CAJ | 학술논문

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、气动式眼压计观察兔眼压。　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，去酰基佛司可林稍弱，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3h。　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。
목적　종전산모후초예화식물중제취도3개불사가림유사물，즉이불사가림、거선기불사가림、1-을선기불사가림，체외측정타문격동선감산배화매활성，병관찰거선기불사가림급1-을선기불사가림대수부하토고안압적영향。　방법　체외측정격동선감산배화매활성용단백질결합방면법、기동식안압계관찰토안압。　결과　이불사가림체외격동선감산배화매활성여불사가림상당，거선기불사가림초약，1-을선기불사가림무활성。1%거선기불사가림급1-을선기불사가림적안액적토안，능억제수부하조성적토고안압，억제솔최고분별체6.0%급10.9%，작용지속지소3h。　결론　연구표명이불사가림급거선기불사가림구유체외격동선감산배화매활성적작용，이거선기불사가림급1-을선기불사가림구유억제수부하토고안압적작용。
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．