滇产毛喉鞘蕊花提取成分的药理作用

Pharmacological Effects of Several Chemical Constituents from Coleus Forskohlii Native to Yunnan

本文进一步证实滇产毛喉鞘蕊花提取成分,isorforskolin,1-acetylforskolin 及乙酸乙酯提取物,在豚鼠整体和离体模型上均显示强大的平喘解痉效应;局部给药效价最佳;乙酸乙酯提取物口服药效不及注射给药。提取物眼膏使清醒免正常眼压发生轻度下降,但统计学差别显著,有短暂局部刺激现象。1-acetylforskolin 体外抑制 ADP 诱导的兔血小板聚集,但其体内给药的抑制作用尚未确定。

Recently,Coleus forskohlii has been found in Yunnan;isoforskolin and 1-acetylforskolin have been isolated from the ethyl acetate extract of the plant.The effects of these constituents on airway smooth muscle,intraocular pressure and platelet aggregation were studied. 1 On isolated guinea pig parenchymal strips,IC_(50)of both isoforskolin and ethyl acetate extract antagonizing histamine(1μg/ml)were 1.0±0.13(vehicle:60% PEG-400,n=9)or 0.9±0.10(DMSO,n=9),and 10.2±1.03(60%PEG-400,n=12)or5.5±1.39(DMSO,n=7) μg/ml,respectively. 2 with in vivo ethly acetate extract either 50 mg/kg ip or 100 mg/kg ig to guinea pig prior to exposure to nebulized 0.4% histamine,the bronchospasm(convulsion)was effectively prevented(P<0.01,0.05). 3 In awaked rabbits topical administration of the extract oculentum caused mild,persist- ent and statistically significant decreases in IOP(P<0.001,0.05). 4 On rabbit platelet aggregation induced by ADP in vitro,IC_(50)of 1-acetylforskolin was 21.7±6.7 umol/L. These experimental results show that the pharmacological effects of isoforskolin, 1-acetylforskolin and ethyl acetate extract from the plant native to Yunnan are similar to those of forskolin.