title: Inhibition of fatty acid synthase by ginkgolic acids from the leaves of Ginkgo biloba and their cytotoxic activity.
abstract: Fatty acid synthase (FAS) has been proposed to be a new drug target for the development of anticancer agents because of the significant difference in expression of FAS between normal and tumour cells. Since a n-hexane-soluble extract from Ginkgo biloba was demonstrated to inhibit FAS activity in our preliminary test, we isolated active compounds from the n-hexane-soluble extract and evaluated their cytotoxic activity in human cancer cells. Three ginkgolic acids 1-3 isolated from the n-hexane-soluble extract inhibited the enzyme with IC(50) values 17.1, 9.2 and 10.5 µM, respectively, and they showed cytotoxic activity against MCF-7 (human breast adenocarcinoma), A549 (human lung adenocarcinoma) and HL-60 (human leukaemia) cells. Our findings suggest that alkylphenol derivatives might be a new type of FAS inhibitor with cytotoxic activity.
authors.affiliation: College of Pharmacy, Yeungnam University, Gyeongsan, Gyeongbuk, Republic of Korea.
authors.forename: Joonseok
authors.initials: J
authors.lastname: Oh
authors.forename: In Hyun
authors.initials: IH
authors.lastname: Hwang
authors.forename: Chang-Eui
authors.initials: CE
authors.lastname: Hong
authors.forename: Su-Yun
authors.initials: SY
authors.lastname: Lyu
authors.forename: MinKyun
authors.initials: M
authors.lastname: Na
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy / Q000473:pathology; D000077192:Adenocarcinoma of Lung; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D064429:Fatty Acid Synthases / Q000037:antagonists & inhibitors*; D005260:Female; D020441:Ginkgo biloba / Q000737:chemistry*; D018922:HL-60 Cells / Q000187:drug effects; D006586:Hexanes / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D008175:Lung Neoplasms / Q000188:drug therapy / Q000473:pathology; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry; D018515:Plant Leaves / Q000737:chemistry; D012459:Salicylates / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004791:Enzyme Inhibitors; D006586:Hexanes; D010936:Plant Extracts; D012459:Salicylates; C112485:ginkgolic acid; C026385:n-hexane; D064429:Fatty Acid Synthases