CN103285008A - Applications of Myriberine A in the preparation of antidiabetic drugs - Google Patents
Applications of Myriberine A in the preparation of antidiabetic drugs Download PDFInfo
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- CN103285008A CN103285008A CN2013102538851A CN201310253885A CN103285008A CN 103285008 A CN103285008 A CN 103285008A CN 2013102538851 A CN2013102538851 A CN 2013102538851A CN 201310253885 A CN201310253885 A CN 201310253885A CN 103285008 A CN103285008 A CN 103285008A
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Abstract
The invention discloses applications of Myriberine A to the preparation of anti-diabetic drugs. According to the invention, brand-new selection and thought are provided to the existing anti-diabetic drugs, the selection field of the anti-diabetic drugs is widened and a contribution is made for the technical field. The applications of Myriberine A prove that Myriberine A has remarkable anti-diabetic effect. According to the invention, a compound with a known chemical structure is selected. The applications of Myriberine A to the preparation of the anti-diabetic drugs is firstly disclosed, the skeleton type thereof is brand-new, the anti-diabetic activity thereof is unexpectedly high, so the possibility of any prompt given by other compounds does not exist, and prominent substantive features are provided and a remarkable progress in the treatment of the diabetes mellitus is made at the same time.
Description
Technical field
The present invention relates to the new purposes of chemical compound Myriberine A, relate in particular to the application of Myriberine A in preparation blood sugar lowering medicine.
Background technology
Diabetes (diabetes mellitus) are one of current modal chronic diseases, type 2 diabetes mellitus (Type II diabetes mellitus wherein, be non-insulin-dependent diabetes mellitus again, non-insulin-depentdiabetes mellitus NIDDM) accounts for more than 90% of diabetics.Diabetes all are serious day by day 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 beings'health in serious threat, and present diabetes have extension and the tendency of rejuvenation, how to prevent that diabetes from having become the big problem that present the world of medicine pays close attention to.
The chemical compound Myriberine A that the present invention relates to is one and delivered (Sheng-Dian Huang in 2013, et al., Myriberine A, a New Alkaloid with an Unprecedented Heteropentacyclic Skeleton from Myrioneuron faberi.Organic Letters, 2013,3 (15), 590 – 593.) noval chemical compound, this chemical compound has brand-new framework types, present purposes only relates to and suppresses hepatitis C virus (Sheng-Dian Huang, et al., Myriberine A, a New Alkaloid with an Unprecedented Heteropentacyclic Skeleton from Myrioneuron faberi.Organic Letters, 2013,3 (15), 590 – 593.), belong to open first for the purposes of the Myriberine A that the present invention relates in preparation blood sugar lowering medicine.
Summary of the invention
The present invention proposes the application of Myriberine A in preparation blood sugar lowering medicine.Find out that from pharmacological evaluation MyriberineA has the effect of blood sugar lowering preferably.Because the present invention discloses the pharmacologic action of Myriberine A aspect blood sugar lowering first.
Described chemical compound Myriberine A structure is shown in formula I:
Technical scheme of the present invention is: the application of Myriberine A specifically is to be 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 Myriberine A of the present invention has been proved to be significant anti-diabetic effect.
The most important thing is: the present invention is to the experimentize blood sugar lowering experiment of animal of Myriberine A, at the lasting stomach fat milk of irritating 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 experimental type 2 diabetes mellitus rat gives Myriberine A treatment, Myriberine A height, in and the blood glucose value of low dose group and model group blood glucose value relatively, also has significant difference (P＜0.01), Myriberine A height, in and the blood glucose value before and after the low dose group administration relatively, also have significant difference (P＜0.01), illustrate that Myriberine A has good hypoglycemic activity to experimental type 2 diabetes mellitus.
The purposes of the Myriberine 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 anti-diabetic simultaneously and obviously have obvious improvement.
The specific embodiment
The preparation method of chemical compound Myriberine A involved in the present invention is referring to document ((Sheng-Dian Huang, et al., Myriberine A, a New Alkaloid with an Unprecedented Heteropentacyclic Skeleton from Myrioneuron faberi.Organic Letters, 2013,3 (15), 590 – 593.)
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 chemical compound Myriberine A tablet involved in the present invention:
Get 5 and digest compound Myriberine A, add dextrin 195 grams, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of chemical compound Myriberine A capsule involved in the present invention:
Get 5 and digest compound Myriberine A, add starch 195 grams, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Experimental example 1:Myriberine A is to the influence of experimental type 2 diabetes mellitus rat
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 into normal control group and modeling group at random, 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, Myriberine 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 1Myriberine A effect experiment animal
| Group | Number of animals (only) | Dosage (mg/kgBW) |
| The normal control 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 is irritated the stomach distilled water every day, and high fat group rat is irritated stomach self-control fat milk (1ml/100gBW) every day sooner or later.After 2 weeks of continuous irrigation stomach fat milk, 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 (face and use preceding 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 blood glucose value respectively 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, Myriberine A is to the influence of experimental type 2 diabetes mellitus rat blood sugar
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, Myriberine A height, 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 the administration, and the T check of blood glucose shows behind the blood glucose and administration, the positive drug group, Myriberine A height, 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 Myriberine A can reduce the blood glucose of experimental type 2 diabetes mellitus rat.
Table 2 experimental result
| Group | Number of animals (only) | Blood glucose value before the administration | Blood glucose value after the administration |
| The normal control group | 10 | 5.97±0.37 | 5.74±1.38 |
| Model control group | 9 | 13.62±2.36 | 36.75±2.44 |
| The positive drug group | 9 | 33.53±2.46 | 18.14±2.92** △△ |
| Low dose group | 8 | 31.26±2.35 | 24.21±2.81** △△ |
| Middle dosage group | 10 | 33.22±1.53 | 19.53±2.51** △△ |
| High dose group | 9 | 37.63±2.25 | 18.25±3.35** △△ |
* 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: Myriberine A can significantly reduce the blood glucose of type 2 diabetes mellitus animal model, can be used for preparing antidiabetic medicine.
Claims (1)
1.Myriberine the application of A in preparation blood sugar lowering medicine, described chemical compound Myriberine A structure is shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102538851A CN103285008A (en) | 2013-06-22 | 2013-06-22 | Applications of Myriberine A in the preparation of antidiabetic drugs |
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| CN2013102538851A CN103285008A (en) | 2013-06-22 | 2013-06-22 | Applications of Myriberine A in the preparation of antidiabetic drugs |
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| CN103285008A true CN103285008A (en) | 2013-09-11 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105168226A (en) * | 2015-08-11 | 2015-12-23 | 南京华宽信息咨询中心 | Medicine for lowering blood glucose and application of medicine |
-
2013
- 2013-06-22 CN CN2013102538851A patent/CN103285008A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| SHENG-DIAN HUANG,ET AL: "Myriberine A, a New Alkaloid with an Unprecedented Heteropentacyclic Skeleton from Myrioneuron faberi", 《ORGANIC LETTERS》 * |
| 侯昕: "《糖尿病药膳食疗182题》", 31 March 2001, 青岛出版社 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105168226A (en) * | 2015-08-11 | 2015-12-23 | 南京华宽信息咨询中心 | Medicine for lowering blood glucose and application of medicine |
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Application publication date: 20130911 |