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Use of Daphnilongeranin A in preparation of monoamine oxidase (MAO) inhibitor

A monoamine oxidase and inhibitor technology, applied in the application field of Daphnilongeranin A in the preparation of monoamine oxidase MAO inhibitors, to achieve strong inhibitory activity and highlight the effect of substantial characteristics

Inactive Publication Date: 2016-02-03
ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But because "cheesereaction" causes high blood pressure, its application is limited

Method used

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  • Use of Daphnilongeranin A in preparation of monoamine oxidase (MAO) inhibitor
  • Use of Daphnilongeranin A in preparation of monoamine oxidase (MAO) inhibitor
  • Use of Daphnilongeranin A in preparation of monoamine oxidase (MAO) inhibitor

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Experimental program
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Embodiment 1

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

[0012] Get 20 grams of compound Daphnilongeranin A and add 180 grams of conventional excipients for preparing tablets, mix well, and make 1000 tablets with a conventional tabletting machine.

Embodiment 2

[0013] Embodiment 2: the preparation of compound DaphnilongeraninA capsule involved in the present invention:

[0014] Get 20 grams of compound Daphnilongeranin A, add conventional auxiliary materials for preparing capsules, such as 180 grams of starch, mix well, and make 1000 capsules.

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

[0016] Compound DaphnilongeraninA was tested for its inhibitory activity on MAO-A and MAO-B by fluorescent probe method,

[0017] The described method proceeds 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, then add probe 7- (3-Aminopropoxy)coumarin 2ul (50mmol / ml), the final concentration of the inhibitor is 0~10-2mmol / l, the mixture is ...

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Abstract

The invention relates to a novel use of Daphnilongeranin A in preparation of a monoamine oxidase (MAO) inhibitor. Compared with the exciting monoamine oxidase inhibitor, the Daphnilongeranin A has higher inhibition activity and MAO-A and MAO-B selectivity. The use of Alistonitrine A in preparation of a MAO inhibitor is disclosed first. The skeleton type of the Daphnilongeranin A belongs a novel skeleton type, the Daphnilongeranin A has unexpected monoamine oxidase inhibition activity, is free of any enlightenment provided by other compounds and has prominent substantive features, and the use of Daphnilongeranin A in treatment on monoamine oxidase disorder-related diseases has substantial progress.

Description

technical field [0001] The present invention relates to a new application of compound Daphnilongeranin A, in particular to the application of Daphnilongeranin 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 "cheesereaction" 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 DaphnilongeraninA involved in the present invention is a new comp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439
Inventor 田丽华
Owner ZIBO DINGLI PATENT INFORMATION CONSULTING CO LTD
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