CN103393662A - Application of Sarcaboside B to preparation of hypoglycemic medicament - Google Patents
Application of Sarcaboside B to preparation of hypoglycemic medicament Download PDFInfo
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- CN103393662A CN103393662A CN2013102651962A CN201310265196A CN103393662A CN 103393662 A CN103393662 A CN 103393662A CN 2013102651962 A CN2013102651962 A CN 2013102651962A CN 201310265196 A CN201310265196 A CN 201310265196A CN 103393662 A CN103393662 A CN 103393662A
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Abstract
The invention discloses application of Sarcaboside B to the preparation of antidiabetic medicaments. The invention provides a brand new choice and thought for antidiabetic medicaments in the prior art, widens selection field of antidiabetic medicaments and contributes to the development of the technical field. The Sarcaboside B is proved to have substantial antidiabetic effects. The invention employs a compound with a clear chemical structure. The application of Sarcaboside B to the preparation of antidiabetic medicaments involved in the invention is disclosed for the first time. As the Sarcaboside B has a novel skeleton type and unimaginably strong activity in prevention and treatment of diabetes, no other compound can give any enlightenment. The invention has outstanding substantive distinguishing features and makes substantial progress in treatment of diabetes.
Description
Technical field
The present invention relates to a kind of new purposes of Sarcaboside B, the specifically application of Sarcaboside B in preparing 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 are all 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 modern disease, it is only second to cancer to the harm of human body, the mankind's health in serious threat, and present diabetes have extension and the tendency of rejuvenation, how to prevent that diabetes from having become the large problem that present the world of medicine pays close attention to.
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 compound has brand-new framework types, there is no at present the report about activity, for the purposes of the Sarcaboside B that the present invention relates in preparation treatment antidiabetic medicine, belong to open first, because framework types belongs to brand-new framework types, and its control diabetic activity is unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possesses 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, for the existing technical field for preparing antidiabetic medicine provides a kind of new way, provides the application of Sarcaboside B in preparing antidiabetic medicine.
The structural formula of Sarcaboside B such as formula I:
Formula I
Technical scheme of the present invention is: the application of Sarcaboside B specifically is applied to prepare antidiabetic medicine.
The invention has the beneficial effects as follows:
1) the present invention, for present 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 Sarcaboside B 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 Sarcaboside B, at lasting gavage fat milk, rat is produced on the basis of insulin resistant, apply 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 Sarcaboside B treatment, Sarcaboside B is high, in and the blood glucose value of low dose group and model group blood glucose value relatively, also has significant difference (P<0.01), Sarcaboside B 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 Sarcaboside B has good hypoglycemic activity to experimental type 2 diabetes mellitus.
The purposes of the Sarcaboside B 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 do not is the possibility that is provided any enlightenment by other 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 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 be 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 that prepare tablet, mix, conventional tablet machine is 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 the conventional adjuvant such as starch 180 grams that prepare capsule, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
The impact of experimental example 1 Sarcaboside B on 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, after modeling success, the model group animal is divided at random to high, normal, basic group of model control group, positive drug gliclazide group, Sarcaboside B, 1 week of according to the form below successive administration again.
Administration time and dosage are in Table 1:
The grouping of table 1 Sarcaboside B 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, the high fat group rat every day of gavage self-control sooner or later 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 (preparation before use).After administration 48h, water 12h is can't help in fasting, every 3 hours eyeball rear vein beards, gets blood, 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, according to the method for test kit, measures respectively blood glucose value.Adopt the SPSS13.0 statistical software, analyze and respectively organize the situation of change of blood glucose value.
4, the impact of Sarcaboside B on 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, and fasting blood sugar >=16.7mmol/L after 72h illustrates the diabetes model success.After administration, the positive drug group, Sarcaboside B is high, in and the blood glucose value of low dose group and model group blood glucose value relatively, significant difference (P<0.01) is all arranged.
Each is organized before administration the T check of blood glucose after blood glucose and administration and shows, the positive drug group, Sarcaboside B 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, Sarcaboside B 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 | 5.1±0.21 | 5.21±0.32 |
| Model control group | 9 | 13.23±2.22 | 31.27±2.42 |
| The positive drug group | 9 | 31.44±2.44 | 18.36±2.34** △△ |
| Low dose group | 8 | 31.15±2.23 | 23.47±2.23** △△ |
| Middle dosage group | 10 | 32.37±1.91 | 19.15±2.62** △△ |
| High dose group | 9 | 35.28±2.52 | 19.26±3.01** △△ |
* p<0.05vs model group * * p<0.01vs model group
△P<0.05vs is on the same group before administration
△ △P<0.01vs is on the same group before administration
Conclusion: Sarcaboside B can significantly reduce the blood glucose of type 2 diabetes mellitus animal model, can be used for preparing antidiabetic medicine.
Claims (1)
1.Sarcaboside B reduces the application in the blood glucose medicine in preparation, described compound S arcaboside B structure as
Formula IShown in:
Formula I.
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| CN2013102651962A CN103393662A (en) | 2013-06-27 | 2013-06-27 | Application of Sarcaboside B to preparation of hypoglycemic medicament |
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| CN2013102651962A CN103393662A (en) | 2013-06-27 | 2013-06-27 | Application of Sarcaboside B to preparation of hypoglycemic medicament |
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Application publication date: 20131120 |