CN103356642B - The application of Chukrasone A in the medicine preparing leukocyte increasing - Google Patents
The application of Chukrasone A in the medicine preparing leukocyte increasing Download PDFInfo
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- CN103356642B CN103356642B CN201310278072.8A CN201310278072A CN103356642B CN 103356642 B CN103356642 B CN 103356642B CN 201310278072 A CN201310278072 A CN 201310278072A CN 103356642 B CN103356642 B CN 103356642B
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- HZUBWSRMDOJYPS-WPCVKUBSSA-N chukrasone A Natural products C=1([C@@H]2OC(=O)C[C@H]3[C@@]4(O)[C@H](O)C(=O)[C@@]5(O)[C@@H](OC(=O)C(C)C)C(C)(C)[C@@H]([C@]5([C@H]4[C@H](OC(C)=O)C[C@]32C)C)CC(=O)OC)C=COC=1 HZUBWSRMDOJYPS-WPCVKUBSSA-N 0.000 title claims abstract description 25
- 210000000265 leukocyte Anatomy 0.000 title claims abstract description 18
- 239000003814 drug Substances 0.000 title claims abstract description 9
- LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 claims abstract description 8
- 150000001875 compounds Chemical class 0.000 abstract description 7
- 230000000694 effects Effects 0.000 abstract description 6
- 238000002360 preparation method Methods 0.000 abstract description 6
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 12
- 241000699670 Mus sp. Species 0.000 description 11
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical group [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 9
- 230000001225 therapeutic effect Effects 0.000 description 7
- 210000004369 blood Anatomy 0.000 description 6
- 239000008280 blood Substances 0.000 description 6
- 241000699666 Mus <mouse, genus> Species 0.000 description 5
- 108010087141 Kv1.2 Potassium Channel Proteins 0.000 description 3
- 102000006628 Kv1.2 Potassium Channel Human genes 0.000 description 3
- 229910019142 PO4 Inorganic materials 0.000 description 3
- 229930187319 chukrasone Natural products 0.000 description 3
- 230000000610 leukopenic effect Effects 0.000 description 3
- 239000010452 phosphate Substances 0.000 description 3
- -1 phosphate amine Chemical class 0.000 description 3
- 239000003450 potassium channel blocker Substances 0.000 description 3
- 208000032467 Aplastic anaemia Diseases 0.000 description 2
- 241001156380 Chukrasia tabularis Species 0.000 description 2
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 210000001185 bone marrow Anatomy 0.000 description 2
- 210000002798 bone marrow cell Anatomy 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 229960004397 cyclophosphamide Drugs 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 230000003203 everyday effect Effects 0.000 description 2
- 230000002607 hemopoietic effect Effects 0.000 description 2
- 230000002008 hemorrhagic effect Effects 0.000 description 2
- 210000005259 peripheral blood Anatomy 0.000 description 2
- 239000011886 peripheral blood Substances 0.000 description 2
- 210000000689 upper leg Anatomy 0.000 description 2
- 0 C*C(CC(C(C)(C)C1OC(C(C)C)=O)C(C)([C@@](C(CC(C)(C(c2c[o]cc2)O2)[C@@]3CC2=O)OC(C)=O)C3(C(C2=O)O)O)C12O)=O Chemical compound C*C(CC(C(C)(C)C1OC(C(C)C)=O)C(C)([C@@](C(CC(C)(C(c2c[o]cc2)O2)[C@@]3CC2=O)OC(C)=O)C3(C(C2=O)O)O)C12O)=O 0.000 description 1
- 238000012449 Kunming mouse Methods 0.000 description 1
- 206010033661 Pancytopenia Diseases 0.000 description 1
- 102000004257 Potassium Channel Human genes 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 208000024389 cytopenia Diseases 0.000 description 1
- 238000003255 drug test Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 201000002364 leukopenia Diseases 0.000 description 1
- 231100001022 leukopenia Toxicity 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 210000004976 peripheral blood cell Anatomy 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 108020001213 potassium channel Proteins 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to the novelty teabag of a kind of Compound C hukrasone A in pharmaceutical field.The present invention relates to the application of Chukrasone A in the medicine preparing leukocyte increasing.The purposes of the Chukrasone A that the present invention relates in preparation treatment low leukocyte counts medicine belongs to first public, because framework types belongs to brand-new framework types, and it is unexpectedly strong for low leukocyte counts inhibit activities, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for low leukocyte counts obviously has significant progress.
Description
Technical field
The present invention relates to the novelty teabag of a kind of Compound C hukrasone A in pharmaceutical field.
Background technology
The Compound C hukrasone A that the present invention relates to is one and delivers (Liu in 2012, H.B.et al., 2012.Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers withNew Skeletons from Chukrasia tabularis.Organic Letters 14 (17), 4438 – 4441.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to potassium-channel inhibit activities (Liu, H.B.et al., 2012.Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers with New Skeletons fromChukrasia tabularis.Organic Letters 14 (17), 4438 – 4441.), the purposes of the Chukrasone A that the present invention relates in preparation treatment low leukocyte counts medicine is belonged to first public, because framework types belongs to brand-new framework types, and it is unexpectedly strong for low leukocyte counts inhibit activities, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for low leukocyte counts obviously has significant progress.
Summary of the invention
The object of the present invention is to provide the new application of Chukrasone A in pharmaceutical field.
The present invention relates to Chukrasone A as the application prepared in the medicine of leukocyte increasing.
Described Compound C hukrasone A structure is as shown in formula I:
The purposes of the Chukrasone A that the present invention relates in preparation treatment low leukocyte counts medicine belongs to first public, because framework types belongs to brand-new framework types, and it is unexpectedly strong for low leukocyte counts inhibit activities, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for low leukocyte counts obviously has significant progress.
Detailed description of the invention
The preparation method of Compound C hukrasone A involved in the present invention is see document (Liu, H.B.et al., 2012.Chukrasones A and B:Potential Kv1.2 Potassium Channel Blockers with NewSkeletons from Chukrasia tabularis.Organic Letters 14 (17), 4438 – 4441.).
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 C hukrasone A tablet involved in the present invention:
Get 20 g of compound Chukrasone A, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of Compound C hukrasone A capsule involved in the present invention:
Get 20 g of compound Chukrasone A, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
In order to understand essence of the present invention better, its novelty teabag in pharmaceutical field will be described by the drug test of Chukrasone A and result below.
The hemoposieis of Chukrasone A:
One, the impact of mouse peripheral blood quantity of leucocyte
Method: Balb/c mice 40,18-22g is female.Be divided into 3 groups by body weight, be respectively normal saline group, Chukrasone A 2.0mg/kg, Chukrasone A 4.0mg/kg, within 1st, be divided into twice oral administration, totally 9 times four and half.Within 1 day, 3 days, 7 days, 14 days before administration, after administration, cut tail and get blood 20ul, F-820 platelet count instrument detects hemogram.
Table 1 Chukrasone A is on the impact (n=11) of mouse peripheral blood quantity of leucocyte
Natural law corresponding to normal saline group compares: * p<0.5
Result: compare with normal saline group, two dosage groups all manifest immediately and rise white effect after administration.
Two, Chukrasone A is to the therapeutical effect of post hemorrhagic mice
ICR mice 40 is affected, ♀ ♂ half and half to post hemorrhagic mice, is divided into 4 groups (n=10).Except normal saline group, other group every mice, from orbital vein blood-letting 0.5ml, is got blood survey again and all respectively organizes index after 24h, then continuous gastric infusion 1 week, after last administration 1h, gets the full whole bliid platelet analyzer of blood F-800 survey These parameters from orbital venous plexus.
Table 2 Chukrasone A is to because of caused leukopenic therapeutical effect of losing blood
Compare with model group: * p<0.05**p<0.01***pLEssT.LTssT. LT0.001
Result shows, blood-letting mice is after taking Chukrasone A and treating 7 days, and 2 administration groups compare respectively at model group, and leukocyte is significantly higher than model group, close to normal saline group.
Three, Chukrasone A is to the hypocellular therapeutical effect of cyclophosphamide hyperamization
To the preventive and therapeutic effect ICR mice 40 of mouse bone marrow cells hemopoietic function damage, ♀ ♂ dual-purpose, is divided into 4 groups (n=10), i.e. normal saline group, modeling group, 1.2mg/kg group and 0.6mg/kg group, oral administration, every day 1 time.0th, except normal saline group, other respectively organized mice lumbar injection cycli phosphate amine 80mg/kg respectively, then continued administration 3 days on 5th, 10.1h after last administration, gets blood from orbital venous plexus, surveys leukocyte, gets femur bone marrow counting number of nucleated cells.
Table 3 Chukrasone A is to the leukopenic therapeutical effect of caused by cyclophosphamide
Compare with model group: * p<0.05**p<0.01***pLEssT.LTssT. LT0.001
Result shows, compares with normal saline group, and cycli phosphate amine can make mouse bone marrow cells damage, peripheral blood cells is caused to decline, Chukrasone A group compares with model group, all obviously can resist cycli phosphate amine induced mice leukopenia, and prompting this product has the effect improving hemopoietic function.
Four, Chukrasone A is to leukopenic therapeutical effect caused by benzene
Impact on Induced Aplastic Anemia Mice: Kunming mouse 48, ♀ ♂ dual-purpose, is divided into 4 groups (n=12), except normal saline group, other group mouse subcutaneous injection benzene 0.5ml/kg, continuous 12 days, the same day of modeling, oral administration simultaneously, every day 1 time, totally 18 days, 1h after last administration, orbital venous plexus gets blood, surveys leukocyte, gets femur bone marrow counting number of nucleated cells.
Table 4 Chukrasone A is to the therapeutical effect of cytopenia caused by benzene
Compare with model group: * p<0.05**p<0.01
Result shows, 2 administration groups compare respectively at model group, all obviously can resist the leukocytic decline of Induced Aplastic Anemia Mice caused by benzene.
Conclusion: Chukrasone A can remarkable leukocyte increasing, can be used for preparing anti-leukocyte and reduce medicine.
Claims (1)
- The application of 1.Chukrasone A in the medicine preparing leukocyte increasing, described Compound C hukrasone A structure as formula Ishown in:formula I.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310278072.8A CN103356642B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone A in the medicine preparing leukocyte increasing |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310278072.8A CN103356642B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone A in the medicine preparing leukocyte increasing |
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| Publication Number | Publication Date |
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| CN103356642A CN103356642A (en) | 2013-10-23 |
| CN103356642B true CN103356642B (en) | 2015-08-12 |
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Effective date of registration: 20170417 Address after: 200051 Anshun Road, Shanghai, No. 350, No. Patentee after: Shanghai Institute of Biological Products Co.,Ltd. Address before: 210009 Gulou District, Jiangsu, Nanjing Gu Ping Kong, No. 4 Patentee before: Ding Shengyu |
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