CN103356679A - Application of Houttuynoid A in preparation of anti-platelet aggregation medicines - Google Patents
Application of Houttuynoid A in preparation of anti-platelet aggregation medicines Download PDFInfo
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- CN103356679A CN103356679A CN2013102576016A CN201310257601A CN103356679A CN 103356679 A CN103356679 A CN 103356679A CN 2013102576016 A CN2013102576016 A CN 2013102576016A CN 201310257601 A CN201310257601 A CN 201310257601A CN 103356679 A CN103356679 A CN 103356679A
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- houttuynoid
- platelet aggregation
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Abstract
The invention relates to an application of Houttuynoid A in preparation of anti-platelet aggregation medicines. The application of the Houttuynoid A in preparation of anti-platelet aggregation medicines provided by the invention is disclosed for the first time. As the framework type is a brand new framework type and the anti-platelet aggregation activity of the Houttuynoid A is unimaginably strong, the probability of giving any enlightenment by other compounds does not exist. The Houttuynoid A has remarkable substantial characteristics and meanwhile has remarkable progress for anti-platelet aggregation.
Description
Technical field
The present invention relates to the new purposes of Houttuynoid A, more specifically to the application of this chemical compound in the preparation medicament for resisting platelet aggregation.
Background technology
Hematoblastic basic physiological function be stick, gathering, release and secretory granule content (such as ATP, 5-hydroxy tryptamine), the platelet of quiescent condition changes states of physiologic function into and is hematoblastic activation.The phospholipid surface can be provided behind the platelet activation, promote the carrying out of blood coagulation, form and hold the thrombosis that platelet forms by fibrin.Therefore platelet, plays a very important role in the thrombosis of physiological hemostasis and pathology as a kind of visible component of blood.Clinical research shows, common cardiovascular and cerebrovascular disease such as hypertension, angina pectoris myocardial infarction, cerebral infarction and cerebral hemorrhage etc. are basic clinically, and is all relevant with Abnormal Blood Rheology with the platelet function variation.Antiplatelet drug commonly used 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 Houttuynoid A has the effect of antiplatelet aggregation.
The compound H outtuynoid A that the present invention relates to is one and delivered (Chen in 2012, S.D.et al., 2012.Houttuynoid A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata.Organic Letters14 (7), 17724 – 1775.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to anti-herpes simplex virus activity (Chen, S.D.et al., 2012.Houttuynoid A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata.Organic Letters14 (7), 17724 – 1775.), belong to open first for the purposes of the Houttuynoid A that the present invention relates in the preparation medicament for resisting platelet aggregation, because framework types belongs to brand-new framework types, and its platelet aggregation inhibitory activity is unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for simultaneously antiplatelet aggregation and obviously have significant progress.
Summary of the invention
The invention provides the application of Houttuynoid A in the preparation medicament for resisting platelet aggregation.
The present invention with aspirin and clopidogrel as positive drug, proof by experiment, Houttuynoid A significantly anticoagulant index all significantly reduces, and maintains an equal level with positive drug.
Described compound H outtuynoid A structure is shown in formula I:
The purposes of the Houttuynoid A that the present invention relates in the preparation medicament for resisting platelet aggregation belongs to open first, because framework types belongs to brand-new framework types, and its platelet aggregation inhibitory activity is unexpectedly strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for simultaneously antiplatelet aggregation and obviously have significant progress.
The specific embodiment
The preparation method of compound H outtuynoid A involved in the present invention is referring to document (Chen, S.D.et al., 2012.Houttuynoid A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata.Organic Letters14 (7), 17724 – 1775.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but limited by claim.
Embodiment 1: the preparation of compound H outtuynoid A tablet involved in the present invention:
Get 20 and digest compound Houttuynoid A, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid A capsule involved in the present invention:
Get 20 and digest compound Houttuynoid A, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Test example 1:Houttuynoid A is on the impact of rat platelet aggregation function
1. animal: a cleaning level Sprague-Dawley rat, male, body weight 200g-250g.
2. method and result
Animal is divided into blank group (waiting the capacity solvent), aspirin group (ASA at random, 50mg/kg), clopidogrel group (7mg/kg), Houttuynoid A0.625mg/kg group, Houttuynoid A1.25mg/kg group, Houttuynoid A2.5mg/kg group, every group 8, gastric infusion, 1 time/d, continuous 5d.1h after the last administration, with 3% pentobarbital sodium difference anesthetized rat (30mg/kg), take a blood sample through ventral aorta, with 3.8% liquor sodii citratis anticoagulant (blood: anticoagulant=9:1), 1000r/min, separate platelet rich plasma (PRP), remainder is again with the centrifugal 15min of 3000r/min, separate platelet poor plasma (PPP), by turbidimetry take ADP(252umol/L) be derivant, measure platelet aggregation rate in the 5min with LBY-NJ blood pool instrument, and calculate as follows platelet aggregation inhibition rate, data are used
Expression is carried out statistical procedures with t check between group, the results are shown in Table 1.
According to experimental result as can be known, each dosage group of Houttuynoid A can obviously suppress platelet aggregation in the body, and drug effect and positive drug aspirin and clopidogrel maintain an equal level.
Table 1Houttuynoid A is to hematoblastic gathering suppression ratio
Compare with the blank group: * * p＜0.01
Conclusion: with aspirin and clopidogrel as positive drug, proof by experiment, Houttuynoid A is anticoagulant significantly, maintains an equal level with positive drug, can be used for preparing medicament for resisting platelet aggregation.
Claims (1)
1.Houttuynoid the application of A in medicament for resisting platelet aggregation, described compound H outtuynoid A structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013102576016A CN103356679A (en) | 2013-06-24 | 2013-06-24 | Application of Houttuynoid A in preparation of anti-platelet aggregation medicines |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN2013102576016A CN103356679A (en) | 2013-06-24 | 2013-06-24 | Application of Houttuynoid A in preparation of anti-platelet aggregation medicines |
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| CN103356679A true CN103356679A (en) | 2013-10-23 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013102576016A Pending CN103356679A (en) | 2013-06-24 | 2013-06-24 | Application of Houttuynoid A in preparation of anti-platelet aggregation medicines |
Country Status (1)
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| CN (1) | CN103356679A (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1124957A (en) * | 1993-03-31 | 1996-06-19 | G·D·瑟尔公司 | 1-amidinophenyl-pyrrolidones piperidinones azetinones as platelet aggregation inhibitors |
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2013
- 2013-06-24 CN CN2013102576016A patent/CN103356679A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1124957A (en) * | 1993-03-31 | 1996-06-19 | G·D·瑟尔公司 | 1-amidinophenyl-pyrrolidones piperidinones azetinones as platelet aggregation inhibitors |
Non-Patent Citations (1)
| Title |
|---|
| SHAO-DAN CHEN等: "Houttuynoids A-E, Anti-herpes simplex virus active flavonoids with novel skeletons from houttuynia cordata", 《ORGANIC LETTERS》 * |
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Application publication date: 20131023 |