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Application of Lycojaponicumin C in monoamine oxidase inhibitor medicine

A monoamine oxidase and inhibitor technology, applied in the application field of Lycojaponicumin C in monoamine oxidase inhibitor drugs, can solve problems such as limited application, and achieve the effect of strong inhibitory activity and outstanding substantive characteristics

Inactive Publication Date: 2013-12-25
赵伟杰
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its application is limited because of the high blood pressure caused by "cheese reaction"

Method used

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  • Application of Lycojaponicumin C in monoamine oxidase inhibitor medicine
  • Application of Lycojaponicumin C in monoamine oxidase inhibitor medicine
  • Application of Lycojaponicumin C in monoamine oxidase inhibitor medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Embodiment 1: the preparation of the compound Lycojaponicumin C tablet involved in the present invention:

[0013] Take 20 grams of compound Lycojaponicumin C, add 180 grams of conventional excipients for tablet preparation, mix well, and make 1000 tablets with a conventional tablet press.

Embodiment 2

[0014] Embodiment 2: the preparation of the compound Lycojaponicumin C capsules involved in the present invention:

[0015] Get 20 grams of compound Lycojaponicumin C, add conventional auxiliary materials for preparing capsules such as 180 grams of starch, mix well, and pack into capsules to make 1000 tablets.

[0016] The following pharmacodynamic experiments will further illustrate its drug activity.

[0017] Compound Lycojaponicumin C detects the inhibitory activity to MAO-A and MAO-B with the method of fluorescent probe, and described method is carried out according to the following steps:

[0018] Dissolve the sample to be tested in DMSO to prepare a series of samples with concentration gradient. Take 4ul of MAO (10mg / ml), boric acid buffer (PH=8.4), 50ul of BSA (50mg / ml), add the sample solution to be tested, mix well, react in a water bath at 30-38°C for 3h, and then add probe 7 -(3-Aminopropoxy)coumarin 2ul (50mmol / ml), final inhibitor concentration 0~10 -2 mmol / l, ...

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Abstract

The invention discloses an application of Lycojaponicumin C in preparation of a monoamine oxidase (MAO) inhibitor. In comparison with the existing monoamine oxidase inhibitor, the inhibitory activity and the selectivity to MAO-A and MAO-B of the monoamine oxidase inhibitor provided by the invention are improved greatly. The application of Lycojaponicumin C in preparation of the monoamine oxidase inhibitor, related to the invention, is disclosed for the first time. The skeleton type is a brand-new one, and the inhibitory activity of the inhibitor on monoamine oxidase is unexpectedly strong, so that no possibility for providing any revelation by other compounds exists. The Lycojaponicumin C has prominent substantial characteristics, meanwhile, has a remarkable progress in treatment of monoamine oxidase disorder related diseases.

Description

1. Technical field [0001] The present invention relates to the application of Lycojaponicumin C in the preparation of monoamine oxidase (MAO) inhibitors. 2. Background technology [0002] Since the anti-tuberculosis drug isoniazid was found to be a potential MAO inhibitor, research on MAO inhibitors has become a hot topic. Iproniazid became the first MAO inhibitor, because it was discovered that this kind of MAO inhibitor containing hydrazine structure can also inactivate P450s and cause liver toxicity; and studied the non-hydrazine MAO inhibition represented by tranylcypromine Agents, this category can be called the second generation. But because "cheese reaction" causes high blood pressure, its application is limited. Therefore, it is quite necessary and urgent to develop a newer and more efficient monoamine oxidase inhibitor. [0003] The compound Lycojaponicumin C involved in the present invention is a new skeleton compound published in 2012 (Wang, X.J. et al., 2012. ...

Claims

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Application Information

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IPC IPC(8): A61K31/438
Inventor 吴俊华王慧
Owner 赵伟杰
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