Inhibition of Coix seed extract on fatty acid synthase, a novel target for anticancer activity.
BACKGROUND
Coix seed has been traditionally used to treat cancers in folk medicine.


OBJECTIVE
Study the anticancer action mechanism of Coix seed extract.


METHODS
After the treatment with Coix seed extract (10 microl/ml), the residual activity of fatty acid synthase (FAS) 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 dehydrogenase (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-PD activity.


CONCLUSIONS
The study supports that FAS is a novel target for anticancer activity, and provides a theoretical foundation for the wide application of Coix seed extract in traditional medicine.
Yu
Fei
F
Department of Pharmaceutical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China.
Gao
Jing
J
Zeng
Yong
Y
Liu
Chang-Xiao
CX
D064431:3-Oxoacyl-(Acyl-Carrier-Protein) Reductase; D000429:Alcohol Oxidoreductases / Q000037:antagonists & inhibitors; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D031742:Coix / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems; D004372:Ducks; D064429:Fatty Acid Synthases / Q000187:drug effects* / Q000378:metabolism; D005954:Glucosephosphate Dehydrogenase / Q000187:drug effects / Q000378:metabolism; D008049:Lipase / Q000187:drug effects / Q000378:metabolism; D008071:Lipoprotein Lipase / Q000187:drug effects / Q000378:metabolism; D008099:Liver / Q000187:drug effects / Q000201:enzymology; D008519:Medicine, Traditional; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012639:Seeds; D014280:Triglycerides / Q000378:metabolism
D000972:Antineoplastic Agents, Phytogenic; D010936:Plant Extracts; D014280:Triglycerides; D000429:Alcohol Oxidoreductases; D064431:3-Oxoacyl-(Acyl-Carrier-Protein) Reductase; D005954:Glucosephosphate Dehydrogenase; D064429:Fatty Acid Synthases; D008049:Lipase; C502353:hepatic lipase, rat; D008071:Lipoprotein Lipase