ABSTRACT
Transient receptor potential vanilloid 3 (TRPV3) is a non-selective cation channel, located on cell membranes. TRPV3 is extensively expressed in various organs such as skin, brain, dorsal root ganglia, heart and colon. It's reported that TRPV3 involves in many physiological processes including sensation, skin barrier formation, hair growth and vasodilatation, and pathological processes like pruritus, cutaneous inflammatory disease and cancer. TRPV3 can respond to innoxious warm stimulation (≥ 33 ℃), endogenous substances (e.g., farnesylpyrophosphate) and exogenous small molecules (e.g., carvacrol, camphor and 2-APB). Recently, several natural or synthetic small molecules (e.g., osthole, 74a and dyclonine) have been shown to suppress TRPV3 activity, accompanying with therapeutic efficacy in animal models of diseases, which suggests the potential of TRPV3 as drug target. This paper reviews the research progress on the structure, physiological functions, related diseases and modulators of the TRPV3 channel to provide theoretical references for the future study on TRPV3 channel.
ABSTRACT
Objective:To observe the effect of Shaoyao Gancaotang and its disassembled prescriptions on the expressions of transient receptor potential vanilloid 3 (TRPV3) and transient receptor potential vanilloid 4 (TRPV4) in myocardium and hypothalamus of rats in the ultra-high temperature environment, in order to explore the mechanism of Shaoyao Gancaotang and its disassembled prescriptions against the high temperature. Method:Seventy five male SPF-grade SD rats were randomly divided into 5 groups according to their body weight, namely normal control group, high temperature normal control group, Shaoyao Gancaotang group (2.16 g·kg-1), single Paeoniae Radix Alba(PRA) group (1.08 g·kg-1) and single Glycyrrhizae Radix et Rhizoma(GRR) group (1.08 g·kg-1). Except normal control group, the remaining groups were fed in artificial climate boxes for 13 days. The normal control group and the high temperature normal control group were given the same volume of pure water. Western blot and quantitative real-time fluorescence polymerase chain reaction(Real-time PCR) were used to determine expressions of TRPV3, TRPV4 protein and mRNA in myocardium and hypothalamus of each group. Result:Compared with the normothermic control group, the expressions of TRPV3 protein, TRPV4 mRNA, TRPV3 protein and TRPV3 mRNA in the myocardium of the hyperthermic control group were significantly higher than those of the normal control group (PPPConclusion:TRPV3, TRPV4 channels in rat myocardium and hypothalamus were activated in the high temperature environment. The anti-hyperthermic mechanism of Shaoyao Gancaotang and its disassembled prescriptions was related to the regulation of TRPV3, TRPV4 channel protein and mRNA expressions in rat myocardium and hypothalamus.