Natural fatty acid synthase inhibitors as potent therapeutic agents for cancers: A review.

Context Fatty acid synthase (FAS) is the only mammalian enzyme to catalyse the synthesis of fatty acid. The expression level of FAS is related to cancer progression, aggressiveness and metastasis. In recent years, research on natural FAS inhibitors with significant bioactivities and low side effects has increasingly become a new trend. Herein, we present recent research progress on natural fatty acid synthase inhibitors as potent therapeutic agents. Objective This paper is a mini overview of the typical natural FAS inhibitors and their possible mechanism of action in the past 10 years (2004-2014). Method The information was collected and compiled through major databases including Web of Science, PubMed, and CNKI. Results Many natural products induce cancer cells apoptosis by inhibiting FAS expression, with fewer side effects than synthetic inhibitors. Conclusion Natural FAS inhibitors are widely distributed in plants (especially in herbs and foods). Some natural products (mainly phenolics) possessing potent biological activities and stable structures are available as lead compounds to synthesise promising FAS inhibitors.

The Structures and Bioactivities of Fatty Acid Synthase Inhibitors.

BACKGROUND: Fatty Acid Synthase (FAS or FASN) is a vital enzyme which catalyzes the de novo synthesis of long chain fatty acids. A number of studies have recently been reported that FAS was combined targets for the discovery of anti-obesity and anti-cancer drugs. Great interest has been developed in finding novel FAS inhibitors, and result in more than 200 inhibitors being reported. METHODS: The reported research literature about the FAS inhibitors was collected and analyzedsised through major databases including Web of Science, and PubMed. Then the chemical stractures, FAS inhibitory activities, and Structure-Activity Relationships (SAR) were summarized focused on all these reported FAS inhibitors. RESULTS: The 248 FAS inhibitors, which were reported during the past 20 years, could be divided into thiolactone, butyrolactone and butyrolactam, polyphenols, alkaloids, terpenoids, and other structures, in view of their structure characteristics. And the SAR of high inhibitory structures of each type was proposed in this paper. CONCLUSION: A series of synthetic quinolinone derivatives show strongest inhibitory activity in the reported FAS inhibitors. Natural polyphenols, existing in food and herbs, show more adaptive in medicine exploration because of their safety and efficiency. Moreover, screening the FAS inhibitors from microorganism and marine natural products could be the hot research directions in the future.

Essential oil composition and antibacterial activity of Lindera nacusua (D. Don) Merr.

This study represents the first report on the chemical composition and biological activity of the essential oils from the leaves of Lindera nacusua (D. Don) Merr. Twenty-two compounds were identified and quantified, and the major components of the oil were Caryophyllene oxide (8.79%), Hexahydrofarnesyl acetone (6.83%), ß-Selinene (5.02%), Neophytadiene (4.53%), Palmitic acid (4.42%), Phytol (4.36%), α-Copaene (3.89%), 4a,5,8,8a-ß-Tetrahydro-2,4,5-trimethyl-1,4-naphthalindione (3.83%), α-Cadinol (3.17%), Bulnesol (2.65%) and 1,4-Dimethyl-7-(1-methylethyl) azulene (2.38%). The in vitro antibacterial activities of the essential oils were evaluated by the disc diffusion method. The inhibition zones against Staphylococcus aureus and Candida albicans were 23.7 and 23 mm. So the essential oil of L. nacusua showed potent antibacterial activity and potential high selectivity against S. aureus and C. albicans.