Effect of Genkwa Flos on Transient Receptor Potential Vanilloid 1 of Thermosensitive Channel
10.13422/j.cnki.syfjx.20192002
- VernacularTitle: 芫花对热敏通道瞬时感受器电位香草素受体1的影响
- Author:
Yin YIN
1
;
Zhen-hong LIU
1
;
Wei GAO
1
;
Hai-ying TONG
1
;
Rong GUO
1
;
Xue-zhen HAN
1
;
Zhi-jun AN
1
;
Zhen YANG
1
;
Hong-xia ZHAO
2
Author Information
1. Beijing University of Chinese Medicine, Beijing 100029, China
2. Institute of Basic Theory, China Academy of Chinese Medical Sciences, Beijing 100700, China
- Publication Type:Research Article
- Keywords:
Genkwa Flos;
transient receptor potential vanilloid 1;
anti-inflammatory;
analgesic
- From:
Chinese Journal of Experimental Traditional Medical Formulae
2019;25(20):56-62
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To study the effect of Genkwa Flos on the thermosensitive channel, transient receptor potential vanilloid 1 (TRPV1) by electrophysiological whole cell patch clamp technique and animal behavior experiment, in order to explore its mechanism. Method:The whole-cell patch clamp technique was used to measure transmembrane currents induced by 75%ethanol extract from different concentrations of Genkwa Flos in HEK293 cells that expressed human TRPV1.TRPV1 specific antagonist capsaicin was used to observe whether it could inhibit the transmembrane current induced by Genkwa Flos. Totally 30 C57BL/6 mice were taken for behavioral detection, and divided into blank group (6 mice), high-dose group (6 mice), medium-dose group (6 mice), low-dose group (6 mice) and ibuprofen positive control group (6 mice). Genkwa Flos treatment group was given low dose (0.195 g·kg-1·d-1), medium dose (0.39 g·kg-1·d-1) and high dose (0.78 g·kg-1·d-1) by gavage. One hour later, the changes of behavioral latency of cold pain and hot pain in mice were observed in cold plate at (0±2)℃ and hot plate at (55±1)℃. Result:Whole cell patch clamp experiment showed that 75%ethanol extract of Genkwa Flos in hTRPV1/HEK293 cells could activate TRPV1 channel to generate obvious transmembrane current, which was similar with that generated by the known TRPV1 agonist capsaicin in current density and current-voltage relationship. The dose-effect experiments showed that compared with extracellular fluid, 10 g·L-1 ethanol extract of Genkwa Flos could activate hTRPV1/HEK293 cells to induce significant transmembrane current (P<0.01). The transmembrane current generated by 10 g·L-1 ethanol extract of Genkwa Flos was more than 3 g·L-1(P<0.01). The TRPV1 specific antagonist capsaicin could completely inhibit the transmembrane current induced by 10 g·L-1 ethanol extract of Genkwa Flos. In the experiment of cold plate and hot plate in mice, there was a dose-effect relationship between the latencies of cold pain behavior and hot pain behavior in mice prolonged by Genkwa Flos. In the experiment of cold plate, compared with the blank group, the cold pain behavior latency of mice in the medium-dose group was significantly prolonged (P<0.01), and that of mice in the high-dose group was significantly prolonged (P<0.01). Compared with the blank group, the cold pain behavior latency of mice in the ibuprofen positive control group was significantly prolonged (P<0.01). In the hot plate experiment, the incubation period of hot pain behavior in the high-dose group of Genkwa Flos was significantly longer than that in the blank group (P<0.01), while that in the ibuprofen positive control group was significantly longer than that in the blank group (P<0.05). Conclusion:More than one TRPV1 agonist was included in 75%ethanol extract of Genkwa Flos. The warm, analgesic and anti-inflammatory effects of Genkwa Flos may be a series of effects after activation of TRPV1.
