CN103120673A - Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor - Google Patents
Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor Download PDFInfo
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- CN103120673A CN103120673A CN2012104129417A CN201210412941A CN103120673A CN 103120673 A CN103120673 A CN 103120673A CN 2012104129417 A CN2012104129417 A CN 2012104129417A CN 201210412941 A CN201210412941 A CN 201210412941A CN 103120673 A CN103120673 A CN 103120673A
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Abstract
The invention provides an application of Aphanamixoid A to the preparation of a monoamine oxidase (MAO) inhibitor. Compared with the existing MAO inhibitor, the MAO inhibitor provided by the invention is greatly improved on the aspects of inhibitory activity and selectivity to MAO-A and MAO-B. The application of the Aphanamixoid A to the preparation of the MAO inhibitor, related by the invention, is disclosed for the first time; a framework type of the Aphanamixoid A is brand new, and Aphanamixoid A has unexpected strong inhibitory activity to MAO, so that no possibility that any revelation is given by other compounds exists, and Aphanamixoid A has remarkable substantive features and is also remarkably improved on the aspect of treating MAO imbalance related diseases.
Description
1, technical field
The present invention relates to the application of Aphanamixoid A in preparation monoamine oxidase, MAO (MAO) inhibitor.
2, background technology
Since finding that the antitubercular agent isoniazid is a kind of potential MAO inhibitor, the research of MAO inhibitor has been become focus.Iproniazid becomes first MAO inhibitor, simultaneously can make the P450s inactivation cause hepatotoxicity because finding the MAO inhibitor that this class contains the hydrazine structure; Studied again the MAO inhibitor of the non-hydrazine class take tranylcypromine as representative, this class can be described as the second filial generation.But because " cheese reaction " causes hypertension, limited its application.Therefore, a kind of more novel, efficient oxidase inhibitor of development is suitable necessity and urgent.
the compd A phanamixoid A that the present invention relates to is one and delivered (Cai in 2012, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to insect antifeedant activity (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), belong to open first for the purposes of the Aphanamixoid A that the present invention relates in preparation monoamine oxidase, MAO (MAO) inhibitor, because framework types belongs to brand-new framework types, and it is unexpectedly strong for monoamine oxidase inhibitory activity, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, the treatment that is used for simultaneously monoamine oxidase, MAO imbalance relevant disease obviously has significant progress.
Summary of the invention
The new purposes that the purpose of this invention is to provide Aphanamixoid A compound, this compound is high to the inhibition activity of MAO, selectivity good.
The technical solution used in the present invention is:
The application of compd A phanamixoid A in the preparation oxidase inhibitor, described compd A phanamixoid A structure is as shown in formula I:
Formula I
Compd A phanamixoid A can detect the inhibition of MAO-A and MAO-B with the method for fluorescent probe active, and described method is carried out according to following steps: sample dissolution to be measured in DMSO, is made into a series of samples with concentration gradient.Get MAO 4ul, borate buffer (PH=8.4), 1 ~ 100ul BSA(1 ~ 100mg/ml), add testing sample solution, mix homogeneously.Then react 3h in 0 ~ 38 ℃ of water-bath, then add probe 2ul(1 ~ 100 mmol/ml), inhibitor ultimate density 0 ~ 10
-2Mmol/l, mixture react 1 ~ 24h again in 0 ~ 38 ℃ of water-bath, (λ ex/ λ em=365/460nm) detects with the global function spectrofluorophotometer.Calculate IC according to the data obtained
50
The purposes of the Aphanamixoid A that the present invention relates in preparation monoamine oxidase, MAO (MAO) inhibitor belongs to open first, because framework types belongs to brand-new framework types, and it is unexpectedly strong for monoamine oxidase inhibitory activity, there is not the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the treatment that is used for simultaneously monoamine oxidase, MAO imbalance relevant disease obviously has significant progress.
(4) specific embodiment
The preparation method of compd A phanamixoid A involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of compd A phanamixoid A tablet involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compd A phanamixoid A capsule involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add the conventional adjuvant such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Compd A phanamixoid A is active to the inhibition of MAO-A and MAO-B with the method detection of fluorescent probe, and described method is carried out according to following steps:
Sample dissolution to be measured in DMSO, is made into a series of samples with Concentraton gradient.Get MAO(10mg/ml) 4ul, borate buffer (PH=8.4), 50ul BSA(50mg/ml), add testing sample solution, mix homogeneously, react 3h in 30 ~ 38 ℃ of water-baths, then add probe 7-(the amino propoxyl group of 3-) coumarin 2ul(50mmol/ml), inhibitor ultimate density 0 ~ 10
-2Mmol/l, mixture react 12h again in 30 ± 5 ℃ of water-baths, (λ ex/ λ em=365/460nm) detects with the global function spectrofluorophotometer.Calculate IC according to the data obtained
50, the results are shown in Table 1.
Table 1: compd A phanamixoid A suppresses activity and selective data
Conclusion: Aphanamixoid A can significantly suppress the activity of MAO, and selectivity is good, can be used for the treatment of monoamine oxidase, MAO imbalance relevant disease.
Claims (1)
1.Aphanamixoid the application of A in the MAO-A inhibitor, described compd A phanamixoid A structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012104129417A CN103120673A (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor |
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| CN2012104129417A CN103120673A (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor |
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| CN103120673A true CN103120673A (en) | 2013-05-29 |
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| CN2012104129417A Pending CN103120673A (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103520185A (en) * | 2013-10-29 | 2014-01-22 | 杨文君 | Application of compound in preparing monoamine oxidase MAO inhibitor |
-
2012
- 2012-10-25 CN CN2012104129417A patent/CN103120673A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| JIE-YUN CAI ET AL.: "Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya", 《ORGANIC LETTERS》 * |
| 王卫霞等: "改善认知功能障碍的传统植物药及其活性成分的药理作用", 《国外医学中医中药分册》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103520185A (en) * | 2013-10-29 | 2014-01-22 | 杨文君 | Application of compound in preparing monoamine oxidase MAO inhibitor |
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Application publication date: 20130529 |