CN103638011A - Application of Artoxanthochromane to monoamine oxidase (MAO) inhibitor - Google Patents
Application of Artoxanthochromane to monoamine oxidase (MAO) inhibitor Download PDFInfo
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- CN103638011A CN103638011A CN201310645642.2A CN201310645642A CN103638011A CN 103638011 A CN103638011 A CN 103638011A CN 201310645642 A CN201310645642 A CN 201310645642A CN 103638011 A CN103638011 A CN 103638011A
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- mao
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- artoxanthochromane
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Abstract
The invention provides application of Artoxanthochromane to a monoamine oxidase (MAO) inhibitor. Compared with an existing MAO inhibitor, the MAO inhibitor has the advantage that the inhibition activity and the selectivity to MAO-A and MAO-B are greatly improved. The application of the Artoxanthochromane to the monoamine oxidase (MAO) inhibitor is firstly disclosed, is high in MAO inhibition activity, has remarkable substantive distinguishing features, and has a remarkable progress in treatment of diseases related to MAO imbalance.
Description
Technical field
The present invention relates to the new purposes of compd A rtoxanthochromane, relate in particular to the application of Artoxanthochromane in preparing monoamine oxidase MAO inhibitor.
Background technology
Since finding that antitubercular agent isoniazid is a kind of potential MAO inhibitor, the research of MAO inhibitor has been become to focus.Iproniazid becomes first MAO inhibitor, because finding that the MAO inhibitor that this class contains hydrazine structure can make P450s inactivation cause hepatotoxicity simultaneously; Studied again and take the MAO inhibitor of the non-hydrazine class that tranylcypromine is representative, this class can be described as the second filial generation.But because " cheese reaction " causes hypertension, limited its application.Therefore it is quite necessary and urgent, developing a kind of more novel, efficient oxidase inhibitor.
The compd A rtoxanthochromane the present invention relates to is one and within 2013, delivers (Horng-Huey Ko, et al., A Novel MonoterpeneStilbene Adduct with a 4, 4-Dimethyl-2, 3-diphenylchromane Skeleton from Artocarpus xanthocarpus.chemistry & biodiversity, 2013 (10): noval chemical compound 1269-1275.), this compound has brand-new framework types, current purposes finds that it can remove oxygen-derived free radicals (Horng-Huey Ko, et al., A Novel MonoterpeneStilbene Adduct with a4, 4-Dimethyl-2, 3-diphenylchromane Skeleton from Artocarpus xanthocarpus.chemistry & biodiversity, 2013 (10): 1269-1275.), it is open first that the purposes of the Artoxanthochromane the present invention relates in preparing monoamine oxidase MAO inhibitor belongs to.
Summary of the invention
The object of the invention is to, according to not finding that it has the present situation of the report of monoamine oxidase MAO inhibitor activity in existing Artoxanthochromane research, provides the application of Artoxanthochromane in preparing monoamine oxidase MAO inhibitor.
Described compd A rtoxanthochromane structure is as shown in formula I:
Formula I
Compd A rtoxanthochromane can detect the inhibition of MAO-A and MAO-B by 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 Concentraton gradient.Get MAO4ul, borate buffer (PH=8.4), 1～100ul BSA(1～100mg/ml), add testing sample solution, mix homogeneously.Then in 0～38 ℃ of water-bath, react 3h, then add probe 2ul(1～100mmol/ml), inhibitor ultimate density 0～10-2mmol/l, mixture reacts 1～24h again in 0～38 ℃ of water-bath, with global function spectrofluorophotometer (λ ex/ λ em=365/460nm), detects.According to the data obtained, calculate IC50.
It is open first that the purposes of the Artoxanthochromane the present invention relates in preparing monoamine oxidase, MAO (MAO) inhibitor belongs to, because framework types belongs to brand-new framework types, and it is strong for monoamine oxidase inhibitory activity, possess outstanding substantive distinguishing features, the treatment for monoamine oxidase, MAO imbalance relevant disease simultaneously obviously has significant progress.
The specific embodiment
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
The preparation method of compd A rtoxanthochromane involved in the present invention is referring to document (Horng-Huey Ko, et al., A Novel MonoterpeneStilbene Adduct with a4,4-Dimethyl-2,3-diphenylchromane Skeleton from Artocarpus xanthocarpus.chemistry & biodiversity, 2013 (10): 1269-1275.), prepare according to the method described above compd A rtoxanthochromane.
Embodiment 1: the preparation of compd A rtoxanthochromane tablet involved in the present invention:
Get 5 and digest compound Artoxanthochromane and add 195 grams, dextrin, mix, routine is pressed into 1000.
Embodiment 2: the preparation of compd A rtoxanthochromane capsule involved in the present invention:
Get 5 and digest compound Artoxanthochromane and add 195 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Experimental example 1: compd A rtoxanthochromane detects the inhibition activity to MAO-A and MAO-B by 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 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, then add probe 7-(the amino propoxyl group of 3-) coumarin 2ul(50mmol/ml), inhibitor ultimate density 0～10-2mmol/l, mixture reacts 12h again in 30 ± 5 ℃ of water-baths, with global function spectrofluorophotometer (λ ex/ λ em=365/460nm), detects.According to the data obtained, calculate IC50, the results are shown in Table 1.
Table 1: compd A rtoxanthochromane suppresses activity and selective data
Conclusion: Artoxanthochromane can significantly suppress the activity of MAO, and selectivity is good, can be for the lack of proper care treatment of relevant disease of monoamine oxidase, MAO.
Claims (1)
- The application of 1.Artoxanthochromane in monoamine oxidase MAO inhibitor, described compd A rtoxanthochromane structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310645642.2A CN103638011A (en) | 2013-12-04 | 2013-12-04 | Application of Artoxanthochromane to monoamine oxidase (MAO) inhibitor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310645642.2A CN103638011A (en) | 2013-12-04 | 2013-12-04 | Application of Artoxanthochromane to monoamine oxidase (MAO) inhibitor |
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| Publication Number | Publication Date |
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| CN103638011A true CN103638011A (en) | 2014-03-19 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310645642.2A Pending CN103638011A (en) | 2013-12-04 | 2013-12-04 | Application of Artoxanthochromane to monoamine oxidase (MAO) inhibitor |
Country Status (1)
| Country | Link |
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| CN (1) | CN103638011A (en) |
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2013
- 2013-12-04 CN CN201310645642.2A patent/CN103638011A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| HORNG-HUEY KO，ET AL.: "A Novel Monoterpene-Stilbene Adduct with a 4,4-Dimethyl-2,3-diphenylchromane Skeleton from Artocarpus xanthocarpus", 《CHEMISTRY & BIODIVERSITY》 * |
| 张颖等: "帕金森病神经保护策略", 《中国老年学杂志》 * |
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Application publication date: 20140319 |