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Application of Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor

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

Inactive Publication Date: 2013-03-27
何晓涛
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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 Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor
  • Application of Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor
  • Application of Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor

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Embodiment 1

[0013] Embodiment 1: the preparation of compound Houttuynoid D tablet involved in the present invention:

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

Embodiment 2

[0015] Embodiment 2: the preparation of the compound Houttuynoid D capsule involved in the present invention:

[0016] Take 20 grams of compound Houttuynoid D, add conventional auxiliary materials 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 Houttuynoid D 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 ...

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Abstract

The invention provides an application of Houttuynoid D in preparation of a monoamine oxidase (MAO) inhibitor. Compared with that of the existing MAO inhibitor, the inhibitory activity and selectivity on MAO-A and MAO-B are greatly improved. The application of Houttuynoid D in preparation of the MAO inhibitor is disclosed for the first time, and because the framework type belongs to a novel framework type, the inhibitory activity on the MAO is unexpectedly high, the possibility that other compounds give enlightenment is avoided, and the Houttuynoid D has outstanding substantial characteristics and has obvious progress in treatment of MAO disorder related diseases.

Description

1. Technical field [0001] The present invention relates to the application of Houttuynoid D 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 Houttuynoid D involved in the present invention is a compound published in 2012 (Cai, J. Y. et al., 2012. Houttuynoid D, a Pote...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P43/00
Inventor 何晓涛
Owner 何晓涛
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