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Use of vanillin receptor agonist in preparation of product for resisting Alzheimer disease

A technology for Alzheimer's disease and receptor agonists, which is applied in the field of vanillin receptor agonists and vanillin receptor agonists for the preparation of anti-Alzheimer's disease products, which can solve the effects of liver function and transaminase index , No problems such as application reports of vanillin receptor agonist anti-Alzheimer's disease products, restrictions on market development, etc. have been found

Inactive Publication Date: 2006-02-22
SHANGHAI MEDICILON INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0039] Tetrahydroaminoacridine is the first cholinesterase inhibitor approved by the FDA and clinically used to treat Alzheimer's disease, but regulations still need to be improved
[0046] The disadvantage of tacrine is that it has a great impact on liver function and transaminase index, which restricts the development of the market, and its sales growth is far behind other AD drugs
[0096] However, through literature search, etc., so far, no reports on the application of vanillin receptor agonists as anti-Alzheimer's disease products have been found.

Method used

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  • Use of vanillin receptor agonist in preparation of product for resisting Alzheimer disease
  • Use of vanillin receptor agonist in preparation of product for resisting Alzheimer disease
  • Use of vanillin receptor agonist in preparation of product for resisting Alzheimer disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0292] Embodiment 1, FLIPR analytical method measures the efficacy of capsaicin on VR1

[0293] First, in SHSY5Y cells stably transfected with TRPV1 and APP695swe (SY5Y / VR1 / SWAPP), an important established human neuroblastoma cell line, fluorescence imaging microplate assay (FLIPR) was used to evaluate the effect of capsaicin on the Effectiveness of VR1 (EC50 value, figure 1 ). Capsaicin showed dose-dependent activity in SY5Y-hVR1 and CHO / hVR1 / rVR1 cell lines.

[0294] like figure 1 (In SY5Y / VR1 / SWAPP cells, using FLIPR assay to measure capsaicin activity), the blue, green, and red curves represent the response of SY5Y-hVR1, CHO / hVR1 and CHO / rVR1 cells to different concentrations of capsaicin, respectively. Reaction. CHO / hVR1 and CHO / rVR1 cell lines are used here as controls. The table shows the EC50 values ​​of capsaicin in the three cell lines calculated from the data measured in the dose-dependent experiments described above. FLIPR assays were performed on 96-well PLI...

Embodiment 2

[0295] Embodiment 2, detect capsaicin on Aβ with ELISA 1-42 generated impact

[0296] The following sandwich ELISA (enzyme-linked immunolabeling assay) shows that capsaicin-induced VR1 channel activation leads to Aβ 1-42 generate reduction ( figure 2 : Detection of capsaicin on Aβ by ELISA 1-42 generated impact). After transfecting SY5Y / VR1 / SWAPP cells with RD for 48 hr, the cells were washed twice with PBS, and after adding fresh medium, different concentrations of capsaicin (eg, capsaicin) were added to the medium. figure 2 shown). Two hours later, the culture medium was collected, and Aβ was detected by ELISA; the cells were collected for the subsequent determination of PKCε kinase activity. like figure 2 shown that capsaicin at a concentration of 0.1 μM or higher greatly reduced Aβ 1-42 generation.

[0297] Quantification of Aβ and Aβ using a sandwich ELISA 1-42 . Briefly described below, with sampling buffer (0.6% BSA, 8 mM Na 2 HPO 4 *7H 2 O, 1.5mM NaH 2...

Embodiment 3

[0298] Example 3. Western blot quantitative determination of PKCε kinase activity

[0299] Subsequent quantitative Western blot assays showed that activation of the VR1 channel resulted in increased PKCε kinase activity (see image 3 : Quantitative quantitative Western blot assay for PKCε kinase activity). Aβ in cell lysate 1-42 The marked decrease in PKCε kinase activity (PKCε is the predominant PKC isoform expressed in the SY5Y cell line) is consistent with phosphorescence-RDα quantitative western blot assay. like image 3 shown, capsaicin above 0.1 M significantly increased PKC kinase activity.

[0300] SY5Y / VR1 / SWAPP cells were transiently transfected with RDα, a unique Pan-PKC substrate expressing strain. PKCε kinase activity was determined by quantitative western blotting using an anti-phospho-RDα antibody. The resulting ink dots were analyzed by densitometry. Densitometric data were normalized with β-actin densitometry from parallel loaded blots.

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Abstract

The invention relates to the use of vanillic aldehyde receptor activator in preparing products against Alzheimer's disease, wherein the vanillic aldehyde receptor activator comprises vanillic aldehyde and its derivative, capsaicin analogue and derivatives.

Description

technical field [0001] The present invention relates to technical fields such as medicine, food and beverage, specifically relates to the application of vanillin receptor agonist, more specifically relates to a vanillin receptor agonist used for preparing anti-Alzheimer's disease product the use of. Background technique [0002] (1) Research progress of vanillin receptor agonists [0003] Transient receptor potential (referred to as: TRP) channel exists widely in both vertebrates and invertebrates, both in activated cells and inactivated cells, and is the main channel for regulating calcium flow. The mammalian transient receptor potential family consists of six protein families: the classical transient receptor potential family (TRPCS), the transient receptor potential vanillin receptor family (abbreviation: TRPVS), the transient receptor potential melastatin family or Long transient receptor potential family (abbreviation: TRPMS), transient receptor potential mucolipin fa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/165A61K31/216A61K31/47A61K31/495A61K31/4035A61P25/28
Inventor 陈春麟毛晨张劲涛
Owner SHANGHAI MEDICILON INC
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