Use of clove oil, eugenol and derivatives thereof in the preparation of medicines for histamine H3 receptor antagonists or inverse agonists

A technology of inverse agonists and receptor antagonists, applied in the direction of drug combinations, pharmaceutical formulas, plant raw materials, etc., can solve the problems of poor penetration of the central nervous system and unfavorable treatment of central nervous system diseases, and achieve clear drug effects, Quality Controlled Effects

Inactive Publication Date: 2011-11-30
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
[0011] There is no report in the existing literature that clove oil, eugenol or its derivatives have histamine H3 receptor antagonistic or inverse agonist activity

Method used

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  • Use of clove oil, eugenol and derivatives thereof in the preparation of medicines for histamine H3 receptor antagonists or inverse agonists
  • Use of clove oil, eugenol and derivatives thereof in the preparation of medicines for histamine H3 receptor antagonists or inverse agonists
  • Use of clove oil, eugenol and derivatives thereof in the preparation of medicines for histamine H3 receptor antagonists or inverse agonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The preparation of embodiment 1 clove oil, eugenol and eugenol derivative

[0028] Clove oil, eugenol and eugenol derivatives are commercially available and can be purchased directly.

[0029]The preparation method of clove oil: After pulverizing cloves, 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. The clove oil-water emulsion that evaporates is moved in the centrifuge, 4000r / min centrifugal separation. Drain the water in the upper layer to obtain the volume of clove oil, and the yield of clove volatile oil is 2.26%. Through HPLC detection, the eugenol content is greater than 80%.

[0030] Except adopting this extraction method to prepare, also can adopt supercritical fluid (CO2) extraction method (Yuan Yujie etc., the supercritical CO2 extraction process research of clove oil and GC-MS analysis, Chinese natural medicine, the 5th peri...

Embodiment 2

[0032] The histamine H3 receptor in vitro affinity determination of embodiment 2 clove oil, eugenol and eugenol 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 TrisHCl, 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 2 and 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 clove oil, eugenol and eugenol derivatives were prepared in 10% DMSO / 50mM Tris (pH 7.4) to prepare serial concentration test solutions respectively. Put 25 microliters of the test solution...

Embodiment 3

[0043] Example 3 Effect of Clove Oil, Eugenol and Eugenol 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); low-dose clove oil group, middle-dose clove oil group, high-dose clove oil group, low-dose eugenol group, middle-dose eugenol group, and high-dose eugenol group dosage group, methyl eugenol group, 4-allyl-1,2-dimethoxybenzene group, 4-allyl-2-methoxyl-1-benzyloxybenzene group, 4-(2 , 3-epoxypropyl)-2-methoxyphenyl acetate group, 4-(3-ethoxy-2-hydroxypropyl)-2-methoxyphenol group, 4-(3-ethoxy Base-2-hydroxypropyl)-2-methoxyphenol group and huperzine A group, bilateral dorsal hippocampus injected with 1μl s...

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Abstract

The present invention provides the application of clove oil, eugenol and derivatives thereof in the preparation of antagonists or inverse agonists of histamine H3 receptors, and also provides a method of using clove oil, eugenol or eugenol derivatives as The main active ingredient, together with other active ingredients, forms a new H3 receptor antagonist or inverse agonist drug, which can be used to prevent and treat senile dementia and depression. The H3 receptor antagonist or inverse agonist medicine provided by the invention has clear efficacy, controllable quality and safety, and provides a new choice for clinical practice.

Description

technical field [0001] The invention relates to the new application of clove oil, eugenol and derivatives thereof, in particular to the application in the preparation of medicaments of histamine H3 receptor antagonist or inverse agonist. 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 neurotransmitters such as 5-hyd...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/61A61K31/336A61K31/222A61K31/09A61K31/085A61P25/28A61P25/24
Inventor 马松涛臧志和刘冬恋李婷婷
Owner CHENGDU MEDICAL COLLEGE
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