佛司可林类似物激动腺苷酸环化酶及抑制免高眼压探讨

目的：从滇产毛喉鞘蕊花植物中提取到3个佛司可林类似物，即异佛司可林、去酰基佛司可林、1－乙酰基佛司可林，体外测定它们激动腺苷酸环化酶活性，并观察去酰基佛司可林及1－乙酰基佛司可林对水负荷兔高眼压的影响。方法：体外测定激动腺苷酸环化酶活性用蛋白质结合放免法、气动式眼压计察兔眼压。结果：异佛司可林体外激动腺苷酸环化酶活性与佛司可林相当，去酰基佛司林林稍弱，1－乙酰基佛司可林无活性。1％去酰基佛司可林及1－乙酰基佛司可林滴眼液滴兔眼，能抑制水负荷造成的兔高眼压，抑制率最高分别达6.0％及10.9％，作用持续至少3h。结论：研究表明异佛司可林及去酰基佛司可林具有体外激动腺苷酸环化酶活性的作用，而去酰基佛司可林及1－乙酰基佛司可林具有抑制水负荷兔高眼压的作用。

Adenylate cyclasestimulation and ocular hypertension inhibition by forskolin analogs

Objective Forskolin (FSK ) analogs, isoforskolin (isoF ), deacetylforskolin (deaF ), and l-acetylforskolin (l 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. Methods Adenylate cyclase stimulation was determined by protein-binding method of radioimmunoassay, and intraocular pressure was monitored by pneumatonometer. Results it showed that isoforskolin and forskolin stimulated adenylate cyclase in vitro with almost equal activity, deacetylforskolin with milder activity., and l-acetylforskolin with little activity in vitro. 1 % deaF and 1-aF suppressed rabbit OHT induced by waterloading for at least 3 h,with the maximal inhibitory rates of 6. 0 1 10. 9% respectively. Conclusion This 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.