Effect of apigenin on the vasodilatory of basilar artery in rats and it mechanism
10.13699/j.cnki.1001-6821.2018.09.026
- VernacularTitle:芹菜素对舒张大鼠基底动脉的作用及机制研究
- Author:
Peng-Mei GUO
1
;
Yu LIU
;
Yi-Xin JING
;
Qi-Ying SONG
;
Miao-Miao DONG
;
Li-Na DONG
;
Ming-Sheng ZHANG
Author Information
1. 山西医科大学药理教研室
- Keywords:
apigenin;
basilar artery;
vasodilatation;
protein kinase
- From:
The Chinese Journal of Clinical Pharmacology
2018;34(9):1100-1104
- CountryChina
- Language:Chinese
-
Abstract:
Objective To study the spasmolytic effect and the underlying mechanism of apigenin in isolated rat basilar artery.Methods Healthy male rats were euthanized by exsanguination.The rat brain was removed and transferred immediately into physiological salt solution.The rat basilar arteries were isolated and cut into 2 mm-long rings under the microscope.Diastolic test:the different segments of the same blood vessel were randomly divided into two groups:the control group (solvent dimethylsulfoxide,diastolic) and the experimental group (apigenin 1-100 μmol · L-1,diastolic).Inhibition of contraction test:the same blood vessel was divided into the control group,low,medium and high dose experimental groups based on the dosage of administration (apigenin 0,10,30,100 μmol · L-1 respectively).The duration of administration was at least 10 min.Calcium ion (Ca2+) deprivation and specific inhibitors:an inhibitor of protein kinase C (Go6983),an inhibitor of extracellular signal-regulated kinase (PD98059),an inhibitor of Rho-associated kinase (Y-27632),an inhibitor of p38 Mitogen-activated protein kinase (SB239063) were used to explore the possible involvement of modulation of Ca2 + availability and activities of protein kinases in apigenin-induced vasorelaxation.The vascular myogenic tone was recorded with a wire myograph.Half maximal diastolic concentration (RC50),half maximal inhibitory concentration (IC50),maximal diastolic rate and maximal inhibition rate were calculated.Results After the administration,apigenin 1 ～ 100 μmol · L-1 concentration-dependently relaxed the arterial rings precontracted with either KCl 60 mmol · L-1,U46619 0.3 μmol · L-1 or vasopressin (VP,3 μmol · L-1) and the RC50 values were (24.27 ±1.14),(4.1 ±1.16),(1.9±1.33) μmol · L-1 respectively.Comparison between experimental groups with control group,the difference had significantly (all P ＜ 0.01).Incubation with apigenin 10 ～ 100 μmol · L-1 shifted the concentration-contraction curves of KCl,U46619,VP or Ca2+ to the right with the maximal contractions depressed.The IC50values of low,medium and high dose experimental groups against KCl,U46619,VP or Ca2+ were (77.73 ± 1.72),(14.91 ± 1.31),(20.66 ± 1.21),(7.53 ± 1.02) μmol · L-1 respectively.Comparison between three doses experimental groups with control group,the difference had significantly (all P ＜ 0.01).Both intracellular Ca2+ release dependent and extracellular Ca2+ influx dependent contractions were reduced after preincubation with apigenin by (24.53 ± 5.32) ％ and (48.58 ± 8.92) ％.Preincubation with Go6983 and PD98059,but not Y-27632 and SB239063 attenuated apigenin-induced vasorelaxation.Relaxation rate of Go6983 made API on the KCl,U46619 shrinkingwere decreased (40.33 ± 2.51)％,(36.51±5.13)％;Relaxation rate of PD98059 made API on the KCl,U46619 shrinkingwere decreased (25.84 ± 3.86)％,(21.80 ± 5.95)％.Compared with control group (without apigenin or inhibitors intervention),the difference were statistically significant (P ＜0.05,P ＜0.01).Conclusion Apigenin are spasmolytic against a variety of vasoconstrictors in rat basilar artery.Reduction of Ca2 + availability,modulation of activities of extracellular signal-regulated kinase and protein kinase C may be,at least in part,contributory to vasorelaxant effects of apigenin.
