Greensporones: Resorcylic Acid Lactones from an Aquatic Halenospora sp.

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• 作者：Tamam El-Elimat ; Huzefa A. Raja ; Cynthia S. Day ; Wei-Lun Chen ; Steven M. Swanson ; Nicholas H. Oberlies
• 刊名：Journal of Natural Products
• 出版年：2014
• 出版时间：September 26, 2014
• 年：2014
• 卷：77
• 期：9
• 页码：2088-2098
• 全文大小：446K
• ISSN：1520-6025

文摘

Fourteen new resorcylic acid lactones (1鈥?b>14) were isolated from an organic extract of a culture of a freshwater aquatic fungus Halenospora sp. originating from a stream in North Carolina. The structures were elucidated using a set of spectroscopic and spectrometric techniques. The absolute configuration of one representative member of the compounds (7) was assigned using X-ray crystallography of an analogue that incorporated a heavy atom, whereas for compounds 8鈥?b>11, a modified Mosher鈥檚 ester method was utilized. The relative configurations of compounds 12鈥?b>14 were determined on the basis of NOE data. Compounds 12鈥?b>14 were proposed as artifacts produced by intramolecular cycloetherification of the 蔚-hydroxy-伪,尾-unsaturated ketone moieties of the parent compounds during the purification processes. The isolated compounds, except for 8 and 12, were tested against the MDA-MB-435 (melanoma) and HT-29 (colon) cancer cell lines. Compound 5 was the most potent, with IC<sub>50sub> values of 2.9 and 7.5 渭M, respectively. The compounds were evaluated as TAK1鈥揟AB1 inhibitors but were found to be inactive.