Discovery of new A- and B-type laxaphycins with synergistic anticancer activity |
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Authors: | Weijing Cai Susan Matthew Qi-Yin Chen Valerie J. Paul Hendrik Luesch |
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Affiliation: | 1. Department of Medicinal Chemistry, University of Florida, 1345 Center Drive, Gainesville, FL 32610, United States;2. Center for Natural Products, Drug Discovery and Development (CNPD3), University of Florida, 1345 Center Drive, Gainesville, FL 32610, United States;3. Smithsonian Marine Station, Fort Pierce, FL 34949, United States |
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Abstract: | Two new cyclic lipopeptides termed laxaphycins B4 (1) and A2 (2) were discovered from a collection of the marine cyanobacterium Hormothamnion enteromorphoides, along with the known compound laxaphycin A. The planar structures were solved based on a combined interpretation of 1D and 2D NMR data and mass spectral data. The absolute configurations of the subunits were determined by chiral LC-MS analysis of the hydrolysates, advanced Marfey’s analysis and 1D and 2D ROESY experiments. Consistent with similar findings on other laxaphycin A- and B-type peptides, laxaphycin B4 (1) showed antiproliferative effects against human colon cancer HCT116 cells with IC50 of 1.7?µM, while laxaphycins A and A2 (2) exhibited weak activities. The two major compounds isolated from the sample, laxaphycins A and B4, were shown to act synergistically to inhibit the growth of HCT116 colorectal cancer cells. |
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Keywords: | Marine natural products Cyanobacteria Laxaphycin Anticancer activity Synergy |
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