Antitumor Actinopyranones Produced by Streptomyces albus POR-04-15-053 Isolated from a Marine Sediment

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• 作者：Carmen Schleissner ; Marta Pe虂rez ; Alejandro Losada ; Pilar Rodri虂guez ; Cristina Crespo ; Paz Zu虂ñ ; iga ; Rogelio Ferna虂ndez ; Fernando Reyes ; Fernando de la Calle
• 刊名：Journal of Natural Products
• 出版年：2011
• 出版时间：July 22, 2011
• 年：2011
• 卷：74
• 期：7
• 页码：1590-1596
• 全文大小：816K
• 年卷期：v.74,no.7(July 22, 2011)
• ISSN：1520-6025

文摘

Four new antitumor pyranones, PM050511 (1), PM050463 (2), PM060054 (3), and PM060431 (4), were isolated from the cell extract of the marine-derived Streptomyces albus POR-04-15-053. Their structures were elucidated by a combination of spectroscopic methods, mainly 1D and 2D NMR and HRESIMS. They consist of an 伪-methoxy-纬-pyrone ring containing a highly substituted tetraene side chain glycosylated at C-10 in the case of 1 and 4. Compounds 1 and 4 displayed strong cytotoxicity against three human tumor cell lines with GI₅₀ values in the submicromolar range, whereas 2 showed subnanomolar activity as an inhibitor of EGFR-MAPK-AP1-mediated mitogenic signaling, causing inhibition of EGF-mediated AP1 trans-activation and EGF-mediated ERK activation and slight inhibition of EGF-mediated JNK activation. Taken together, these results suggest that members of the pyranone family of compounds could be developed as potential antitumor agents.