Inhibition of neutral lipid synthesis by avarols from a marine sponge |
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| Institution: | 1. Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo 108-8641, Japan;2. Medicinal Research Laboratories, School of Pharmacy, Kitasato University, Tokyo, Japan;3. Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai 981-8558, Japan;1. State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, PR China;2. Institute of Pharmaceutical Biology and Biotechnology, Heinrich-Heine University, 40225 Duesseldorf, Germany;1. Department of Bioinformatics, Applied Botany Centre (ABC), University School of Sciences, Gujarat University, Ahmedabad, 380009, India;2. Department of Botany, University School of Sciences, Gujarat University, Ahmedabad, 380009, India;1. Innovation Center of Faculty of Chemistry, University of Belgrade, Studentski trg 12-16, 11000 Belgrade, Serbia;2. Institute for Biological Research “Sini?a Stankovi?”, University of Belgrade, Despota Stefana 142, 11060 Belgrade, Serbia;3. Institute of Chemistry, Technology and Metallurgy, University of Belgrade, Center for Chemistry, Njego?eva 12, 11000 Belgrade, Serbia;4. Faculty of Chemistry, University of Belgrade, Studentski trg 12-16, 11000 Belgrade, Serbia;1. Department of Toxicology, College of Pharmacy, Chungnam National University, Daejeon, Republic of Korea;2. Department of Chemistry, University of Iowa, Iowa City, USA;3. Department of Food and Medicine, International University of Korea, Jinju, Republic of Korea;4. Department of Food Science and Culinary, International University of Korea, Jinju, Republic of Korea;5. College of Pharmacy, Yeungnam University, Gyeongsan, Republic of Korea |
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| Abstract: | The effects of 14 sesquiterpene hydroquinones, including 8 marine sponge-derived avarols (1–8) and 6 semisynthetic derivatives (9–14), on lipid droplet accumulation and neutral lipid synthesis in Chinese hamster ovary (CHO) K1 cells were investigated. In intact CHO-K1 cell assays, avarol (1) markedly decreased the number and size of lipid droplets in CHO-K1 cells and exhibited the most potent inhibitory activity on the synthesis of cholesteryl ester (CE) and triglyceride (TG) with IC50 values of 5.74 and 6.80 µM, respectively. In enzyme assays, sterol O-acyltransferase (SOAT), the final enzyme involved in CE biosynthesis, and diacylglycerol acyltransferase (DGAT), the final enzyme involved in TG biosynthesis, were inhibited by 1 with IC50 values of 7.31 and 20.0 µM, respectively, which correlated well with those obtained in the intact cell assay. These results strongly suggest that 1 inhibited SOAT and DGAT activities in CHO-K1 cells, leading to a reduction in the accumulation of CE and TG in lipid droplets. |
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| Keywords: | Sesquiterpene hydroquinone Neutral lipid synthesis Inhibitor |
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