[The structure activity relationship of saikosaponins and glycyrrhizin derivatives for Na+, K(+)-ATPase inhibiting action].
The study on structure-activity relationship of saikosaponins and glycyrrhizin derivatives for Na+, K(+)-ATPase inhibiting action has been made in vitro. The results showed that the order of potency of inhibitory effect of saikosaponins on Na+, K(+)-ATPase is as follows: b1 > d > b2 > b4 > a > b3 > e > c. The chemical structure C23-OH, C16-OH and the C11, C13 conjugated double diene of saikosaponins are important for its inhibitory activity. The inhibitory potency of glycyrrhizin (GL), glycyrrhetinic acid (GA) and carbenoxolone (CX) for Na+, K(+)-ATPase activity is as follows: GA > or = CX > GL. In addition, the inhibitory effect of saikosaponin d on Na+, K(+)-ATPase was found to be non-competitive.
Institute of Preclinical Sciences, Norman Bethune University of Medical Sciences, Changchun.
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Zhou
Z Q
ZQ
Zhang
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Nagasawa
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Hiai
D002474:Cell-Free System; D019695:Glycyrrhizic Acid / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D009828:Oleanolic Acid / Q000031:analogs & derivatives*; D012502:Sapogenins / Q000737:chemistry / Q000494:pharmacology*; D012503:Saponins; D000254:Sodium-Potassium-Exchanging ATPase / Q000378:metabolism*; D013329:Structure-Activity Relationship
D012502:Sapogenins; D012503:Saponins; D019695:Glycyrrhizic Acid; D009828:Oleanolic Acid; D000254:Sodium-Potassium-Exchanging ATPase; C025759:saikosaponin D