基于抗炎活性的桂枝茯苓胶囊抗痛经作用机制研究  

Anti-dysmenorrhea mechanism of Guizhifuling capsule based on its anti-inflammation effect

作　　者：仲云熙[1] 金孝亮 谷世寅 彭英[1] 肖伟[2] 王振中[2] 郑伟然[2] 孙建国[1] 王广基[1] ZHONG Yunxi JIN Xiaoliang GU Shiyin PENG Ying XIAO Wei WANG Zhenzhong ZHENG Weiran SUN Jianguo WANG Guangji(Key Lab of Drug Metabolism and Pharmacokinetics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, Jiangsu, China KANION Pharmaceutical, Lianyungang 222000, Jiangsu, China)

机构地区：[1]中国药科大学药物代谢动力学重点实验室 [2]江苏康缘药业股份有限公司

出　　处：《中国临床药理学与治疗学》2016年第10期1095-1102,共8页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：中央高校基本科研业务费专项基金项目(JKZD2013007);国家自然科学基金重点项目基金项目(81530098);国家重大新药创制专项基金项目(2013ZX09402203)

摘　　要：目的:探讨桂枝茯苓(GZFL)胶囊中原型成分的药效,并研究GZFL胶囊治疗原发性痛经的作用机制。方法:建立大鼠急性痛经模型并分别灌胃给予GZFL胶囊内容物、苦杏仁苷(AMY)、肉桂酸(CA)、没食子酸(GA)、丹皮酚(PA)以及芍药苷(PAE),通过测定其对疼痛抑制、子宫内膜增生抑制以及相关因子生成抑制的效果,研究GZFL胶囊原型成分的药效。由于原发性痛经与炎症反应机理相类似,均由炎症因子介导发生,因此结合大鼠急性痛经模型的结果,使用大鼠足趾肿胀模型,通过测定GZFL胶囊对肿胀抑制程度以及对相关炎症因子生成的抑制作用,判断其是否通过抑制相关炎症因子的生成而发挥治疗痛经的作用。结果:在大鼠急性痛经模型中,GZFL胶囊中原型成分PA表现出明显的抑制疼痛、抑制子宫内膜增生、促进超氧化物歧化酶(SOD)、NO、丙二醛(MDA)水平正常化的作用,结果与模型组相比具有统计学差异(P<0.05);PAE存在与PA相似的作用,但是效果相对较弱。在大鼠足趾肿胀模型中,PA表现出明显的抑制肿胀与抑制相关炎症因子生成的作用(P<0.05)。结论:GZFL胶囊可能通过抑制炎症介质的表达,发挥其治疗原发性痛经的作用,且该作用可能主要通过PA发挥。AIM： To explore the pharmacodynamics of prototype of Guizhifuling（ GZFL） capsule and mechanism about primary dysmenorrhea treated by GZFL. METHODS： Five main medicative ingredients amygdalin（ AMY）,cinnamic acid（ CA）,gallic acid（ GA）,paeoniflorin（ PAE） and paeonol（ PA）） of GZFL were administered respectively intragastrically in acute dysmenorrhea model rats. The inhibition level of pain,endometrial hyperplasia and relative factors generation were observed to evaluate its pharmacodynamics of GZFL. Because of the similar mechanisms between primary dysmenorrhea and inflammation that both are induced by inflammatory factors,paw edema model in rats are used to evaluate the treating dysmenorrhea effect of GZFL by inhibition swelling extent and relative factors generation.RESULTS： In acute dysmenorrheal model,the result of GZFL prototype PA inhibiting pain,restraining hyperplasia of endometrium and normalizing the level of relative factors（ SOD,NO,MDA） has statistical differences（ P 〈 0. 05） compared with Model group. PAE showed weaker effects compared with PA. In paw edema model,PA inhibition of swelling extent and relative factors generation has statistical differences（ P 〈 0. 05） compared with Model group,which is consistent with the result in acute dysmenorrheal model. CONCLUSION： GZFL can treat primary dysmenorrhea by inhibiting expression of inflammatory factors. The prototype PA of GZFL may be the medicative of anti-dysmenorrhea.

关 键 词：桂枝茯苓胶囊 原发性痛经 炎症因子 丹皮酚 

分 类 号：R965.2[医药卫生—药理学]