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Application of ligustrazine nitrone derivative in prevention and treatment of diabetic complication diseases

By synthesizing ligustrazine nitrone derivatives TBN and TN-2, and combining their antioxidant and free radical scavenging activities, the problem of ligustrazine's insufficient free radical scavenging ability has been solved, significantly improving the therapeutic effect of diabetic nephropathy and retinopathy, and delaying disease progression and improved efficacy.

Inactive Publication Date: 2017-09-15
QINGDAO HAILAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] In summary, ligustrazine can improve diabetic nephropathy and its fundus diseases through anti-apoptosis, anti-inflammation, anti-oxidation and other ways, and has shown certain therapeutic effect on diabetic nephropathy in clinical research, but its effect on free radicals Insufficient clearance capacity, the therapeutic effect cannot meet the clinical needs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1. The making and grouping of STZ-induced diabetic nephropathy rat model

[0034] 1. Model making

[0035] Select SD rats (200 ± 10g) as model animals, fast for 12 hours before injection, dissolve STZ with a concentration of 1% in citrate buffer solution during injection, and inject 55 mg / kg STZ intraperitoneally after weighing the fasted rats. In the cage, ensure that the rats have sufficient drinking water for 24 hours. STZ injection needs to be done quickly, within 10 minutes. The normal control group was injected with an equal volume of citric acid-sodium citrate buffer at pH 4.5. The state of the animals was observed (polydipsia and polyuria), blood was collected from tail vein 3 weeks after STZ injection, and fasting blood glucose ≥ 16.7mmol / L was measured as the standard for diabetic nephropathy in rats.

[0036] 2. Grouping

[0037] The DKD rats were randomly divided into 6 groups, which were given different drugs, and the experiment was terminated a...

Embodiment 2

[0038] Example 2. Effects of Ligustrazine Derivatives on Body Weight, Diet and Drinking Water of STZ-Induced DKD Rats

[0039] The general situation and body weight changes of the rats after modeling were observed every week. The general situation included the activity, mental state, coat color, diet, water intake and urine output of the rats. The amount of water and feed consumed was recorded weekly.

[0040] Effects of Ligustrazine Derivatives on Body Weight of STZ-induced Diabetic Nephropathy Rats figure 1 As shown in a, TBN and TN-2 have basically no effect on the body weight of rats with diabetic nephropathy; figure 1 b and figure 1 As shown in c, the water intake and diet of DKD rats given TBN and TN-2 treatment group were significantly lower than those of the model group, indicating that TBN and TN-2 can slow down the progression of diabetic disease in DKD rats, thereby improving the polyphagia and hyperphagia of DKD rats symptoms of diabetes.

Embodiment 3

[0041] Example 3. Effect of Ligustrazine Derivatives on STZ-Induced DKD Rat Retinopathy

[0042] During the experiment, the retinal lesions of the rats were observed every day when the drug was administered, and the dates on which the retinopathy occurred in the rats of different groups were recorded.

[0043] Retinopathy is one of the common complications of diabetic nephropathy, and it is highly correlated with diabetic nephropathy. The effects of Ligustrazine derivatives on STZ-induced retinopathy in DKD rats are shown in Table 1. After treatment with TBN and TN-2, the number of cases of retinopathy in DKD rats decreased, and the time point of retinopathy was relatively delayed. The results showed that ligustrazine derivatives TBN and TN-2 can reduce and delay the occurrence of retinopathy.

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PUM

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Abstract

The invention belongs to the technical field of drugs and discloses application of a ligustrazine nitrone derivative and a pharmaceutical composition thereof in the preparation of drugs and the prevention and treatment of diabetic complication diseases. Experiments show that by utilizing the ligustrazine nitrone derivative, the blood glucose of an STZ-induced diabetic nephropathy model rat can be remarkably decreased, the levels of serum creatinine, urea nitrogen and urine proteins can be decreased, the kidney index can be decreased, and the probability of retinopathy of the diabetic nephropathy model rat can be remarkably decreased. Therefore, the ligustrazine nitrone derivative can be prepared into various dose forms together with drug carriers.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application of a tetramethylpyrazine nitrone derivative and a pharmaceutical composition thereof in the prevention and treatment of diabetic complications. Background technique [0002] Diabetes mellitus is a metabolic disease characterized by hyperglycemia due to defects in insulin secretion or insulin action. Sustained high blood sugar and long-term metabolic disorders can cause damage to the tissues and organs of the whole body, especially the eyes, kidneys, cardiovascular and nervous systems, as well as their dysfunction and failure. In severe cases, acute Complications ketoacidosis and hyperosmolar coma. [0003] Diabetic Kidney Disease (DKD) is one of the most important microvascular complications of diabetes. The clinical features are proteinuria, progressive renal damage, hypertension, edema, and severe renal failure in the late stage. DKD is currently...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4965A61P13/12A61P27/02A61P27/06A61P27/12A61P25/00A61P3/10
CPCA61K31/4965A61P3/10A61P13/12A61P27/02A61P27/06A61P27/12A61P9/10A61K45/06A61K31/519A61P27/10A61P25/00A61K2300/00
Owner QINGDAO HAILAN PHARMA CO LTD