Relaxant Effect and Underlying Mechanisms of Evodiamine on Isolated Myometrium of Rats
- VernacularTitle:吴茱萸碱对大鼠离体子宫平滑肌的舒张作用及机制研究
- Author:
Xiaoya LI
1
;
Jinyu LIU
;
Yuxue MU
;
Lin PENG
;
Shasha GE
;
Xin ZHAO
;
Yulin LIN
;
Dayong CAI
Author Information
1. 中国医学科学院/北京协和医学院药用植物研究所 北京100193
- Keywords:
Primary dysmenorrhea;
Evodiamine;
Capsaicin receptor 1;
Phospholipase Cβ;
Calmodulin
- From:
China Pharmacist
2017;20(10):1713-1717
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To study the relaxant effect and underlying mechanisms of evodiamine on isolated myometrium of rats. Methods:Prostaglandin F2α( PGF2α) was used to induce isolated myometrium contraction. The relaxant effect of evodiamine and the influence of capsazepine (an antagonist of transient receptor potential cation channel, subfamily V, member 1, TRPV1), U73122 (an antagonist of phospholipase Cβ,PLCβ) and W-7 ( an antagonist of camodulin, CaM) on the relaxant effect of evodiamine on myometri-um were observed respectively by biological function experiments. The median effective concentration ( EC50 ) was analyzed by non-line-ar various slope regressions using Prism-5. 01 software. Results:Evodiamine showed concentration-dependent relaxant effect on PGF2α-induced myometrium contraction with the EC50of 9.56 ×10 -9mol·L-1. Incubation with capsazepine (6.30 ×10 -11 mol·L-1), U73122 (2. 57 × 10 -11 mol·L-1 ) and W-7 (5. 65 × 10 -13 mol·L-1 ) markedly increased the relaxant effect of evodiamine, the EC50 of evodiamine decreased and dose-effect curves left shifted. The order of EC50 was as follows: W-7- evodiamine (8. 88 × 10 -15 mol· L-1) < capsazepine-evodiamine (7.35 ×10 -13 mol·L-1) < U73122-evodiamine (1.95 ×10 -12mol·L-1). Conclusion: Evodia-mine can inhibit myometrium contraction induced by PGF2αobviously, and the mechanisms are probably related to TRPV1, PLCβand CaM.
