CN103356544A - Application of Sarcaboside B in monoamine oxidase inhibitor drug - Google Patents
Application of Sarcaboside B in monoamine oxidase inhibitor drug Download PDFInfo
- Publication number
- CN103356544A CN103356544A CN 201310263867 CN201310263867A CN103356544A CN 103356544 A CN103356544 A CN 103356544A CN 201310263867 CN201310263867 CN 201310263867 CN 201310263867 A CN201310263867 A CN 201310263867A CN 103356544 A CN103356544 A CN 103356544A
- Authority
- CN
- China
- Prior art keywords
- sarcaboside
- monoamine oxidase
- mao
- inhibitor
- application
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention provides application of Sarcaboside B in preparation of monoamine oxidase (MAO) inhibitor. Compared with the existing monoamine oxidase inhibitor, the inhibitory activity and the selecitivty for MAO-A and MAO-B of the monoamine oxidase inhibitor prepared by Sarcaboside B are greatly improved. The application of Sarcaboside B in preparation of monoamine oxidase (MAO) inhibitor is disclosed by the invention for the first time. As the skeleton type is brand new and Sarcaboside B has unexpectedly strong activity for inhibiting monoamine oxidase, the possibility that any enlightenments are given by other compounds does not exist. Sarcaboside B has prominent substantive features and has remarkable progress when being used for treating monoamine oxidase imbalance-associated diseases.
Description
1, technical field
The present invention relates to the application of Sarcaboside B 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 S arcaboside B that the present invention relates to is one and delivered (Li in 2012, X. et al., 2012. Two New-Skeleton Compounds from Sarcandra glabra. Helvetica Chimica Acta 95 (6), 998-1002.) New skeleton compound, this chemical compound has brand-new framework types, there is not at present the report about activity, belong to open first for the purposes of the Sarcaboside 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.
3, summary of the invention
The new purposes that the purpose of this invention is to provide Sarcaboside B 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 S arcaboside B in the preparation oxidase inhibitor, described compound S arcaboside B structure is shown in formula I:
Formula I
Compound S arcaboside 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 Sarcaboside 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.
(4) specific embodiment
The preparation method of compound S arcaboside B involved in the present invention is referring to document (Li, X. et al., 2012. Two New-Skeleton Compounds from Sarcandra glabra. Helvetica Chimica Acta 95 (6), 998-1002.).
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 S arcaboside B tablet involved in the present invention:
Get 20 and digest compound Sarcaboside B, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound S arcaboside B capsule involved in the present invention:
Get 20 and digest compound Sarcaboside 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 S arcaboside 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 S arcaboside B suppresses activity and selective data
Conclusion: Sarcaboside 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.Sarcaboside the application of B in the oxidase inhibitor medicine, described compound S arcaboside B structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201310263867 CN103356544A (en) | 2013-06-27 | 2013-06-27 | Application of Sarcaboside B in monoamine oxidase inhibitor drug |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201310263867 CN103356544A (en) | 2013-06-27 | 2013-06-27 | Application of Sarcaboside B in monoamine oxidase inhibitor drug |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103356544A true CN103356544A (en) | 2013-10-23 |
Family
ID=49359366
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201310263867 Pending CN103356544A (en) | 2013-06-27 | 2013-06-27 | Application of Sarcaboside B in monoamine oxidase inhibitor drug |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103356544A (en) |
-
2013
- 2013-06-27 CN CN 201310263867 patent/CN103356544A/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2612979A1 (en) | Parp modulators and treatment of cancer | |
| EP1971690B1 (en) | Translational dysfunction based therapeutics | |
| Liu et al. | Development of highly potent and specific AKR1C3 inhibitors to restore the chemosensitivity of drug-resistant breast cancer | |
| CN103393643A (en) | Application of Sarcaboside A to monoamine oxidase inhibitor | |
| CN102988397A (en) | Application of Houttuynoid A for preparing monoamine oxidase (MAO) inhibitor medicine | |
| CN103120673A (en) | Application of Aphanamixoid A to preparation of monoamine oxidase (MAO) inhibitor | |
| CN103356544A (en) | Application of Sarcaboside B in monoamine oxidase inhibitor drug | |
| CN103479634B (en) | The application of Lycojaponicumin A in preparation monoamine oxidase inhibitor drug | |
| CN103463036B (en) | The application of Lycojaponicumin B in preparation monoamine oxidase inhibitor drug | |
| CN101703501B (en) | Propargyl imine compounds and use thereof in preparation of MAO inhibitor | |
| CN103463079B (en) | The application of Lycojaponicumin C in preparation monoamine oxidase inhibitor drug | |
| CN103251602A (en) | Application of Myriberine A in preparation of monoamine oxidase (MAO) inhibitor | |
| CN103446096A (en) | Application of Incarviatone A in monoamine oxidase inhibitor drug | |
| CN103520185A (en) | Application of compound in preparing monoamine oxidase MAO inhibitor | |
| CN103356652A (en) | Application of Chukrasone A in preparing MAO (Monoamine Oxidase) inhibitor medicines | |
| CN103356601A (en) | Application of Chukrasone B in preparing MAO (Monoamine Oxidase) inhibitor medicines | |
| CN102988396A (en) | Application of Houttuynoid D in preparation of monoamine oxidase (MAO) inhibitor | |
| CN103393675B (en) | Application of Aphanamgrandiol A in preparing monoamine oxidase (MAO) inhibitor | |
| CN103463010B (en) | Application of fluevirosines A in preparation of monoamine oxidase (MAO) inhibitor | |
| CN103462983B (en) | Application of spirooliganones B in preparation of monoamine oxidase (MAO) inhibitor | |
| CN103463101A (en) | Application of Kadcoccitones A in preparing monoamine oxidase (MAO) inhibitor | |
| CN103285012A (en) | Applications of Aspeverin to the preparation of inhibitors of monoamine oxidase (MAO) | |
| CN103120674A (en) | Application of Eryngiolide A in preparation of MAO (Monoamine Oxidottom) inhibitor | |
| CN103520155A (en) | Application of neonectrolide A in preparing monoamine oxidase (MAO) inhibitor | |
| CN102885825A (en) | Application of Gypensapogenin A in preparation of monoamine oxidase (MAO) inhibitor |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20131023 |