CN103372018B - The application of Chukrasone A in the medicine of preparation increased platelets counts - Google Patents
The application of Chukrasone A in the medicine of preparation increased platelets counts Download PDFInfo
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- CN103372018B CN103372018B CN201310280779.2A CN201310280779A CN103372018B CN 103372018 B CN103372018 B CN 103372018B CN 201310280779 A CN201310280779 A CN 201310280779A CN 103372018 B CN103372018 B CN 103372018B
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- medicine
- chukrasone
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- chukrasonea
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- 238000002360 preparation method Methods 0.000 title claims abstract description 11
- 239000003814 drug Substances 0.000 title claims abstract description 9
- 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 description 2
- 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
- 206010043554 thrombocytopenia Diseases 0.000 abstract description 9
- 150000001875 compounds Chemical class 0.000 abstract description 7
- 229930187319 chukrasone Natural products 0.000 abstract 2
- 210000001772 blood platelet Anatomy 0.000 description 16
- 241000699670 Mus sp. Species 0.000 description 11
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical group [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 8
- 230000001225 therapeutic effect Effects 0.000 description 8
- 241000699666 Mus <mouse, genus> Species 0.000 description 5
- 210000004369 blood Anatomy 0.000 description 5
- 239000008280 blood Substances 0.000 description 5
- 230000000694 effects Effects 0.000 description 4
- 210000005259 peripheral blood Anatomy 0.000 description 4
- 239000011886 peripheral blood Substances 0.000 description 4
- 229910019142 PO4 Inorganic materials 0.000 description 3
- 230000002607 hemopoietic effect Effects 0.000 description 3
- 239000010452 phosphate Substances 0.000 description 3
- -1 phosphate amine Chemical class 0.000 description 3
- 230000003582 thrombocytopenic effect Effects 0.000 description 3
- 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
- 210000002798 bone marrow cell Anatomy 0.000 description 2
- 239000002775 capsule Substances 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
- 230000002008 hemorrhagic effect Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 230000005855 radiation Effects 0.000 description 2
- 208000001395 Acute radiation syndrome Diseases 0.000 description 1
- 206010062713 Haemorrhagic diathesis Diseases 0.000 description 1
- 102000004257 Potassium Channel Human genes 0.000 description 1
- 206010068142 Radiation sickness syndrome Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 210000001185 bone marrow Anatomy 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000015271 coagulation Effects 0.000 description 1
- 238000005345 coagulation Methods 0.000 description 1
- 238000003255 drug test Methods 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 208000031169 hemorrhagic disease Diseases 0.000 description 1
- 230000023597 hemostasis 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
- 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
- 238000011084 recovery Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000000630 rising effect Effects 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 210000000689 upper leg Anatomy 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Abstract
Do you the present invention relates to a kind of Compound C hukrasone? the novelty teabag of A in pharmaceutical field.Do you the present invention relates to Chukrasone? the application of A in the medicine of preparation increased platelets counts.The Chukrasone that the present invention relates to? the purposes of A in preparation treatment thrombocytopenia medicine belongs to first public, because framework types belongs to brand-new framework types, and its treatment thrombocytopenia is active unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for thrombocytopenia obviously has significant progress.
Description
Technical field
The present invention relates to the novelty teabag of a kind of Compound C hukrasoneA in pharmaceutical field.
Background technology
The Compound C hukrasoneA that the present invention relates to is one and delivers (Liu in 2012, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (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.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (17), 4438 – 4441.), the purposes of the ChukrasoneA that the present invention relates in preparation treatment thrombocytopenia medicine is belonged to first public, because framework types belongs to brand-new framework types, and its treatment thrombocytopenia is active unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for thrombocytopenia obviously has significant progress.
Summary of the invention
The object of the present invention is to provide the new application of ChukrasoneA in pharmaceutical field.
The present invention relates to ChukrasoneA as the application in the medicine of preparation increased platelets counts.
Described Compound C hukrasoneA structure is as shown in formula I:
The purposes of the ChukrasoneA that the present invention relates in preparation treatment thrombocytopenia medicine belongs to first public, because framework types belongs to brand-new framework types, and its treatment thrombocytopenia is active unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for thrombocytopenia obviously has significant progress.
Detailed description of the invention
The preparation method of Compound C hukrasoneA involved in the present invention is see document (Liu, H.B.etal., 2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBloc kerswithNewSkeletonsfromChukrasiatabularis.OrganicLetter s14 (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 hukrasoneA tablet involved in the present invention:
Get 20 g of compound ChukrasoneA, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of Compound C hukrasoneA capsule involved in the present invention:
Get 20 g of compound ChukrasoneA, 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 ChukrasoneA and result below.
The hemoposieis of ChukrasoneA:
One, ChukrasoneA oral administration is on the impact of mouse peripheral blood platelet counts
Method: Balb/c mice 40,18-22g is female.Be divided into three groups by body weight, be respectively normal control, ChukrasoneA1mg/kg, ChukrasoneA2mg/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 1ChukrasoneA oral administration is on the impact (n=10) of mouse peripheral blood platelet counts
Compare with normal saline group: * p<0.5**p<0.01***pLEssT.LTssT.L T0.001
Result: hematoblastic major function is for participating in hemostasis.Platelet counts and dysfunction can cause bleeding tendency.Table 1 shows the impact of ChukrasoneA oral administration on rat peripheral blood platelet counts.Can find out, compare with normal saline group platelet count, namely administration group platelet counts has rising in 3-7 days upon administration, within 10-14 days, has a more obvious elevation process.
These results show, the ChukrasoneA oral administration of doses can increase rat peripheral blood platelet counts, and this is one of ChukrasoneA curative effect playing its hemoposieis.
Two, ChukrasoneA 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 2ChukrasoneA is to because of thrombocytopenic therapeutical effect caused by losing blood
Compare with model group: * p<0.05**p<0.01***pLEssT.LTssT. LT0.001
Result shows, blood-letting mice is after taking ChukrasoneA and treating 7 days, and 2 administration groups compare respectively at model group, and its platelet value is significantly higher than model group, and has exceeded the level of normal saline group mice.
Three, ChukrasoneA 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 platelet, gets femur bone marrow counting number of nucleated cells.
Table 3ChukrasoneA is to the thrombocytopenic therapeutical effect of caused by cyclophosphamide
Compare with normal saline group: * p<0.05
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, ChukrasoneA group compares with model group, all obviously can resist cycli phosphate amine induced mice platelet cell and decline, and prompting this product has the effect improving hemopoietic function.
Four, ChukrasoneA therapeutical effect that coagulation function caused by radiation is reduced
For the therapeutical effect of research to acute radiation sickness, the ChukrasoneA observing various dose irradiates the impact of mouse hemopoietic recovery on 6.5Gy.
Table 4ChukrasoneA is to thrombocytopenic therapeutical effect (the 10th day) caused by radiation
Compare with modeling group: * p<0.05**p<0.01***pLEssT.LTssT. LT0.001
Result shows, give and being subject to according to after mice ChukrasoneA0.5 and 2.0mg/kg every day treatment, hematoblastic Restoration model is accelerated, and is good with 2.0mg/kg dosage group effect.
Conclusion: ChukrasoneA can remarkable increased platelets counts, can be used for preparing the medicine of increased platelets counts.
Claims (1)
1.ChukrasoneA preparation increased platelets counts medicine in application, described Compound C hukrasoneA structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310280779.2A CN103372018B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone A in the medicine of preparation increased platelets counts |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310280779.2A CN103372018B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone A in the medicine of preparation increased platelets counts |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103372018A CN103372018A (en) | 2013-10-30 |
| CN103372018B true CN103372018B (en) | 2015-11-25 |
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| CN201310280779.2A Expired - Fee Related CN103372018B (en) | 2013-07-04 | 2013-07-04 | The application of Chukrasone A in the medicine of preparation increased platelets counts |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1593436A (en) * | 2003-09-08 | 2005-03-16 | 成都地奥制药集团有限公司 | Application of ursane type triterpenoid saponin in the preparing process of leucocyte and/or platelet increasing medicine |
-
2013
- 2013-07-04 CN CN201310280779.2A patent/CN103372018B/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1593436A (en) * | 2003-09-08 | 2005-03-16 | 成都地奥制药集团有限公司 | Application of ursane type triterpenoid saponin in the preparing process of leucocyte and/or platelet increasing medicine |
Non-Patent Citations (1)
| Title |
|---|
| Chukrasone A and B: Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis;Liu,H.B.et al.;《Organic Letters》;20121231;第14卷(第17期);第4438–4441页 * |
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| Publication number | Publication date |
|---|---|
| CN103372018A (en) | 2013-10-30 |
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Effective date of registration: 20151027 Address after: 266000 Licang, Qingdao, No. nine East water road, No. 320, No. Applicant after: Gu Xiangmao Address before: 210009 Gulou District, Jiangsu, Nanjing Gu Ping Kong, No. 4 Applicant before: Ding Shengyu |
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| CB03 | Change of inventor or designer information |
Inventor after: Liu Honglei Inventor after: Wang Jian Inventor before: Ding Shengyu |
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Effective date of registration: 20170112 Address after: No. 262400 Shandong city of Weifang province Changle County Street No. 110, building 2, unit 2, Room 201 Patentee after: Liu Honglei Address before: 266000 Licang, Qingdao, No. nine East water road, No. 320, No. Patentee before: Gu Xiangmao |
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Inventor after: Zhou Xuemei Inventor after: Sun Yurong Inventor before: Liu Honglei Inventor before: Wang Jian |
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Effective date of registration: 20170329 Address after: The government of Shandong Province Huang Qi Bao Zhen Street 262100 Weifang city Anqiu City, No. 19 Building 1, unit 2, No. 404 Patentee after: Zhou Xuemei Address before: No. 262400 Shandong city of Weifang province Changle County Street No. 110, building 2, unit 2, Room 201 Patentee before: Liu Honglei |
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