BRS1, A C30 BIS-AMINO, BIS-HYDROXY POLYUNSATURATED LIPID FROM AN AUSTRALIAN CALCAREOUS SPONGE THAT INHIBITS PROTEIN-KINASE-C

In the course of screening for activity at the phorbol ester binding s ite of protein kinase C, activity was identified within an unidentifie d calcareous sponge (class Calcarea) collected in the central region o f the Great Barrier Reef off the north-east coast of Australia. Using high-performance liquid chromatographic fractionation guided by activi ty at the enzyme, the C30 polyunsaturated lipid was isolated and its s tructure assigned on the basis of spectroscopic analysis. The compound was given the trivial name BRS1. It exhibited a 50% effective concent ration for inhibiting phorbol ester binding of 9 mu M and for inhibiti ng enzymic activity of 98 mu M. This compound represents a novel prote in kinase C inhibitor. (C) 1997 Elsevier Science Ltd.