetrahydroxystilbene4-[(E)-2-(3,5-dihydroxyphenyl)vinyl]benzene-1,2-diol3,4,3′,5′–tetrahydroxy-trans-stilbene
02

Targets

SIRT1 (NAD-dependent protein deacetylase sirtuin-1)SYK (Spleen Tyrosine Kinase)VEGFR (VEGFR family)

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