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基于目标成分“敲入”的四制香附质量控制研究

Research on the quality control of four times processing Rhizoma Cyperi based on target component‘Knock-in Strategy’
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摘要 目的:通过目标成分“敲入”,建立以关键药效组分为标示量的质量控制限度。方法:采用硅胶柱色谱技术结合高效液相色谱法对四制香附石油醚部位中具有活性的成分α-香附酮、香附烯酮及sugeonol进行敲出,获得阴性样品,将不同梯度α-香附酮(A)、香附烯酮(B)和sugeonol(C)分别依次按照敲入A、B、C、AB、AC、BC、ABC的方法不断敲入到其相对应阴性部位样品A^-、B^-、C^-、AB^-、AC^-、BC^-、ABC-中,探索香附药效成分对小鼠离体子宫平滑肌收缩的影响,建立量-效关系。结果:当α-香附酮敲入的量达到0.75倍量时,对离体子宫肌的抑制作用与石油醚部位等效,即α-香附酮在香附石油醚部位中的含量达到2.48%时;当香附烯酮敲入的量达到0.68倍时,即石油醚部位中香附烯酮的含量达到1.97%时,就可以与石油醚整体拥有相同的效果;当sugeonol敲入的量达到0.25倍,即石油醚部位中香附烯酮的含量达到0.028%时,对离体子宫肌的抑制作用与石油醚部位等效;将目标成分α-香附酮、香附烯酮及sugeonol进行组合敲入时,则含量要达目标成分1.00倍敲入时,才能达到与香附石油醚部位相同的作用效果,说明香附中的这3种化学成分之间可能存在着相互作用的关系。结论:建立了四制香附中各目标成分逐步敲入到其阴性品中的量与离体子宫肌收缩平均抑制率的“量-效”关系曲线,结果表明四制香附石油醚部位中α-香附酮的含量应该不低于2.48%,香附烯酮不低于1.97%,sugeonol不低于0.028%。 Objective:To establish the quality control of the key pharmacodynamics group by the target component‘Knock-in Strategy’.Methods:Silica gel column chromatography and HPLC were used to knock-outα-carbutenone(A),cyperotundone(B)and sugeonol(C)from petroleum ether extract,obtained negative sample.Type different gradients A,B,C,AB,AC,BC,ABC Knock-in negative samples A^-,B^-,C^-,AB^-,AC^-,BC^-,ABC-.To explore the effect of the pharmacodynamics on the contractile of isolated uterine smooth muscle in mice and establish the quantity-effect relationship.Results:While the amount ofα-acanthone knocked-in reaches 0.75 times,that is the content ofα-acanthone in the oil ether site reaches 2.48%,the inhibition of isolated uterine muscles is equivalent to that of petroleum ether.While the amount of aromaenone knocked in reaches 0.68 times,that is the content of aromaenone in the oil ether site reaches 1.97%,it can have the same effect as the oil ether as a whole.While sugeonol knocked in 0.25 times,that is,the content of carbenone in the petroleum ether site reached 0.028%,the inhibition of the isolated uterine muscle was equivalent to that of the petroleum ether site.While the target componentsα-acidone,acidone and sugeonol are combined,the content must reach 1.00 time the target component to achieve the same effect as the acidine ether site.This shows that there may be interaction between the three chemical components.Conclusion:This experiment establishes the‘volume-effect’relationship between the amount of each target component of the four perfumed middle school and the average inhibition rate of isolated uterine muscle contraction.The experimental results show that the content ofα-coupletone should not be less than 2.48%,the content of coupletenone should not be less than 1.97%,and the content of sugeonol should not be less than 0.028%.
作者 胡律江 赵晓娟 郭慧玲 胡志方 高文军 HU Lv-jiang;ZHAO Xiao-juan;GUO Hui-ling;HU Zhi-fang;GAO Wen-jun(Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,China;Jiangxi College of Traditional Chinese Medicine,Fuzhou 344000,China)
出处 《中华中医药杂志》 CAS CSCD 北大核心 2020年第4期1969-1973,共5页 China Journal of Traditional Chinese Medicine and Pharmacy
基金 江西省科技厅自然科学基金(No.20151BAB205073) 江西省科技厅重点研发计划(No.20161BBG70072) 江西省高校落地计划产学研项目(No.KJLD14057) 江西省教育厅科技项目(No.170721) 江西省卫计委中医药科研项目(No.2016Z01)。
关键词 四制香附 抗痛经 “敲入”模式 质量控制 Four times processing Rhizoma Cyperi Anti-dysmenorrhea ‘Knock-in’Strategy Quality control
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