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Application of Gypensapogenin B to preparation of MAO (monoamine oxidase) inhibitor

A technology of gypensapogeninb, 1. gypensapogeninb, which is applied in the field of 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: 2013-01-23
吴俊华
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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 Gypensapogenin B to preparation of MAO (monoamine oxidase) inhibitor
  • Application of Gypensapogenin B to preparation of MAO (monoamine oxidase) inhibitor
  • Application of Gypensapogenin B to preparation of MAO (monoamine oxidase) inhibitor

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Embodiment 1

[0013] Embodiment 1: the preparation of the compound Gypensapogenin B tablet involved in the present invention:

[0014] Take 20 grams of compound Gypensapogenin B, 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 Gypensapogenin B capsules involved in the present invention:

[0016] Take 20 grams of compound Gypensapogenin B, add conventional auxiliary materials such as starch 180 grams for the preparation of capsules, mix well, and pack into capsules to make 1000 tablets.

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

[0018] Compound Gypensapogenin B 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...

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Abstract

The invention provides application of Gypensapogenin B to preparation of a MAO (monoamine oxidase) inhibitor. Compared with the existing MAO inhibitor, the MAO inhibitor provided by the invention has greatly improved inhibitory activity and selectivity on MAO-A and MAO-B. The application of Gypensapogenin B to preparation of the MAO inhibitor is firstly publicized; and as a framework type belongs to a brand-new framework type, the framework type has unexpectedly strong inhibitory activity on the MAO inhibitor without any possibility shown by other compounds, and has outstanding substantial characteristics and remarkable progress for treating the diseases related to MAO unbalance at the same time.

Description

1. Technical field [0001] The invention relates to the application of Gypensapogenin B 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 Gypensapogenin B involved in the present invention was published in 2012 (Li, N. et al., 2012. Triterpenes possessing an unprecedent...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61P43/00
Inventor 王泽正俞骁吴俊华
Owner 吴俊华
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