CN102988349A - Application of Aphanamixoid A for preparing platelet aggregation resistant medicine - Google Patents
Application of Aphanamixoid A for preparing platelet aggregation resistant medicine Download PDFInfo
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- CN102988349A CN102988349A CN2012104688736A CN201210468873A CN102988349A CN 102988349 A CN102988349 A CN 102988349A CN 2012104688736 A CN2012104688736 A CN 2012104688736A CN 201210468873 A CN201210468873 A CN 201210468873A CN 102988349 A CN102988349 A CN 102988349A
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- aphanamixoid
- platelet aggregation
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- resistant medicine
- aggregation resistant
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Abstract
The invention relates to application of Aphanamixoid A for preparing a platelet aggregation resistant medicine. The application of Aphanamixoid A for preparing the platelet aggregation resistant medicine is disclosed for the first time; because the skeleton type belongs to a brand new skeleton type and the platelet aggregation resistant activity of Aphanamixoid A is strong unexpectedly, the possibility that other compounds give any inspiration does not exist; Aphanamixoid A has outstanding substantive characteristics; and simultaneously, Aphanamixoid A has obvious progress for resisting platelet aggregation.
Description
Technical field
The present invention relates to the new purposes of Aphanamixoid 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 that common cardiovascular and cerebrovascular disease such as hypertension, angina pectoris myocardial infarction, cerebral infarction and cerebral hemorrhage etc. are basic clinically, all changes relevant with Abnormal Blood Rheology with platelet function.Antiplatelet drug commonly used has heavier untoward reaction at present, and it is very urgent with the medicine of prevention platelet aggregation therefore to develop novel treatment effective, that untoward reaction is little.The inventor studies by experiment, finds that Aphanamixoid A has the effect of antiplatelet aggregation.
The compd A phanamixoid A that the present invention relates to is one and delivered (Cai in 2012, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this chemical compound has brand-new framework types, present purposes only relates to insect antifeedant activity (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), belong to open first for the purposes of the Aphanamixoid 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 Aphanamixoid A in the preparation medicament for resisting platelet aggregation.
The present invention with aspirin and clopidogrel as positive drug, proof by experiment, Aphanamixoid A significantly anticoagulant index all significantly reduces, and maintains an equal level with positive drug.
Described compd A phanamixoid A structure is shown in formula I:
Formula I
The purposes of the Aphanamixoid 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 compd A phanamixoid A involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.).
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 compd A phanamixoid A tablet involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compd A phanamixoid A capsule involved in the present invention:
Get 20 and digest compound Aphanamixoid 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:Aphanamixoid 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, 50 mg/kg), clopidogrel group (7 mg/kg), Aphanamixoid A 0.625 mg/kg group, Aphanamixoid A 1.25 mg/kg group, Aphanamixoid A 2.5 mg/kg group, every group 8, gastric infusion, 1 time/d, continuous 5d.1h after the last administration, with 3% pentobarbital sodium difference anesthetized rat (30 mg/kg), take a blood sample through ventral aorta, with 3.8% liquor sodii citratis anticoagulant (blood: anticoagulant=9:1), 1000 r/min, separate platelet rich plasma (PRP), remainder is again with centrifugal 15 min of 3000 r/min, separate platelet poor plasma (PPP), by turbidimetry take ADP(252 umol/L) be derivant, measure platelet aggregation rate in 5 min 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 Aphanamixoid A can obviously suppress platelet aggregation in the body, and drug effect and positive drug aspirin and clopidogrel maintain an equal level.
Table 1 Aphanamixoid A to hematoblastic gathering suppression ratio (
, n=8)
Compare with the blank group: * * p＜0.01
Conclusion: with aspirin and clopidogrel as positive drug, proof by experiment, Aphanamixoid A is anticoagulant significantly, maintains an equal level with positive drug, can be used for preparing medicament for resisting platelet aggregation.
Claims (1)
1.Aphanamixoid the application of A in the preparation medicament for resisting platelet aggregation, described compd A phanamixoid A structure is shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN2012104688736A CN102988349A (en) | 2012-11-19 | 2012-11-19 | Application of Aphanamixoid A for preparing platelet aggregation resistant medicine |
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| CN2012104688736A CN102988349A (en) | 2012-11-19 | 2012-11-19 | Application of Aphanamixoid A for preparing platelet aggregation resistant medicine |
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| CN102988349A true CN102988349A (en) | 2013-03-27 |
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| CN2012104688736A Pending CN102988349A (en) | 2012-11-19 | 2012-11-19 | Application of Aphanamixoid A for preparing platelet aggregation resistant medicine |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103638015A (en) * | 2013-11-28 | 2014-03-19 | 常州科立信医疗器械有限公司 | Application of Manzamenone O in platelet aggregation inhibitor |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1689563A (en) * | 2004-04-23 | 2005-11-02 | 中奇制药技术（石家庄）有限公司 | Application of butylbenzene phthalein homolog in preparation of medicine for treating cerebral ischemia disease |
-
2012
- 2012-11-19 CN CN2012104688736A patent/CN102988349A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1689563A (en) * | 2004-04-23 | 2005-11-02 | 中奇制药技术（石家庄）有限公司 | Application of butylbenzene phthalein homolog in preparation of medicine for treating cerebral ischemia disease |
Non-Patent Citations (2)
| Title |
|---|
| JIE-YUN CAI, ET AL.: "Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya", 《ORGANIC LETTERS》 * |
| 张虹等: "柠檬苦素类似物的研究进展", 《食品与发酵工业》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103638015A (en) * | 2013-11-28 | 2014-03-19 | 常州科立信医疗器械有限公司 | Application of Manzamenone O in platelet aggregation inhibitor |
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Application publication date: 20130327 |