Application of PKC enzyme inhibitor in preparing drug for improving and protecting islet beta cell functions

A technology of inhibitors and uses, applied in the field of medicine, can solve problems such as unoptimistic control of type 2 diabetes, loss of islet beta cell function, and aggravation of diabetes, etc., to improve and protect islet beta cells, endoplasmic reticulum stress inhibition, good inhibitory effect

Inactive Publication Date: 2019-10-18
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The long pathological process of diabetes will lead to the loss of islet beta cell function, and even lead to apoptosis and failure, which will lead to absolute insufficient insulin secretion, elevated blood sugar, and further aggravate diabetes. Although there are many treatment methods for diabetes, there are also clinically There are many therapeutic drugs, but most of them only lower blood sugar concentration and delay the progress of diabetes. They have little effect on improving and protecting pancreatic beta cells. Therefore, the current control of type 2 diabetes is not optimistic. Therefore, the discovery of drugs aimed at improving and protecting pancreatic beta cells has important biological research and practical significance, and provides support for the development of effective drugs for the treatment of diabetes

Method used

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  • Application of PKC enzyme inhibitor in preparing drug for improving and protecting islet beta cell functions
  • Application of PKC enzyme inhibitor in preparing drug for improving and protecting islet beta cell functions
  • Application of PKC enzyme inhibitor in preparing drug for improving and protecting islet beta cell functions

Examples

Experimental program
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Effect test

Embodiment 1

[0031] This example is illustrated with the non-selective PKC enzyme inhibitor Ro31-8220. The structure of the compound Ro31-8220 is as follows:

[0032]

[0033] The non-selective PKC enzyme inhibitor Ro31-8220 can inhibit the apoptosis of beta cells induced by thapsigargin (THAP) at a lower concentration (1.25μM). Ro31-8220 can also significantly inhibit the expression of TXNIP at a lower concentration, and can also effectively inhibit the expression of mRNA and protein related to endoplasmic reticulum stress. It can be further developed as a drug for treating diabetes and has broad application prospects. The following experiments are used for verification.

[0034] 1. The experiment of Ro31-8220 inhibiting the apoptosis of INS-1 cells induced by THAP

[0035] INS-1 cells are rat pancreatic tumor cells, which are one of the most widely used cells in diabetes research. It is reported that THAP can induce endoplasmic reticulum stress, inflammatory response, autophagy and...

Embodiment 2

[0070] Sotrastaurin, a non-selective PKC enzyme inhibitor, inhibits the expression of TXNIP induced by thapsigargin (THAP)

[0071] TXNIP plays an important role in INS-1 cells, it can mediate the endoplasmic reticulum stress of INS-1 cells, induce inflammation and promote apoptosis and autophagy, and the overexpression of TXNIP can also inhibit INS-1 Cellular insulin secretion, in order to verify that other PKC inhibitors also have this effect, so the inhibitory level of Sotrastaurin on the expression of TXNIP protein was detected under a series of concentration gradients, so as to confirm the inhibitory effect of other PKC inhibitors, which can further clarify the effect of PKC inhibitors on INS- 1 Effects on cell function.

[0072] The experimental steps are as follows:

[0073] 1 Collect the total cell protein: INS-1 cells were treated with Sotrastaurin and THAP drugs, extract the protein for 24 hours: wash the cells with cold PBS, add RIPA lysate to each well of the 6-we...

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Abstract

The invention discloses application of a PKC enzyme inhibitor in preparing a drug for improving and protecting islet beta cell functions. Through a series of experiments, it is verified that the PKC enzyme inhibitor has a good inhibitory effect on THAP-induced islet beta cell apoptosis, can significantly inhibit the expression of TXNIP and can effectively inhibit the expression of mRNA and proteinwhich are related to endoplasmic reticulum stress. The PKC enzyme inhibitor can provide a good candidate drug for clinical treatment of diabetes caused by the apoptosis and decrease of islet beta cells, and has a very good application prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to the use of a PKC enzyme inhibitor in the preparation of drugs for improving and protecting the function of pancreatic islet beta cells. Background technique [0002] Diabetes mellitus (DM) is a group of metabolic diseases characterized by hyperglycemia caused by defects in insulin secretion and / or insulin action disorders. Cardiovascular disease is the third chronic non-communicable disease. In recent years, with the improvement of living standards, the number of diabetic patients has been increasing year by year in both developed and developing countries, especially in countries such as China and Africa. It is predicted that the number of diabetic patients will reach 300 million in 2025. increased global economic burden. [0003] Diabetes is mainly divided into type 1 and type 2 diabetes. Type 1 diabetes is caused by the destruction of pancreatic β cells mediated by autoimmune d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/404A61K31/506A61K31/4709A61P3/10
CPCA61K31/404A61K31/4709A61K31/506A61K45/00A61P3/10
Inventor 姚新刚吴文玉何士俊刘叔文
Owner SOUTHERN MEDICAL UNIVERSITY
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