SQUALESTATIN

Uses

Zaragozic acid A trisodium salt is a potent inhibitor of squalene synthase.

Uses

Zaragozic acid A trisodium salt has been used as:

• a component of serum-free medium for human embryonic kidney cells in a wound scratch assay to test its effect on wound healing
• a farnesyl-diphosphate farnesyltransferase 1 (FDFT1) or squalene synthase inhibitor in stromal cells
• a cholesterol synthesis inhibitor in T cells

Biochem/physiol Actions

Potent inhibitor, in vivo and in vitro, of mammalian, fungal and Saccharomyces cervisiae squalene synthase. Squalene synthase is the first committed enzyme in sterol synthesis, catalyzing the reductive condensation of farnesyl pyrophosphate to form squalene. As a squalene synthase inhibitor, zaragozic acid produces lower plasma cholesterol levels in primates. Treatment of rats with zaragozic acid A caused an increase in hepatic low density lipoprotein (LDL) receptor mRNA levels.