醋柴胡水提取液不同部位对大黄酸单次给药体内分布影响及其作用机制初探  

Different parts of Vinegar-baked Bupleuri Radix water extract affect the distribution of rhein and hepatic nuclear factor 1/4αby single administration

作　　者：赵亚 王锦秋 刘丽娟 胡巧红[2] 赵瑞芝 ZHAO Ya;WANG Jin-qiu;LIU Li-juan;HU Qiao-hong;ZHAO Rui-zhi(State Key Laboratory of Chinese Medicine for Dampness Syndrome,the Second Affiliated Hospital of Guangzhou University of Chinese Medicine,Guangzhou 510006;Guangdong Pharmaceutical University,Guangzhou 510006;Guangdong Provincial Key Laboratory of Clinical Research on Traditional Chinese Medicine Syndrome,Guangzhou 510120)

机构地区：[1]广州中医药大学第二附属医院省部共建中医湿证重点实验室,广州510006 [2]广东药科大学,广州510083 [3]广东省中医证候临床研究重点实验室,广州510120

出　　处：《中南药学》2024年第7期1812-1816,共5页Central South Pharmacy

基　　金：国家自然科学基金项目(No.81073063,No.82173981,No.81573612);广东省科技计划项目(No.2023B1212060063)。

摘　　要：目的考察醋柴胡不同部位对大黄酸在大鼠体内的分布及其对肝核因子1α和4α的影响,初步探讨醋柴胡肝靶向增强作用的活性部位和调控环节。方法大黄酸分别联用醋柴胡多糖(PSS)、正丁醇(BUF)、小分子部位(MHE)灌胃大鼠,给药后分别于5、15、30、90、210 min腹主动脉取血和各组织;测定血浆及组织中大黄酸和Ⅱ相代谢酶的含量,以相对靶向率(RTE)和相对摄取率(Re)评价醋柴胡各部位对大黄酸组织靶向作用的影响。结果醋柴胡3个部位均可增加大黄酸的肝靶向性,顺序为MHE>PSS>BUF。大黄酸给药后30 min,PSS和BUF部位显著降低了SULT1A的活性,MHE显著升高了肝核因子HNF1α/HNF4α含量。结论3个部位均为醋柴胡活性部位,不同部位具有不同作用机制,有待进一步探讨。Objective To determine the distribution of different parts of Vinegar-baked Bupleuri Radix(VBRB)on rhein in rats and its effect on liver nuclear factor 1αand 4αand to preliminarily explore the active sites and regulatory links of the liver targeted enhancement effect of VBRB.Methods Rhein was orally administered in rats in combination with polysaccharides(PSS),n-butanol(BUF),and small molecule fraction(MHE)of VBRB.The blood and tissues were collected from the abdominal aorta at 5,15,30,90,and 210 min after the administration.The contents of rhein and phaseⅡmetabolic enzymes in the plasma and the tissues were measured,and the relative targeting rate(RTE)and relative uptake rate(Re)were calculated to evaluate the effects of different parts of VBRB on rhein tissue targeting.Results Based on the RTE and Re,all three parts of VBRB increased the liver targeting of rhein in the order of MHE>PSS>BUF.After the administration of rhein for 30 min,PSS and BUF decreased the activity of SULT1A,while HNF1α/4αcontent was increased by MHE.Conclusion All three parts are the active parts of VBRB,with different parts aiming different targets,and the mechanism needs verification.

关 键 词：醋柴胡 肝靶向 肝核因子 Ⅱ相代谢酶 

分 类 号：R285[医药卫生—中药学]