Adenylate cyclase stimulation and ocular hypertension inhibition by forskolin analogs / 中华实验眼科杂志

ABSTRACT

ObjectiveForskolin （FSK） analogs，isoforskolin （isoF），deacetylforskolin（deaF），and 1-acetylforskolin（1-aF），extracted from Coleus forskohlii native to Yunnan，were assayed for their adenylate cyclase stimulating activities in vitro and for effects of two analogs on ocular hypertension （OHT） in water-loaded rabbits．MethodsAdenylate cyclase stimulation was determined by protein-binding method of radioimmunoassay，and intraocular pressure was monitored by pneumatonometer．ResultsIt showed that isoforskolin and forskolin stimulated adenylate cyclase in vitro with almost equal activity，deacetylforskolin with milder activity，and 1-acetylforskolin with little activity in vitro．1％ deaF and 1-aF suppressed rabbit OHT induced by water-loading for at least 3h，with the maximal inhibitory rates of 6.0，10.9% respectively．ConclusionThis study suggests that two foskolin analogs （isoforskolin，deacetylforskolin） possess adenylate cyclase stimulation activities in vitro；deacetylforskolin and 1-acetylforskolin suppress OHT induced by water-loading in rabbits．