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Applications of Isovitexin in preparation of monoamine oxidase (MAO) inhibitors

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

Inactive Publication Date: 2018-03-27
ZIBO DINGLI PATENT INFORMATION CONSULTING 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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  • Applications of Isovitexin in preparation of monoamine oxidase (MAO) inhibitors
  • Applications of Isovitexin in preparation of monoamine oxidase (MAO) inhibitors
  • Applications of Isovitexin in preparation of monoamine oxidase (MAO) inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1: the preparation of compound Isovitexin tablet involved in the present invention:

[0016] Take 5 grams of compound Isovitexin and add 195 grams of dextrin, mix well, and make 1000 tablets with a conventional tablet machine.

Embodiment 2

[0017] Embodiment 2: the preparation of compound Isovitexin capsules involved in the present invention:

[0018] Take 5 grams of compound Isovitexin, add 195 grams of starch, mix well, and pack into capsules to make 1000 capsules.

[0019] The following pharmacodynamic experiments will further illustrate its drug activity.

[0020] Compound Isovitexin 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:

[0021] 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, 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°C for 12h, and then tested wit...

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Abstract

The invention provides the application of isovitexin in the preparation of monoamine oxidase (MAO) inhibitors. Compared with the existing monoamine oxidase inhibitors, the inhibitory activity and the selectivity to MAO‑A and MAO‑B are greatly improved. The use of Isovitexin in the preparation of monoamine oxidase (MAO) inhibitors involved in the present invention is disclosed for the first time. Since the skeleton type belongs to a new skeleton type, and its inhibitory activity against monoamine oxidase is unexpectedly strong, there is no possibility of giving any inspiration from other compounds , has outstanding substantive features, and it is obviously a significant progress in the treatment of diseases related to monoamine oxidase disorders.

Description

technical field [0001] The present invention relates to a new application of compound Isovitexin, in particular to the application of Isovitexin 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 Isovitexin involved in the present invention is a new compound published in 2013...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K9/48A61K9/20
CPCA61K31/7048A61K9/2059A61K9/4866
Inventor 田丽华
Owner ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD