New applications of triptorelin

A technology of inflammation and inhibitors, applied in the direction of medical preparations containing active ingredients, peptide/protein components, nervous system diseases, etc., to achieve increased resolution of new and old things, high clinical application value and development prospects, and increased spontaneous turnover rate Effect

Active Publication Date: 2018-11-30
NANHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report in the literature that triptorelin can inhibit neuroinflammation, and based on this, it has related research on the treatment of central nervous system diseases

Method used

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  • New applications of triptorelin
  • New applications of triptorelin
  • New applications of triptorelin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Effects of triptorelin on LPS-induced mouse microglial activation markers CD68 and CD11b and corresponding inflammation-related factors IL-1β and iNOS

[0030] 1. Experimental animals:

[0031] 24 male C57BL / 6 mice, 3 months old, weighing about 25g. Animals were kept at room temperature (22±2)°C, humidity (45%-65%) and light and dark (12h:12h) environment, free to eat and drink. Animal grouping and treatment The mice were divided into 3 groups according to the random number table method: normal control group (NS, n=8), neuroinflammation model group (LPS, n=8), triptorelin (LPS+TRIP, n=8) 8), intraperitoneal injection (i.p) once a day, for a total of 1 week of treatment.

[0032] 2. Experimental drugs: lipopolysaccharide (Lipopolysaccharide, LPS); triptorelin.

[0033] 3. Experimental method:

[0034] (1) Establishment of neuroinflammation model in mice: intraperitoneal injection of 0.83 mg / kg LPS.

[0035] (2) Determination of CD68, CD11b, IL-1β and iNOS ...

Embodiment 2

[0048] Example 2: Effect of triptorelin on novel object discrimination ability of LPS-induced learning and memory impairment mice

[0049] Experimental animals: 36 male C57BL / 6 mice, 3 months old, weighing about 25g. Animals were kept at room temperature (22±2)°C, humidity (45%-65%) and light and dark (12h:12h) environment, free to eat and drink.

[0050] Animal grouping and treatment The mice were divided into 3 groups according to the random number table method: normal control group (NS, n=12), neuroinflammation model group (LPS, n=12), triptorelin (LPS+TRIP, n=12) 12), intraperitoneal injection (i.p) once a day, a total of 1 week of treatment, 1 hour after the last drug injection, 0.83mg / kg LPS was injected intraperitoneally in the LPS group and LPS+TRIP group, and the new object discrimination experiment was started on the 8th day .

[0051] Experimental principle: Mice show greater curiosity about things they have never seen before. During the pre-experiment, place two...

Embodiment 3

[0054] Example 3: Effect of triptorelin on working memory ability of LPS-induced learning and memory impairment mice

[0055] experimental method:

[0056] Animals: 36 male C57BL / 6 mice, 3 months old, weighing about 25 g. Animals were kept at room temperature (22±2)°C, humidity (45%-65%) and light and dark (12h:12h) environment, free to eat and drink.

[0057] Animal grouping and treatment The mice were divided into 3 groups according to the random number table method: normal control group (NS, n=12), neuroinflammation model group (LPS, n=12), triptorelin (LPS+TRIP, n=12) 12), intraperitoneal injection (i.p) once a day for a total of 1 week of treatment, 1 hour after the last drug injection, LPS group and LPS+TRIP group were injected with 0.83mg / kg LPS intraperitoneally, and the Y maze test was started on the 8th day. The spontaneous alternation rate of each mouse was measured, and the results were as follows: Figure 4 shown.

[0058] Experimental principle: The Y-maze de...

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Abstract

The invention belongs to the field of medicine, and discloses new applications of triptorelin, especially applications of triptorelin in preparation of drugs for inhibiting neuroinflammation. According to the present invention, the experiment results show that triptorelin can inhibit microglia activation, can significantly inhibit LPS-induced inflammatory mediator (TNF-alpha and iNOS) release in mouse hippocampus, and can significantly increase the resolution of new and old things in LPS-induced learning and memory impairment mice, wherein the spontaneous alternation rate in Y maze is increased significantly, such that it is indicated that triptorelin has significant protection effects on LPS-induced learning and memory impairment in mice; and triptorelin has remarkable neuroinflammation inhibition activity, can be used for preparing drugs for preventing and / or treating neuroinflammation, acute and chronic neurodegenerative diseases and other related diseases, and has high clinical application value and development prospect.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a new application of triptorelin, in particular to the application of triptorelin in the preparation of medicines for inhibiting neuroinflammation. Background technique [0002] The immune system plays an important role in maintaining tissue homeostasis and in responding to infection and injury. Microglia is a resident immune cell of the central nervous system, a member of the mononuclear macrophage family, and participates in the solid immune response in the brain (Thompson, K K, Tsirka, S E. The Diverse Roles of Microglia in the Neurodegenerative Aspects of Central Nervous System (CNS) Autoimmunity. Int JMol Sci, 2017, 18:3). Under normal circumstances, microglia play the role of immune surveillance, clearing metabolites through simple swallowing and drinking, and maintaining the purification of tissue stability. Under normal physiological conditions, the brain is considered immune pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61P25/28A61P25/16A61P25/14A61P29/00A61P25/00
CPCA61K38/09A61P25/00A61P25/14A61P25/16A61P25/28A61P29/00
Inventor 曹文宇万炜王贞徐杨牛磊钟小林刘政海
Owner NANHUA UNIV
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