2. Academic Validation
  3. Cytotoxic xanthone constituents of the stem bark of Garcinia mangostana (mangosteen)

Cytotoxic xanthone constituents of the stem bark of Garcinia mangostana (mangosteen)

  • J Nat Prod. 2009 Nov;72(11):2028-31. doi: 10.1021/np900517h.
Ah-Reum Han 1,  Jeong-Ah Kim,  Daniel D Lantvit,  Leonardus B S Kardono,  Soedarsono Riswan,  Heebyung Chai,  Esperanza J Carcache de Blanco,  Norman R Farnsworth,  Steven M Swanson,  A Douglas Kinghorn
Affiliations

Affiliation

  • 1 College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA.
PMID: 19839614 DOI: 10.1021/np900517h
Abstract

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-kappaB 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), 11alpha-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 microM, respectively. In an ELISA NF-kappaB 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 microM, respectively, and 6 showed p50 inhibitory activity with an IC50 value of 7.5 microM. 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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