Nose M, Amagaya S, Ogihara Y
Chem Pharm Bull (Tokyo). 1989 Dec;37(12):3306-10. doi: 10.1248/cpb.37.3306.
The hemolytic properties and the adsorbability on red blood cells of saikosaponin a, saikosaponin d and 13 metabolites formed in the alimentary tract were investigated. Among these compounds, saikosaponin d and its intestinal product, prosaikogenin G, which possess an alpha-hydroxyl function at C16, showed the strongest hemolytic activity at the dose range of 1.0 to 5.0 micrograms/ml. Saikosaponin a and its intestinal product, prosaikogenin F, which possess a beta-hydroxyl function at C16, showed activity above 10 micrograms/ml. In this case, the monoglycoside, prosaikogenin F, showed the stronger activity than the diglycoside, saikosaponin a. Among the gastric products whose ether ring was cleaved to produce a carbinol, the monoglycosides, prosaikogenin A and prosaikogenin H, showed a slight activity above 25 micrograms/ml, and the saikogenins except saikogenin A were inactive. Saikogenin A, however, had hemolytic activity at a dose of 15 micrograms/ml. The adsorbabilities of these compounds on red blood cell membranes closely paralleled their degrees of hemolytic activity.
研究了柴胡皂苷a、柴胡皂苷d以及在消化道中形成的13种代谢产物的溶血特性和对红细胞的吸附性。在这些化合物中，柴胡皂苷d及其肠道产物原柴胡皂苷G在C16位具有α-羟基官能团，在1.0至5.0微克/毫升的剂量范围内表现出最强的溶血活性。柴胡皂苷a及其肠道产物原柴胡皂苷F在C16位具有β-羟基官能团，在高于10微克/毫升时表现出活性。在这种情况下，单糖苷原柴胡皂苷F比双糖苷柴胡皂苷a表现出更强的活性。在醚环断裂生成甲醇的胃产物中，单糖苷原柴胡皂苷A和原柴胡皂苷H在高于25微克/毫升时表现出轻微活性，除柴胡皂苷元A外的其他柴胡皂苷元无活性。然而，柴胡皂苷元A在15微克/毫升的剂量下具有溶血活性。这些化合物对红细胞膜的吸附性与其溶血活性程度密切相关。
