CN103372016A - Application of Chukrasone A in preparation of medicines for lowering blood glucose - Google Patents
Application of Chukrasone A in preparation of medicines for lowering blood glucose Download PDFInfo
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- CN103372016A CN103372016A CN2013102803397A CN201310280339A CN103372016A CN 103372016 A CN103372016 A CN 103372016A CN 2013102803397 A CN2013102803397 A CN 2013102803397A CN 201310280339 A CN201310280339 A CN 201310280339A CN 103372016 A CN103372016 A CN 103372016A
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Abstract
The invention discloses an application of Chukrasone A in the preparation of anti-diabetic medicines. The application of the Chukrasone A has the advantages of providing bran-new choice and idea for the existing anti-diabetic medicines, widening the choice field of the anti-diabetic medicines and contributing to the development of the technical field. The application of the Chukrasone A is proven to have an obvious anti-diabetic effect. The Chukrasone A is a compound with a definite chemical structure. The application of the Chukrasone A in the preparation of the anti-diabetic medicines is disclosed for the first time. As the skeleton type of the Chukrasone A belongs to a bran-new skeleton type and the Chukrasone A has unexpected strong activity on the prevention and treatment of diabetes, 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 treating the diabetes.
Description
Technical field
The present invention relates to a kind of new purposes of Chukrasone A, the specifically application of Chukrasone A in the preparation antidiabetic medicine.
Background technology
Diabetes (diabetes mellitus) are one of current modal chronic diseases, type 2 diabetes mellitus (Type II diabetes mellitus wherein, be again non-insulin-dependent diabetes mellitus, non-insulin-depentdiabetes mellitus, NIDDM) account for more than 90% of diabetics.Diabetes all are day by day serious problems in developed country and developing country, and it has caused serious and costly consequence, comprise blind, heart disease and nephropathy etc.According to estimates, from 2000 to the year two thousand fifty, the number of whole world diabetics will increase by 165%.According to the statistics of IDF, at present in state-owned 4.3% population suffer from diabetes, patient's number will break through 5,000 ten thousand in following 20 years.Diabetes are second killers in the modern disease, it is only second to cancer to the harm of human body, human health in serious threat, and present diabetes have the tendency of extension and rejuvenation, how to prevent that diabetes from having become the large problem that present the world of medicine pays close attention to.
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 treatment antidiabetic medicine, because framework types belongs to brand-new framework types, and its control diabetic activity is unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for the treatment of simultaneously anti-diabetic and obviously have significant progress.
Summary of the invention
The objective of the invention is provides a kind of new way for the technical field of existing preparation antidiabetic medicine, and the application of Chukrasone A in the preparation antidiabetic medicine is provided.
The structural formula of Chukrasone A such as formula I:
Formula I
Technical scheme of the present invention is: the application of Chukrasone A specifically is applied to prepare antidiabetic medicine.
The invention has the beneficial effects as follows:
1) the present invention has widened diabetes and has selected the field for present antidiabetic medicine provides a kind of brand-new selection and thinking, also contributes for the development of this technical field; 2) application of Chukrasone A of the present invention has been proved to be significant anti-diabetic effect.
The most important thing is: the present invention carries out the blood sugar lowering experiment of laboratory animal to Chukrasone A, at lasting gavage fat milk rat is produced on the basis of insulin resistant, use low dose of streptozotocin damage beta Cell of islet, cause rat blood sugar to raise, institute makes animal model and type 2 diabetes mellitus is similar.After rat model of type 2 diabetes mellitus gives Chukrasone A treatment, Chukrasone A is high, in and the blood glucose value and the comparison of model group blood glucose value of low dose group, also has significant difference (P＜0.01), Chukrasone A is high, in and the blood glucose value before and after the low dose group administration relatively, also have significant difference (P＜0.01), illustrate that Chukrasone A has good hypoglycemic activity to experimental type 2 diabetes mellitus.
The purposes of the Chukrasone A that the present invention relates in preparation treatment antidiabetic medicine belongs to open first, because framework types belongs to brand-new framework types, and its control diabetic activity is unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for the treatment of simultaneously anti-diabetic and obviously have 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 Chukrasone A is on the impact of rat model of type 2 diabetes mellitus
1, animal grouping
Healthy Wistar rat (SPF level), male, body weight 180-220g(is provided by Nanfang Medical Univ's Experimental Animal Center), the feed of freely drinking water, be divided at random Normal group and modeling group, the modeling group is set up model as follows, the model group animal is divided at random high, normal, basic group of model control group, positive drug gliclazide group, Chukrasone A after the modeling success, 1 week of according to the form below successive administration again.
Administration time and dosage see Table 1:
The grouping of table 1 Chukrasone A effect experiment animal
| Group | Number of animals (only) | Dosage (mg/kgBW) |
| Normal group | 12 | |
| Model control group | 12 | |
| The positive drug group | 12 | 35.5 |
| Low dose group | 12 | 0.16 |
| Middle dosage group | 12 | 0.5 |
| High dose group | 12 | 1.5 |
2, rat model preparation
Normal rats gavage every day distilled water, high fat group rat sooner or later gavage self-control every day fat milk (1ml/100gBW).Continuously the gavage fat milk is after 2 weeks, and water 24h is can't help in the animal fasting, 10 tail vein injection salines of blank group, the equal tail vein injection 30mg/kgBW of all the other rats streptozotocin (below be abbreviated as STZ) solution (before use preparation).Behind the administration 48h, water 12h is can't help in fasting, gets blood every 3 hours eyeball rear vein beards, according to blood sugar detection test kit time-and-motion study fasting blood sugar, and METHOD FOR CONTINUOUS DETERMINATION 3 times, fasting blood sugar 〉=16.7mmol/L's is modeling success rat.
3, the mensuration of blood glucose
After the last administration, water 12h is can't help in the animal fasting, and the eyeball rear vein beard is got blood, measures respectively blood glucose value according to the method for test kit.Adopt the SPSS13.0 statistical software, analyze and respectively organize the situation of change of blood glucose value.
4, Chukrasone A is on the impact of rat model of type 2 diabetes mellitus blood glucose
Experimental result sees Table 2, and as known from Table 2, behind the injection STZ, rat blood sugar rises, and fasting blood sugar 〉=16.7mmol/L behind the 72h illustrates the diabetes model success.After the administration, the positive drug group, Chukrasone A is high, in and the blood glucose value and the comparison of model group blood glucose value of low dose group, significant difference (P＜0.01) is all arranged.
Each is organized before the administration, and the T check of blood glucose shows behind the blood glucose and administration, the positive drug group, Chukrasone A is high, in and the blood glucose value before and after the low dose group administration relatively, have significant difference (P＜0.01).Above result shows that Chukrasone A can reduce the blood glucose of rat model of type 2 diabetes mellitus.
Table 2 experimental result
| Group | Number of animals (only) | Blood glucose value before the administration | Blood glucose value after the administration |
| Normal group | 10 | 5.6±0.24 | 5.24±0.37 |
| Model control group | 9 | 13.04±2.25 | 31.15±2.46 |
| The positive drug group | 9 | 31.35±2.45 | 18.76±2.35** △△ |
| Low dose group | 8 | 31.96±2.27 | 23.67±2.24** △△ |
| Middle dosage group | 10 | 32.95±1.97 | 19.64±2.67** △△ |
| High dose group | 9 | 35.36±2.56 | 19.85±3.06** △△ |
* p＜0.05vs model group * * p＜0.01vs model group
△P＜0.05vs is on the same group before the administration
△ △P＜0.01vs is on the same group before the administration
Conclusion: Chukrasone A can significantly reduce the blood glucose of type 2 diabetes mellitus animal model, can be used for preparing antidiabetic medicine.
Claims (1)
1.Chukrasone the application of A in the blood sugar lowering medicine, described Compound C hukrasone A structure as
Formula IShown in:
Formula I.
Priority Applications (1)
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| CN2013102803397A CN103372016A (en) | 2013-07-04 | 2013-07-04 | Application of Chukrasone A in preparation of medicines for lowering blood glucose |
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| CN2013102803397A CN103372016A (en) | 2013-07-04 | 2013-07-04 | Application of Chukrasone A in preparation of medicines for lowering blood glucose |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1980923A (en) * | 2004-04-13 | 2007-06-13 | 安克进药物公司 | Polycyclic pyridines as potassium ion channel modulators |
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2013
- 2013-07-04 CN CN2013102803397A patent/CN103372016A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1980923A (en) * | 2004-04-13 | 2007-06-13 | 安克进药物公司 | Polycyclic pyridines as potassium ion channel modulators |
Non-Patent Citations (1)
| Title |
|---|
| LIU,H.B.ET AL.: "Chukrasone A and B:Potential Kv1.2Potassium Channel Blockers with New Skeletons from Chukrasia tabularis.", 《ORGANIC LETTERS》, vol. 14, no. 17, 31 December 2012 (2012-12-31), pages 4438 - 4441 * |
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Application publication date: 20131030 |