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Inhibition of tumor cells interacting with stromal cells by xanthones isolated from a Costa Rican Penicillium sp.

ABSTRACT: CR1642D, an endophytic isolate of Penicillium sp. collected from a Costa Rican rainforest, was identified through a high-throughput approach to identify natural products with enhanced antitumor activity in the context of tumor-stromal interactions. Bioassay-guided separation led to the identification of five xanthones (1-5) from CR1642D. The structures of the xanthone dimer penexanthone A (1) and monomer penexanthone B (2) were elucidated on the basis of spectroscopic analyses, including 2D NMR experiments. All of the compounds were tested against a panel of tumor cell lines in the presence and absence of bone marrow stromal cells. Compound 3 was the most active, with IC(50) values of 1-17 ?M, and its activity was enhanced 2-fold against tumor cell line RPMI8226 in the presence of stromal cells (IC(50) 1.2 ?M, but 2.4 ?M without stromal cells).

SUBMITTER: Cao S

PROVIDER: S-EPMC3338863 | biostudies-literature | 2012 Apr

REPOSITORIES: biostudies-literature

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Inhibition of tumor cells interacting with stromal cells by xanthones isolated from a Costa Rican Penicillium sp.

Cao Shugeng S McMillin Douglas W DW Tamayo Giselle G Delmore Jake J Mitsiades Constantine S CS Clardy Jon J

Journal of natural products 20120329 4

CR1642D, an endophytic isolate of Penicillium sp. collected from a Costa Rican rainforest, was identified through a high-throughput approach to identify natural products with enhanced antitumor activity in the context of tumor-stromal interactions. Bioassay-guided separation led to the identification of five xanthones (1-5) from CR1642D. The structures of the xanthone dimer penexanthone A (1) and monomer penexanthone B (2) were elucidated on the basis of spectroscopic analyses, including 2D NMR ...[more]

PMID: 22458669

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