期刊
JOURNAL OF NATURAL PRODUCTS
卷 72, 期 11, 页码 2028-2031出版社
AMER CHEMICAL SOC
DOI: 10.1021/np900517h
关键词
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资金
- National Cancer Institute, NIH, Bethesda, Maryland [U19-CA52956, P01-CA125066]
- Korea Research Foundation [KRF-2007-357-E00035]
- Korean Government (MOEHRD), Seoul, South Korea
- National Research Foundation of Korea [2007-357-E00035] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Bioassay-guided fractionation of a chloroform-soluble extract of Garcinia mangostana stem bark, using the HT-29 human colon cancer cell line and an enzyme-based ELISA NF-kappa B assay, led to the isolation of a new xanthone, 11-hydroxy-3-O-methyl-1-isomangostin (1). The structure of 1 was elucidated by spectroscopic data analysis. In addition, 10 other known compounds, 11-hydroxy-1-isomangostin (2), 11 alpha-mangostanin (3), 3-isomangostin (4), alpha-mangostin (5), beta-mangostin (6), garcinone D (7), 9-hydroxycalabaxanthone (8), 8-deoxygartanin (9), gartanin (10), and cratoxyxanthone (11), were isolated. Compounds 4-8 exhibited cytotoxicity against the HT-29 cell line with ED50 values of 4.9, 1.7, 1.7, 2.3, and 9.1 mu M, respectively. In an ELISA NF-kappa B assay, compounds 5-7, 9, and 10 inhibited p65 activation with IC50 values of 15.9, 12.1, 3.2 11.3, and 19.0 mu M, respectively, and 6 showed p50 inhibitory activity with an IC50 value of 7.5 mu M. alpha-Mangostin (5) was further tested in an in vivo hollow fiber assay, using HT-29, LNCaP, and MCF-7 cells, but it was found to be inactive at the highest dose tested (20 mg/kg).
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