柳珊瑚酸构效关系研究

 目的：初步研究柳珊瑚酸(Sub)的羧基与其生理活性的关系。方法：Sub酰化合成N-丁基柳珊瑚酰胺(NBS)，N-环己基柳珊瑚酰胺(NCS)和N-柳珊瑚酰N-N-二环己基脲(SDU)；制备人红细胞膜和小鼠脑提取物作为乙酰胆碱酯酶(AChE)的组织样品，比色法测定AChE活力。结果：3种衍生物的收率分别为90%，92%和90%。上述4种化合物抑制人红细胞膜AChE的pI₅₀(抑制酶活力50%的药物摩尔浓度的负对数)分别为4.92，2.79，2.78和4.87，抑制小鼠脑AChE的pI₅₀分别为4.22，2.18，2.17和4.19；对小鼠的LD₅₀分别为23.6，96.0，84.0，35.8mg·kg^-1。结论：Sub的羧基与其生理活性和毒性是密切相关的。

Relationship between the structure and effect of suberogorgin

OBJECTIVE:To initially investigate the relationship between the carboxyl and physiological effect of suberogorgin(Sub).METHODS:N-butyl suberogorgamide(NBS),N-cyclohexyl suberogorgamide(N-CS),and N-suberogorgamide N-N-dicyclohexyl urea(SDU) were synthetized.Human RBC membrane and mice brain extract were prepared as tissue samples of acetylcholinesterase(AChE).The activity of AChE was determined with colorimetry.RESULTS:Four compounds dose dependently inhibited AChE,with pI₅₀(negative logarithm of molar concentration causing 50% inhibition of AChE)4.92,2.79,2.78,and 4.87 in human RBC,and 4.22,2.18,2.17,and 4.19 in mice brain,respectively.Their LD₅₀ in mice iv were separately 23.6,96.0,84.0,and 35.8 mg·kg^-1 .CONCLUSION:The carboxyl of Sub was closely related to its activity and toxicity.