CN103638006B - Application of Oleaceran in medicine for lowering blood glucose - Google Patents
Application of Oleaceran in medicine for lowering blood glucose Download PDFInfo
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- CN103638006B CN103638006B CN201310647545.7A CN201310647545A CN103638006B CN 103638006 B CN103638006 B CN 103638006B CN 201310647545 A CN201310647545 A CN 201310647545A CN 103638006 B CN103638006 B CN 103638006B
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- oleaceran
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- blood glucose
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- medicine
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- XEOIJMSRWFEZRQ-HXUWFJFHSA-N oleaceran Natural products COc1cccc2c1CO[C@@]23Oc4cc(C)cc5ccc(O)c3c45 XEOIJMSRWFEZRQ-HXUWFJFHSA-N 0.000 title claims abstract description 37
- 239000003814 drug Substances 0.000 title claims abstract description 15
- 239000008280 blood Substances 0.000 title abstract description 24
- 210000004369 blood Anatomy 0.000 title abstract description 24
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 title abstract description 16
- 239000008103 glucose Substances 0.000 title abstract description 16
- 150000001875 compounds Chemical class 0.000 claims abstract description 13
- 238000002360 preparation method Methods 0.000 claims description 9
- 230000002218 hypoglycaemic effect Effects 0.000 claims description 7
- 230000003178 anti-diabetic effect Effects 0.000 abstract description 5
- 230000000694 effects Effects 0.000 abstract description 3
- 230000002265 prevention Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 241001465754 Metazoa Species 0.000 description 8
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 6
- 206010012601 diabetes mellitus Diseases 0.000 description 6
- 241000700159 Rattus Species 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 239000003472 antidiabetic agent Substances 0.000 description 4
- 238000011552 rat model Methods 0.000 description 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 4
- 210000003462 vein Anatomy 0.000 description 4
- 241000187180 Streptomyces sp. Species 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 238000003304 gavage Methods 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 125000003003 spiro group Chemical group 0.000 description 3
- ZSJLQEPLLKMAKR-GKHCUFPYSA-N streptozocin Chemical compound O=NN(C)C(=O)N[C@H]1[C@@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O ZSJLQEPLLKMAKR-GKHCUFPYSA-N 0.000 description 3
- 210000005252 bulbus oculi Anatomy 0.000 description 2
- 230000003203 everyday effect Effects 0.000 description 2
- 235000013336 milk Nutrition 0.000 description 2
- 239000008267 milk Substances 0.000 description 2
- 210000004080 milk Anatomy 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- BOVGTQGAOIONJV-BETUJISGSA-N 1-[(3ar,6as)-3,3a,4,5,6,6a-hexahydro-1h-cyclopenta[c]pyrrol-2-yl]-3-(4-methylphenyl)sulfonylurea Chemical group C1=CC(C)=CC=C1S(=O)(=O)NC(=O)NN1C[C@H]2CCC[C@H]2C1 BOVGTQGAOIONJV-BETUJISGSA-N 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 241000700157 Rattus norvegicus Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- ZSJLQEPLLKMAKR-UHFFFAOYSA-N Streptozotocin Natural products O=NN(C)C(=O)NC1C(O)OC(CO)C(O)C1O ZSJLQEPLLKMAKR-UHFFFAOYSA-N 0.000 description 1
- 238000013295 T2DM animal model Methods 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 230000000843 anti-fungal effect Effects 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 208000017169 kidney disease Diseases 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 235000002639 sodium chloride Nutrition 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 229960001052 streptozocin Drugs 0.000 description 1
Abstract
The invention discloses application of Oleaceran in medicine for lowering blood glucose. The application of Oleaceran disclosed in the invention is proved to have evident anti-diabetic effect; the Oleaceran is a compound having definite chemical structure, belongs to a brand new skeleton type, and has strong glycuresis prevention and treatment activity; the Oleaceran has outstanding substantive features and has an obvious progress in the treatment or resisting of glycuresis.
Description
Technical field
The present invention relates to the novelty teabag of compound Oleaceran, particularly relate to the application of Oleaceran in preparation reduction hypoglycemic medicament.
Background technology
Diabetes (diabetes mellitus) 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, and it is only second to cancer to the harm of human body, and the health of the mankind in serious threat.
The compound Oleaceran that the present invention relates to is one and delivers (Ritesh Raju in 2013, et al., Oleaceran:A Novel Spiro [isobenzofuran-1, 20 – naptho [1, 8-bc] furan] Isolated from aTerrestrial Streptomyces sp.Organic Letters, 2013, 15 (14): 3487 – 3489.) noval chemical compound, this compound has brand-new framework types, current purposes finds its energy antifungal and colon cancer (Ritesh Raju, et al., Oleaceran:A Novel Spiro [isobenzofuran-1, 20 – naptho [1, 8-bc] furan] Isolated from a Terrestrial Streptomyces sp.Organic Letters, 2013, 15 (14): 3487 – 3489.), the purposes that the Oleaceran that the present invention relates to reduces in hypoglycemic medicament in preparation belongs to first public.
Summary of the invention
The present invention proposes the application of Oleaceran in preparation reduction hypoglycemic medicament.Find out from pharmacological evaluation, Oleaceran has and falls hypoglycemic effect preferably.Because the first public Oleaceran of the present invention is reducing the pharmacologic action in blood glucose.
Described compound Oleaceran structure is as shown in formula I:
Technical scheme of the present invention is: the application of Oleaceran, is specifically applied to and prepares antidiabetic medicine.
The invention has the beneficial effects as follows:
The present invention carries out the blood sugar lowering experiment of laboratory animal to Oleaceran, illustrates that Oleaceran has good hypoglycemic activity to experimental type 2 diabetes mellitus.The purposes of the Oleaceran 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 strong, possesses outstanding substantive distinguishing features, is used for the treatment of anti-diabetic and obviously has significant progress simultaneously.
Detailed description of the invention
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.
The preparation method of compound Oleaceran involved in the present invention is see document (Ritesh Raju, et al., Oleaceran:A Novel Spiro [isobenzofuran-1,20 – naptho [1,8-bc] furan] Isolated froma Terrestrial Streptomyces sp.Organic Letters, 2013,15 (14): 3487 – 3489.), prepare compound Oleaceran according to the method described above.
Embodiment 1: the preparation of compound Oleaceran tablet involved in the present invention:
Get 5 g of compound Oleaceran, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound Oleaceran capsule involved in the present invention:
Get 5 g of compound Oleaceran, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1:Oleaceran 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(is 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 Oleaceran, 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:
Table 1 Oleaceran effect experiment animal divides into groups
| 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, and 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, Oleaceran 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, Oleaceran 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, Oleaceran 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, Oleaceran 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 | 6.23±0.54 | 5.79±1.74 |
| Model control group | 9 | 13.36±2.35 | 34.46±2.51 |
| Positive drug group | 9 | 31.56±2.84 | 18.49±2.21** △△ |
| Low dose group | 8 | 31.86±2.26 | 24.78±2.53** △△ |
| Middle dosage group | 10 | 35.96±1.58 | 19.41±2.43** △△ |
| High dose group | 9 | 36.21±2.35 | 17.75±3.39** △△ |
* 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: Oleaceran significantly can reduce the blood glucose of type 2 diabetes mellitus animal model, can be used for preparing antidiabetic medicine.
Claims (1)
1.Oleaceran reduce the application in hypoglycemic medicament in preparation, described compound Oleaceran structure is as shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310647545.7A CN103638006B (en) | 2013-12-04 | 2013-12-04 | Application of Oleaceran in medicine for lowering blood glucose |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310647545.7A CN103638006B (en) | 2013-12-04 | 2013-12-04 | Application of Oleaceran in medicine for lowering blood glucose |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103638006A CN103638006A (en) | 2014-03-19 |
| CN103638006B true CN103638006B (en) | 2015-04-22 |
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|---|---|---|---|
| CN201310647545.7A Expired - Fee Related CN103638006B (en) | 2013-12-04 | 2013-12-04 | Application of Oleaceran in medicine for lowering blood glucose |
Country Status (1)
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102895226A (en) * | 2012-10-25 | 2013-01-30 | 南京大学 | Application of Aphanamixoid A in medicines for reducing blood sugar |
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2013
- 2013-12-04 CN CN201310647545.7A patent/CN103638006B/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102895226A (en) * | 2012-10-25 | 2013-01-30 | 南京大学 | Application of Aphanamixoid A in medicines for reducing blood sugar |
Non-Patent Citations (1)
| Title |
|---|
| Oleaceran: A Novel Spiro[isobenzofuran-1,20-naptho[1,8-bc]furan] Isolated from a Terrestrial Streptomyces sp.;Raju R.et al;《ORGANIC LETTERS》;20130626;第15卷(第14期);第3487-3489页 * |
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| Publication number | Publication date |
|---|---|
| CN103638006A (en) | 2014-03-19 |
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Owner name: HAN YING Free format text: FORMER OWNER: CHANGZHOU COLLECTION MEDICAL INSTRUMENT CO., LTD. Effective date: 20150323 Owner name: WANG XIUTAO WANG RENXIANG Effective date: 20150323 |
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Inventor after: Han Ying Inventor after: Wang Xiutao Inventor after: Wang Renxiang Inventor before: Chen Jun |
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Free format text: CORRECT: INVENTOR; FROM: CHEN JUN TO: HAN YING WANG XIUTAO WANG RENXIANG Free format text: CORRECT: ADDRESS; FROM: 213000 CHANGZHOU, JIANGSU PROVINCE TO: 262100 WEIFANG, SHANDONG PROVINCE |
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Effective date of registration: 20171027 Address after: 542800, Hezhou Zijin Mountain Town, Zijin Mountain Town, the Guangxi Zhuang Autonomous Region, 25 Patentee after: Zijin Mountain Hospital of traditional Chinese Medicine Address before: 262100 obstetrics and Gynecology, Anqiu people's Hospital, 246 health Road, Shandong, Weifang, Anqiu Co-patentee before: Wang Xiutao Patentee before: Han Ying Co-patentee before: Wang Renxiang |
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