摘要
目的:探讨桑寄生总黄酮祛风湿的功效物质在佐剂型关节炎模型大鼠体内的组织分布及药动学研究。方法:雄性SD大鼠54只,分为正常给药组和佐剂型关节炎组,通过注射弗式完全佐剂建造佐剂型关节炎模型。第9天开始给予桑寄生总黄酮(TFTC)360mg/kg,连续给药22d,末次给药后按不同时间点取血,并取出心、肝、脾、肺、肾、胃、大肠、小肠、脑等组织。HPLC法测定各大鼠血液和组织中芦丁、萹蓄苷、槲皮苷的含量,并用DAS 3.0处理分析药动学参数。结果:在佐剂型关节炎模型大鼠组织中,维持时间比较结果是槲皮苷为肝=肾=心=脑=脾=小肠>大肠=肺>胃>血清,萹蓄苷为肾=胃>小肠=脑>心。槲皮苷在组织中的AUC0-t依次为胃>肾>肝>脾>小肠>脑>心>肺>大肠>血清,萹蓄苷在组织中的AUC0-t依次为胃>肾>小肠>脑>心,芦丁只在血清和胃里有少量分布。在正常给药组大鼠组织中,维持时间比较结果是槲皮苷为胃>肾>肝>小肠>脾>脑>肺>心>大肠>血清,萹蓄苷为:肾>胃>心>小肠。槲皮苷在组织中的AUC0-t依次为胃>肾>肝>小肠>脾>脑>心>肺>大肠>血清,萹蓄苷在组织中的AUC0-t依次为:胃>肾>小肠>心,芦丁只在胃里有少量分布。结论:萹蓄苷与槲皮苷是桑寄生总黄酮祛风湿的功效物质,其中,槲皮苷是桑寄生黄酮归经和祛风湿功效的重要物质基础。证实了桑寄生总黄酮是桑寄生祛风湿作用的有效部位。萹蓄苷和槲皮苷的组织分布与桑寄生归肝、肾经的传统认识相吻合。
Objective: To explore the effective substances of total flavonoids of Taxilluschinensis (DC.) (TFTC) and its tissue distribution and pharmacokinetics in adjuvant arthritis rats. Methods: Fifty-four male Sprague-Dawley rats were divided into normal administration group and adjuvant arthritis group. The adjuvant arthritis model was constructed by injecting Freund's complete adjuvant. The drug was administered on the ninth day. TFTC group was given TFTC 360mg/kg, continuous administration of 22 days. Blood was taken at different time points after the last administration, and the heart, liver, spleen, lung, kidney, stomach, large intestine, small intestine, and brain were removed. Contents in different tissues of rats of rutin, avicularin and quercetin were detected by HPLC method, and DAS3.0 software was used for data processing of pharmacokinetic parameters. Results: In the model of adjuvant arthritis model rats, the time of comparison was that: quercitin was liver--kidney=heart=brain= spleen=small intestine〉large intestine=lung〉stomach〉serum; avicularin was kidney〉stomach〉small intestine=brain〉heart. The quercitin AUC0-t in the tissues was in the order of stomach〉kidney〉liver〉spleen〉small intestine〉brain heart〉lung〉large intestine〉serum, the avicularin AUC0-t, in the tissues were in the order of stomach〉kidney〉small intestine〉brain〉heart, while rutin only existed in the serum and stomach with small amount. In the normal group, the time of quercetin comparison was stomach〉 kidney〉liver〉small intestine〉spleen〉brain〉lung〉heart〉large intestine〉serum. Avicularin was kidney〉stomach〉heart〉small intestine. The quercetin AUC0-t in the tissues was in the order of stomach〉kidney〉liver〉spleen〉small intestine〉spleen〉brain〉heart〉lung〉large intestine〉serum, the avicularin AUC0-t in the tissues were in the order of stomach〉small intestine〉kidney〉heart, while rutin only existed in the stomach with small amount. Conclusion: Avi
作者
李玲玲
管俊
冯静
马开
崔瑛
LI Ling-ling;GUAN Jun;FENG Jingl;MA Kai;CUI Ying(School of Pharmacy, Henan Umverslty of Chinese medicine, Zhengzhou 450046, China;Chinese Medicine Research Institute of Henan Province, Zhengzhou 450004, China)
出处
《中华中医药杂志》
CAS
CSCD
北大核心
2018年第5期2203-2208,共6页
China Journal of Traditional Chinese Medicine and Pharmacy
基金
国家自然科学基金项目(No.81473368)~~