CN103356592B - Chukrasone B reduces the application in hypoglycemic medicament in preparation - Google Patents
Chukrasone B reduces the application in hypoglycemic medicament in preparation Download PDFInfo
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- CN103356592B CN103356592B CN201310278053.5A CN201310278053A CN103356592B CN 103356592 B CN103356592 B CN 103356592B CN 201310278053 A CN201310278053 A CN 201310278053A CN 103356592 B CN103356592 B CN 103356592B
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Abstract
Do you the invention discloses a kind of Chukrasone? B is preparing the application in antidiabetic medicine.The present invention is that current antidiabetic medicine provides a kind of brand-new selection and thinking, has widened the selection field of antidiabetic medicine, also for the development of this technical field contributes; Chukrasone of the present invention? the application of B has been proved to be significant anti-diabetic effect; What the present invention selected is the compound with clear and definite chemical constitution.The Chukrasone that the present invention relates to? the purposes of B in preparation treatment antidiabetic medicine belongs to first public, because framework types belongs to brand-new framework types, and its control diabetic activity is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, be used for the treatment of anti-diabetic simultaneously and obviously there is significant progress.
Description
Technical field
The present invention relates to a kind of novelty teabag of ChukrasoneB, specifically ChukrasoneB is preparing the application in antidiabetic medicine.
Background technology
Diabetes (diabetesmellitus) are one of current modal chronic diseases, wherein type 2 diabetes mellitus (Type II diabetesmellitus, be non-insulin-dependent diabetes mellitus again, non-insulin-depentdiabetesmellitus, NIDDM) account for more than 90% of diabetics.Diabetes are all day by day serious problems in developed country and developing country, and it causes serious and costly consequence, comprises 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, the population of state-owned 4.3% suffers from diabetes, and in following 20 years, the number of patient is by breakthrough 5,000 ten thousand.Diabetes are second killers in modern diseases, it is only second to cancer to the harm of human body, the health of the mankind in serious threat, and present diabetes have extension and the tendency of rejuvenation, the large problem how preventing from diabetes from having become current the world of medicine paying close attention to.
The Compound C hukrasoneB that the present invention relates to is one and delivers (Liu in 2012, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (17), 4438 – 4441.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to potassium-channel inhibit activities (Liu, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (17), 4438 – 4441.), the purposes of the ChukrasoneB that the present invention relates in preparation treatment antidiabetic medicine is belonged to first public, because framework types belongs to brand-new framework types, and its control diabetic activity is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, be used for the treatment of anti-diabetic simultaneously and obviously there is significant progress.
Summary of the invention
The object of the invention is, for the existing technical field preparing antidiabetic medicine provides a kind of new way, to provide ChukrasoneB preparing the application in antidiabetic medicine.
The structural formula of ChukrasoneB is as formula I:
Technical scheme of the present invention is: the application of ChukrasoneB, is specifically applied to and prepares antidiabetic medicine.
The invention has the beneficial effects as follows:
1) the present invention is that current antidiabetic medicine provides a kind of brand-new selection and thinking, has widened diabetes and has selected field, also for the development of this technical field contributes; 2) application of ChukrasoneB 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 ChukrasoneB, rat is made to produce on the basis of insulin resistant at lasting gavage fat milk, apply low dose of streptozotocin impaired isle β cell, 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 ChukrasoneB treatment, ChukrasoneB is high, in and the blood glucose value of low dose group compare with model group blood glucose value, also there is significant difference (P<0.01), ChukrasoneB is high, in and blood glucose value before and after low dose group administration compare, also there is significant difference (P<0.01), illustrate that ChukrasoneB has good hypoglycemic activity to experimental type 2 diabetes mellitus.
The purposes of the ChukrasoneB that the present invention relates in preparation treatment antidiabetic medicine belongs to first public, because framework types belongs to brand-new framework types, and its control diabetic activity is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, be used for the treatment of anti-diabetic simultaneously and obviously there is significant progress.
Detailed description of the invention
The preparation method of Compound C hukrasoneB involved in the present invention is see document (Liu, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (17), 4438 – 4441.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of Compound C hukrasoneB tablet involved in the present invention:
Get 20 g of compound ChukrasoneB, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of Compound C hukrasoneB capsule involved in the present invention:
Get 20 g of compound ChukrasoneB, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1ChukrasoneB 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 (being provided by Nanfang Medical Univ's Experimental Animal Center), freely to drink water feed, be divided into Normal group and modeling group at random, modeling group Modling model as follows, is divided into model control group, positive drug gliclazide group, high, normal, basic group of ChukrasoneB, according to the form below successive administration 1 week after modeling success more at random by model group animal.
Administration time and dosage are in table 1:
The grouping of table 1ChukrasoneB effect experiment animal
| Group | Number of animals (only) | Dosage (mg/kgBW) |
| Normal group | 12 |
| Model control group | 12 | |
| 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, the high fat group rat every day of gavage self-control fat milk (1ml/100gBW) sooner or later.Continuous gavage fat milk is after 2 weeks, water 24h is can't help in animal fasting, blank group 10 tail vein injection salines, all the other rats equal tail vein injection 30mg/kgBW streptozotocin (hereinafter abbreviated as STZ) solution (prepared before use).After administration 48h, water 12h is can't help in fasting, gets blood every 3 hours eyeball rear vein beards, and according to blood sugar detection test kit time-and-motion study fasting blood sugar, METHOD FOR CONTINUOUS DETERMINATION 3 times, fasting blood sugar >=16.7mmol/L's is modeling success rat.
3, the mensuration of blood glucose
After last administration, water 12h is can't help in animal fasting, and eyeball rear vein beard gets blood, measures blood glucose value respectively according to the method for test kit.Adopt SPSS13.0 statistical software, analyze and respectively organize the situation of change of blood glucose value.
4, ChukrasoneB is on the impact of rat model of type 2 diabetes mellitus blood glucose
Experimental result is in table 2, and as known from Table 2, after injection STZ, rat blood sugar rises, fasting blood sugar >=16.7mmol/L after 72h, and diabetes model success is described.After administration, positive drug group, ChukrasoneB is high, in and the blood glucose value of low dose group compare with model group blood glucose value, all have significant difference (P<0.01).
The T inspection display of blood glucose after blood glucose and administration before each group of administration, positive drug group, ChukrasoneB is high, in and blood glucose value before and after low dose group administration compare, there is significant difference (P<0.01).Above result shows, ChukrasoneB 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 administration | Blood glucose value after administration |
| Normal group | 10 | 5.3±0.22 | 5.22±0.35 |
| Model control group | 9 | 13.03±2.23 | 31.13±2.44 |
| Positive drug group | 9 | 31.34±2.44 | 18.74±2.33** △△ |
| Low dose group | 8 | 31.95±2.25 | 23.65±2.22** △△ |
| Middle dosage group | 10 | 32.93±1.92 | 19.65±2.65** △△ |
| High dose group | 9 | 35.32±2.53 | 19.82±3.04** △△ |
* p<0.05vs model group * * p<0.01vs model group
△p<0.05vs is with before group administration
△ △p<0.01vs is with before group administration
Conclusion: ChukrasoneB significantly can reduce the blood glucose of type 2 diabetes mellitus animal model, can be used for preparing antidiabetic medicine.
Claims (1)
1.ChukrasoneB reduces the application in hypoglycemic medicament in preparation, described Compound C hukrasoneB structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310278053.5A CN103356592B (en) | 2013-07-04 | 2013-07-04 | Chukrasone B reduces the application in hypoglycemic medicament in preparation |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310278053.5A CN103356592B (en) | 2013-07-04 | 2013-07-04 | Chukrasone B reduces the application in hypoglycemic medicament in preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103356592A CN103356592A (en) | 2013-10-23 |
| CN103356592B true CN103356592B (en) | 2016-01-20 |
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| CN201310278053.5A Expired - Fee Related CN103356592B (en) | 2013-07-04 | 2013-07-04 | Chukrasone B reduces the application in hypoglycemic medicament in preparation |
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| CN (1) | CN103356592B (en) |
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2013
- 2013-07-04 CN CN201310278053.5A patent/CN103356592B/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| Chukrasones A and B: Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis;Hong-Bing Liu等;《Org. Lett.》;20121008;第14卷(第17期);4438–4441 * |
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| CN103356592A (en) | 2013-10-23 |
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Inventor after: Ma Qiusheng Inventor before: Ding Shengyu |
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Effective date of registration: 20151125 Address after: 252100 Chiping County People's Hospital, 136 Wenhua Road, Liaocheng, Shandong, Chiping Applicant after: Ma Qiusheng Address before: 210009 Gulou District, Jiangsu, Nanjing Gu Ping Kong, No. 4 Applicant before: Ding Shengyu |
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