Bioassay-guided l Isolation of Fatty Acid Synthase Inhibitory Diterpenoids from the Roots of Salvia miltiorrhiza Bunge

초록

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 mu M), compounds 1-4 inhibited the enzyme activity with IC50 values ranging from 12.0 to 30.3 mu M. 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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