CN103372020A - Application of Chukrasone A in preparation of medicines for promoting insulin secretion - Google Patents
Application of Chukrasone A in preparation of medicines for promoting insulin secretion Download PDFInfo
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- CN103372020A CN103372020A CN2013102808210A CN201310280821A CN103372020A CN 103372020 A CN103372020 A CN 103372020A CN 2013102808210 A CN2013102808210 A CN 2013102808210A CN 201310280821 A CN201310280821 A CN 201310280821A CN 103372020 A CN103372020 A CN 103372020A
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- chukrasone
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- insulin secretion
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Abstract
The invention belongs to the pharmaceutical field, and discloses an application of Chukrasone A in the preparation of medicines for promoting insulin secretion. The application of the Chukrasone A in the preparation of the medicines for promoting the insulin secretion is disclosed by the invention for the first time. As the skeleton type of the Chukrasone A belongs to a bran-new skeleton type and the Chukrasone A has an unexpected strong promotion effect on the insulin secretion, the possibility that other compounds provide revelation does not exist. The Chukrasone A has prominently substantial characteristics and meanwhile has remarkably progressive significance when being used for preventing and treating type 2 diabetes mellitus.
Description
Technical field
The invention belongs to pharmaceutical field, relate to the application of Chukrasone A in preparation Insulin-secreting agent thing.
Background technology
Type 2 diabetes mellitus is a kind of disease that has a strong impact on health and quality of life, not only involves at present the adult of western countries 6%, and its morbidity is tending towards rejuvenation, and just with 6% annual rate of growth rapid growth.Its hazardness and the sickness rate that constantly rises in children population have caused various countries scholars' extensive concern, and become an important research direction in the medical research field.
The Compound C hukrasone A 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 A that the present invention relates in preparation Insulin-secreting agent thing, because framework types belongs to brand-new framework types, and its insulin secretion accelerating is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, the control that is used for simultaneously type 2 diabetes mellitus obviously has significant progress.
Summary of the invention
The objective of the invention is to test by following technical measures: the application of Chukrasone A in preparation Insulin-secreting agent thing.
Beneficial effect of the present invention:
Find that Chukrasone A does not affect the cell viability of islet cells strain RINm5F, expression Chukrasone A does not have toxic action to cell.Chukrasone A is 10
-10, 10
-11, 10
-12Insulin secretion ability to the islet cells strain in the M scope has facilitation, and this effect has concentration and time-dependent trend.
Described Compound C hukrasone A structure is shown in formula I:
Formula I
The purposes of the Chukrasone A that the present invention relates in preparation Insulin-secreting agent thing belongs to open first, because framework types belongs to brand-new framework types, and its insulin secretion accelerating is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, the control that is used for simultaneously type 2 diabetes mellitus obviously has significant progress.
The specific embodiment:
The preparation method of Compound C hukrasone A 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 A tablet involved in the present invention:
Get 20 and digest compound Chukrasone A, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of Compound C hukrasone A capsule involved in the present invention:
Get 20 and digest compound Chukrasone A, 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.
Experimental example 1
1, Chukrasone A determining the safety range of islet cells strain RINm5F
The RINm5F cell is pressed every hole 2 * 10
4The concentration of individual cell is inoculated in 96 orifice plates, in 37 ℃ of 5%CO
2Cultivate in the incubator when cell reaches 80% density, use Chukrasone A(final concentration 0,10
-8, 10
-9, 10
-10, 10
-11, 10
-12M) (1M=1mol/L, lower same) adopts mtt assay to detect cell viability to cytositimulation after 3 hours.At first adding MTT liquid.Make the MTT final concentration reach 0.5mg/ml, and hatched 2 hours at 37 ℃.Suck supernatant, add DMSO dissolving crystal, survey absorbance at the 570nm place.The result is: not with Chukrasone A MTT value=0.2463 ± 0.01314; Chukrasone A 10
-8Mol/L MTT value=0.2474 ± 0.0815; Chukrasone A 10
-9Mol/L MTT value=0.2476 ± 0.01063; Chukrasone A 10
-10Mol/L MTT value=0.2474 ± 0.05; Chukrasone A 10
-11Mol/L MTT value=0.2475 ± 0.0746; Chukrasone A 10
-12Mol/L MTT value=0.2453 ± 0.07424.Not having significant difference, P between each group〉0.05 explanation Chukrasone A do not affect cell viability.The result shows that Chukrasone A does not affect the vigor of cell in each concentration.
2, Chukrasone A is on the impact of islet cells secretory function
The RINm5F cell is inoculated in 6 orifice plates, reaches 3 * 10 at cell
5Individual/as during the hole, to suck supernatant and wash three times with PBS, use KRB buffer (128.8mM NaCl, 4.8mM KCl, 1.2mM KH
2PO
4, 1.2mM MgSO
4, 1.0mM CaCl
2, 5.0mM HEPES, 0.1% hyclone, 2.8mM glucose), in buffer, add Chukrasone A 10
-12M stimulated 2 hours.Experiment is got supernatant after finishing, and uses insulin ELISA test kit (Mercodia AB Sweden) to detect insulin in the supernatant in the centrifugal removal supernatant behind the cell.The result shows that Chukrasone A stimulates the free and concentration dependence trend of secretion of insulin, sees Table respectively 1,2.
Table 1 10
-12The Chukrasone A of M stimulates different time on the impact of insulin secretion
Compare * P＜0.05 with matched group.
The Chukrasone A of table 2 variable concentrations stimulates the impact on insulin secretion in 2 hours
Compare * P＜0.05 with matched group.
Conclusion: Chukrasone A can the significant stimulation insulin secretion, can be used for preparation treatment diabetes medicament.
Claims (1)
1.Chukrasone the application of A in the Insulin-secreting agent thing, described Compound C hukrasone A structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102808210A CN103372020A (en) | 2013-07-04 | 2013-07-04 | Application of Chukrasone A in preparation of medicines for promoting insulin secretion |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102808210A CN103372020A (en) | 2013-07-04 | 2013-07-04 | Application of Chukrasone A in preparation of medicines for promoting insulin secretion |
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| CN103372020A true CN103372020A (en) | 2013-10-30 |
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|---|---|---|---|
| CN2013102808210A Pending CN103372020A (en) | 2013-07-04 | 2013-07-04 | Application of Chukrasone A in preparation of medicines for promoting insulin secretion |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1101349A (en) * | 1992-07-25 | 1995-04-12 | 史密丝克莱恩比彻姆有限公司 | Novel compounds |
| CN1244193A (en) * | 1997-01-23 | 2000-02-09 | 山之内制药株式会社 | Novel amide derivatives and medicinal compositions thereof |
-
2013
- 2013-07-04 CN CN2013102808210A patent/CN103372020A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1101349A (en) * | 1992-07-25 | 1995-04-12 | 史密丝克莱恩比彻姆有限公司 | Novel compounds |
| CN1244193A (en) * | 1997-01-23 | 2000-02-09 | 山之内制药株式会社 | Novel amide derivatives and medicinal compositions thereof |
Non-Patent Citations (1)
| Title |
|---|
| HONG-BING LIU等: "Chukrasones A and B: Potential Kv1.2 Potassium channel blockers with new skeletons from chukrasia tabularis", 《ORGANIC LETTERS》 * |
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Application publication date: 20131030 |