CN103520154A - Application of neonectrolide A in preparing medicament for anti-platelet aggregation - Google Patents
Application of neonectrolide A in preparing medicament for anti-platelet aggregation Download PDFInfo
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- CN103520154A CN103520154A CN201310496456.7A CN201310496456A CN103520154A CN 103520154 A CN103520154 A CN 103520154A CN 201310496456 A CN201310496456 A CN 201310496456A CN 103520154 A CN103520154 A CN 103520154A
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- neonectrolide
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- 0 COc(c*(c1c(*)cc2O)O*)c([C@](CCO[C@](**#*)*=C)O3)c1c2C3=O Chemical compound COc(c*(c1c(*)cc2O)O*)c([C@](CCO[C@](**#*)*=C)O3)c1c2C3=O 0.000 description 1
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Abstract
The invention relates to an application of neonectrolide A in preparing a medicament for anti-platelet aggregation. The application of the neonectrolide A in preparing the medicament for fighting platelet aggregation is published for the first time. The Neonectrolide A belongs to a brand-new skeleton type, and has strong anti-platelet aggregation activities, remarkable substantial characteristics and significant progresses apparently when being used for anti-platelet aggregation at the same time.
Description
Technical field
The present invention relates to the new purposes of compound N eonectrolide A, relate in particular to the application of Neonectrolide A in preparing medicament for resisting platelet aggregation.
Background technology
Hematoblastic basic physiological function be stick, gathering, release and secretory granule content (as ATP, 5-hydroxy tryptamine), the platelet of quiescent condition changes states of physiologic function into and is hematoblastic activation.Phospholipid surface can be provided after platelet activation, promote the carrying out of blood coagulation, form and hold by fibrin the thrombosis that platelet forms.Therefore 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, common cardiovascular and cerebrovascular disease is as basic in hypertension, angina pectoris myocardial infarction, cerebral infarction and cerebral hemorrhage etc. clinically, all relevant with Abnormal Blood Rheology with platelet function variation.Conventional antiplatelet drug has heavier untoward reaction at present, therefore develops novel treatment effective, that untoward reaction is little very urgent with the medicine of prevention platelet aggregation.The inventor studies by experiment, finds that Neonectrolide A has the effect of antiplatelet aggregation.
The compound N eonectrolide A the present invention relates to is one and within 2012, delivers (Jinwei Ren, et al., Neonectrolide A, a New Oxaphenalenone Spiroketal from the Fungus Neonectria sp.Organic Letters, 2012, 14(24) 6226 – 6229) noval chemical compound, this compound has brand-new framework types, current purposes only relates to and suppresses part tumor cell proliferation (Jinwei Ren, et al., Neonectrolide A, a New Oxaphenalenone Spiroketal from the Fungus Neonectria sp.Organic Letters, 2012, 14(24) 6226 – 6229.), it is open first that the purposes of the Neonectrolide A the present invention relates in preparing medicament for resisting platelet aggregation belongs to.
Summary of the invention
The invention provides the application of Neonectrolide A in preparing medicament for resisting platelet aggregation.
The present invention is usingd aspirin and clopidogrel as positive drug, proof by experiment, and Neonectrolide A is anticoagulant significantly, and index all significantly reduces, and maintains an equal level with positive drug.
Described compound N eonectrolide A structure is as shown in formula I:
Formula I
It is open first that the purposes of the Neonectrolide A the present invention relates in preparing medicament for resisting platelet aggregation belongs to, 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.
The specific embodiment
The preparation method of compound N eonectrolide A involved in the present invention is referring to document (Jinwei Ren, et al., Neonectrolide A, a New Oxaphenalenone Spiroketal from the Fungus Neonectria sp.Organic Letters, 2012,14(24) 6226 – 6229)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound N eonectrolide A tablet involved in the present invention:
Get 5 and digest compound Neonectrolide A, add 195 grams, dextrin, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compound N eonectrolide A capsule involved in the present invention:
Get 5 and digest compound Neonectrolide A, add 195 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
The impact of test example 1:Neonectrolide A on rat platelet aggregation function
1. animal: a clean level 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), Neonectrolide A0.625mg/kg group, Neonectrolide A1.25mg/kg group, Neonectrolide A2.5mg/kg group, every group 8, gastric infusion, 1 time/d, continuous 5d.1h after last administration, with 3% pentobarbital sodium difference anesthetized rat (30mg/kg), through ventral aorta, take a blood sample, with 3.8% liquor sodii citratis anticoagulant (blood: anticoagulant=9:1), 1000r/min, separated platelet rich plasma (PRP), remainder is again with the centrifugal 15min of 3000r/min, separated platelet poor plasma (PPP), by turbidimetry, take ADP(252umol/L) be derivant, with LBY-NJ blood pool instrument, measure platelet aggregation rate in 5min, and calculate as follows platelet aggregation inhibition rate, data represent with %, with t check between group, carry out statistical procedures, 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%
Known according to experimental result, each dosage group of Neonectrolide A can obviously suppress platelet aggregation in body, and drug effect and positive drug aspirin and clopidogrel maintain an equal level.
Table 1Neonectrolide A to hematoblastic gathering suppression ratio (, n=8)
With the comparison of blank group, * * P < 0.001*P < 0.01
Conclusion: using aspirin and clopidogrel as positive drug, proof by experiment, Neonectrolide A is anticoagulant significantly, maintains an equal level with positive drug, can be used for preparing medicament for resisting platelet aggregation.
Claims (1)
- The application of 1.Neonectrolide A in preparing medicament for resisting platelet aggregation, described compound N eonectrolideA structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310496456.7A CN103520154A (en) | 2013-10-21 | 2013-10-21 | Application of neonectrolide A in preparing medicament for anti-platelet aggregation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310496456.7A CN103520154A (en) | 2013-10-21 | 2013-10-21 | Application of neonectrolide A in preparing medicament for anti-platelet aggregation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103520154A true CN103520154A (en) | 2014-01-22 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310496456.7A Pending CN103520154A (en) | 2013-10-21 | 2013-10-21 | Application of neonectrolide A in preparing medicament for anti-platelet aggregation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103520154A (en) |
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2013
- 2013-10-21 CN CN201310496456.7A patent/CN103520154A/en active Pending
Non-Patent Citations (1)
| Title |
|---|
| JINWEI REN,ET AL: "Neonectrolide A, a New Oxaphenalenone Spiroketal from the Fungus Neonectria sp.", 《ORGANIC LETTERS》 * |
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Application publication date: 20140122 |