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Application of koumine and koumine homolog in preparation of medicines for treating diabetic complications

A technology of kelkinin and diabetes, which is applied in the field of medicine to achieve a large therapeutic window, no tolerance and addiction, and the effect of improving neuropathy

Active Publication Date: 2014-04-02
FUJIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no literature report on the effect of kinesin on the treatment of diabetic complications and its possible use

Method used

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  • Application of koumine and koumine homolog in preparation of medicines for treating diabetic complications
  • Application of koumine and koumine homolog in preparation of medicines for treating diabetic complications
  • Application of koumine and koumine homolog in preparation of medicines for treating diabetic complications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Improvement of hyperalgesia in diabetic rats by subcutaneous injection of kelkinin in the back of the neck.

[0027] 1.1 Drugs and reagents:

[0028] Gelkinin is extracted, separated and purified from the natural plant Gelkins by the applicant of the present invention, see Patent No.: 200810071469.9, the title of the invention is "Method for Separating and Preparing Gelkins Alkaloid Monomers from Gelkins by High-speed Countercurrent Chromatography" and Patent No. 2011101746576 The disclosed technology is the prior art with a purity of >98.5% (precisely weigh kelkinin, dissolve it with 1mol / l HCl, dilute it with normal saline, adjust the pH (4<pH<7) with 1mol / l NaOH, and use physiological Diluted with saline to the solution required for each dose group.). Gabapentin injection (10mg / ml), product of Shenyang No. 1 Pharmaceutical Factory, batch number 102090936065021. Streptozotocin, Tianjin Beichen Fangzheng Reagent Factory, batch number 20070828.

[0029] 1.2 Animals: ...

Embodiment 2

[0042] Improvement of nerve conduction impairment in diabetic rats by subcutaneous injection of kelezin in the back of the neck.

[0043] 2.1 Drugs and reagents:

[0044] Kiskinin is obtained by the applicant of the present invention by extracting, separating and purifying the natural plant Gelkins, with a purity of >98.5% (accurately weigh kelkinin, dissolve it with 1mol / l HCl, dilute with normal saline, adjust the pH with 1mol / l NaOH (4 <pH<7), diluted with normal saline to the required solution for each dosage group.). Gabapentin injection (10mg / ml), product of Shenyang No. 1 Pharmaceutical Factory, batch number 102090936065021. Streptozotocin, Tianjin Beichen Fangzheng Reagent Factory, batch number 20070828.

[0045] 2.2 Animals:

[0046] SD rats, male, 180-220g, provided by Shanghai Slack Animal Center. They were raised at room temperature at 25°C under a light-dark cycle of 12 / 12h, free to eat and drink, and used for formal experiments after 3 days of adaptation to t...

Embodiment 3

[0057] Improvement of neurofiber pathology in diabetic rats by subcutaneous injection of kelkinin in the back of the neck.

[0058] 3.1 Drugs and reagents:

[0059] Kiskinin is obtained by the applicant of the present invention by extracting, separating and purifying the natural plant Gelkins, with a purity of >98.5% (accurately weigh kelkinin, dissolve it with 1mol / l HCl, dilute with normal saline, adjust the pH with 1mol / l NaOH (4 <pH<7), diluted with normal saline to the required solution for each dosage group.). Gabapentin injection (10mg / ml), product of Shenyang No. 1 Pharmaceutical Factory, batch number 102090936065021. Streptozotocin, Tianjin Beichen Fangzheng Reagent Factory, batch number 20070828.

[0060] 3.2 Animals:

[0061] SD rats, male, 180-220g, provided by Shanghai Slack Animal Center. They were raised at room temperature at 25°C under a light-dark cycle of 12 / 12h, free to eat and drink, and used for formal experiments after 3 days of adaptation to the lab...

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Abstract

The invention discloses an application of koumine and koumine homolog in the preparation of medicines for treating diabetic complications. The koumine is high in therapeutic index, the therapeutic index of the koumine for treating the pain hypersensitivity of diabetic rats is estimated to reach 4762, the koumine can be used for obviously improving the neuropathy of the diabetic rats, the details are explained in the embodiment 1, and the koumine is large in safe therapeutic window and suitable for the preparation of the medicines for treating the diabetic complications, is likely to have no tolerance or addiction, and has low side effects, and therefore, the koumine has potentially great economic effect. The koumine and the koumine homolog or pharmaceutically acceptable salts of the koumine can be applied to the preparation of the medicines for treating the diabetic complications, have no disadvantages of two types of clinically frequently-used medicines for treating the diabetic complications, are developed and researched according to national specifications about innovative drug examination and approval and are expected to be prepared into the novel national class-1 medicines for treating the diabetic complications which are capable of effectively treating the diabetic complications, have small side effects, clear industrialization prospect, no tolerance and no addiction and possess the national proprietary intellectual property rights.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the application of koumine alkaloid monomers, in particular to the application of koumine and its homologues in the preparation of medicines for treating diabetic complications. Background technique [0002] Complications of diabetes include diabetic neuropathy and pain, among others. Among them, diabetic neuropathy is the most common, which can affect the central and peripheral nerves, especially distal sensory neuropathy, which accounts for more than 50% of all diabetic neuropathies. The specific symptoms are hyperalgesia, decreased peripheral nerve conduction velocity, and nerve fiber degeneration. etc. seriously affect the quality of life. Drug therapy is currently one of the main means of clinically treating patients with diabetic complications, and gabapentin is currently the first-line drug for treating diabetic peripheral neuropathy. As of 2011, there were 366 million diabetic pat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/475A61P3/10A61P25/00A61P29/00
Inventor 俞昌喜刘铭凌倩许盈黄慧慧杨渐苏燕评
Owner FUJIAN MEDICAL UNIV
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