CN106265687A - Friedolanostanes application in preparation monoamine oxidase MAO inhibitor - Google Patents
Friedolanostanes application in preparation monoamine oxidase MAO inhibitor Download PDFInfo
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- CN106265687A CN106265687A CN201610800711.6A CN201610800711A CN106265687A CN 106265687 A CN106265687 A CN 106265687A CN 201610800711 A CN201610800711 A CN 201610800711A CN 106265687 A CN106265687 A CN 106265687A
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- mao
- friedolanostanes
- monoamine oxidase
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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- Pharmacology & Pharmacy (AREA)
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- Life Sciences & Earth Sciences (AREA)
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- General Health & Medical Sciences (AREA)
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention provides Friedolanostanes application in preparing monoamine oxidase, MAO (MAO) inhibitor, compared with existing oxidase inhibitor, its inhibitory activity, MAO A and MAO B selectivity are improved a lot, Friedolanostanes purposes in preparing monoamine oxidase, MAO (MAO) inhibitor belongs to first public, and it is strong for monoamine oxidase inhibitory activity, possessing prominent substantive distinguishing features, the treatment being simultaneously used for monoamine oxidase, MAO dysfunction obviously has the most progressive.
Description
Technical field
The present invention relates to the new application of compound Friedolanostanes, particularly relate to Friedolanostanes in system
Application in standby monoamine oxidase MAO inhibitor.
Background technology
Since finding that antitubercular agent isoniazid is a kind of potential MAO inhibitor, the research to MAO inhibitor becomes
Focus.Iproniazid becomes first MAO inhibitor, because finding that this kind of MAO inhibitor containing hydrazine structure can make simultaneously
P450s inactivates and causes hepatotoxicity；Have studied again the MAO inhibitor of non-hydrazine with tranylcypromine as representative, this
Class can be described as the second filial generation.But because " cheese reaction " causes hypertension, limit its application.Therefore, development one is more
It is reasonably necessary and urgent for oxidase inhibitor novel, efficient.
The compound Friedolanostanes that the present invention relates to be one within 2013, deliver (Saranyoo Klaiklay,
et al.,Friedolanostanes and xanthones from the twigs of Garcinia
Hombroniana.Phytochemistry, 85 (2013) 161 166.) noval chemical compound, this compound has brand-new skeleton
Type, current purposes merely facilitates germination, (Saranyoo Klaiklay, et al., Friedolanostanes
and xanthones from the twigs of Garcinia hombroniana.Phytochemistry,85(2013)
161 166.) Friedolanostanes that, the present invention relates to purposes in preparation monoamine oxidase MAO inhibitor belongs to first
Secondary disclosure.
Summary of the invention
Do not find that it has monoamine oxidase, MAO in it is an object of the invention to study according to existing Friedolanostanes
The present situation of the report of MAO inhibitor activity, it is provided that Friedolanostanes is in preparation monoamine oxidase MAO inhibitor
Application.
Described compound Friedolanostanes structure is as shown in formula I:
Compound Friedolanostanes can detect the inhibitory activity to MAO-A and MAO-B by the method for fluorescent probe,
Described method follows the steps below: be dissolved in DMSO by sample to be measured, is made into and a series of has Concentraton gradient
Sample.Take MAO 4ul, borate buffer (PH=8.4), 1～100ul BSA (1～100mg/ml), add testing sample molten
Liquid, mix homogeneously.Then reacting 3h in 0～38 DEG C of water-bath, be subsequently adding probe 2ul (1～100mmol/ml), inhibitor is
Final concentration 0～10-2mmol/l, mixture reacts 1～24h again in 0～38 DEG C of water-bath, uses global function spectrofluorophotometer
(λ ex/ λ em=365/460nm) detects.IC50 is calculated according to the data obtained.
The Friedolanostanes that the present invention relates to purposes in preparing monoamine oxidase, MAO (MAO) inhibitor belongs to first
Secondary disclosure, owing to framework types belongs to brand-new framework types, and it must be expected not for monoamine oxidase inhibitory activity is strong
Arrive, there is not the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for monoamine oxidation
The treatment of enzyme dysfunction obviously has the most progressive.
Detailed description of the invention
The preparation method of compound Friedolanostanes involved in the present invention sees document (Saranyoo
Klaiklay, et al., Friedolanostanes and xanthones from the twigs of Garcinia
hombroniana.Phytochemistry,85(2013)161–166.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by concrete real
Execute any restriction of example, but be defined in the claims.
Embodiment 1: the preparation of compound Friedolanostanes tablet involved in the present invention:
Taking 5 g of compound Friedolanostanes and add 195 grams of dextrin, mixing, routine is pressed into 1000.
Embodiment 2: the preparation of compound Friedolanostanes capsule involved in the present invention:
Take 5 g of compound Friedolanostanes and add starch 195 grams, mixing, encapsulated make 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
The method detection of the compound Friedolanostanes fluorescent probe inhibitory activity to MAO-A and MAO-B, institute
The method stated follows the steps below:
Sample to be measured is dissolved in DMSO, is made into a series of sample with Concentraton gradient.Take MAO (10mg/ml)
4ul, borate buffer (PH=8.4), 50ul BSA (50mg/ml), add testing sample solution, mix homogeneously, 30～38
Reacting 3h in DEG C water-bath, be subsequently adding probe 7-(3-aminopropan epoxide) coumarin 2ul (50mmol/ml), inhibitor is the denseest
Degree 0～10-2mmol/l, mixture reacts 12h again in 30 ± 5 DEG C of water-baths, with global function spectrofluorophotometer (λ ex/ λ em
=365/460nm) detect.Calculate IC50 according to the data obtained, the results are shown in Table 1.
Table 1: compound Friedolanostanes inhibitory activity and selective data
Conclusion: Friedolanostanes can significantly inhibit the activity of MAO, and selectivity is good, may be used for monoamine oxygen
Change the treatment of enzyme dysfunction.
Claims (1)
1.Friedolanostanes application in monoamine oxidase MAO inhibitor, described compound
Friedolanostanes structure is as shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610800711.6A CN106265687A (en) | 2016-09-03 | 2016-09-03 | Friedolanostanes application in preparation monoamine oxidase MAO inhibitor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610800711.6A CN106265687A (en) | 2016-09-03 | 2016-09-03 | Friedolanostanes application in preparation monoamine oxidase MAO inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106265687A true CN106265687A (en) | 2017-01-04 |
Family
ID=57709603
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610800711.6A Pending CN106265687A (en) | 2016-09-03 | 2016-09-03 | Friedolanostanes application in preparation monoamine oxidase MAO inhibitor |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106265687A (en) |
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2016
- 2016-09-03 CN CN201610800711.6A patent/CN106265687A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170104 |