Application of compound in preparing monoamine oxidase MAO inhibitor

A monoamine oxidase and compound technology, which can be applied to medical preparations containing active ingredients, organic active ingredients, pharmaceutical formulations, etc., can solve problems such as limited application, and achieve the effect of strong inhibitory activity and outstanding substantive characteristics.

Inactive Publication Date: 2014-01-22
杨文君
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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 compound in preparing monoamine oxidase MAO inhibitor
  • Application of compound in preparing monoamine oxidase MAO inhibitor
  • Application of compound in preparing monoamine oxidase MAO inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Example 1: Preparation of the compound Phyllanthoid A tablets of the present invention:

[0012] Take 5 grams of compound Phyllanthoid A and add 195 grams of dextrin, mix well, and conventionally press to make 1000 tablets.

Embodiment 2

[0013] Example 2: Preparation of the compound Phyllanthoid A capsule of the present invention:

[0014] Take 5 grams of the compound Phyllanthoid A and add 195 grams of starch, mix them, and encapsulate them to make 1000 tablets.

[0015] The following pharmacodynamic experiments will further illustrate its drug activity.

[0016] The compound Phyllanthoid A was tested for its inhibitory activity on MAO-A and MAO-B by a fluorescent probe method, and the method was carried out according to the following steps:

[0017] Dissolve the sample to be tested in DMSO to prepare a series of samples with a concentration gradient. Take 4ul of MAO (10mg / ml), boric acid buffer (PH=8.4), 50ul BSA (50mg / ml), add the sample solution to be tested, mix well, react in 30~38℃ water bath for 3h, then add probe 7 -(3-Aminopropoxy) coumarin 2ul (50mmol / ml), the final concentration of inhibitor is 0~10-2mmol / l, and the mixture is reacted in a water bath at 30±5℃ for 12h, using a full-function fluorescence sp...

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Abstract

The invention provides an application of a compound phyllanthoid A in preparing a monoamine oxidase (MAO) inhibitor. Compared with existing MAO inhibitors, the inhibiter has greatly improved inhibition activity and selectivity upon MAO-A and MAO-B. The application of phyllanthoid A in preparing the MAO inhibitor is disclosed for a first time, and the compound has high inhibition activity against MAO. The compound has outstanding substantive feature. The application has significant progress in treatments of diseases related to MAO disorder.

Description

Technical field [0001] The present invention relates to a new use of a compound Phyllanthoid A, in particular to the application of Phyllanthoid A in the preparation of monoamine oxidase MAO inhibitors. Background technique [0002] Since the discovery of the anti-tuberculosis drug Isoniazid as a potential MAO inhibitor, the research on MAO inhibitors has become a hot spot. Isonicotinic hydrazide became the first MAO inhibitor, because it was discovered that this type of MAO inhibitor containing a hydrazine structure can also inactivate P450s and cause liver toxicity; also studied non-hydrazine MAO inhibition represented by tranylcypromine Agents, this type can be called the second generation. But because the "cheese reaction" triggers 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 Phyllanthoid A involved in the present invention is a new compoun...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58
Inventor 杨文君
Owner 杨文君
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