Application of Sarcaboside A to monoamine oxidase inhibitor

A monoamine oxidase and inhibitor technology, which is applied in the field of preparing monoamine oxidase (MAO) inhibitors, can solve problems such as limited application, and achieve the effect of strong inhibitory activity and outstanding substantive characteristics

Inactive Publication Date: 2013-11-20
丁圣雨
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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 Sarcaboside A to monoamine oxidase inhibitor
  • Application of Sarcaboside A to monoamine oxidase inhibitor
  • Application of Sarcaboside A to monoamine oxidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Embodiment 1: the preparation of compound Sarcaboside A tablet involved in the present invention:

[0014] Take 20 grams of compound Sarcaboside A, add 180 grams of conventional excipients for tablet preparation, mix well, and make 1000 tablets with a conventional tablet press.

Embodiment 2

[0015] Embodiment 2: the preparation of compound Sarcaboside A capsule involved in the present invention:

[0016] Get 20 grams of compound Sarcaboside A, add conventional adjuvants for preparing capsules such as 180 grams of starch, mix well, and pack into capsules to make 1000 tablets.

[0017] The following pharmacodynamic experiments will further illustrate its drug activity.

[0018] Compound Sarcaboside A 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:

[0019] 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, the mixture was then reacte...

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Abstract

The invention provides application of Sarcaboside A to preparation of a monoamine oxidase (MAO) inhibitor. Compared with an existing monoamine oxidase inhibitor, the Sarcaboside A has greatly improved inhibition activity and selectivity on MAO-A and MAO-B. The application of Sarcaboside A to the preparation of the monoamine oxidase (MAO) inhibitor involved in the invention is disclosed for the first time. As the Sarcaboside A has a novel skeleton type and unimaginably strong activity in inhibition of monoamine oxidase, no other compound can give any enlightenment. The invention has outstanding substantive distinguishing features and makes substantial progress in the treatment of diseases correlative to monoamine oxidase imbalance.

Description

1. Technical field [0001] The invention relates to the application of Sarcaboside A 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 Sarcaboside A involved in the present invention is a new skeleton compound published in 2012 (Li, X. et al., 2012. Two New-Skeleton Com...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P43/00
Inventor 丁圣雨
Owner 丁圣雨
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