CN105534975A - Applications of herqueiazole in preparation of platelet aggregation inhibiting medicines - Google Patents
Applications of herqueiazole in preparation of platelet aggregation inhibiting medicines Download PDFInfo
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- CN105534975A CN105534975A CN201510967538.4A CN201510967538A CN105534975A CN 105534975 A CN105534975 A CN 105534975A CN 201510967538 A CN201510967538 A CN 201510967538A CN 105534975 A CN105534975 A CN 105534975A
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- herqueiazole
- platelet aggregation
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- General Health & Medical Sciences (AREA)
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Abstract
The invention relates to applications of herqueiazole in preparation of platelet aggregation inhibiting medicines. The applications of the herqueiazole in preparation of the anti-platelet aggregation medicines are disclosed for the first time. The herqueiazole has a novel skeleton type, has high platelet aggregation inhibiting activity and substantive features, and is obvious in progress when being used for inhibiting platelet aggregation.
Description
Technical field
The present invention relates to the novelty teabag of compound H erqueiazole, particularly relate to Herqueiazole 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 Herqueiazole has the effect of antiplatelet aggregation.
The compound H erqueiazole that the present invention relates to is one and delivers (ElinJulianti in 2013, etal., NewPolyaromaticMetabolitesfromaMarine-DerivedFungusPenic illiumsp..OrganicLetters, 2013, 15 (6) 1286 – 1289.) noval chemical compound, this compound has brand-new framework types, there is cytotoxicity (ElinJulianti, etal., NewPolyaromaticMetabolitesfromaMarine-DerivedFungusPenic illiumsp..OrganicLetters, 2013, 15 (6) 1286 – 1289.) the invention provides Herqueiazole and prepare the application in medicament for resisting platelet aggregation.
The present invention, using aspirin and clopidogrel as positive drug, proves by experiment, and Herqueiazole can obvious anticoagulant, and index all significantly reduces, and maintains an equal level with positive drug.
Described compound H erqueiazole structure is as shown in formula I:
The application of described Herqueiazole in medicament for resisting platelet aggregation, Herqueiazole can anticoagulant.
A kind of medicament for resisting platelet aggregation, be that active component interpolation adjuvant is prepared from by Herqueiazole, preparation method, for getting 5 g of compound Herqueiazole, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
A kind of medicament for resisting platelet aggregation, be that active component adds adjuvant and is prepared from by Herqueiazole, preparation method, for getting 5 g of compound Herqueiazole, adds starch 195 grams, mixing, encapsulatedly makes 1000.
The Herqueiazole 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 H erqueiazole involved in the present invention is see document (ElinJulianti, etal., NewPolyaromaticMetabolitesfromaMarine-DerivedFungusPenic illiumsp..OrganicLetters, 2013,15 (6) 1286 – 1289.)
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 H erqueiazole tablet involved in the present invention:
Get 5 g of compound Herqueiazole, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound H erqueiazole capsule involved in the present invention:
Get 5 g of compound Herqueiazole, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1:Herqueiazole 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), Herqueiazole0.625mg/kg group, Herqueiazole1.25mg/kg group, Herqueiazole2.5mg/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) for 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 Herqueiazole can obviously suppress platelet aggregation in body, and drug effect and positive drug aspirin and clopidogrel maintain an equal level.
Table 1Herqueiazole 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, Herqueiazole can obvious anticoagulant, maintains an equal level, can be used for preparing medicament for resisting platelet aggregation with positive drug.
Claims (4)
- The application of 1.Herqueiazole in medicament for resisting platelet aggregation, described compound H erqueiazole structure is as shown in formula I:
- 2. the application of Herqueiazole in medicament for resisting platelet aggregation as claimed in claim 1, is characterized in that Herqueiazole can anticoagulant.
- 3. a medicament for resisting platelet aggregation, it is characterized in that by Herqueiazole described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound Herqueiazole, adds 195 grams, dextrin, mixing, Conventional compression makes 1000.
- 4. a medicament for resisting platelet aggregation, it is characterized in that by Herqueiazole described in claim 1 being that active component adds adjuvant and is prepared from, preparation method, for getting 5 g of compound Herqueiazole, adds starch 195 grams, and mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510967538.4A CN105534975A (en) | 2015-12-20 | 2015-12-20 | Applications of herqueiazole in preparation of platelet aggregation inhibiting medicines |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510967538.4A CN105534975A (en) | 2015-12-20 | 2015-12-20 | Applications of herqueiazole in preparation of platelet aggregation inhibiting medicines |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105534975A true CN105534975A (en) | 2016-05-04 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510967538.4A Pending CN105534975A (en) | 2015-12-20 | 2015-12-20 | Applications of herqueiazole in preparation of platelet aggregation inhibiting medicines |
Country Status (1)
| Country | Link |
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| CN (1) | CN105534975A (en) |
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2015
- 2015-12-20 CN CN201510967538.4A patent/CN105534975A/en active Pending
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Application publication date: 20160504 |