摘要
目的 探讨人参皂苷RdC12 手性碳构型改变与其药理活性的关系。方法 制备RdC12 位差向异构体 (12 epi Rd) ;观察比较 12 epi Rd与Rd对苯肾上腺素 (phenyle phrine ,Phe)收缩大鼠离体主动脉环作用的影响。结果 首次成功制备了 12 epi Rd ;Rd(40、80 μmol·L-1)与 12 epi Rd(40、80 μmol·L-1)均可浓度依赖性抑制Phe收缩血管环的最大效应 ,其拮抗指数 pD2 ′分别为 :4 0 8± 0 15和 4 0 7±0 16 ,二者差异无显著性 (P >0 0 5 )。结论 人参皂苷RdC12
AIM To investigate the relationship between the construction of chiral C 12 of ginsenoside(GS) and its pharmacological effects METHODS 12 epi Rd was synthesized; The effects of Rd and 12 epi Rd on phenylephrine (phe) induced contraction of rat aortic rings were investigated and compared RESULTS 12 epi Rd was synthesized successfully; Rd(40 μmol·L -1 and 80 μmol·L -1 ) and 12 epi Rd(40 μmol·L -1 and 80 μmol·L -1 ) produced a concentration dependent inhibitory effect on Phe induced contractile response in a non competitive manner The values of PD 2′ for Rd and 12 epi Rd were (4 08±0 15) and (4 07±0 16)( P> 0 05), respectively CONCLUSION The changing of the construction of chiral C 12 of Rd doesn't change its effects on phe induced contractile response of rat aortic rings
出处
《中国药理学通报》
CAS
CSCD
北大核心
2003年第3期282-286,共5页
Chinese Pharmacological Bulletin
基金
国家自然科学基金资助课题 No 3 9970 849
广东省自然科学基金
