Brown L, Thomas R
Arzneimittelforschung. 1984;34(5):572-4.
The inotropic activity of eleven 5 alpha-cardenolides and six 5 beta-cardenolides was determined using guinea pig left atria and the results were compared with published data obtained from cat toxicity studies. The guinea pig atrial studies showed that the configuration of the A/B ring junction did not influence significantly the cardiotonic potency of digitoxigenin and its 5 alpha-epimer, uzarigenin, but was of significance with respect to the influence of substituent groups. Glucosidation decreased the potency of uzarigenin but increased that of digitoxigenin. By contrast, conjugation with rhamnose increased the activity of both uzarigenin and digitoxigenin. Cat toxicity data did not correlate well with that obtained using guinea pig atria, possibly because of the variable influence of pharmacokinetic factors applicable to the cat toxicity studies.
使用豚鼠左心房测定了11种5α-强心甾烯和6种5β-强心甾烯的变力活性，并将结果与从猫毒性研究中获得的已发表数据进行了比较。豚鼠心房研究表明，A/B环连接处的构型对洋地黄毒苷配基及其5α-差向异构体乌沙苷元的强心效力没有显著影响，但在取代基的影响方面具有重要意义。葡萄糖苷化降低了乌沙苷元的效力，但增加了洋地黄毒苷配基的效力。相比之下，与鼠李糖结合增加了乌沙苷元和洋地黄毒苷配基的活性。猫毒性数据与使用豚鼠心房获得的数据相关性不佳，可能是因为适用于猫毒性研究的药代动力学因素的可变影响。
