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	Inhibition of fatty acid synthase by polyphenols
	Tian, WX
刊名	Current medicinal chemistry
	2006
卷号	13期号:8页码:967-977
关键词	Fatty acid synthase Inhibition Polyphenols Catechins Theaflavins Flavonoids Obesity Cancer
ISSN号	0929-8673
通讯作者	Tian, wx(tianweixi@gucas.ac.cn)
英文摘要	Recently, animal fatty acid synthase (fas) is reported as a potential therapeutic target for obesity and cancer. considerable interest has been developed in identifying novel inhibitors of the enzyme. it is found that tea polyphenols inhibit fas in both reversible and irreversible manners. epigallocatechin gallate (egcg) and epicatechin gallate (ecg) inhibit fas with ic50 values of 52 mu m and 42 mu m mainly by reacting on the beta-ketoacyl reductase (kr) domain of fas. the inhibitory ability of catechin gallate (cg) is 15 and 12 folds higher than that of egcg and ecg. its major reacting site on fas is not kr. all of these irreversibly inactivate fas on the kr domain with similar rates. mulliken population analysis suggests that the positive charge is distributed on the carbon atom of galloyl ester, and this carbon becomes more susceptible for a nucleophilic attack. 12 flavonoids inhibit fas with ic50 values ranging from 2 to 112 mu m. sar analysis shows that the flavonoids containing two hydroxyl groups in b ring and 5, 7-hydroxyl groups in a ring with c-2, 3 double bond are the most potent inhibitors. the inhibition kinetics shows that they inhibit fas competitively with acetyl coa and most likely react mainly on acyl transferase domain. further studies show that c ring of flavonoids is not necessary for the inhibition. resveratrol, phlorizin and ndga contain two phenyl rings connected by 2 to 4 atom chains instead of c ring. their ic50 values range from 5 mu m to 40 mu m. from these results, it common model for polyphenol inhibitor of fas is conceived.
WOS关键词	BREAST-CANCER CELLS ; TEA EPIGALLOCATECHIN GALLATE ; GREEN TEA ; FOOD-INTAKE ; NATURAL INHIBITOR ; PROSTATE-CANCER ; BODY-WEIGHT ; EXPRESSION ; APOPTOSIS ; DISEASE
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
WOS类目	Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Pharmacology & Pharmacy
语种	英语
出版者	BENTHAM SCIENCE PUBL LTD
WOS记录号	WOS:000236160100008
内容类型	期刊论文
URI标识	http://www.corc.org.cn/handle/1471x/2378814
专题	中国科学院大学
通讯作者	Tian, WX
作者单位	Grad Univ Chinese Acad Sci, Dept Biol, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	Tian, WX. Inhibition of fatty acid synthase by polyphenols[J]. Current medicinal chemistry,2006,13(8):967-977.
APA	Tian, WX.(2006).Inhibition of fatty acid synthase by polyphenols.Current medicinal chemistry,13(8),967-977.
MLA	Tian, WX."Inhibition of fatty acid synthase by polyphenols".Current medicinal chemistry 13.8(2006):967-977.

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