CN103446120B - Fluevirosines A is preparing the application in medicament for resisting platelet aggregation - Google Patents
Fluevirosines A is preparing the application in medicament for resisting platelet aggregation Download PDFInfo
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- CN103446120B CN103446120B CN201310433343.2A CN201310433343A CN103446120B CN 103446120 B CN103446120 B CN 103446120B CN 201310433343 A CN201310433343 A CN 201310433343A CN 103446120 B CN103446120 B CN 103446120B
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- Prior art keywords
- fluevirosines
- platelet aggregation
- medicament
- preparing
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- 229930193033 fluevirosine Natural products 0.000 title claims abstract description 22
- 208000010110 spontaneous platelet aggregation Diseases 0.000 title claims abstract description 17
- 239000003814 drug Substances 0.000 title claims abstract description 16
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 claims description 14
- 150000001875 compounds Chemical class 0.000 claims description 11
- 229960000890 hydrocortisone Drugs 0.000 claims description 7
- 239000003146 anticoagulant agent Substances 0.000 abstract description 7
- 238000004220 aggregation Methods 0.000 abstract description 3
- 230000002776 aggregation Effects 0.000 abstract description 3
- 230000000702 anti-platelet effect Effects 0.000 abstract description 3
- 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
- 240000007003 Flueggea virosa Species 0.000 description 3
- 229960001138 acetylsalicylic acid Drugs 0.000 description 3
- 230000000975 bioactive effect Effects 0.000 description 3
- 230000008436 biogenesis Effects 0.000 description 3
- 238000002360 preparation method Methods 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
- 208000026106 cerebrovascular disease Diseases 0.000 description 2
- 210000004623 platelet-rich plasma Anatomy 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
- 206010020772 Hypertension Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 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
- 208000007536 Thrombosis Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 229940127218 antiplatelet drug Drugs 0.000 description 1
- 210000000709 aorta Anatomy 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
- 230000003013 cytotoxicity Effects 0.000 description 1
- 231100000135 cytotoxicity Toxicity 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
- 230000000694 effects Effects 0.000 description 1
- 238000005516 engineering process Methods 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
- 208000032839 leukemia Diseases 0.000 description 1
- 201000005296 lung carcinoma Diseases 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
- 210000002381 plasma Anatomy 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
- 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
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to Fluevirosines A and prepare the application in medicament for resisting platelet aggregation.The Fluevirosines A 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, possess outstanding substantive distinguishing features, for antiplatelet aggregation, obviously there is significant progress simultaneously.
Description
Technical field
The present invention relates to the novelty teabag of compound F 17-hydroxy-corticosterone luevirosines A, particularly relate to Fluevirosines A and preparing the application in medicament for resisting platelet aggregation.
Background technology
Platelet, 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 Fluevirosines A has the effect of antiplatelet aggregation.
The compound F 17-hydroxy-corticosterone luevirosines A that the present invention relates to is one and delivers (Hua Zhang in 2013, et al., Fluevirosines A-C:A Biogenesis Inspired Example in the Discovery of New Bioactive Scaffolds from Flueggea virosa.Organic Letters, 2013, noval chemical compound 15(1): 120 – 123.), this compound has brand-new framework types, current purposes only has certain cytotoxicity (Hua Zhang to leukemia and lung carcinoma cell, et al., Fluevirosines A-C:A Biogenesis Inspired Example in the Discovery of New Bioactive Scaffolds from Flueggea virosa.Organic Letters, 2013, 15(1): 120 – 123.), the Fluevirosines A 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 Fluevirosines A and prepare the application in medicament for resisting platelet aggregation.
The present invention, using aspirin and clopidogrel as positive drug, proves by experiment, and Fluevirosines A can obvious anticoagulant, and index all significantly reduces, and maintains an equal level with positive drug.
Described compound F 17-hydroxy-corticosterone luevirosines A structure is as shown in formula I:
The Fluevirosines A 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, possess outstanding substantive distinguishing features, for antiplatelet aggregation, obviously there is significant progress simultaneously.
Detailed description of the invention
The preparation method of compound F 17-hydroxy-corticosterone luevirosines A involved in the present invention is see document (Hua Zhang, et al., Fluevirosines A-C:A Biogenesis Inspired Example in the Discovery of New Bioactive Scaffolds from Flueggea virosa.Organic Letters, 2013,15(1): 120 – 123.)
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 F 17-hydroxy-corticosterone luevirosines A tablet involved in the present invention:
Get 5 g of compound Fluevirosines A, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound F 17-hydroxy-corticosterone luevirosines A capsule involved in the present invention:
Get 5 g of compound Fluevirosines A, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1:Fluevirosines A is on the impact of rat platelet aggregation function
1. animal: cleaning grade Sprague-Dawley rat, Nanjing Medical University's Experimental Animal Center, male, body weight 200g-250g.
2. method and result
Animal is divided into blank group (waiting capacity solvent), aspirin group (ASA at random, 50mg/kg), clopidogrel group (7mg/kg), Fluevirosines A0.625mg/kg group, Fluevirosines A1.25mg/kg group, Fluevirosines A2.5mg/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 Fluevirosines A can obviously suppress platelet aggregation in body, and drug effect and positive drug aspirin and clopidogrel maintain an equal level.
Table 1Fluevirosines A 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, Fluevirosines A can obvious anticoagulant, maintains an equal level, can be used for preparing medicament for resisting platelet aggregation with positive drug.
Claims (1)
1.Fluevirosines A is preparing the application in medicament for resisting platelet aggregation, and described compound F 17-hydroxy-corticosterone luevirosinesA structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310433343.2A CN103446120B (en) | 2013-09-22 | 2013-09-22 | Fluevirosines A is preparing the application in medicament for resisting platelet aggregation |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310433343.2A CN103446120B (en) | 2013-09-22 | 2013-09-22 | Fluevirosines A is preparing the application in medicament for resisting platelet aggregation |
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| Publication Number | Publication Date |
|---|---|
| CN103446120A CN103446120A (en) | 2013-12-18 |
| CN103446120B true CN103446120B (en) | 2015-08-05 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310433343.2A Expired - Fee Related CN103446120B (en) | 2013-09-22 | 2013-09-22 | Fluevirosines A is preparing the application in medicament for resisting platelet aggregation |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105412099A (en) * | 2015-10-28 | 2016-03-23 | 淄博齐鼎立专利信息咨询有限公司 | Application of Denudatine-type diterpenoid in preparation of medicine for resisting platelet aggregation |
-
2013
- 2013-09-22 CN CN201310433343.2A patent/CN103446120B/en not_active Expired - Fee Related
Non-Patent Citations (3)
| Title |
|---|
| Chemical synthesis and biological activities of Securinega alkaloids;Wen Zhang;《Journal of Chinese Pharmaceutical Sciences》;20111230;第20卷;全文 * |
| Fluevirosines A-C: A Biogenesis Inspired;Hua Zhang;《ORGANIC LETTERS》;20130131;第15卷(第1期);第121页和第123页以及表1 * |
| 新型海洋双吲哚类生物碱的研究进展;谷晓辉;《有机化学》;20000228;第20卷(第2期);全文 * |
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| Publication number | Publication date |
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| CN103446120A (en) | 2013-12-18 |
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Inventor after: Deng Naimei Inventor after: Zheng Jun Inventor after: Yang Sumin Inventor after: Shao Mingxin Inventor before: Gao Zhongqing |
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Effective date of registration: 20150709 Address after: 266000 Jiaozhou Road, Shandong, China, No. 1, No. Applicant after: Qingdao Municipal Hospital Address before: Industrial Park No. 87 Yu Bridge 255086 Shandong province Zibo high tech Zone Wanjie Road Room 301 Applicant before: Zibo Qidingli Patent Information Consulting Co., Ltd. |
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