CN103142626B - Application of triacetyl glucal in preparation of antitumor drug - Google Patents
Application of triacetyl glucal in preparation of antitumor drug Download PDFInfo
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- CN103142626B CN103142626B CN201310088363.0A CN201310088363A CN103142626B CN 103142626 B CN103142626 B CN 103142626B CN 201310088363 A CN201310088363 A CN 201310088363A CN 103142626 B CN103142626 B CN 103142626B
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Abstract
The invention provides application of triacetyl glucal in the preparation of drugs and particularly provides application of triacetyl glucal in the preparation of a hypoglycemic, antiviral or antitumor drug. According to the application, shown by the determination of animals or MIC (Minimal Inhibitory Concentration), triacetyl glucal has hypoglycemic, antiviral or antitumor actions. According to the application, the drug is prepared from triacetyl glucal serving as an active ingredient, and a conventional pharmaceutical excipient by conventional methods and is of oral tablets, capsules, oral liquid or granules or percutaneous absorption injections or patches. Triacetyl glucal has a high practical value in the field of medicines.
Description
Present patent application is number of patent application 201010232434.6, invention and created name: triacetyl glucal is preparing the divisional application of the application in medicine.
Technical field
The present invention relates to pharmaceutical chemistry.Be specifically related to triacetyl glucal in the application of preparing in medicine.Relate in particular to triacetyl glucal in the application of preparing in blood sugar lowering, antiviral and antitumor drug.
Background technology
Carbohydrate chemistry and glycobiology have now become forward position and the hot fields of life sciences, and saccharide not only forms as the energy or structure in organism, and is undertaking very important biological function.Oligosaccharide in saccharide complex is the informational molecule in body, and to the generation of human diseases, development and prognosis play an important role, and are the important medicines of a class simultaneously.
The inventor studies and finds that the major function of saccharide medicine has following several respects: improve immunocompetence, hypoglycemic effect, radiation resistance, antivirus action, resisting rheumatoid disease arthritis etc.Because triacetyl glucal is anti-metabolism antibiotic, there is again the effect of blood sugar lowering, antiviral and antitumor etc., therefore, can be used for pre-anti-virus and pathogenic bacterial infection, prevent influenza virus, the infectious disease that hepatitis virus causes, and blood sugar lowering and antitumor etc.Triacetyl glucal can effectively reduce and delay arteriosclerosis, hypertension, heart disease, the incidence rate of the diseases such as diabetes and disease time.But, yet there are no up to now relevant report triacetyl glucose at blood sugar lowering, the application of antiviral and anti-tumor aspect.
Summary of the invention
Technical problem to be solved by this invention is to overcome above-mentioned weak point, and design triacetyl glucose is in the application of preparing aspect blood sugar lowering, defying age, antiviral or antitumor drug.
The invention provides triacetyl glucal in the application of preparing in medicine, particularly, provide triacetyl glucal in the application of preparing blood sugar lowering, antiviral or antitumor drug.
Another object of the present invention has been to provide triacetyl glucal in the application of preparing in hypoglycemic drug.Triacetyl glucose reduces blood glucose by restriction carbohydrate metabolism, can be as the medicine of preparation treatment diabetes.
Another object of the present invention has been to provide the application of triacetyl glucal in preparation antiviral drugs.Triacetyl glucal can suppress viral infection, is natural antimetabolite class antibiotic, has multiple physiological and pharmacological effect, can suppress viral glycoprotein synthetic, changes wherein polysaccharide structures, causes virus to lose appeal, thereby reduces virus breeding.This compound can be prepared as antiviral agent, conventionally herpesvirus, influenza virus is had to activity.
A further object of the invention has been to provide triacetyl glucal in the application of preparing in antitumor drug.
Medicine of the present invention refers to injection or the patch that oral tablet, capsule, oral liquid or granule that triacetyl glucal is made according to a conventional method as active component and conventional pharmaceutic adjuvant or percutaneous absorb.
The present invention is through the mensuration of animal or MIC, the impact of triacetyl glucal on diabetic mice due to alloxan, impact on diabetes rat due to streptozotocin STZ, impact on diabetic mice due to alloxan, result all shows to have blood sugar reducing function.Triacetyl glucal is to Madin-Darby canine kidney(cell line) (MDCK) (MDCK) and Parainfluenza type 1 virus (HVJ) cell and the toxicity test to mdck cell, and result is showed no mdck cell is caused to cytopathy in the concentration range of 0.01～10mg/mL.The impact of triacetyl glucal on pathological changes caused by virus effect, triacetyl glucal variable concentrations all has obvious inhibitory action to pathological changes caused by virus.Triacetyl glucal anti-tumor biological body outer screening test, result demonstration, triacetyl glucal all has potent to BEL-7402 people's hepatocarcinoma, P338 mouse leukemia, A-549 human lung adenocarcinoma.
The above results explanation triacetyl glucal has blood sugar lowering, antiviral or antitumor action, can be used for preparing blood sugar lowering, antiviral or antitumor drug, has larger practical value at field of medicaments.
Detailed description of the invention
Triacetyl glucal is commercially available
Purchase in Shanghai Shengyao Biological Technology Co., Ltd.
CAS：2873-29-2
Specification: 5g/ bottle
Purity: 99%
Following examples 1-3 all tests with the commercially available triacetyl glucal obtaining.
Embodiment 1
The impact of triacetyl glucal on diabetic mice due to alloxan
Testing program: get Kunming mouse, after fasting 12h, tail vein injection alloxan 80mg/kg, after 3 days, survey blood glucose, get the above person of blood glucose 11.2～22.4mmol/L and be divided at random model control group and triacetyl glucal group, as Normal group tail vein injection saline 0.2ral/ only separately get 10, every group is 10.Triacetyl glucal group is gastric infusion, and every day 1 time, dosage is respectively 125,250mg/kg body weight; Model control group and Normal group give sterile purified water.After successive administration 14 days, tail venous blood sampling is surveyed blood glucose, and the body weight of blood mice on the same day got in record simultaneously, the consumption of drinking-water and feedstuff.
The impact of triacetyl glucal on diabetic mice due to alloxan (± s)
Result shows to have blood sugar reducing function.
The impact of triacetyl glucal on diabetes rat due to streptozotocin STZ
Experimental program: get Wistar rat, after fasting 12h, lumbar injection streptozotocin 50mg/kg, separately gets 10 rats as Normal group, the heavy normal saline of lumbar injection consubstantiality.After 10 days, get blood glucose 16.8～28mmol/L person, be divided at random model control group by blood glucose value, insoral group and triacetyl glucal group, 10 every group.Insoral group is gastric infusion, every day 1 time, and successive administration 14 days, dosage is 100mg/kg body weight; Triacetyl glucal group gastric infusion, every day 1 time, successive administration 14 days, dosage is 250mg/kg body weight; Model control group and Normal group give sterile purified water.Duration of test the 7th, 15,30 and 45 days, tail venous blood sampling was surveyed change of blood sugar, and record is got the body weight of blood rat on the same day, drinking-water and feed consumption.Result shows to have blood sugar reducing function.
The impact of triacetyl glucal on diabetic mice due to alloxan (± s)
Result shows that triacetyl glucal has blood sugar reducing function.
Embodiment 2
Triacetyl glucal antiviral activity
Strain: Madin-Darby canine kidney(cell line) (MDCK) (MDCK) and Parainfluenza type 1 virus (HVJ) cell and the toxicity test to mdck cell
Triacetyl glucal is mixed with to the medicinal liquid of 20mg/mL concentration with distilled water, filtration sterilization, and be diluted to different concentration with cell maintenance medium.By mdck cell digestion in bottle, be inoculated in 96 porocyte culture plates, put 37 DEG C, in 5%CO2 incubator, cultivate 2d, after growing up to cell monolayer, remove original fluid, add the medicinal liquid 100 μ L of different diluted concentrations, and establish the cell contrast that only adds 100 μ L maintenance mediums, each concentration is all established 4 multiple holes, put in incubator and continue to cultivate, every daily inverted microscope is observed the cytopathic effect (CPE) of medicine, represent 0%CPE with "-", "+" represents 1%～25%CPE, ++ represent 25%～50%CPE, +++ represent 50%～75%CPE, ++++represent 75%～100%CPE.
Result: result triacetyl glucal is showed no mdck cell is caused to cytopathy in the concentration range of 0.01～10mg/mL.
The impact of triacetyl glucal on pathological changes caused by virus effect
HVJ parainfluenza virus Embryo Gallus domesticus goes down to posterity, and carries out titration before experiment, and getting 100TCID50 is infective dose.Be " synthetic method " according to different 3 kinds of scheme: A of medication design, the parainfluenza virus of triacetyl glucal 100,30,10 μ g/ml and 100TCID50 adds cell simultaneously; B is " prophylaxis ", and TRH-02, with the first function cells of concentration of 100,30,10 μ g/ml, adds 100TCID50 parainfluenza virus again after 24h; C is " neutralisation ", and the parainfluenza virus that triacetyl glucal 100,30,10 μ g/ml are added to 100TCID50 is put 4 DEG C and spends the night, d2 inoculating cell.Establish cell matched group, virus control group and positive drug (ribavirin 100 μ g/ml) matched group simultaneously.After application of sample completes, put 37 DEG C, the cultivation of 5%CO2 incubator, observe CPE every day, represent 0%CPE with "-", "+" represents 1%～25%CPE, ++ represent 25%～50%CPE, +++ represent 50%～75%CPE, ++++expression 75%～100%CPE.When virus control group occurs ++++, and cell matched group is when normal, records the CPE in each hole.
Result: as shown above, ribavirin 100 μ g/ml3 kind medications all can suppress the cytopathy that parainfluenza virus causes completely, triacetyl glucal variable concentrations all has obvious inhibitory action to pathological changes caused by virus, but different slightly difference of medication inhibitory action, wherein synthetic method inhibitory action is the strongest.
Embodiment 3
Triacetyl glucal anti-tumor biological body outer screening test
Screening technique: tetrazolium (Methyl-Thiazol-Tetrozlium, MTT reducing process)
Sulphonyl rhodamine B (sulforhodamine B, SRB) albumen beam color method.
Cell strain: BEL-7402 people's hepatocarcinoma, P338 mouse leukemia, A-549 human lung adenocarcinoma
Action time: 72 hours
Result evaluation: invalid: 10
-5mol/L < 85%;
Weak effect: 10
-5mol/L>=85% or 10
-6mol/L > 50%;
Potent: 10
-6mol/L>=85% or 10
-7mol/L > 50%.
Following table result shows the suppression ratio % of triacetyl glucal to growth of tumour cell
Note: in following table, administration group is and gives triacetyl glucal.
According to result of the test demonstration above, triacetyl glucal all has potent to BEL-7402 people's hepatocarcinoma, P338 mouse leukemia, A-549 human lung adenocarcinoma.
Claims (2)
1. triacetyl glucal is in the application of preparing in antitumor drug; It is characterized in that, described in be applied as the application in anti-BEL-7402 people's hepatocarcinoma, P338 mouse leukemia or A-549 human lung adenocarcinoma medicine in preparation of triacetyl glucal.
2. application according to claim 1, is characterized in that injection or patch that described medicine oral tablet, capsule, oral liquid or granule that to be triacetyl glucal make according to a conventional method as active component and conventional pharmaceutic adjuvant or percutaneous absorb.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310088363.0A CN103142626B (en) | 2010-07-21 | 2010-07-21 | Application of triacetyl glucal in preparation of antitumor drug |
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| CN201310088363.0A CN103142626B (en) | 2010-07-21 | 2010-07-21 | Application of triacetyl glucal in preparation of antitumor drug |
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| CN 201010232434 Division CN102335182B (en) | 2010-07-21 | 2010-07-21 | Application of triacetylglucal in medicine preparation |
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| CN103142626A CN103142626A (en) | 2013-06-12 |
| CN103142626B true CN103142626B (en) | 2014-08-20 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5622936A (en) * | 1988-10-20 | 1997-04-22 | Deutsches Krebsforschungszentrum Stiftung Des Offentlichen Rechts | Tumor inhibiting saccharide conjugates |
| CN1803818A (en) * | 2005-12-30 | 2006-07-19 | 江苏汉发贸易发展有限公司 | Method for preparing acetylated glucal |
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2010
- 2010-07-21 CN CN201310088363.0A patent/CN103142626B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5622936A (en) * | 1988-10-20 | 1997-04-22 | Deutsches Krebsforschungszentrum Stiftung Des Offentlichen Rechts | Tumor inhibiting saccharide conjugates |
| CN1803818A (en) * | 2005-12-30 | 2006-07-19 | 江苏汉发贸易发展有限公司 | Method for preparing acetylated glucal |
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| CN103142626A (en) | 2013-06-12 |
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