Drug intelligence / Profile preview

2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intraperitoneal, Intravenous
01

Overview

2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside (THSG or TSG) is a compound isolated from the rhizome of the traditional Chinese herb, Polygonum multiflorum. It functions as an arginase inhibitor, specifically showing noncompetitive inhibition of arginase II and dose-dependent inhibition of both arginase I and II. This inhibition leads to increased nitric oxide production and decreased reactive oxygen species generation, along with enhanced dimerization of endothelial nitric oxide synthase. THSG has demonstrated vasoprotective effects by augmenting nitric oxide signaling, suggesting its potential in treating vascular diseases like atherosclerosis. Additionally, THSG exhibits neuroprotective properties, particularly in models of Parkinson's disease, by preventing reactive oxygen species-induced neuron loss. Its mechanism in neuroprotection involves blocking the activation of JNK and P38 pathways, downregulating the bax/bcl-2 ratio, and inhibiting the release of cytochrome c and smac, as well as the activation of caspases-3, -6, and -9.

Other names
tetrahydroxystilbene glucoside
02

Targets

ARG2 (Arginase 2)NOS3 (eNOS)ARG1 (Arginase 1)CASP3 (Caspase-3)CYCS (Cytochrome c)

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