Description
Linderane is a sesquiterpene that has been found in
L. aggregata. It inhibits the cytochrome P450 (CYP) isoform CYP2C9 (K
i = 1.26 μM) in an irreversible and NADPH-dependent manner. Linderane decreases phosphoenolpyruvate carboxykinase (
Pck1) and glucose-6-phosphatase (
G6pc) gene expression, cAMP concentration, and CREB phosphorylation, increases phosphodiesterase 3 (PDE3) activity, and inhibits gluconeogenesis in rat primary hepatocytes.
In vivo, linderane (50 mg/kg twice per day) decreases serum and hepatic triglyceride levels, as well as random-fed and fasting blood glucose levels in
ob/
ob mice.
