Using a kinase screen to investigate the constituents of the sponge Stelletta clavosa obtained from diverse habitats.
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.
Department of Chemistry and Biochemistry and Institute of Marine Sciences, University of California, Santa Cruz, CA 95064, USA.
Christopher J
CJ
Wegerski
Dennis
D
France
Susan
S
Cornell-Kennon
Phillip
P
Crews
D000818:Animals; D004777:Environment; D004797:Enzyme-Linked Immunosorbent Assay / Q000379:methods; D011161:Porifera / Q000201:enzymology*; D011166:Porphyrins / Q000032:analysis; D019908:Proto-Oncogene Proteins c-raf / Q000032:analysis* / Q000378:metabolism; D012623:Seawater
D011166:Porphyrins; D019908:Proto-Oncogene Proteins c-raf