KMID : 0043320120350030481
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Archives of Pharmacal Research 2012 Volume.35 No. 3 p.481 ~ p.486
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Bioassay-guided isolation of fatty acid synthase inhibitory diterpenoids from the roots of Salvia miltiorrhiza Bunge
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Jang Tae-Su
Zhang HaiYan Kim Geum-Jin Kim Dong-Woo Min Byung-Sun Kang Won-Ku Son Kun-Ho Na Min-Kyun Lee Seung-Ho
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Abstract
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Fatty acid synthase (FAS) is considered as a novel drug target for the development of anticancer and anti-obesity agents. Bioassay-guided fractionation of a n-hexane-soluble extract prepared from the roots of Salvia miltiorrhiza Bunge (Labiatae), using an in vitro enzyme assay, led to the isolation of five abietane diterpenoids: 15,16-dihydrotanshinone I (1), cryptotanshinone (2), tanshinone I (3), tanshinone IIA (4), and dansenspiroketallactone (5). Compounds 1?5 were tested for their in vitro FAS inhibitory activity and, except for compound 5 (IC50 > 100 ¥ìM), compounds 1?4 inhibited the enzyme activity with IC50 values ranging from 12.0 to 30.3 ¥ìM. Our findings may be partially related to the anticancer activity of abietane diterpenoids from the plant, suggesting a further study on the anticancer potential of tanshinone derivatives.
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KEYWORD
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Salvia miltiorrhiza Bunge, Fatty acid synthase, Bioassay-guided isolation, Abietane diterpenoids
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