Using a kinase screen to investigate the constituents of the sponge Stelletta clavosa obtained from diverse habitats

Bioorg Med Chem. 2004 Nov 1;12(21):5631-7. doi: 10.1016/j.bmc.2004.07.061.

Abstract

Fourteen collections of the marine sponge Stelletta clavosa have been obtained from diverse Indo-Pacific locations in order to conduct a comparison of their major constituents. The dichloromethane extract of one collection (no. 00369) exhibited activity in a c-Raf-1 kinase assay. Bioactivity-directed isolation resulted in the known porphyrin analogs pyropheophorbide a (2) and purpurin 18 methyl ester (3). Further spectroscopic screening of the various sponge extracts resulted in the isolation of four swinholide polyketides, a carotenoid, and three diketopiperazines. Pyropheophorbide a (2) exhibited the best IC(50) among the porphyrin type compounds (IC(50)<0.31microg/mL). This prompted further screening of 2 against a panel of 85 kinases.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Environment
  • Enzyme-Linked Immunosorbent Assay / methods
  • Porifera / enzymology*
  • Porphyrins / analysis
  • Proto-Oncogene Proteins c-raf / analysis*
  • Proto-Oncogene Proteins c-raf / metabolism
  • Seawater*

Substances

  • Porphyrins
  • Proto-Oncogene Proteins c-raf