Open AccessSpheciosterol Sulfates, PKCζ Inhibitors from a Philippine Sponge Spheciospongia sp.
Author(s) -
Emily L. Whitson,
Tim S. Bugni,
Priya Chockalingam,
Gisela P. Concepción,
Mary Kay Harper,
Min He,
John N. A. Hooper,
Gina C. Mangalindan,
Frank V. Ritacco,
Chris M. Ireland
Publication year - 2008
Publication title -
journal of natural products
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.976
H-Index - 139
eISSN - 1520-6025
pISSN - 0163-3864
DOI - 10.1021/np8001628
Subject(s) - sponge , sulfate , stereochemistry , ec50 , sterol , protein kinase c , chemistry , pharmacognosy , biology , biochemistry , in vitro , biological activity , enzyme , botany , organic chemistry , cholesterol
Three new sterol sulfates, spheciosterol sulfates A-C (1-3), and the known sterol sulfate topsentiasterol sulfate E (4) have been isolated from the sponge Spheciospongia sp., collected in the Philippines. Structures were assigned on the basis of extensive 1D and 2D NMR studies as well as analysis by HRESIMS. Compounds 1-4 inhibited PKCzeta with IC50 values of 1.59, 0.53, 0.11, and 1.21 microM, respectively. In a cell-based assay, 1-4 also inhibited NF-kappaB activation with EC50 values of 12-64 microM.