Spheciosterol sulfates, PKCzeta inhibitors from a philippine sponge Spheciospongia sp

J Nat Prod. 2008 Jul;71(7):1213-7. doi: 10.1021/np8001628. Epub 2008 Jun 18.

Abstract

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.

Publication types

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

MeSH terms

  • Animals
  • Cartilage / drug effects
  • Cartilage / metabolism
  • Dose-Response Relationship, Drug
  • Humans
  • Isoenzymes
  • NF-kappa B / drug effects*
  • Philippines
  • Porifera / chemistry*
  • Protein Kinase C / antagonists & inhibitors*
  • Sterols / chemistry
  • Sterols / isolation & purification*
  • Sterols / pharmacology*
  • Sulfuric Acid Esters / chemistry
  • Sulfuric Acid Esters / isolation & purification*
  • Sulfuric Acid Esters / pharmacology*

Substances

  • Isoenzymes
  • NF-kappa B
  • Sterols
  • Sulfuric Acid Esters
  • spheciosterol sulfate A
  • spheciosterol sulfate B
  • spheciosterol sulfate C
  • Protein Kinase C