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Pentacyclic compound capable of adjusting polarization of macrophages and resisting diabetes and application thereof

A cyclic compound and anti-diabetic technology, applied in medical preparations containing active ingredients, digestive system, metabolic diseases, etc., can solve the problems of inability to regulate, high-throughput screening and difficulty, and achieve the effect of relieving insulin resistance

Active Publication Date: 2015-07-08
艾美斐生物医药科技(上海)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

However, due to the difficulty of high-throughput screening based on macrophage polarization, so far, there is no drug that can regulate macrophage polarization to treat the above diseases

Method used

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  • Pentacyclic compound capable of adjusting polarization of macrophages and resisting diabetes and application thereof
  • Pentacyclic compound capable of adjusting polarization of macrophages and resisting diabetes and application thereof
  • Pentacyclic compound capable of adjusting polarization of macrophages and resisting diabetes and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1: The therapeutic effect of JM-00121 on animal models of type 2 diabetes

[0057] see image 3 As shown, the weight of the diabetic model db / db mice was significantly larger than that of the normal control mice (db / dm), and began to show elevated blood glucose after 7 weeks, and its fasting blood glucose reached its peak at 8 weeks of age. In order to observe the effect of JM-00121 on body weight and blood sugar of db / db mice, we divided db / db and db / dm mice into control group (Vehicle) and administration group (Test Cpd, 3mg / kg), each group of animals Count 8-12 rats, start the administration time from the 5th week, and observe the changes of body weight and fasting blood sugar continuously for 5 weeks. We found that the fasting blood glucose of db / db mice in the JM-00121 administration group was significantly lower than that of the control group from the 7th week, but had no significant effect on body weight (such as image 3 (a) and image 3 (b)).

[0058]...

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Abstract

The invention discloses a pentacyclic compound capable of adjusting polarization of macrophages and resisting diabetes, and application thereof. The pentacyclic compound JM-00121 has a molecular structure shown in the description and can be used for curing type II diabetes and symptoms related to the diseases including adiposity, lipid disease, diabetes nephrosis, diabetes type dyslipidemia, hyperlipidemia, atherosclerosis, hepatic fibrosis and the like.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a pentacyclic compound. Background technique [0002] Macrophages are an important cellular component of the innate immune response. There are two main activation pathways. The classically activated M1 phenotype secretes pro-inflammatory cytokines, while the alternatively activated M2 phenotype secretes anti-inflammatory cytokines and is related to damage repair. In diseases characterized by chronic inflammation, such as type 2 diabetes, atherosclerosis, autoimmune diseases, neurodegenerative diseases and other pathological processes, it is observed that macrophages are polarized to the M1 type. Phage cells produce large amounts of pro-inflammatory cytokines, which lead to insulin resistance and tissue damage. [0003] Therefore, in theory, drugs that inhibit the polarization of macrophages to M1 and promote their polarization to M2 have the potential to treat the above di...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D249/12A61K31/4196A61P3/10A61P3/06A61P3/04A61P9/10A61P1/16
Inventor 范国煌
Owner 艾美斐生物医药科技(上海)有限公司
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