CN102988386B - Application of Houttuynoid E in preparation of medicine for reducing blood sugar - Google Patents
Application of Houttuynoid E in preparation of medicine for reducing blood sugar Download PDFInfo
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- CN102988386B CN102988386B CN201210468874.0A CN201210468874A CN102988386B CN 102988386 B CN102988386 B CN 102988386B CN 201210468874 A CN201210468874 A CN 201210468874A CN 102988386 B CN102988386 B CN 102988386B
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Abstract
The invention discloses application of Houttuynoid E in preparation of a medicine for reducing blood sugar. The invention provides a novel choice and thinking for the present antidiabetic medicines, the selection field of the antidiabetic medicines is widened, and contribution is made to the development of the technical field. The application of Houttuynoid E proves that the Houttuynoid E has an obvious antidiabetic effect. A compound with a clear chemical structure is selected. The application of Houttuynoid E in preparation of the medicine for treating the diabetes is disclosed for the first time, and because the framework type belongs to a novel framework type, the activity for treating the diabetes is unexpectedly high, the possibility that other compounds give enlightenment is avoided, and the Houttuynoid E has outstanding substantial characteristics and has obvious progress in treatment of the diabetes.
Description
Technical field
The present invention relates to a kind of new purposes of Houttuynoid E, the specifically application of Houttuynoid E 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 the 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, in following 20 years, patient's number will break through 5,000 ten thousand.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 current the world of medicine pays close attention to.
The compound H outtuynoid E the present invention relates to is one and within 2012, delivers (Cai, J. Y. et al., 2012. Houttuynoid E, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to DEF(Cai, J. Y. et al., 2012. Houttuynoid E, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), purposes for the Houttuynoid E 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, 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 of preparing antidiabetic medicine provides a kind of new way, provides the application of Houttuynoid E in preparing antidiabetic medicine.
The structural formula of Houttuynoid E is as formula I:
Formula I
Technical scheme of the present invention is: the application of Houttuynoid E, is specifically applied to prepare antidiabetic medicine.
The invention has the beneficial effects as follows:
1) the present invention, for 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 Houttuynoid E 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 Houttuynoid E, 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.Rat model of type 2 diabetes mellitus gives after Houttuynoid E treatment, Houttuynoid E is high, in and blood glucose value and the comparison of model group blood glucose value of low dose group, also there is significant difference (P<0.01), Houttuynoid E is high, in and the blood glucose value comparison before and after low dose group administration, also there is significant difference (P<0.01), illustrate that Houttuynoid E has good hypoglycemic activity to experimental type 2 diabetes mellitus.
The purposes of the Houttuynoid E 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 anti-diabetic simultaneously and obviously there is significant progress.
The specific embodiment
The preparation method of compound H outtuynoid E involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Houttuynoid E, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.).
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 H outtuynoid E tablet involved in the present invention:
Get 20 and digest compound Houttuynoid E, add 180 grams of conventional adjuvants preparing tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound H outtuynoid E capsule involved in the present invention:
Get 20 and digest compound Houttuynoid E, add the conventional adjuvant of preparing capsule as 180 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Experimental example 1 impact of Houttuynoid E 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, modeling group is set up model as follows, model group animal is divided at random to high, normal, basic group of model control group, positive drug gliclazide group, Houttuynoid E, according to the form below successive administration 1 week after modeling success again.
Administration time and dosage are in Table 1:
The grouping of table 1 Houttuynoid E 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 sooner or later fat milk (1ml/100gBW).Gavage fat milk is after 2 weeks continuously, and water 24h is can't help in animal fasting, 10 tail vein injection salines of blank group, the equal tail vein injection 30mg/kgBW of all the other rats streptozotocin (being abbreviated as below 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 last administration, water 12h is can't help in animal fasting, and eyeball rear vein beard is got blood, according to the method for test kit, measures respectively blood glucose value.Adopt SPSS13.0 statistical software, analyze and respectively organize the situation of change of blood glucose value.
4, the impact of Houttuynoid E 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 diabetes model success.After administration, positive drug group, Houttuynoid E is high, in and blood glucose value and the comparison of model group blood glucose value of low dose group, all have significant difference (P<0.01).
Each is organized before administration the T check of blood glucose after blood glucose and administration and shows, positive drug group, Houttuynoid E is high, in and the blood glucose value comparison before and after low dose group administration, there is significant difference (P<0.01).Above result shows, Houttuynoid E 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 |
| Positive drug group | 9 | 31.33±2.42 | 18.74±2.34** △△ |
| Low dose group | 8 | 31.94±2.24 | 23.69±2.23** △△ |
| Middle dosage group | 10 | 32.96±1.93 | 19.68±2.69** △△ |
| High dose group | 9 | 35.37±2.55 | 19.88±3.06** △△ |
* 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: Houttuynoid E can significantly reduce the blood glucose of type 2 diabetes mellitus animal model, can be used for preparing antidiabetic medicine.
Claims (1)
1.Houttuynoid E is the application in anti-type 2 diabetes mellitus medicine in preparation, described compound H outtuynoid E structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210468874.0A CN102988386B (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid E in preparation of medicine for reducing blood sugar |
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| CN201210468874.0A CN102988386B (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid E in preparation of medicine for reducing blood sugar |
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| CN102988386A CN102988386A (en) | 2013-03-27 |
| CN102988386B true CN102988386B (en) | 2014-04-16 |
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| CN201210468874.0A Expired - Fee Related CN102988386B (en) | 2012-11-19 | 2012-11-19 | Application of Houttuynoid E in preparation of medicine for reducing blood sugar |
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2012
- 2012-11-19 CN CN201210468874.0A patent/CN102988386B/en not_active Expired - Fee Related
Non-Patent Citations (4)
| Title |
|---|
| Shao-dan Chen et al..Houttuynoids A-E,anti-herpes simplex virus active flavonoids with novel skeletons from houttuynia cordata.《Organic Letters》.2012,第14卷(第7期), * |
| Shao-danChenetal..HouttuynoidsA-E anti-herpes simplex virus active flavonoids with novel skeletons from houttuynia cordata.《Organic Letters》.2012 |
| 王海颖等.鱼腥草对糖尿病大鼠脂联素与结缔组织生长因子的改善作用.《中国中西医结合肾病杂志》.2009,第10卷(第10期), |
| 鱼腥草对糖尿病大鼠脂联素与结缔组织生长因子的改善作用;王海颖等;《中国中西医结合肾病杂志》;20091031;第10卷(第10期);第902-905页 * |
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