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Application of cinnamon oil, cinnamyl aldehyde and derivatives of cinnamyl aldehyde in preparation of histamine H3 acceptor antagonist or inverse agonist medicaments

An inverse agonist and receptor antagonist technology is applied in the field of use of cinnamon oil, cinnamaldehyde and derivatives thereof in the preparation of histamine H3 receptor antagonist or inverse agonist drugs, and can solve the problem of the central nervous system. Poor penetration ability, unfavorable treatment of central nervous system diseases, etc., to achieve the effect of clear drug effect and controllable quality

Inactive Publication Date: 2011-10-19
CHENGDU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Histamine H3 receptor antagonists containing imidazole ring structure have two major defects: one is that the penetration ability to the central nervous system is very poor, which is not conducive to the treatment of central nervous system diseases; the other is that they have a tendency to inhibit cytochrome P450, Easily interacts with other medications
[0010] There are no reports in the existing literature that cinnamon oil, cinnamon aldehyde or cinnamon aldehyde derivatives have histamine H3 receptor antagonistic or inverse agonist activity

Method used

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  • Application of cinnamon oil, cinnamyl aldehyde and derivatives of cinnamyl aldehyde in preparation of histamine H3 acceptor antagonist or inverse agonist medicaments
  • Application of cinnamon oil, cinnamyl aldehyde and derivatives of cinnamyl aldehyde in preparation of histamine H3 acceptor antagonist or inverse agonist medicaments
  • Application of cinnamon oil, cinnamyl aldehyde and derivatives of cinnamyl aldehyde in preparation of histamine H3 acceptor antagonist or inverse agonist medicaments

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Experimental program
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Effect test

Embodiment 1

[0027] The preparation of embodiment 1 cinnamon oil, cinnamon aldehyde and cinnamon aldehyde derivative

[0028] Cinnamon oil, cinnamaldehyde and cinnamaldehyde derivatives are commercially available and can be purchased directly.

[0029] The preparation method of cinnamon oil: After pulverizing cinnamon, weigh 500g and place it in a 2000ml flask, add 3 times of water and soak for 60min, then add 15% NaCl solution as an auxiliary agent, and heat to keep the system in a boiling state. Move the steamed cinnamon oil-water emulsion into a centrifuge, and centrifuge at 4000r / min. Drain the water in the upper layer to obtain the volume of cinnamon oil. The yield of cinnamon volatile oil was 2.13%. Detected by HPLC, the cinnamaldehyde content is 83.56%.

[0030] Except adopting the cinnamon oil extraction method of the present invention to prepare, also can adopt supercritical fluid (CO 2 ) extraction method (He Cuiwei, orthogonal test optimal supercritical fluid CO of cinnamon ...

Embodiment 2

[0032] The H3 receptor affinity in vitro of embodiment 2 cinnamon oil, cinnamon aldehyde and cinnamon aldehyde derivative

[0033] 1. Experimental method:

[0034] (1) Take the frontal brain of the rat under freezing, and put it into 20 times the solution containing 2mM MgCl 2 and 50mM Tris HCl, the pH was adjusted to 7.4, and the homogenate was centrifuged at 45,000G for 10 minutes. Remove the supernatant, pass through a Polytron, and resuspend the cell membrane pellet in a solution containing 2 mM MgCl 2and 50mM Tris HCl, the pH was adjusted to 7.4, and centrifuged again. At a concentration of 12 mg / ml, the final pellet was resuspended in a solution containing 2 mM MgCl 2 and 50mM Tris HCl, the pH was adjusted to 7.4, and the temperature was adjusted to 25°C;

[0035] (2) Dilutions of cinnamon oil, cinnamon aldehyde and cinnamon aldehyde derivatives were prepared in 10% DMSO / 50mM Tris (pH 7.4) to prepare serial concentration test solutions respectively. Put 25 microlite...

Embodiment 3

[0043] Example 3 Effects of Cinnamon Oil, Cinnamaldehyde and Cinnamaldehyde Derivatives on Alzheimer's Disease

[0044] 1. Grouping of animals: Wistar rats, half male and half female, weighing (220±20) g, were purchased from the Animal Center of Sichuan University. After 1 week of adaptive feeding, they were randomly divided into: normal group; AD group (both dorsal hippocampus injected with Aβ 25-35 ); sham operation group (1 μl normal saline was injected into bilateral dorsal hippocampus); cinnamon oil low-dose group, cinnamon oil middle-dose group, cinnamon oil high-dose group, cinnamon aldehyde low-dose group, cinnamon aldehyde middle-dose group, cinnamon aldehyde high-dose group Dose group, p-chlorocinnamaldehyde group, α-bromo-p-aminocinnamaldehyde group, α-bromo-p-methylcinnamaldehyde group, and huperzine A tablet group, bilateral dorsal hippocampus injected with 1 μl of normal saline, followed by cinnamon Oil, cinnamaldehyde, cinnamaldehyde derivatives and huperzine A...

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Abstract

The invention provides application of cinnamon oil, cinnamyl aldehyde and derivatives of cinnamyl aldehyde in the preparation of histamine H3 acceptor antagonist or inverse agonist medicaments, and also provides a novel H3 acceptor antagonist or inverse agonist medicament which is formed by using cinnamon oil, cinnamyl aldehyde or derivatives of cinnamyl aldehyde as a main active ingredient and adding other active ingredients. The medicament can be used for preventing and treating senile dementia depression. The H3 acceptor antagonist or inverse agonist medicament provided by the invention has the advantages of clear curing effect, controllable quality and safety, and provides a new choice for clinical work.

Description

technical field [0001] The present invention relates to the new application of cinnamon oil, cinnamon aldehyde and derivatives thereof, in particular the application in the preparation of drugs of antagonist or inverse agonist of histamine H3 receptor. Background technique [0002] Histamine is produced by the decarboxylation of histidine by decarboxylase, and is a neurotransmitter with a wide range of physiological effects in the body. It has been found that histamine receptors consist of several different subtypes, namely H1, H2, H3 and H4 receptors. Both histamine H1 and H2 receptors are postsynaptic receptors, while histamine H3 receptor is a presynaptic autoreceptor widely distributed in the central nervous system and peripheral nervous system, in the central nervous system, the receptor The body not only participates in the regulation of the release, synthesis and metabolism of histamine in the brain, but also participates in the regulation of various neurotransmitter...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/54A61K31/11A61P25/28A61P25/24A61K127/00A61K135/00
Inventor 马松涛刘冬恋李婷婷曹丽萍
Owner CHENGDU MEDICAL COLLEGE
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