Inhibition of Coix seed extract on fatty acid synthase, a novel target for anticancer activity

Ethnopharmacological relevance: Coix seed has been traditionally used to treat cancers in folk medicine. Aim of the study: Study the anticancer action mechanism of Coix seed extract. Materials and methods: After the treatment with Coix seed extract (10 mu l/ml), the residual activity of fatty acid synthase (EAS) as overall reaction, beta-ketoacyl reduction, enoyl reduction, and acetyl acetyl coenzyme A (AcAcCoA) reduction was separately detected at 340 nm in the UV-190 spectrophotometer. After rats were administrated Coix seed extract (2.5, 5.0, and 10.0 ml/kg) intragastrically for 10 days consecutively, activities of FAS, malate dehydrogenase (MDH), lipid protein lipase (LPL), hepatic lipase (HL), triglyceride (TG), and glucose-6-phosphate clehydrogenase (G-6-PD) in the plasma, liver and fatty tissues were determined. Results: Experiments in vitro showed that the inhibition of Coix seed extract on FAS activity was significant and dose dependent, and two active sites inhibited were beta-ketoacyl reductases (KR) and enoyl reductase (ER). Experiments in vivo showed that Coix seed extract inhibited FAS activity in the liver, and elevated LPL and HL activity in the plasma, and effected G-6-PID activity. Conclusions: The study supports that EAS is a novel target for anticancer activity, and provides a theoretical foundation for the wide application of Coix seed extract in traditional medicine. (C) 2008 Elsevier Ireland Ltd. All rights reserved.