CN103462985B - Application of spirooliganones B in preparation of medicine inhibiting platelet aggregation - Google Patents
Application of spirooliganones B in preparation of medicine inhibiting platelet aggregation Download PDFInfo
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- CN103462985B CN103462985B CN201310466681.6A CN201310466681A CN103462985B CN 103462985 B CN103462985 B CN 103462985B CN 201310466681 A CN201310466681 A CN 201310466681A CN 103462985 B CN103462985 B CN 103462985B
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- Prior art keywords
- spirooliganones
- platelet aggregation
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- application
- inhibiting
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- 229930185169 spirooliganone Natural products 0.000 title claims abstract description 23
- 208000010110 spontaneous platelet aggregation Diseases 0.000 title claims abstract description 20
- 239000003814 drug Substances 0.000 title claims abstract description 16
- 230000002401 inhibitory effect Effects 0.000 title abstract description 6
- 238000002360 preparation method Methods 0.000 title abstract description 6
- 150000001875 compounds Chemical class 0.000 claims description 11
- 230000000694 effects Effects 0.000 abstract description 2
- 239000011159 matrix material Substances 0.000 abstract 1
- 239000003146 anticoagulant agent Substances 0.000 description 6
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 5
- 210000004369 blood Anatomy 0.000 description 5
- 239000008280 blood Substances 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- 239000005552 B01AC04 - Clopidogrel Substances 0.000 description 4
- 229940127219 anticoagulant drug Drugs 0.000 description 4
- GKTWGGQPFAXNFI-HNNXBMFYSA-N clopidogrel Chemical compound C1([C@H](N2CC=3C=CSC=3CC2)C(=O)OC)=CC=CC=C1Cl GKTWGGQPFAXNFI-HNNXBMFYSA-N 0.000 description 4
- 229960003009 clopidogrel Drugs 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 241001302000 Illicium oligandrum Species 0.000 description 3
- 229960001138 acetylsalicylic acid Drugs 0.000 description 3
- 230000000840 anti-viral effect Effects 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 2
- 206010050661 Platelet aggregation inhibition Diseases 0.000 description 2
- 241000700159 Rattus Species 0.000 description 2
- 208000007536 Thrombosis Diseases 0.000 description 2
- 238000004220 aggregation Methods 0.000 description 2
- 230000002776 aggregation Effects 0.000 description 2
- 230000000702 anti-platelet effect Effects 0.000 description 2
- 208000026106 cerebrovascular disease Diseases 0.000 description 2
- 210000004623 platelet-rich plasma Anatomy 0.000 description 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 2
- 206010002383 Angina Pectoris Diseases 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 102000009123 Fibrin Human genes 0.000 description 1
- 108010073385 Fibrin Proteins 0.000 description 1
- BWGVNKXGVNDBDI-UHFFFAOYSA-N Fibrin monomer Chemical compound CNC(=O)CNC(=O)CN BWGVNKXGVNDBDI-UHFFFAOYSA-N 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 241000134304 Influenza A virus H3N2 Species 0.000 description 1
- 241000701076 Macacine alphaherpesvirus 1 Species 0.000 description 1
- 241001597008 Nomeidae Species 0.000 description 1
- QGMRQYFBGABWDR-UHFFFAOYSA-M Pentobarbital sodium Chemical compound [Na+].CCCC(C)C1(CC)C(=O)NC(=O)[N-]C1=O QGMRQYFBGABWDR-UHFFFAOYSA-M 0.000 description 1
- 241000700157 Rattus norvegicus Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 229940127218 antiplatelet drug Drugs 0.000 description 1
- 210000000709 aorta Anatomy 0.000 description 1
- 230000023555 blood coagulation Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 206010008118 cerebral infarction Diseases 0.000 description 1
- 238000004140 cleaning Methods 0.000 description 1
- 229940125758 compound 15 Drugs 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 229950003499 fibrin Drugs 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 230000023597 hemostasis Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 229960002275 pentobarbital sodium Drugs 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 210000002381 plasma Anatomy 0.000 description 1
- 230000010118 platelet activation Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 238000000518 rheometry Methods 0.000 description 1
- 210000004739 secretory vesicle Anatomy 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 238000012109 statistical procedure Methods 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000004879 turbidimetry Methods 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to the application of spirooliganones B in preparation of the medicine inhibiting the platelet aggregation. The application of spirooliganones B in preparation of the medicine inhibiting the platelet aggregation is disclosed for the first time. The spirooliganones B belongs to a brand new matrix type, has the advantages of being high in activity for inhibiting the platelet aggregation and prominent in substantive features, and makes remarkable progress in inhibiting the platelet aggregation.
Description
Technical field
The present invention relates to the novelty teabag of compound S pirooliganones B, particularly relate to Spirooliganones B and preparing the application in medicament for resisting platelet aggregation.
Background technology
Hematoblastic basic physiological function is sticked, assembles, discharges and secretory granule content (as ATP, 5-hydroxy tryptamine), and the platelet of quiescent condition changes states of physiologic function into and is hematoblastic activation.Can phospholipid surface be provided after platelet activation, promote the carrying out of blood coagulation, be formed and hold by fibrin the thrombosis that platelet forms.Therefore platelet is as a kind of visible component of blood, in the thrombosis of physiological hemostasis and pathology, plays a very important role.Clinical research shows, cardiovascular and cerebrovascular disease common is clinically as basic in hypertension, angina pectoris myocardial infarction, cerebral infarction and cerebral hemorrhage etc., all changes relevant with Abnormal Blood Rheology with platelet function.Antiplatelet drug conventional at present has heavier untoward reaction, therefore develops novel effective, that untoward reaction is little treatment very urgent with the medicine of prevention platelet aggregation.The present inventor studies by experiment, finds that Spirooliganones B has the effect of antiplatelet aggregation.
The compound S pirooliganones B that the present invention relates to is one and delivers (Shuang-Gang Ma in 2013, et al., Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters, 2013, noval chemical compound 15(17): 4450 – 4453.), this compound has brand-new framework types, current purposes finds that it can suppress Coxsackie B virus 3 and influenza A virus H3N2(Shuang-Gang Ma, et al., Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters, 2013, 15(17): 4450 – 4453.), the Spirooliganones B that the present invention relates to belongs to first public preparing the purposes in medicament for resisting platelet aggregation.
Summary of the invention
The invention provides Spirooliganones B and prepare the application in medicament for resisting platelet aggregation.
The present invention, using aspirin and clopidogrel as positive drug, proves by experiment, and Spirooliganones B can obvious anticoagulant, and index all significantly reduces, and maintains an equal level with positive drug.
Described compound S pirooliganones B structure is as shown in formula I:
Formula I
The Spirooliganones B that the present invention relates to belongs to first public preparing the purposes in medicament for resisting platelet aggregation, because framework types belongs to brand-new framework types, and its platelet aggregation inhibitory activity is strong, possess outstanding substantive distinguishing features, for antiplatelet aggregation, obviously there is significant progress simultaneously.
Detailed description of the invention
The preparation method of compound S pirooliganones B involved in the present invention is see document (Shuang-Gang Ma, et al., Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters, 2013,15(17): 4450 – 4453.)
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 S pirooliganones B tablet involved in the present invention:
Get 5 g of compound Spirooliganones B, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound S pirooliganones B capsule involved in the present invention:
Get 5 g of compound Spirooliganones B, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1:Spirooliganones B is on the impact of rat platelet aggregation function
1. animal: cleaning grade Sprague-Dawley rat, male, body weight 200g-250g, Nanjing Medical University's Experimental Animal Center.
2. method and result
Animal is divided into blank group (waiting capacity solvent), aspirin group (ASA at random, 50mg/kg), clopidogrel group (7mg/kg), Spirooliganones B0.625mg/kg group, Spirooliganones B1.25mg/kg group, Spirooliganones B2.5mg/kg group, often organize 8, gastric infusion, 1 time/d, continuous 5d.1h after last administration, with 3% pentobarbital sodium anesthetized rat (30mg/kg) respectively, take a blood sample through ventral aorta, with 3.8% liquor sodii citratis anticoagulant (blood: anticoagulant=9:1), 1000r/min, be separated platelet rich plasma (PRP), remainder is again with the centrifugal 15min of 3000r/min, be separated platelet poor plasma (PPP), by turbidimetry with ADP(252umol/L) be derivant, platelet aggregation rate in 5min is measured with LBY-NJ blood pool instrument, and calculate platelet aggregation inhibition rate as follows, data % represents, statistical procedures is carried out with t inspection between group, the results are shown in Table 1.
Platelet aggregation inhibition rate=(blank platelet aggregation rate %-delivery tube platelet aggregation rate %)/blank platelet aggregation rate %*100%
Experimentally result is known, and each dosage group of Spirooliganones B can obviously suppress platelet aggregation in body, and drug effect and positive drug aspirin and clopidogrel maintain an equal level.
Table 1Spirooliganones B is to hematoblastic gathering suppression ratio (, n=8)
Compare with blank group, * * P<0.001*P<0.01
Conclusion: using aspirin and clopidogrel as positive drug, prove by experiment, Spirooliganones B can obvious anticoagulant, maintains an equal level, can be used for preparing medicament for resisting platelet aggregation with positive drug.
Claims (1)
1.Spirooliganones B is preparing the application in medicament for resisting platelet aggregation, and described compound S pirooliganones B structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310466681.6A CN103462985B (en) | 2013-10-09 | 2013-10-09 | Application of spirooliganones B in preparation of medicine inhibiting platelet aggregation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310466681.6A CN103462985B (en) | 2013-10-09 | 2013-10-09 | Application of spirooliganones B in preparation of medicine inhibiting platelet aggregation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103462985A CN103462985A (en) | 2013-12-25 |
| CN103462985B true CN103462985B (en) | 2015-06-17 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310466681.6A Expired - Fee Related CN103462985B (en) | 2013-10-09 | 2013-10-09 | Application of spirooliganones B in preparation of medicine inhibiting platelet aggregation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103462985B (en) |
-
2013
- 2013-10-09 CN CN201310466681.6A patent/CN103462985B/en not_active Expired - Fee Related
Non-Patent Citations (2)
| Title |
|---|
| Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum;Shuang-Gang Ma,et al.;《Organic Letters》;20130812;第15卷(第17期);第4450–4453页 * |
| 唐文照.少药八角果实及茎皮化学成分和药理活性研究.《中国博士学位论文全文数据库,医药卫生科技辑(月刊)》.2008,(第09期),第1-26页. * |
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| Publication number | Publication date |
|---|---|
| CN103462985A (en) | 2013-12-25 |
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