Callyaerins from the Marine Sponge Callyspongia aerizusa: Cyclic Peptides with Antitubercular Activity

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• 作者：Georgios Daletos ; Rainer Kalscheuer ; Hendrik Koliwer-Brandl ; Rudolf Hartmann ; Nicole J. de Voogd ; Victor Wray ; Wenhan Lin ; Peter Proksch
• 刊名：Journal of Natural Products
• 出版年：2015
• 出版时间：August 28, 2015
• 年：2015
• 卷：78
• 期：8
• 页码：1910-1925
• 全文大小：580K
• ISSN：1520-6025

文摘

Chemical investigation of the Indonesian sponge Callyspongia aerizusa afforded five new cyclic peptides, callyaerins I鈥揗 (1鈥?b>5), along with the known callyaerins A鈥揋 (6鈥?b>12). The structures of the new compounds were unambiguously elucidated on the basis of one- and two-dimensional NMR spectroscopy and mass spectrometry. In addition, the structures of callyaerins D (9), F (11), and G (12), previously available in only small amounts, have been reinvestigated and revised. All compounds were tested in vitro against Mycobacterium tuberculosis, as well as against THP-1 (human acute monocytic leukemia) and MRC-5 (human fetal lung fibroblast) cell lines, in order to assess their general cytotoxicity. Callyaerins A (6) and B (7) showed potent anti-TB activity with MIC₉₀ values of 2 and 5 渭M, respectively. Callyaerin C (8) was found to be less active, with an MIC₉₀ value of 40 渭M. Callyaerin A (6), which showed the strongest anti-TB activity, was not cytotoxic to THP-1 or MRC-5 cells (IC₅₀ > 10 渭M), which highlights the potential of these compounds as promising anti-TB agents.