CN103285012A - Applications of Aspeverin to the preparation of inhibitors of monoamine oxidase (MAO) - Google Patents
Applications of Aspeverin to the preparation of inhibitors of monoamine oxidase (MAO) Download PDFInfo
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- CN103285012A CN103285012A CN2013102538847A CN201310253884A CN103285012A CN 103285012 A CN103285012 A CN 103285012A CN 2013102538847 A CN2013102538847 A CN 2013102538847A CN 201310253884 A CN201310253884 A CN 201310253884A CN 103285012 A CN103285012 A CN 103285012A
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- mao
- aspeverin
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- monoamine oxidase
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Abstract
The invention discloses applications of Aspeverin to the preparation of inhibitors of monoamine oxidase (MAO). Compared with existing inhibitors of monoamine oxidase, the MAO inhibitors provided by the invention have greatly improved inhibitory activity and selectivity to MAO-A and MAO-B. The applications of the Aspeverin to the preparation of inhibitors of MAO, related by the invention, are disclosed for the first time; the skeleton type thereof is brand new, and the inhibitory activity to MAO thereof is unexpectedly high, so the possibility of any prompt given by other compounds does not exist, and prominent substantive features are provided and a remarkable progress in treating MAO imbalance related diseases is made at the same time.
Description
Technical field
The present invention relates to the new purposes of compd A speverin, relate in particular to the application of Aspeverin in preparation monoamine oxidase MAO inhibitor.
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; Having studied again is the MAO inhibitor of the non-hydrazine class of representative with tranylcypromine, and this class can be described as the second filial generation.But because " cheese reaction " causes hypertension, limited its application.Therefore, the development a kind of more novel, efficiently oxidase inhibitor be quite necessity and urgent.
The compd A speverin that the present invention relates to is one and delivered (Nai-Yun Ji in 2013, et al., 2013.Aspeverin, a New Alkaloid from an Algicolous Strain of Aspergillus versicolor.Organic Letters10 (15), 2327 – 2329.) noval chemical compound, this chemical compound has brand-new framework types, present purposes only relates to and suppresses to swim vegeto-animal growth (Nai-Yun Ji, et al., 2013.Aspeverin, a New Alkaloid from an Algicolous Strain of Aspergillus versicolor.Organic Letters10 (15), 2327 – 2329.), belong to open first for the purposes of the Aspeverin that the present invention relates in preparation monoamine oxidase MAO inhibitor.
Summary of the invention
The objective of the invention is to provides the application of Aspeverin in preparation monoamine oxidase MAO inhibitor according to not finding that it has the present situation of the report of monoamine oxidase MAO inhibitor activity in the existing Aspeverin research.
Described compd A speverin structure is shown in formula I:
Compd A speverin can detect the inhibition activity to MAO-A and MAO-B with the method for 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 MAO4ul, borate buffer (PH=8.4), 1～100ul BSA(1～100mg/ml), add testing sample solution, mix homogeneously.In 0～38 ℃ of water-bath, react 3h then, add probe 2ul(1～100mmol/ml) then, 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.Go out IC50 according to the gained data computation.
The purposes of the Aspeverin 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 chemical compounds, possess outstanding substantive distinguishing features, the treatment that is used for monoamine oxidase, MAO imbalance relevant disease simultaneously obviously has obvious improvement.
The specific embodiment
The preparation method of compd A speverin involved in the present invention is referring to document (Nai-Yun Ji, et al., 2013.Aspeverin, a New Alkaloid from an Algicolous Strain of Aspergillus versicolor.Organic Letters10 (15), 2327 – 2329.)
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 speverin tablet involved in the present invention:
Get 5 and digest compound Aspeverin adding dextrin 195 grams, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compd A speverin capsule involved in the present invention:
Get 5 and digest compound Aspeverin and add starch 195 grams, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
The method of fluorescent probe of using compd A speverin detects the inhibition activity to MAO-A and MAO-B, 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, in 30～38 ℃ of water-baths, react 3h, add probe 7-(the amino propoxyl group of 3-) coumarin 2ul(50mmol/ml then), inhibitor ultimate density 0～10-2mmol/l, mixture reacts 12h again in 30 ± 5 ℃ of water-baths, (λ ex/ λ em=365/460nm) detects with the global function spectrofluorophotometer.Go out IC50 according to the gained data computation, the results are shown in Table 1.
Table 1: compd A speverin suppresses activity and selective data
Conclusion: Aspeverin 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.Aspeverin the application in preparation monoamine oxidase MAO inhibitor, described compd A speverin structure is shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102538847A CN103285012A (en) | 2013-06-22 | 2013-06-22 | Applications of Aspeverin to the preparation of inhibitors of monoamine oxidase (MAO) |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102538847A CN103285012A (en) | 2013-06-22 | 2013-06-22 | Applications of Aspeverin to the preparation of inhibitors of monoamine oxidase (MAO) |
Publications (1)
| Publication Number | Publication Date |
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| CN103285012A true CN103285012A (en) | 2013-09-11 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013102538847A Pending CN103285012A (en) | 2013-06-22 | 2013-06-22 | Applications of Aspeverin to the preparation of inhibitors of monoamine oxidase (MAO) |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103285012A (en) |
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2013
- 2013-06-22 CN CN2013102538847A patent/CN103285012A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| NAI-YUN JI，ET A1.: "Aspeverin, a new alkaloid from an algicolous strain of Aspergillus versicolor", 《ORGANIC LETTERS》 * |
| 李庆欣等: "海洋真菌来源吲哚生物碱类化合物的结构和活性研究", 《热带海洋学报》 * |
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| PB01 | Publication | ||
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20130911 |