CN106727538A - A kind of pharmaceutical composition for treating diabetes B - Google Patents
A kind of pharmaceutical composition for treating diabetes B Download PDFInfo
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- CN106727538A CN106727538A CN201710091022.7A CN201710091022A CN106727538A CN 106727538 A CN106727538 A CN 106727538A CN 201710091022 A CN201710091022 A CN 201710091022A CN 106727538 A CN106727538 A CN 106727538A
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- pharmaceutical composition
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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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Investigating Or Analysing Biological Materials (AREA)
Abstract
The present invention relates to a kind of pharmaceutical composition for treating diabetes B, compound of the described pharmaceutical composition comprising following formula or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier：Wherein R1 independently selected from：Halogen or alkyl.Medicine of the present invention can effectively reduce the blood sugar level of diabetes B patient, be had certain effect for control blood sugar, be expected to turn into the new drug for the treatment of diabetes B.
Description
Technical field
The present invention relates to field of medicaments, specifically, the present invention relates to a kind of pharmaceutical composition for treating diabetes B.
Background technology
The various clinical forms of known diabetes, most commonly 2 types and type 1 diabetes.People's diabetes B is by being related to
It is chronic and gradual caused by the complicated Pathological Physiology of insulin resistance and the dual endocrine defects for weakening insulin secretion
Disease, middle and advanced stage is often accompanied by one or more chronic complicating diseases, and most of patients can use in early metaphase and keep on a diet and orally-taken blood sugar reducing
Medicine controls blood sugar, and some people are not required to rely on insulin therapy and survive throughout one's life, but have a big chunk patient to be still needed in the middle and later periods
Giving exogenous insulin supplement could control blood sugar.
The content of the invention
It is an object of the invention to provide a kind of pharmaceutical composition for treating diabetes B.
In order to realize the purpose of the present invention, the present invention provides a kind of pharmaceutical composition for treating diabetes B, the medicine
Compound of the composition comprising following formula or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier：
Wherein
R1 independently selected from：Halogen or alkyl.
Preferably, R1 is CH3。
The present invention also provides purposes of the compound in the medicine for preparing treatment diabetes B, under the compound has
Array structure：
Wherein
R1 independently selected from：Halogen or alkyl.
Preferably, R1 is CH3。
Medicine of the present invention can effectively reduce the blood sugar level of diabetes B patient, have certain work for control blood sugar
With, be expected to turn into treatment diabetes B new drug.
Brief description of the drawings
Fig. 1 is OGTT curves and OGTT TG-AUCs.
Fig. 2 is each group mouse pathological examination.
A. normal group；B. model group；C. low dose group；D. high dose group.
Fig. 3 is the cleaved caspase-3 of Immunofluorescence test hepatic tissue.
A. normal group；B. model group；C. low dose group；D. high dose group.
Specific embodiment
It will be appreciated by those skilled in the art that the concept and specific embodiment disclosed in description above can be easy to
With making an amendment or design the basis of the other embodiment for implementing identical purpose of the invention.What those skilled in the art also will be understood that
It is that these equivalent implementation methods are without departing from the spirit and scope of the present invention illustrated in appended claims.
The sign of the medicine of the present invention of experimental example 1
1H-NMR (400MHz, CDC13) δ 9.03 (1H, d), 8.00 (1H, s), 7.48 (1H, d), 7.26 (1H, with solvent
Signal merges), 7.09-7.21 (3H, m), 6.90 (1H, d), 4.73 (1H, t), 4.38-4.43 (4H, m), 4.26 (1H, d),
3.42 (1H, m), 1.85-1.87 (2H, m), 1.54-1.57 (1H merges with solvents signals), 1.43 (3H, t), 1.23-1.32
(3H,m),0.99-1.14(4H,m)
Therapeutic effect of the medicine of the present invention of experimental example 2 for diabetes B
Selection SD rats 80, after adaptability is fed 1 week, wherein 65 high fat diets are after 4 weeks, intraperitoneal injection 100mg/kg
Streptozotocin (STZ) replicates diabetes B mouse model, and fasting blood-glucose is detected after 4 weeks, chooses blood sugar in 7.8~15mmol/L
45 mouse include and test and be randomly divided into 3 groups, i.e. model group, medicine low dose group of the present invention, medicine high dose of the present invention
Group, remaining 15 normal mouse is used as normal group.The μ gkg of medicine low dose group of the present invention hypodermic injection 50-1·d-1, the present invention
The μ gkg of medicine high dose group hypodermic injection 100-1·d-1, normal group and the μ gkg of model group hypodermic injection physiological saline 100-1·d-1.After being administered 4 weeks, pluck eyeball and take blood, 3500r/min centrifugation 15min, draw supernatant be stored in it is stand-by in -80 DEG C of refrigerators.
Separate a liver part and be stored in -80 DEG C of refrigerators, a part is fixed on stand-by in 10% formalin.
The measure of biochemical indicator
After mouse fasting 12h, orbital venous plexus take blood, detection fasting blood-glucose (FBG), TC, TG, HDL-C, LDL-C, ALT
And AST contents.
Oral glucose tolerance test (OGTT)
OGTT is carried out after being administered 4 weeks, after all mouse overnight fastings, 40% glucose (2g/kg) treatment is given, respectively at
0min, 30min, 60min, 90min and 120min orbital venous plexus take blood sample, 3500r/min centrifugation 15min to draw supernatant
For determining blood sugar.
HE is dyeed
Routine paraffin wax embedding, section after the hepatic tissue dehydration that will be fixed in 10% formalin.Section is de- through dimethylbenzene
Wax, graded ethanol aquation, eosin stains, haematoxylin redyeing, serial dehydration, dimethylbenzene is transparent, resin mounting, light Microscopic observation,
Carry out pathological analysis.
The cleavedcaspase-3 of Immunofluorescence test hepatic tissue
Routine paraffin wax embedding, section after the hepatic tissue dehydration that will be fixed in 10% formaldehyde.The following treatment of section：Dimethylbenzene
Dewaxing, graded ethanol rehydration, PBS is washed 5min3 times, and 5%~10% lowlenthal serum is incubated at room temperature 30min, and 0.3%TritonX beats
Hole, the anti-cleavedcaspase-3 (1 of I:100) overnight incubation, PBS is washed 5min3 times, fluorescence II anti-(1:200) room temperature lucifuge is incubated
120min is educated, PBS washes 5min 3 times, the room temperature lucifuges of Hoechst 33342 dye 120min, PBS is washed 5min3 times, and mounting is micro-
Microscopic observation.
Statistical procedures
Statistical procedures measurement data represented with mean ± standard error, and data statistics is carried out using SPSS17.0 softwares.
Compare between group using one-way analysis of variance (one-way ANOVA), compare two-by-two using SNK-q inspections, be side with P ＜ 0.05
Difference is statistically significant.
The change of each group mice serum biochemical indicator
Compared with normal group, model group mouse blood sugar level significantly raises (P ＜ 0.01), and lipid-metabolism serious diseases are blood
TC, TG, LDL-C, ALT and AST content are significantly raised (P ＜ 0.01) in clear, and HDL-C contents are significantly reduced (P ＜ 0.05)；With mould
Type group compares, and medicine high and low dose group mouse fasting blood-glucose of the present invention substantially reduces (P ＜ 0.05), and disorders of lipid metabolism is obtained
Certain to improve, i.e., TC, TG, LDL-C, ALT and AST content substantially reduce (P ＜ 0.05) in serum, and HDL-C contents are significantly raised
(P ＜ 0.05), and in dose dependent, it is shown in Table 1.
Table 1
* P ＜ 0.05, * * P ＜ 0.01vs normal groups；#P ＜ 0.05,##P ＜ 0.01vs model groups
Glucose tolerance test
Normal group, model group and medicine high and low dose group mouse blood sugar of the present invention reach after glucose 30min is given
To peak value, then decline.Compared with normal group, model group mouse blood sugar is at each time point in high-level state；With model group ratio
Compared with, medicine high and low dose group mouse blood sugar level of the present invention is decreased significantly, and in dose dependent.TG-AUC is calculated
Result also display model group apparently higher than normal group, and administration group is significantly lower than model group (P ＜ 0.05), sees Fig. 1.
The influence that medicine of the present invention changes to diabetic mice liver histopathology
Normal group murine liver tissue structure is normal, hepatic cell cords, sinus hepaticus queueing discipline, and lobuli hepatis boundary is obvious, and liver is thin
Born of the same parents' kytoplasm is uniform, without particle, fat, fibre modification etc.；And model group murine liver tissue structure disturbance, hepatic cell cords, sinus hepaticus row
Row are irregular, liver cell enlargement, slight deformation；Administration group murine liver tissue tends to normal, and hepatic cell cords, sinus hepaticus arrangement are relatively advised
Then, and the therapeutic action of high dose group be better than low dose group, see Fig. 2.
The change of Immunofluorescence test hepatic tissue cleaved caspase-3
Compare with normal group, model group murine liver tissue green fluorescence intensity is remarkably reinforced, and cleaved caspase-3 are bright
It is aobvious to increase；Compare with model group, medicine high and low dose group murine liver tissue green fluorescence intensity of the present invention substantially weakens,
Cleaved caspase-3 are substantially reduced, and in dose dependent, see Fig. 3.
Claims (5)
1. a kind of pharmaceutical composition for treating diabetes B, it is characterised in that compound of the described pharmaceutical composition comprising following formula
Or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier：
Wherein
R1 independently selected from：Halogen or alkyl.
2. it is according to claim 1 treatment diabetes B pharmaceutical composition, it is characterised in that R1 is CH3。
3. it is according to claim 2 treatment diabetes B pharmaceutical composition, it is characterised in that can further be made
Any form of preparation.
4. compound prepare treatment diabetes B medicine in purposes, it is characterised in that the compound has following knot
Structure：
Wherein
R1 independently selected from：Halogen or alkyl.
5. purposes according to claim 4, it is characterised in that R1 is CH3。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710091022.7A CN106727538A (en) | 2017-02-20 | 2017-02-20 | A kind of pharmaceutical composition for treating diabetes B |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710091022.7A CN106727538A (en) | 2017-02-20 | 2017-02-20 | A kind of pharmaceutical composition for treating diabetes B |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106727538A true CN106727538A (en) | 2017-05-31 |
Family
ID=58958337
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710091022.7A Withdrawn CN106727538A (en) | 2017-02-20 | 2017-02-20 | A kind of pharmaceutical composition for treating diabetes B |
Country Status (1)
| Country | Link |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106414458A (en) * | 2014-03-27 | 2017-02-15 | 托伦特药物有限公司 | Novel fused imidazobenzothiazole compounds |
-
2017
- 2017-02-20 CN CN201710091022.7A patent/CN106727538A/en not_active Withdrawn
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106414458A (en) * | 2014-03-27 | 2017-02-15 | 托伦特药物有限公司 | Novel fused imidazobenzothiazole compounds |
Non-Patent Citations (1)
| Title |
|---|
| ZHENQIN LIU ET AL.: "p38 Mitogen-Activated Protein Kinase: A Critical Node Linking Insulin Resistance and Cardiovascular Disease in Type 2 Diabetes Mellitus", 《ENDOCRINE, METABOLIC & IMMUNE DISORDRS-DRUG TARGETS》 * |
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