期刊
JOURNAL OF NATURAL PRODUCTS
卷 71, 期 6, 页码 1082-1084出版社
AMER CHEMICAL SOC
DOI: 10.1021/np800098f
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资金
- NCI NIH HHS [P01 CA048112-08A1, P01 CA48112, P01 CA048112-11, P01 CA048112-10, P01 CA048112-09, P01 CA048112-12, P01 CA048112-12S1, P01 CA048112-13A1, P01 CA048112] Funding Source: Medline
Aromatase is a well-established target for the chemoprevention of breast cancer. The dihydroisocoumarin (3R,4R)-(-)-6-methoxy-1-oxo-3-pentyl-3,4-dihydro-1H-isochromen-4-yl acetate (1) (IC50 = 1.6 +/- 0.1 mu M), isolated from aerial parts of Xyris ptetygoblephara, showed aromatase inhibitory activity. The specificity of 1 was evaluated by inhibition assays with cytochrome P450 enzymes. CYP1A1 was inhibited modestly (IC50 = 3 8.0 +/- 2.0 mu M), while CYP2C8 and CYP3A4 enzymes were not affected. Dihydroisocoumarin 1 showed weak antiproliferative activity against MCF-7 (IC50 = 66.9 +/- 2.3 mu M) and LNCaP (IC50 = 57.5 +/- 2.0 mu M) cells and was inactive against LU-1 and HepG2 cells in culture. These results demonstrate the potential of dihydroisocoumarin 1 to serve as a selective aromatase inhibitor.
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