二苯乙烯苷对血管活性物质引起的体外血管收缩作用的影响  

Effects of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glycoside on Vasoconstriction Induced by Vasoactive Substances in Vitro

作　　者：张欣 贾敏 秦巧红 张寒[3] 侯颖 苏兴利 陈玉龙 ZHANG Xin;JIA Min;QIN Qiaohong;ZHANG Han;HOU Ying;SU Xingli;CHEN Yulong(Institute of Basic and Translational Medicine,Xi'an Medical College,Xi'an 710021Shaanxi,China;College of Basic Medical Science,Xi'an Medical College,Xi'an 710021 Shaanxi,China;College of Pharmacy,Xi'an Medical College,Xi'an 710021 Shaanxi,China)

机构地区：[1]西安医学院基础与转化医学研究所,陕西西安710021 [2]西安医学院基础医学部,陕西西安710021 [3]西安医学院药学院生药教研室,陕西西安710021

出　　处：《中药新药与临床药理》2021年第8期1114-1119,共6页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：陕西省科技创新基地—科技资源开放共享平台项目(2019PT-26);陕西省科技厅一般项目(社会发展领域,2020SF-156);西安医学院校内振兴计划人才基金项目(2018XNRC04)。

摘　　要：目的研究二苯乙烯苷(2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glycoside,TSG)在体外对高钾(KCl)、苯肾上腺素(PE)、5-羟色胺(5-HT)、内皮素-1(ET-1)、内皮素B型受体激动剂蛇毒类似物(S6c)诱导的血管环收缩的影响。方法显微操作下取大鼠肠系膜上动脉,制备成1.0~1.5 mm血管环,随机分为正常对照组、新鲜对照组及二苯乙烯苷低、中、高剂量组(10-4、10-3.5、10-3 mol·L^(-1))。采用离体血管环实验方法,通过DMT Myograph动态描记系统测定K+(60 mmol·L^(-1))、PE、5-HT、ET-1、S6c对血管环收缩的变化;采用Western Blot法检测血管环中内皮素A型(ETA)、内皮素B型(ETB)受体蛋白的表达。结果与正常对照组比较,TSG与离体血管环共同孵育24 h后能够呈浓度依赖性地舒张K+(60 mmol·L^(-1))、PE、5-HT引起的血管环收缩(P<0.05,P<0.01);TSG能够抑制ETB受体激动剂S6c对血管环引起的收缩,呈剂量依赖性(P<0.05,P<0.01),但对ET-1引起的血管收缩无明显影响(P>0.05)。Western Blot法检测结果发现,与新鲜对照组比较,体外培养24 h后血管环的ETA、ETB受体表达均显著增加(P<0.05,P<0.01);与正常对照组比较,TSG与离体血管环共同孵育24 h后,ETB受体蛋白表达明显下调(P<0.01),ETA受体蛋白表达无明显变化(P>0.05)。结论TSG在体外具有舒张血管的作用,与其拮抗血管活性物质引起的血管收缩,下调ETB受体表达有关。Objective To study in vitro effect of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glycoside(TSG)against vasoconstriction induced by high potassium(KCl),phenylephrine(PE),5-hydroxy tryptamine(5-HT),endothelin-1(ET-1),Sarafotoxin6c(S6c).Methods The superior mesenteric artery of rats was taken under a micromanipulation to prepare 1.0-1.5 mm vascular rings,and the rings were randomly divided into normal control group,fresh control group,TSG group low,medium and high dose groups(10-4,10-3.5,10-3 mol·L^(-1)).Using the isolated vascular ring experiment method,DMT Myograph dynamic tracing system was used to determine the changes of K+(60 mmol·L^(-1)),PE,5-HT,ET-1,S6c on the contraction of vascular ring.Western Blot method was used to detect the expression of endothelin A(ETA)and endothelin B(ETB)receptors in the vascular ring.Results Compared with the control group,TSG and the isolated vascular ring were able to show a concentration-dependent relaxation of vascular ring contraction caused by K+(60 mmol·L^(-1)),PE,and 5-HT after 24 hours of incubation(P<0.05,P<0.01).TSG can inhibit the contraction of vascular ring caused by ETB receptor agonist S6c in a dose-dependent manner(P<0.05,P<0.01),but has no effect on ET-1 induced vasoconstriction(P>0.05).Western Blot detection results showed that the expression of ETA and ETB receptors increased significantly after 24 hours of in vitro culture compared with the fresh group(P<0.05,P<0.01).Compared with the control group,after 24 hours of incubation with TSG and isolated vascular rings,the expression of ETB receptor was down-regulated(P<0.01),and the expression of ETA receptor was basically unchanged(P>0.05).Conclusion TSG has a concentration-dependent relaxation effect on K+,PE,5-HT,S6c pre-constricted vascular rings,which may relate to inhibiting the vasoconstriction caused by vasoactive substances and down-regulating expression of ETB receptor(s).

关 键 词：二苯乙烯苷 血管收缩剂 肠系膜上动脉 内皮素受体 

分 类 号：R285.5[医药卫生—中药学]