CN103462986A - Application of spirooliganones B in preparation of medicine reducing blood glucose - Google Patents
Application of spirooliganones B in preparation of medicine reducing blood glucose Download PDFInfo
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- CN103462986A CN103462986A CN201310466691XA CN201310466691A CN103462986A CN 103462986 A CN103462986 A CN 103462986A CN 201310466691X A CN201310466691X A CN 201310466691XA CN 201310466691 A CN201310466691 A CN 201310466691A CN 103462986 A CN103462986 A CN 103462986A
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Abstract
The invention discloses the application of spirooliganones B in preparation of the medicine reducing the blood glucose. The spirooliganones B has remarkable effect on inhibiting the diabetes mellitus, is a compound with a clear chemical structure and belongs to a brand new matrix type. The spirooliganones B has the advantages of being high in activity for preventing and treating the diabetes mellitus and prominent in substantive features, and makes remarkable progress in treating the diabetes mellitus.
Description
Technical field
The present invention relates to the new purposes of compound S pirooliganones B, relate in particular to Spirooliganones B and reduce the application in the blood glucose medicine in preparation.
Background technology
Diabetes (diabetes mellitus) 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, in following 20 years, patient's number will break through 5,000 ten thousand.Diabetes are second killers in modern disease, and it is only second to cancer to the harm of human body, and the mankind's health in serious threat.
The compound S pirooliganones B the present invention relates to is one and within 2013, delivers (Shuang-Gang Ma, et al., Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters, 2013, 15(17): noval chemical compound 4450 – 4453.), this compound has brand-new framework types, current purposes finds that it can suppress Coxsackie B virus 3 and influenza A virus H3N2(Shuang-Gang Ma, et al., Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters, 2013, 15(17): 4450 – 4453.), the purposes that the Spirooliganones B the present invention relates to reduces in the blood glucose medicine in preparation belongs to open first.
Summary of the invention
The present invention proposes Spirooliganones B and reduces the application in the blood glucose medicine in preparation.From pharmacological evaluation, find out, Spirooliganones B has and falls preferably hypoglycemic effect.Because the present invention discloses Spirooliganones B first at the pharmacologic action aspect reduction blood glucose.
Described compound S pirooliganones B structure is as shown in formula I:
Technical scheme of the present invention is: the application of Spirooliganones B specifically is applied to prepare antidiabetic medicine.
The invention has the beneficial effects as follows:
The blood sugar lowering experiment that the present invention carries out laboratory animal to Spirooliganones B, illustrate that Spirooliganones B has good hypoglycemic activity to experimental type 2 diabetes mellitus.The purposes of the Spirooliganones B 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 anti-diabetic simultaneously and obviously there is significant progress.
The specific embodiment
The preparation method of compound S pirooliganones B involved in the present invention is referring to document (Shuang-Gang Ma, et al., Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters, 2013,15(17): 4450 – 4453.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound S pirooliganones B tablet involved in the present invention:
Get 5 and digest compound Spirooliganones B, add dextrin 195 grams, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compound S pirooliganones B capsule involved in the present invention:
Get 5 and digest compound Spirooliganones B, add starch 195 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The impact of experimental example 1:Spirooliganones 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 Nanjing Medical University'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 to high, normal, basic group of model control group, positive drug gliclazide group, Spirooliganones B after modeling success, according to the form below successive administration 1 week again.
Administration time and dosage are in Table 1:
The grouping of table 1Spirooliganones 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 | 0.2 |
| Middle dosage group | 12 | 0.4 |
| High dose group | 12 | 0.8 |
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 Spirooliganones 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, Spirooliganones 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, Spirooliganones B is high, in and the blood glucose value before and after the low dose group administration relatively, there is significant difference (P<0.01).Above result shows, Spirooliganones 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 | 5.96±0.36 | 5.89±1.64 |
| Model control group | 9 | 13.18±2.74 | 34.26±2.27 |
| The positive drug group | 9 | 31.35±2.25 | 18.74±2.18** △△ |
| Low dose group | 8 | 31.75±2.62 | 24.27±2.41** △△ |
| Middle dosage group | 10 | 34.81±1.64 | 19.60±2.49** △△ |
| High dose group | 9 | 36.20±2.93 | 17.57±3.83** △△ |
* 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: Spirooliganones B can significantly reduce the blood glucose of type 2 diabetes mellitus animal model, can be used for preparing antidiabetic medicine.
Claims (1)
1.Spirooliganones B reduces the application in the blood glucose medicine in preparation, described compound S pirooliganones B structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310466691XA CN103462986A (en) | 2013-10-09 | 2013-10-09 | Application of spirooliganones B in preparation of medicine reducing blood glucose |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310466691XA CN103462986A (en) | 2013-10-09 | 2013-10-09 | Application of spirooliganones B in preparation of medicine reducing blood glucose |
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| Publication Number | Publication Date |
|---|---|
| CN103462986A true CN103462986A (en) | 2013-12-25 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201310466691XA Pending CN103462986A (en) | 2013-10-09 | 2013-10-09 | Application of spirooliganones B in preparation of medicine reducing blood glucose |
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| CN (1) | CN103462986A (en) |
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2013
- 2013-10-09 CN CN201310466691XA patent/CN103462986A/en active Pending
Non-Patent Citations (3)
| Title |
|---|
| SHUANG-GANG MA,ET AL.: "Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum", 《ORGANIC LETTERS》 * |
| T. J. COLEMAN，ET.AL.: "Diabetes in Mice after Coxsackie B4 Virus Infection", 《BRITISH MEDICAL JOURNAL》 * |
| 陈建烟等: "植物精油生物活性作用机理研究进展", 《天然产物研究与开发》 * |
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Application publication date: 20131225 |