Novel antidiabetic medicine

An anti-diabetic and drug technology, applied in the field of new chemical drugs and their design, can solve the problems of low drug action intensity, and achieve the effects of not easy to degrade, low cost, and simple drug synthesis

Inactive Publication Date: 2013-12-25
KINDEESU ZHOUMEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although ISIS-388626, due to the characteristics of "antisense drug design", makes the drug more specific and reduces side effects, but due to the characteristics of this type of drug, its drug effect is significantly lower than that of traditional chemical drugs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1 Determination of the optimal lasso structure

[0034] By culturing DNA molecules of various drug candidate compounds in the immortal cell line HEK293 for 1 week, and then measuring the degradation rate of DNA molecules of various drug compounds, that is, 100% degradation rate means complete degradation, 0% degradation rate means no degradation, The lower the degradation rate of the DNA molecule of the drug compound, the more the structure of the drug compound can resist the degradation of various nucleases, the stronger the degradation ability, and the more stable the structure.

[0035] Among them, (1) CCCATCTCTGGTGCC, (2) CGGCCACACACCAT, (3) CACGGGTGCAAACAG were divided into 6 experimental groups according to the modified structure, which were recorded as A, B, C, D, E, F, and the modification method was selected from both ends of the methyl group. The specific modification structure is shown in Table 1.

[0036] test group modified struct...

Embodiment 2

[0038] Example 2 Determination of the ratio of lead compound to modified compound

[0039] For the following compound CACGGGTGCAAACAG (referred to as compound A), the chemical modification of methylation at both ends was carried out according to 5 modified bases-5 unmodified bases-5 modified bases (referred to as compound B ), mix compounds A and B in 5 different ratios. Specifically, 10 μM of Compound B modified with the optimal lasso structure was added to each group, and then each group was added with different concentrations of chemically modified Compound A, the concentrations were 0.1 μM, 0.2 μM, 0.5 μM, 1 μM, 2 μM , so the ratio of A:B is 1:100, 1:50, 1:20, 1:10 and 1:5. The above-mentioned groups were mixed and cultured in the kidney cell line MDCK for 2 weeks, and then the contents of SGLT1 and SGLT2 were detected by RT-PCR method, and the results were shown by the efficiency of inhibiting the mRNA of total SGLT.

[0040] The result is as figure 2 As shown, the ...

Embodiment 3

[0041] Example 3 Best MgCl 2 determination of concentration

[0042] For the following compound CACGGGTGCAAACAG (referred to as compound A), the chemical modification of methylation at both ends was carried out according to 5 modified bases-5 unmodified bases-5 modified bases (referred to as compound B ), mixed according to the optimal ratio of 1:20 (A:B), and then dissolved in 1mM, 2mM, 5mM, 10mM, 20mM and 50mM MgCl 2 After that, the mixed cells were cultured in the kidney cell line MDCK for 2 weeks, and then the contents of SGLT1 and SGLT2 were detected by RT-PCR method, and the results were shown by the efficiency of inhibiting the mRNA of total SGLT.

[0043] The result is as image 3 As shown, the drug is in 1mM, 2mM, 5mM, 10mM, 20mM and 50mM MgCl 2 The inhibition efficiencies in the solvents were 86%, 88%, 95%, 89%, 75%, 74% and 72%, respectively, and the higher the inhibition efficiency, the higher the potency of the drug. From the results it can be seen that t...

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PUM

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Abstract

The invention provides a novel antidiabetic medicine. The novel antidiabetic medicine is obtained by the steps of finding a lead compound acting on sodium-sugar transport synergistic protein with an 'antisense chemical medicine design' method and performing targeted chemical modification (for example: methylated modification of the two ends of the lead compound, synergistic design of an unmodified compound and a modified compound, and development of MgCl2 serving as a medicine efficacy enhancer). Therefore, the novel antidiabetic medicine provided by the invention can inhibited integrated sodium-sugar transport synergistic protein efficiently and specifically, has low side effects and achieves an effect which is more excellent than that of the existing sodium-sugar transport protein II inhibitor, so as to achieve an effect of effectively treating type II diabetes and fill the gap in the chemical design of antisense medicines in China.

Description

technical field [0001] The invention relates to the field of biomedical engineering, in particular to a novel chemical drug for diabetes and a design method thereof. Background technique [0002] Diabetes is an absolute or relative lack of insulin in the blood, leading to hyperglycemia, diabetes, and fat and protein metabolism disorders. It is a common endocrine and metabolic disease. Diabetes is mainly divided into type I diabetes and type II diabetes. Type I is caused by the inability of pancreatic beta cells to produce enough insulin (absolute insulin deficiency), and type II is caused by insufficient insulin secretion or insulin resistance (relative insulin deficiency). Among diabetic patients, 90-95% have type 2 diabetes. Along with the raising of people's living standard, this pathological change has become common disease and frequently-occurring disease, and the age of onset also spreads from middle-aged and elderly people to young people and even teenagers. [0003...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12N15/113A61K48/00A61P3/10
CPCA61P3/10C12N15/11C12N15/113
Inventor 岳朋周锦源
Owner KINDEESU ZHOUMEDICAL TECH
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