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Application of echinacoside to preparation of product for treating pruritus by inhibiting transient receptor potential vanillin receptor 3 channel

A technology of vanilloid receptor and echinacoside, applied in the field of medicine, can solve the problems such as no research report on vanilloid receptor 3 channel and anti-pruritic effect, and achieve the effect of clear action mechanism and less toxic and side effects

Inactive Publication Date: 2019-03-08
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] But there is no research report on echinacoside's inhibition of transient receptor potential vanilloid receptor 3 channel and antipruritic effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Evaluation of the inhibitory effect of echinacoside on the transient receptor potential vanilloid receptor 3 channel by calcium fluorescence method

[0020] HEK293 cells were cultured and subcultured in DMEM complete medium containing 10% fetal bovine serum. After the HEK293 cells grew to 90-100% density in a 10 cm diameter culture dish, the cells were digested with 0.25% trypsin, and the cells were prepared into 2 ml cells Suspension, 80 μl of cell suspension per well was dropped on a 12-well plate, supplemented with 1 ml of complete medium, mixed well and placed in an incubator at 37 °C, 5% CO 2 After 24 hours of culture, the cells in the 12-well plate grew to 80-90% density, and the human transient sensor potential vanilloid receptor 3 plasmid was transfected using liposome transfection reagent Lipofectamine 2000. For transfection, dilute 1.6 μl of liposome 2000 and 0.8 μg of human transient receptor potential vanilloid receptor 3 plasmid with 50 μl of reduced serum ...

Embodiment 2

[0022] Determination of the inhibitory effect and dose-effect relationship of echinacoside on transient receptor potential vanilloid receptor 3 channel by manual patch clamp technique

[0023] HEK293 cells transiently expressing the human transient receptor potential vanilloid receptor 3 channel were cultured for 24 h, and the patch-clamp whole-cell recording was performed using the EPC10 USB amplifier and Patchmaster software from HEKA, Germany. The glass electrode is completed with a P-97 electrode drawing instrument, and the water resistance after polishing is 4-5 MΩ. External fluid and compound solution use gravity perfusion device. The membrane potential was kept at 0 mV, and the ramp voltage was from -100 to +100 mV for 400 milliseconds, and the average value of -80 and +80 mV represented the time-effect diagram of the compound on the ion channel. The results showed that echinacoside 50 μM inhibited the transient receptor potential vanilloid receptor 3 channel current i...

Embodiment 3

[0025] Inhibition of echinacoside on transient receptor potential vanilloid receptor 1 channel, transient receptor potential vanilloid receptor 4 channel and transient receptor potential ankyrin receptor 1 channel

[0026] HEK293 cells transiently transfected with human transient receptor potential vanilloid receptor 1 channel, human transient receptor potential vanilloid receptor 4 channel, and human transient receptor potential ankyrin receptor 1 channel were detected by manual patch clamp technique. The inhibition rate of echinacoside B50 μM on the transient receptor potential vanilloid receptor 1 channel current induced by capsaicin 1 μM was 3.3 ± 0.4%, and the inhibition rate of echinacoside 50 μM on the transient receptor potential vanilloid receptor 4 induced by GSK101 The inhibition rate of the channel current was 1.2 ± 0.6%, and the inhibition rate of echinacoside B50 μM on the transient receptor potential ankyrin receptor 1 channel current induced by 300 μM propyl iso...

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Abstract

The invention provides an application of echinacoside to preparation of a product for treating pruritus by inhibiting a transient receptor potential vanillin receptor 3 channel. The inhibiting effectof the echinacoside on the transient receptor potential vanillin receptor 3 channel is verified by a calcium fluorescence method and a manual patch clamp technique, and the median inhibitory concentration IC50 of the echinacoside for the transient receptor potential vanillin receptor 3 channel is 14.7+ / -0.6 micrometers. The echinacoside is a specific inhibitor of the transient receptor potential vanillin receptor 3 channel. The anti-pruritus activity of the echinacoside is evaluated by a mouse skin pruritus model, and the echinacoside has an anti-pruritus effect on mouse acute pruritus causedby histamine. The echinacoside serving as the inhibitor of the transient receptor potential vanillin receptor 3 channel can be used for preparing the product for treating pruritus by inhibiting the transient receptor potential vanillin receptor 3 channel.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the application of echinacoside in the preparation of a product for inhibiting transient receptor potential vanilloid receptor 3 channel for treating pruritus. Background technique [0002] Pruritus is an extremely uncomfortable skin sensation that urgently requires scratching for relief. As a common dermatological disease, pruritus is the most common clinical manifestation of skin diseases such as atopic dermatitis, urticaria, contact dermatitis, prurigo nodularis, fungal disease and psoriasis, and it is also the most common clinical manifestation of many systemic diseases. Such as the accompanying symptoms of kidney disease, biliary tract disease, thyroid disease, malignant tumor and AIDS. Repeated scratching will trigger the release of itching factors and aggravate skin damage, which will cause more severe itching and seriously affect the quality of life of patients. [0003] At presen...

Claims

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Application Information

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IPC IPC(8): A61K31/7032A61P17/04
CPCA61P17/04A61K31/7032
Inventor 王威刘洋孙晓颖刘小红孙世伟王克威
Owner QINGDAO UNIV
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