CN103127065A - Application of Eryngiolide A in medicines reducing blood sugar - Google Patents
Application of Eryngiolide A in medicines reducing blood sugar Download PDFInfo
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- CN103127065A CN103127065A CN 201210411445 CN201210411445A CN103127065A CN 103127065 A CN103127065 A CN 103127065A CN 201210411445 CN201210411445 CN 201210411445 CN 201210411445 A CN201210411445 A CN 201210411445A CN 103127065 A CN103127065 A CN 103127065A
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- eryngiolide
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Abstract
The invention discloses application of Eryngiolide A in preparation of anti-diabetic medicines. The application of the Eryngiolide A in preparation of anti-diabetic medicines provides a brand new selection and thought for existing anti-diabetic medicines, widens the selecting field of anti-diabetic medicines, and makes great contribution to development of the anti-diabetic medicines technical field. The application of the Eryngiolide A in preparation of medicines reducing blood sugar is proved to have evident anti-diabetic effect, and chooses composition with definite chemical structures. Use of the Eryngiolide A in preparation of medicines reducing blood sugar is made public for the first time, the skeleton type is completely novel, and the Eryngiolide A has an unexpectedly high activity of preventing and curing diabetes, probability of other compounds giving any revelation for the Eryngiolide A does not exist, outstanding substantive features are provided, meanwhile, prominent improvement is evidently possessed in curing diabets.
Description
Technical field
The present invention relates to a kind of new purposes of Eryngiolide A, the specifically application of Eryngiolide 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 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 compd E ryngiolide A that the present invention relates to is one and delivered (Wang in 2012, S. J. et al., 2012. Eryngiolide A, a Cytotoxic Macrocyclic Diterpenoid with an Unusual Cyclododecane Core Skeleton Produced by the Edible Mushroom Pleurotus eryngii. Organic Letters 14 (14), 3672 – 3675.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to the cytotoxic activity (Wang of cancerous cell, S. J. et al., 2012. Eryngiolide A, a Cytotoxic Macrocyclic Diterpenoid with an Unusual Cyclododecane Core Skeleton Produced by the Edible Mushroom Pleurotus eryngii. Organic Letters 14 (14), 3672 – 3675.), belong to open first for the purposes of the Eryngiolide 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 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 provides a kind of new way for the technical field of existing preparation antidiabetic medicine, and the application of Eryngiolide A in the preparation antidiabetic medicine is provided.
The structural formula of Eryngiolide A as
Formula I:
Formula I
Technical scheme of the present invention is: the application of Eryngiolide A 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 the field, also contributes for the development of this technical field; 2) application of Eryngiolide 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 Eryngiolide 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 Eryngiolide A treatment, Eryngiolide A 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), Eryngiolide 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 Eryngiolide A has good hypoglycemic activity to experimental type 2 diabetes mellitus.
The purposes of the Eryngiolide 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 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 compd E ryngiolide A involved in the present invention is referring to document (Wang, S. J. et al., 2012. Eryngiolide A, a Cytotoxic Macrocyclic Diterpenoid with an Unusual Cyclododecane Core Skeleton Produced by the Edible Mushroom Pleurotus eryngii. Organic Letters 14 (14), 3672 – 3675.).
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 compd E ryngiolide A tablet involved in the present invention:
Get 20 and digest compound Eryngiolide A, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compd E ryngiolide A capsule involved in the present invention:
Get 20 and digest compound Eryngiolide A, add the conventional adjuvant such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Below further illustrate technical scheme of the present invention by specific embodiment.
Experimental example 1The impact of Eryngiolide A 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, the model group animal is divided at random high, normal, basic group of model control group, positive drug gliclazide group, Eryngiolide A after 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 Eryngiolide 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, 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, 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, the impact of Eryngiolide A on rat model of type 2 diabetes mellitus blood glucose
Experimental result sees 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, Eryngiolide A 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, and after blood glucose and administration, the T check of blood glucose shows, the positive drug group, Eryngiolide 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, Eryngiolide 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 administration | Blood glucose value after administration |
| Normal group | 10 | 5.5±0.27 | 5.27±0.30 |
| Model control group | 9 | 13.02±2.23 | 31.16±2.46 |
| The positive drug group | 9 | 31.33±2.42 | 18.74±2.34** △△ |
| Low dose group | 8 | 31.94±2.24 | 21.67±2.21** △△ |
| Middle dosage group | 10 | 32.96±1.93 | 19.66±2.68** △△ |
| High dose group | 9 | 35.37±2.55 | 17.85±3.07** △△ |
* 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:Eryngiolide A can significantly reduce the blood glucose of type 2 diabetes mellitus animal model, can be used for preparing antidiabetic medicine.
Claims (1)
1.Eryngiolide the application of A in reducing the blood glucose medicine, described compd E ryngiolide A structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210411445 CN103127065A (en) | 2012-10-25 | 2012-10-25 | Application of Eryngiolide A in medicines reducing blood sugar |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210411445 CN103127065A (en) | 2012-10-25 | 2012-10-25 | Application of Eryngiolide A in medicines reducing blood sugar |
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| Publication Number | Publication Date |
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| CN103127065A true CN103127065A (en) | 2013-06-05 |
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| CN 201210411445 Withdrawn CN103127065A (en) | 2012-10-25 | 2012-10-25 | Application of Eryngiolide A in medicines reducing blood sugar |
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2012
- 2012-10-25 CN CN 201210411445 patent/CN103127065A/en not_active Withdrawn
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Application publication date: 20130605 |