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Application of Houttuynoid A for preparing monoamine oxidase (MAO) inhibitor medicine

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: 2013-03-27
何晓涛
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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 Houttuynoid A for preparing monoamine oxidase (MAO) inhibitor medicine
  • Application of Houttuynoid A for preparing monoamine oxidase (MAO) inhibitor medicine
  • Application of Houttuynoid A for preparing monoamine oxidase (MAO) inhibitor medicine

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Embodiment 1

[0012] Embodiment 1: the preparation of compound Houttuynoid A tablet involved in the present invention:

[0013] Take 20 grams of compound Houttuynoid A, add 180 grams of conventional excipients for tablet preparation, mix well, and make 1000 tablets with a conventional tabletting machine.

Embodiment 2

[0014] Embodiment 2: the preparation of compound Houttuynoid A capsule involved in the present invention:

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

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

[0017] Compound Houttuynoid 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:

[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, the mixture was then...

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Abstract

The invention provides application of Houttuynoid A for preparing a monoamine oxidase (MAO) inhibitor. Compared with the original MAO inhibitor, the inhibitory activity and the selectivity on MAO-A and MAO-B of the MAO inhibitor provided by the invention are greatly increased. The application of Houttuynoid A for preparing the MAO inhibitor is disclosed for the first time; because the skeleton type belongs to a brand new skeleton type and the MAO inhibitory activity of Houttuynoid A is strong unexpectedly, the possibility that other compounds give any inspiration does not exist; Houttuynoid A has outstanding substantive characteristics; and simultaneously, Houttuynoid A has obvious progress for treating diseases related to MAO imbalance.

Description

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

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P43/00
Inventor 何晓涛
Owner 何晓涛
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