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研究在离体条件下各种单体柴胡皂甙和甘草甜素抑制Na+,K+ATP酶活性的构效关系。实验结果表明,各种柴胡皂甙抑制Na+,K+ATP酶活性的作用强度依次为:b1>d>b2>b4>a>b3>e>c。柴胡皂甙化学结构中的C23OH,C16OH及C11和C13的共轭双烯可能对其抑制活性起重要作用。甘草甜素(GL),甘草次酸(GA)和生胃酮(18β甘草次酸半琥珀酸双钠盐,CX)抑制Na+,K+ATP酶活性的作用强度依次为GA≥CX>GL。研究还证明,柴胡皂甙d对Na+,K+ATP酶的抑制为非竟争性抑制
To study the structure-activity relationship of various saikosaponins and glycyrrhizin inhibiting Na +, K + -ATPase activity under ex vivo conditions. The experimental results showed that the inhibitory effects of various saikosaponins on the activities of Na + and K + -ATPase were as follows: b1> d> b2> b4> a> b3> e> c. The chemical structure of saikosaponin C23 OH, C16 OH and C11 and C13 conjugated dienes may play an important role in its inhibitory activity. The intensities of inhibition of Na + and K + -ATPase activity by glycyrrhizin (GL), glycyrrhetinic acid (GA) and carbenoxolone (18 β-glycyrrhetinic acid hemisuccinate bis-sodium salt, CX) were GA ≥ CX > GL. Studies also show that saikosaponin d Na +, K + ATP enzyme inhibition of non-competitive inhibition