oltipraz

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

Oltipraz metabolite M2 is the active metabolite of Oltipraz and acts as an orally effective HIF-1α inhibitor. In a high-fat diet mouse model, it enhances mitochondrial fuel oxidation and suppresses hepatic lipogenesis by dual activation of AMPK. Oltipraz metabolite M2 is applicable for research in hepatic steatosis and fatty liver disease.