CN105456251A - Application of Rhodomicranols B in preparation of drug for lowering blood glucose - Google Patents
Application of Rhodomicranols B in preparation of drug for lowering blood glucose Download PDFInfo
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- CN105456251A CN105456251A CN201510961099.6A CN201510961099A CN105456251A CN 105456251 A CN105456251 A CN 105456251A CN 201510961099 A CN201510961099 A CN 201510961099A CN 105456251 A CN105456251 A CN 105456251A
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- rhodomicranolsb
- rhodomicranols
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
Abstract
The invention discloses application of Rhodomicranols B in preparation of an antidiabetic drug. A brand new selection and thought are provided for present antidiabetic drugs, the selection scope of the antidiabetic drugs is widened, and contribution is made to the development of the technical field; the application of Rhodomicranols B is proved to have a remarkable antidiabetic effect; a compound having a clear chemical structure is selected and used. The use of the related Rhodomicranols B in preparing the antidiabetic drug is disclosed for the first time; a skeleton type belongs to a brand new skeleton type, the strong activity in preventing and treating diabetes is unexpected, and the possibility that another compound gives enlightenment does not exist, so outstanding substantive distinguishing features are achieved, and a remarkable improvement is obviously achieved when the Rhodomicranols B is used for treating diabetes.
Description
Technical field
The present invention relates to the novelty teabag of compound R hodomicranolsB, particularly relate to the application of a kind of RhodomicranolsB in preparation reduction hypoglycemic medicament.
Background technology
Diabetes (diabetesmellitus) are one of current modal chronic diseases, wherein type 2 diabetes mellitus (Type II diabetesmellitus, be non-insulin-dependent diabetes mellitus again, non-insulin-depentdiabetesmellitus, NIDDM) account for more than 90% of diabetics.Diabetes are all day by day serious problems in developed country and developing country, and it causes serious and costly consequence, comprises 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, the population of state-owned 4.3% suffers from diabetes, and in following 20 years, the number of patient is by breakthrough 5,000 ten thousand.Diabetes are second killers in modern diseases, it is only second to cancer to the harm of human body, the health of the mankind in serious threat, and present diabetes have extension and the tendency of rejuvenation, the large problem how preventing from diabetes from having become current the world of medicine paying close attention to.
The compound R hodomicranolsB that the present invention relates to is one and delivers (MengkeZhang in 2013, etal., MicranthanoneA, aNewDiterpenewithanUnprecedentedCarbonSkeletonfromRhodod endronmicranthum, OrganicLetters, 2013, 15 (12): 3094 – 3097.) noval chemical compound, this compound has brand-new framework types, current purposes is immunomodulating (MengkeZhang only, etal., MicranthanoneA, aNewDiterpenewithanUnprecedentedCarbonSkeletonfromRhodod endronmicranthum, OrganicLetters, 2013, 15 (12): 3094 – 3097.), the purposes reduced in hypoglycemic medicament in preparation for a kind of RhodomicranolsB that the present invention relates to belongs to first public.
Summary of the invention
The present invention proposes the application of a kind of RhodomicranolsB in preparation reduction hypoglycemic medicament.Find out from pharmacological evaluation, this RhodomicranolsB has and falls hypoglycemic effect preferably.Because the first public a kind of RhodomicranolsB of the present invention is reducing the pharmacologic action in blood glucose.
Described compound R hodomicranolsB structure is as shown in formula I:
Technical scheme of the present invention is: the application of this RhodomicranolsB, is specifically applied to and prepares antidiabetic medicine.
Described RhodomicranolsB is reducing the application in hypoglycemic medicament, and RhodomicranolsB has hypoglycemic activity to experimental type 2 diabetes mellitus.
A kind of reduction hypoglycemic medicament, be that active component interpolation adjuvant is prepared from by RhodomicranolsB, preparation method, for getting 5 g of compound RhodomicranolsB, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
A kind of reduce hypoglycemic medicament, be that active component adds adjuvant and is prepared from by RhodomicranolsB, preparation method, for getting 5 g of compound RhodomicranolsB, adds starch 195 grams, mixing, encapsulatedly makes 1000.
The invention has the beneficial effects as follows:
1) the present invention is that 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 RhodomicranolsB 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 RhodomicranolsB, rat is made to produce on the basis of insulin resistant at lasting gavage fat milk, apply low dose of streptozotocin impaired isle β cell, 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 RhodomicranolsB treatment, RhodomicranolsB is high, in and the blood glucose value of low dose group compare with model group blood glucose value, also there is significant difference (P<0.01), RhodomicranolsB is high, in and blood glucose value before and after low dose group administration compare, also there is significant difference (P<0.01), illustrate that RhodomicranolsB has good hypoglycemic activity to experimental type 2 diabetes mellitus.
The purposes of the RhodomicranolsB that the present invention relates in preparation treatment antidiabetic medicine belongs to first public, because framework types belongs to brand-new framework types, and its control diabetic activity is unexpectedly strong, there is not the possibility being 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.
Detailed description of the invention
The preparation method of compound R hodomicranolsB involved in the present invention is see document (MengkeZhang, etal., MicranthanoneA, aNewDiterpenewithanUnprecedentedCarbonSkeletonfromRhodod endronmicranthum, OrganicLetters, 2013,15 (12): 3094 – 3097.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound R hodomicranolsB tablet involved in the present invention:
Get 5 g of compound RhodomicranolsB, add 195 grams, dextrin, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound R hodomicranolsB capsule involved in the present invention:
Get 5 g of compound RhodomicranolsB, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1:RhodomicranolsB is on the impact of rat model of type 2 diabetes mellitus
1, animal grouping
Healthy Wistar rat (SPF level), male, body weight 180-220g (being provided by Nanjing Medical University's Experimental Animal Center), freely to drink water feed, be divided into Normal group and modeling group at random, modeling group Modling model as follows, is divided into model control group, positive drug gliclazide group, high, normal, basic group of RhodomicranolsB, according to the form below successive administration 1 week after modeling success more at random by model group animal.
Administration time and dosage are in table 1:
The grouping of table 1RhodomicranolsB 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 | 0.2 |
| 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 fat milk (1ml/100gBW) sooner or later.Continuous gavage fat milk is after 2 weeks, water 24h is can't help in animal fasting, blank group 10 tail vein injection salines, all the other rats equal tail vein injection 30mg/kgBW streptozotocin (hereinafter abbreviated as STZ) solution (prepared before use).After administration 48h, water 12h is can't help in fasting, gets blood every 3 hours eyeball rear vein beards, and according to blood sugar detection test kit time-and-motion study fasting blood sugar, 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 gets blood, measures blood glucose value respectively according to the method for test kit.Adopt SPSS13.0 statistical software, analyze and respectively organize the situation of change of blood glucose value.
4, RhodomicranolsB is on the impact of 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, fasting blood sugar >=16.7mmol/L after 72h, and diabetes model success is described.After administration, positive drug group, RhodomicranolsB is high, in and the blood glucose value of low dose group compare with model group blood glucose value, all have significant difference (P<0.01).
The T inspection display of blood glucose after blood glucose and administration before each group of administration, positive drug group, RhodomicranolsB is high, in and blood glucose value before and after low dose group administration compare, there is significant difference (P<0.01).Above result shows, RhodomicranolsB 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 | 5.76±0.38 | 5.83±1.45 |
| Model control group | 9 | 16.68±2.23 | 36.54±2.39 |
| Positive drug group | 9 | 34.32±2.18 | 18.21±2.43** △△ |
| Low dose group | 8 | 32.79±2.57 | 23.16±3.26** △△ |
| Middle dosage group | 10 | 35.35±1.75 | 18.42±2.17** △△ |
| High dose group | 9 | 38.86±2.14 | 17.48±3.21** △△ |
* p<0.05vs model group * * p<0.01vs model group
△p<0.05vs is with before group administration
△ △p<0.01vs is with before group administration
Conclusion: RhodomicranolsB of the present invention significantly can reduce the blood glucose of type 2 diabetes mellitus animal model, can be used for preparing antidiabetic medicine.
Claims (4)
1.RhodomicranolsB is reducing the application in hypoglycemic medicament, and described compound R hodomicranolsB structure is as shown in formula I:
Formula I.
2. RhodomicranolsB, reducing the application in hypoglycemic medicament, is characterized in that RhodomicranolsB has hypoglycemic activity to experimental type 2 diabetes mellitus as claimed in claim 1.
3. one kind is reduced hypoglycemic medicament, it is characterized in that by RhodomicranolsB described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound RhodomicranolsB, adds 195 grams, dextrin, mixing, Conventional compression makes 1000.
4. one kind is reduced hypoglycemic medicament, it is characterized in that by RhodomicranolsB described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound RhodomicranolsB, adds starch 195 grams, mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510961099.6A CN105456251A (en) | 2015-12-20 | 2015-12-20 | Application of Rhodomicranols B in preparation of drug for lowering blood glucose |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510961099.6A CN105456251A (en) | 2015-12-20 | 2015-12-20 | Application of Rhodomicranols B in preparation of drug for lowering blood glucose |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105456251A true CN105456251A (en) | 2016-04-06 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510961099.6A Pending CN105456251A (en) | 2015-12-20 | 2015-12-20 | Application of Rhodomicranols B in preparation of drug for lowering blood glucose |
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| CN (1) | CN105456251A (en) |
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- 2015-12-20 CN CN201510961099.6A patent/CN105456251A/en active Pending
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| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160406 |
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| WD01 | Invention patent application deemed withdrawn after publication |