Pulicatins A-E, Neuroactive Thiazoline Metabolites from Cone Snail-Associated Bacteria

作者:Lin Zhenjian; Antemano Rowena R; Hughen Ronald W; Tianero Ma Diarey B; Peraud Olivier; Haygood Margo G; Concepcion Gisela P; Olivera Baldomero M; Light Alan; Schmidt Eric W*
来源:Journal of Natural Products, 2010, 73(11): 1922-1926.
DOI:10.1021/np100588c

摘要

The cone snail Conus pulicarius from the Philippines provides a specific habitat for actinomycetes and other bacteria. A phenotypic screen using primary cultures of mouse dorsal root ganglion neurons revealed that one C. pulicarius associate, Streptomyces sp. CP32, produces a series of natural products that enhance or diminish whole-cell Ca(2+) flux. These compounds include known thiazoline compounds and a series of new derivatives, pulicatins A-E (6-10). Individual compounds were shown to hind to a series of human receptors, with selective binding to the human serotonin 5-HT(2B) receptor. Here, we report the structure elucidation of the new compounds and results of the neurological assays.

  • 出版日期2010-11