CN102988396A - Application of Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor - Google Patents
Application of Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor Download PDFInfo
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- CN102988396A CN102988396A CN2012104697754A CN201210469775A CN102988396A CN 102988396 A CN102988396 A CN 102988396A CN 2012104697754 A CN2012104697754 A CN 2012104697754A CN 201210469775 A CN201210469775 A CN 201210469775A CN 102988396 A CN102988396 A CN 102988396A
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Abstract
The invention provides an application of Houttuynoid D in preparation of a monoamine oxidase (MAO) inhibitor. Compared with that of the existing MAO inhibitor, the inhibitory activity and selectivity on MAO-A and MAO-B are greatly improved. The application of Houttuynoid D in preparation of the MAO inhibitor is disclosed for the first time, and because the framework type belongs to a novel framework type, the inhibitory activity on the MAO is unexpectedly high, the possibility that other compounds give enlightenment is avoided, and the Houttuynoid D has outstanding substantial characteristics and has obvious progress in treatment of MAO disorder related diseases.
Description
1, technical field
The present invention relates to the application of Houttuynoid D 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 quite necessary and urgent.
The compound H outtuynoid D that the present invention relates to is one and delivered (Cai in 2012, J. Y. et al., 2012. Houttuynoid D, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to DEF(Cai, J. Y. et al., 2012. Houttuynoid D, 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 Houttuynoid D 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 chemical compounds, possess outstanding substantive distinguishing features, the treatment that is used for simultaneously monoamine oxidase, MAO imbalance relevant disease obviously has significant progress.
3, summary of the invention
The new purposes that the purpose of this invention is to provide Houttuynoid D chemical compound, this chemical compound is good to the active height of the inhibition of MAO, selectivity.
The technical solution used in the present invention is:
The application of compound H outtuynoid D in the preparation oxidase inhibitor, described compound H outtuynoid D structure is shown in formula I:
Formula I
Compound H outtuynoid D 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 in 0 ~ 38 ℃ of water-bath, react 3h, 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 Houttuynoid D 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 simultaneously monoamine oxidase, MAO imbalance relevant disease obviously has significant progress.
(4) specific embodiment
The preparation method of compound H outtuynoid D involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Houttuynoid D, 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 compound H outtuynoid D tablet involved in the present invention:
Get 20 and digest compound Houttuynoid D, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid D capsule involved in the present invention:
Get 20 and digest compound Houttuynoid D, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Compound H outtuynoid D 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, 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 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: compound H outtuynoid D suppresses activity and selective data
Conclusion: Houttuynoid D 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.Houttuynoid the application of D in preparation oxidase inhibitor medicine, described compound H outtuynoid D structure is shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012104697754A CN102988396A (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012104697754A CN102988396A (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor |
Publications (1)
| Publication Number | Publication Date |
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| CN102988396A true CN102988396A (en) | 2013-03-27 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2012104697754A Withdrawn CN102988396A (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor |
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| Country | Link |
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| CN (1) | CN102988396A (en) |
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2012
- 2012-11-19 CN CN2012104697754A patent/CN102988396A/en not_active Withdrawn
Non-Patent Citations (3)
| Title |
|---|
| SHAO-DAN CHEN ET AL.: "Houttuynoids A-E,anti-herpes simplex virus active flavonoids with novel skeletons from houttuynia cordata", 《ORGANIC LETTERS》 * |
| 许二平: "《抑郁症中西医诊疗学》", 30 June 2010, 军事医学科学出版社 * |
| 龚乃超: "鱼腥草黄酮类化合物的提取纯化记抗抑郁作用的研究", 《中国优秀硕士学位论文全文数据库工程科技Ⅰ辑》 * |
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Application publication date: 20130327 |