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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenocarcinoma / drug therapy
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Adenocarcinoma / pathology
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Adenocarcinoma of Lung
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Antineoplastic Agents, Phytogenic / chemistry
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Antineoplastic Agents, Phytogenic / pharmacology*
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Breast Neoplasms / drug therapy
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Breast Neoplasms / pathology
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Fatty Acid Synthases / antagonists & inhibitors*
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Female
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Ginkgo biloba / chemistry*
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HL-60 Cells / drug effects
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Hexanes / chemistry
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Humans
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Inhibitory Concentration 50
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Lung Neoplasms / drug therapy
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Lung Neoplasms / pathology
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Molecular Structure
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Plant Extracts / chemistry
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Plant Leaves / chemistry
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Salicylates / chemistry
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Salicylates / isolation & purification
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Salicylates / pharmacology*
Substances
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Antineoplastic Agents, Phytogenic
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Enzyme Inhibitors
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Hexanes
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Plant Extracts
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Salicylates
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ginkgolic acid
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n-hexane
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Fatty Acid Synthases