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Application of Aphanamgrandiol A in preparing monoamine oxidase (MAO) inhibitor

A monoamine oxidase and inhibitor technology, which is applied in the application field of Aphanamgrandiol A in the preparation of 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
HUAIAN UNIV SCI PARK MANAGEMENT CO LTD
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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 Aphanamgrandiol A in preparing monoamine oxidase (MAO) inhibitor
  • Application of Aphanamgrandiol A in preparing monoamine oxidase (MAO) inhibitor
  • Application of Aphanamgrandiol A in preparing monoamine oxidase (MAO) inhibitor

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Embodiment 1

[0011] Embodiment 1: the preparation of the compound Aphanamgrandiol A tablet involved in the present invention:

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

Embodiment 2

[0013] Embodiment 2: the preparation of compound Aphanamgrandiol A capsules involved in the present invention:

[0014] Get 5 grams of compound Aphanamgrandiol A, add 195 grams of starch, mix well, and pack into capsules to make 1000 capsules.

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

[0016] Compound Aphanamgrandiol 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:

[0017] 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), the final concentration of the inhibitor is 0~10-2mmol / l, and the mixture is reacted in a water bath at 30±5℃ for 1...

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Abstract

The invention provides an application of Aphanamgrandiol A in preparing a monoamine oxidase (MAO) inhibitor. Compared with existing MAO inhibitors, the inhibiting activity and the selectivity to MAO-A and MAO-B of Aphanamgrandiol A are greatly improved. The use of Aphanamgrandiol A for preparing the MAO inhibitor provided by the invention is disclosed for the first time. As the framework type belongs to a brand-new framework type, and the inhibiting activity of Aphanamgrandiol A to MAO is unexpectedly strong, the probability of giving any indication by other compounds does not exist, so that Aphanamgrandiol A has remarkable substantive characteristics and meanwhile obviously has remarkable progress for treating MAO disorder related diseases.

Description

technical field [0001] The present invention relates to a new application of compound Aphanamgrandiol A, in particular to the application of Aphanamgrandiol A in the preparation of monoamine oxidase MAO inhibitors. Background technique [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 Aphanamgrandiol A involved in the present invention is published i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/366
Inventor 张康
Owner HUAIAN UNIV SCI PARK MANAGEMENT CO LTD
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