CN1363274A - Application of ligustrazine and aminoguanidin in treating II-type diabetes and its complication - Google Patents
Application of ligustrazine and aminoguanidin in treating II-type diabetes and its complication Download PDFInfo
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- CN1363274A CN1363274A CN 02109906 CN02109906A CN1363274A CN 1363274 A CN1363274 A CN 1363274A CN 02109906 CN02109906 CN 02109906 CN 02109906 A CN02109906 A CN 02109906A CN 1363274 A CN1363274 A CN 1363274A
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- ligustrazine
- aminoguanidine
- diabetes
- aminoguanidin
- diabetic
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Abstract
A ligustrazine-aminoguanidin composition for protecting pancreatic island, reducing blood sugar, and preventing and treating diabetic arteriosclerosis, peripheral nerve damage, diabtic nephrosis, etc is disclosed. Its advantages are high curative effect and low cost.
Description
The present invention relates to the Chinese medicine ligustrazine and but low dose of aminoguanidine compound recipe is applied to treat type ii diabetes and complication thereof.
The basic ideas of traditional TCM treatment of diabetes are YIN nourishing, QI invigorating, promote the production of body fluid, relieve inflammation or internal heat.The application of activating blood circulation to dissipate blood stasis class medicine in treating diabetes in recent years more and more comes into one's own.The promoting blood flow and remove blood stasis drug ligustrazine is the alkaloid monomer of extraction separation from Umbelliferae Ligustrum plant Rhizoma Chuanxiong rhizome.Its chemical constitution is tetramethylpyazine (tetramethel pyrazine), but existing synthetic.Recently find that ligustrazine can increase the synthetic of vascular endothelial cell structure type nitricoxide synthase (cNOS), has the application report that reduces diabetic complication.
Aminoguanidine is the old medicine of treatment diabetes, because routine dose application toxic and side effects is bigger, replaced by biguanides the fifties at home.In recent years clear and definite along with nitric oxide (NO) metabolism and function, find that aminoguanidine plays an important role in the relation of NO metabolism and disease as special inducible nitric oxide synthase (iNOS) inhibitor, be widely used in the experiment and the clinical research of diabetes abroad.Several years ago, Britain has two patent of invention WO97/23203 and WO97/23204 to register in China, has disclosed this medicine by inhibition iNOS, and has had treatment diabetes effect.
NO is the important medium of regulating multiple physiology and pathophysiological process.Clear and definite, the NO that comes from cNOS mainly regulates different physiological roles; And come from the NO of iNOS, mainly mediate multiple pathophysiological process.CNOS is different with the cell source of iNOS, and the former is mainly from tissues such as vascular endothelial cell and nerves, and the NO of generation works in the part; The latter is mainly from macrophage and blood granulocyte, and the NO of generation can discharge to target site with chemotactic, migration and the gathering of cell, when iNOS activates, often shows as diseased region and continues a large amount of NO of generation, causes pathologic lesion.
Zoopery shows, the diabetes rat model of high fructose preparation, and except hyperglycemia, hyperinsulinism, hyperlipemia, hypertension were arranged, the expression that peripheral blood leucocyte iNOS-mRNA also occurred strengthened.This diabetic animal is used ligustrazine and aminoguanidin treatment, can reduce the blood sugar level of animal significantly.Other has the research prompting, destroys the cNOS gene of mice, can cause that animal produces insulin resistant.
At present, the medicine of adjusting the amphitypy NOS imbalance of expression of diabetes still belongs to blank, although the report of independent application iNOS inhibitor (as aminoguanidine) or medicine (as ligustrazine) treatment diabetes is arranged, only is difficult to reach ideal therapeutic effect by adjusting a type NOS.
The present invention relates to ligustrazine and express, promote islet function to recover and alleviate the vitals infringement that diabetes cause to adjust the organ blood circulation by promoting cNOS.Aminoguanidine is by anti-glycosylation and suppress iNOS with to damage of diabetes islets of langerhans and insulin resistant, and the restriction aminoguanidine alleviates its side effect in low dose of range of application; Two medicine compatibilities play and get the two medicines chief separately with the imbalance state that the amphitypy NOS that adjusts diabetes expresses, and offset mutual weak point, learn from other's strong points to offset one's weaknesses the effect of action compensating.
The purpose of this invention is to provide a kind of more effective, cheap treatment diabetes medicament.
The mechanism of ligustrazine and aminoguanidine treatment diabetes is main to be realized by three approach:
1. ligustrazine is expressed by promoting cNOS, plays and improves the pancreas blood circulation, the pancreas due to the antagonism aminoguanidine
Island ischemic injuries and control diabetic artherosclerosis, peripheral lesion and diabetic nephropathy are done
With.
2. aminoguanidine suppresses glycosylation, block macromolecular crosslinked, with control diabetic artherosclerosis, week
Enclose nervous lesion and diabetic nephropathy, play synergism by this approach and ligustrazine.
3. aminoguanidine suppresses iNOS by specificity, plays the protection islet cells and alleviates the insulin resistant effect.
Claims (4)
1. ligustrazine (tetramethylpyazine, 2,3,5,6-Tetramethylpyrazine...C who prevents and treats diabetes and complication thereof
8H
12N
2) and the aminoguanidin medicine, ligustrazine is the pharmaceutical products of Chinese medicine Rhizoma Chuanxiong extract or synthetic;
Aminoguanidine is for its solvate, hydrate or officinal salt and pharmaceutically acceptable derivates thereof
(i) structural formula of ligustrazine is as follows:
(ii) aminoguanidine structural formula as follows:
2. according to the described ligustrazine of claim 1, its pharmaceutical dosage is expressed by promoting cNOS, play and improve the pancreas blood circulation, islets of langerhans ischemic injuries and control diabetic artherosclerosis, peripheral lesion and the diabetic nephropathy effect of antagonism due to the aminoguanidine.
3. according to the described aminoguanidine of claim 1, its low dose is used to prevent and treat diabetes complicated atherosclerosis, senile cataract, alzheimer disease and glomerular sclerosis by anti-glycosylation.
4. according to the described aminoguanidine of claim 1, its low dose suppresses iNOS by specificity, the insulin resistant that exists when being used for anti-diabetic and diabetes complicated glaucoma and vision and Aging.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021099065A CN1158080C (en) | 2002-01-08 | 2002-01-08 | Application of ligustrazine and aminoguanidin in treating II-type diabetes and its complication |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021099065A CN1158080C (en) | 2002-01-08 | 2002-01-08 | Application of ligustrazine and aminoguanidin in treating II-type diabetes and its complication |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1363274A true CN1363274A (en) | 2002-08-14 |
| CN1158080C CN1158080C (en) | 2004-07-21 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB021099065A Expired - Fee Related CN1158080C (en) | 2002-01-08 | 2002-01-08 | Application of ligustrazine and aminoguanidin in treating II-type diabetes and its complication |
Country Status (1)
| Country | Link |
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| CN (1) | CN1158080C (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8507451B1 (en) | 2011-03-07 | 2013-08-13 | Zhili Wang | Method for the treatment of type II diabetes |
| CN116850188A (en) * | 2023-05-29 | 2023-10-10 | 广州喜鹊医药有限公司 | Application of ligustrazine nitrone derivative in preparing medicament for preventing or treating type 2 diabetes |
-
2002
- 2002-01-08 CN CNB021099065A patent/CN1158080C/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8507451B1 (en) | 2011-03-07 | 2013-08-13 | Zhili Wang | Method for the treatment of type II diabetes |
| CN116850188A (en) * | 2023-05-29 | 2023-10-10 | 广州喜鹊医药有限公司 | Application of ligustrazine nitrone derivative in preparing medicament for preventing or treating type 2 diabetes |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1158080C (en) | 2004-07-21 |
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