CN105412099A - Application of Denudatine-type diterpenoid in preparation of medicine for resisting platelet aggregation - Google Patents
Application of Denudatine-type diterpenoid in preparation of medicine for resisting platelet aggregation Download PDFInfo
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- CN105412099A CN105412099A CN201510710923.0A CN201510710923A CN105412099A CN 105412099 A CN105412099 A CN 105412099A CN 201510710923 A CN201510710923 A CN 201510710923A CN 105412099 A CN105412099 A CN 105412099A
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- denudatine
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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- Medicinal Chemistry (AREA)
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- Life Sciences & Earth Sciences (AREA)
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Abstract
The invention relates to application of Denudatine-type diterpenoid in preparation of a medicine for resisting platelet aggregation. The application is disclosed for the first time and belongs to a brand-new framework type, the anti-platelet aggregation activity of Denudatine-type diterpenoid is high, Denudatine-type diterpenoid has remarkable substantive features, and meanwhile remarkable progress is obviously made when Denudatine-type diterpenoid is used for resisting platelet aggregation.
Description
Technical field
The present invention relates to the novelty teabag of Compound D enudatine-typediterpenoid, particularly relate to Denudatine-typediterpenoid 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 Denudatine-typediterpenoid has the effect of antiplatelet aggregation.
The Compound D enudatine-typediterpenoid that the present invention relates to is one and delivers (Ru-HuaiMei in 2013, etal., Synthesisofthe10-Azatricyclo [3.3.2.04, 8] decaneCoreofC20-DiterpenoidAlkaloidRacemulsonineviaIodin e (III) PromotedTransannularAziridinationReaction.OrganicLetters, 2013, 15 (9) 2206 – 2209.) noval chemical compound, this compound has brand-new framework types (Ru-HuaiMei, etal., Synthesisofthe10-Azatricyclo [3.3.2.04, 8] decaneCoreofC20-DiterpenoidAlkaloidRacemulsonineviaIodin e (III) PromotedTransannularAziridinationReaction.OrganicLetters, 2013, 15 (9) 2206 – 2209.) the invention provides Denudatine-typediterpenoid and prepare the application in medicament for resisting platelet aggregation.
The present invention, using aspirin and clopidogrel as positive drug, proves by experiment, and Denudatine-typediterpenoid can obvious anticoagulant, and index all significantly reduces, and maintains an equal level with positive drug.
Described Compound D enudatine-typediterpenoid structure is as shown in formula I:
Formula I
The Denudatine-typediterpenoid 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 D enudatine-typediterpenoid involved in the present invention is see document (Ru-HuaiMei, etal., Synthesisofthe10-Azatricyclo [3.3.2.04,8] decaneCoreofC20-DiterpenoidAlkaloidRacemulsonineviaIodin e (III) PromotedTransannularAziridinationReaction.OrganicLetters, 2013,15 (9) 2206 – 2209.)
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 D enudatine-typediterpenoid tablet involved in the present invention:
Get 5 g of compound Denudatine-typediterpenoid, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of Compound D enudatine-typediterpenoid capsule involved in the present invention:
Get 5 g of compound Denudatine-typediterpenoid, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Test example 1:Denudatine-typediterpenoid 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), Denudatine-typediterpenoid0.625mg/kg group, Denudatine-typediterpenoid1.25mg/kg group, Denudatine-typediterpenoid2.5mg/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 Denudatine-typediterpenoid can obviously suppress platelet aggregation in body, and drug effect and positive drug aspirin and clopidogrel maintain an equal level.
Table 1Denudatine-typediterpenoid 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, Denudatine-typediterpenoid can obvious anticoagulant, maintains an equal level, can be used for preparing medicament for resisting platelet aggregation with positive drug.
Claims (1)
- The application of 1.Denudatine-typediterpenoid in medicament for resisting platelet aggregation, described Compound D enudatine-typediterpenoid structure is as shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510710923.0A CN105412099A (en) | 2015-10-28 | 2015-10-28 | Application of Denudatine-type diterpenoid in preparation of medicine for resisting platelet aggregation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201510710923.0A CN105412099A (en) | 2015-10-28 | 2015-10-28 | Application of Denudatine-type diterpenoid in preparation of medicine for resisting platelet aggregation |
Publications (1)
| Publication Number | Publication Date |
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| CN105412099A true CN105412099A (en) | 2016-03-23 |
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| CN201510710923.0A Withdrawn CN105412099A (en) | 2015-10-28 | 2015-10-28 | Application of Denudatine-type diterpenoid in preparation of medicine for resisting platelet aggregation |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103127153A (en) * | 2012-10-26 | 2013-06-05 | 吴俊华 | Application of Gypensapogenin B in anti-platelet aggregation medicines |
| CN103446120A (en) * | 2013-09-22 | 2013-12-18 | 淄博齐鼎立专利信息咨询有限公司 | Application of Fluevirosines A in preparation of anti-platelet aggregation drug |
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2015
- 2015-10-28 CN CN201510710923.0A patent/CN105412099A/en not_active Withdrawn
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103127153A (en) * | 2012-10-26 | 2013-06-05 | 吴俊华 | Application of Gypensapogenin B in anti-platelet aggregation medicines |
| CN103446120A (en) * | 2013-09-22 | 2013-12-18 | 淄博齐鼎立专利信息咨询有限公司 | Application of Fluevirosines A in preparation of anti-platelet aggregation drug |
Non-Patent Citations (1)
| Title |
|---|
| RU-HUAI MEI，等: "Synthesis of the 10-Azatricyclo[3.3.2.04,8]decane Core of C20-Diterpenoid Alkaloid Racemulsonine via Iodine(III) Promoted Transannular Aziridination Reaction", 《ORGANIC LETTERS》 * |
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Application publication date: 20160323 |