CN103356601A - Application of Chukrasone B in preparing MAO (Monoamine Oxidase) inhibitor medicines - Google Patents
Application of Chukrasone B in preparing MAO (Monoamine Oxidase) inhibitor medicines Download PDFInfo
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- CN103356601A CN103356601A CN 201310279783 CN201310279783A CN103356601A CN 103356601 A CN103356601 A CN 103356601A CN 201310279783 CN201310279783 CN 201310279783 CN 201310279783 A CN201310279783 A CN 201310279783A CN 103356601 A CN103356601 A CN 103356601A
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- mao
- chukrasone
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Abstract
The invention relates to an application of Chukrasone B in preparing MAO (Monoamine Oxidase) inhibitor medicines. Compared with existing MAO inhibitors, the MAO inhibitor provided by the invention is greatly improved in inhibitory activity and selectivity to MAO-A and MAO-B. The use of the Chukrasone B in preparing MAO inhibitor medicines provided by the invention is disclosed for the first time. As the framework type belongs to a brand-new framework type, and the inhibitory activity of the Chukrasone B to MAO is unimaginably strong, the probability of giving any enlightenment by other compounds does not exist. The Chukrasone B has remarkable substantial characteristics and meanwhile has a remarkable progress for treating diseases associated to MAO disorder.
Description
Technical field
The present invention relates to the application of Chukrasone B in preparation monoamine oxidase, MAO (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; 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 C hukrasone B that the present invention relates to is one and delivered (Liu in 2012, H. B. et al., 2012. Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis. Organic Letters 14 (17), 4438 – 4441.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to potassium-channel and suppresses active (Liu, H. B. et al., 2012. Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis. Organic Letters 14 (17), 4438 – 4441.), belong to open first for the purposes of the Chukrasone B 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.
Summary of the invention
The new purposes that the purpose of this invention is to provide Chukrasone B chemical compound, this chemical compound is high to the inhibition activity of MAO, selectivity good.
The technical solution used in the present invention is:
The application of Compound C hukrasone B in the preparation oxidase inhibitor, described Compound C hukrasone B structure is shown in formula I:
Formula I
Compound C hukrasone B 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 Chukrasone B 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.
The specific embodiment
The preparation method of Compound C hukrasone B involved in the present invention is referring to document (Liu, H. B. et al., 2012. Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis. Organic Letters 14 (17), 4438 – 4441.).
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 C hukrasone B tablet involved in the present invention:
Get 20 and digest compound Chukrasone B, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of Compound C hukrasone B capsule involved in the present invention:
Get 20 and digest compound Chukrasone B, 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 C hukrasone B 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 C hukrasone B suppresses activity and selective data
Conclusion: Chukrasone B 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.Chukrasone the application of B in the oxidase inhibitor medicine, described Compound C hukrasone B structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201310279783 CN103356601A (en) | 2013-07-04 | 2013-07-04 | Application of Chukrasone B in preparing MAO (Monoamine Oxidase) inhibitor medicines |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201310279783 CN103356601A (en) | 2013-07-04 | 2013-07-04 | Application of Chukrasone B in preparing MAO (Monoamine Oxidase) inhibitor medicines |
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| CN103356601A true CN103356601A (en) | 2013-10-23 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201310279783 Pending CN103356601A (en) | 2013-07-04 | 2013-07-04 | Application of Chukrasone B in preparing MAO (Monoamine Oxidase) inhibitor medicines |
Country Status (1)
| Country | Link |
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| CN (1) | CN103356601A (en) |
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2013
- 2013-07-04 CN CN 201310279783 patent/CN103356601A/en active Pending
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
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Application publication date: 20131023 |