摘要
目的:研究5种二苯乙烯类化合物(白藜芦醇,RES;己烯雌酚,DES;二苯乙烯苷,THSG;反式二苯乙烯,TS和二苯乙烯苷水加成产物,SWA)对一氧化氮(NO)介导的舒张血管反应的影响,并探讨其作用与化学结构的关系。方法:采用血管张力记录法,观察药物对大鼠主动脉血管环张力的作用,并测定药物对NO含量和对一氧化氮合酶(NOS)活性的影响。结果:RES、DES、THSG、TS和SWA(1、3、10、30、100μmol.L-1)能剂量依赖性地舒张苯肾上腺素(10μmol.L-1)诱发的血管收缩反应,其效价强度,依次为THSG>DES>RES>SWA=TS;与二甲亚砜比较,TS和SWA的作用不明显。L-Arg(1μmol.L-1)可增强RES、DES、THSG的舒张血管作用,而亚甲蓝(1μmol.L-1)却可削弱之。另外,RES、DES、THSG(10μmol.L-1)可增加血管总NO含量及NOS活性,其增加NOS活性作用的强度,依次为THSG>DES>RES>SWA>TS。结论:RES、DES、THSG具有剂量依赖性依内皮性舒张血管作用,此作用与增加NO含量及NOS活性有关。它们结构中的乙烯双键对发挥舒张血管作用是必需的,苯环上的羟基的数量及位置决定着其作用强度。
OBJECTIVE To study the effects of five stilbene compounds, that is resveratrol （RES）, diethylstilbestrol （DES）, tetrahydroxystilbene-glucoside （THSG）, trans-stilbene （TS） and stilbene water addition （SWA）, on nitric oxide （NO）-mediated vasodilation and to explore the relationship between their effects and the chemical structures. METHODS In the rat thoracic aorta with and without endothelium, the vascular tension was observed. NO contents and nitric oxide synthase （NOS） activity of vessel were detected byNO kit and NOS kit respectively. RESULTS RES, DES and THSG（1-100 μmol·L^-1） could dose-dependently antagonize vessel contraction induced by phenylephrine （ 10μmol·L^-1）, with the potency of TH- SG〉DES〉RES, it means they possess vasodilation, but TS and SWA （1-100μmol·L^-1 ）could not markedly dilate vessel. The vasodilational effect of RES, DES and THSG could he strengthened by L arginine （1μmol·L^-1）, while attenuated by methylene blue （1 μmol·L^-1）. In addition, the vascular total NO content and NOS activity were increased by RES, DES and THSO（ 10μmol·L^-1 ） ,with the potency of THSG 〉 DES 〉 RES. CONCLUSION The vasodilation of RES, DES and THSG is endothelia-dependent, which is related to the increase in NO content and NOS activity. These indicate that diphenylethylene structure and existence of hydroxyl group in diphenyl are essential for vasodilational effect and the quantity and situation of hydroxyl group is important for their potencies.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2006年第7期826-829,共4页
Chinese Journal of Hospital Pharmacy
关键词
白藜芦醇
己烯雌酚
二苯乙烯苷
L-精氨酸
亚甲蓝
一氧化氮
一氧化氮合酶
resveratrol
diethylstilbestrol
tetrahydroxystilbene-glucoside
L-arginine
methylene blue
nitric oxide
nitric oxide synthase
