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
赵亚 1王锦秋 2刘丽娟 1胡巧红 2赵瑞芝3
作者信息
- 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;广东省中医证候临床研究重点实验室,广州 510120
- 折叠
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 SULT 1A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.
Abstract
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 1α and 4α and 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 phase Ⅱ metabolic 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/4α content 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Key words
Vinegar-baked Bupleuri Radix/liver targeting/liver nuclear factor/phase Ⅱ metabolic enzyme引用本文复制引用
基金项目
国家自然科学基金项目(81073063)
国家自然科学基金项目(82173981)
国家自然科学基金项目(81573612)
广东省科技计划项目(2023B1212060063)
出版年
2024
NETL
NSTL
万方数据