CN103127153A - Application of Gypensapogenin B in anti-platelet aggregation medicines - Google Patents
Application of Gypensapogenin B in anti-platelet aggregation medicines Download PDFInfo
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- CN103127153A CN103127153A CN2012104153613A CN201210415361A CN103127153A CN 103127153 A CN103127153 A CN 103127153A CN 2012104153613 A CN2012104153613 A CN 2012104153613A CN 201210415361 A CN201210415361 A CN 201210415361A CN 103127153 A CN103127153 A CN 103127153A
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Abstract
The invention relates to application of Gypensapogenin B in preparing anti-platelet aggregation medicines. The application of the Gypensapogenin B in preparing anti-platelet aggregation medicines is made public for the first time, due to the fact that matrix type is brand novel, besides, the Eryngiolide B has an unexpectedly high anti-platelet aggregation inhibitory activity, the probability that inspiration is obtained from other compounds does not exist, and the Gypensapogenin B possesses outstanding substantial characteristics, meanwhile, significant progress is obviously achieved by the application of the Gypensapogenin B in anti-platelet aggregation.
Description
Technical field
The present invention relates to the new purposes of Gypensapogenin B, more specifically to the application of this compound in the preparation 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.Can provide phospholipid surperficial 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 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.At present antiplatelet drug commonly used has heavier untoward reaction, therefore develop novel effectively, the little treatment of untoward reaction is very urgent with the medicine of prevention platelet aggregation.The inventor studies by experiment, finds that Gypensapogenin B has the effect of antiplatelet aggregation.
the compound Gypensapogenin B that the present invention relates to is one and delivered (Li in 2012, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to the cytotoxic activity (Li of human tumor cell line, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178.), belong to open first for the purposes of the Gypensapogenin B 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 compounds, possesses 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 Gypensapogenin B in the preparation medicament for resisting platelet aggregation.
The present invention with aspirin and clopidogrel as positive drug, proof by experiment, Gypensapogenin B significantly anticoagulant index all significantly reduces, and maintains an equal level with positive drug.
Described compound Gypensapogenin B structure is as shown in formula I:
Formula I
The purposes of the Gypensapogenin B 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 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 Gypensapogenin B involved in the present invention is referring to document (Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173 – 178. and Wei, J.X. et al., 1982. Two new dammaran sapogenins from leaves of Panax notoginseng. Planta Medica, 45 (3): 167-171.).
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 Gypensapogenin B tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound Gypensapogenin B capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add the conventional adjuvant such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
The impact of test example 1:Gypensapogenin B on the 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), Gypensapogenin B 0.625 mg/kg group, Gypensapogenin B 1.25 mg/kg groups, Gypensapogenin B 2.5 mg/kg groups, 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 the centrifugal 15min of 3000r/min, separate platelet poor plasma (PPP), by turbidimetry take ADP(252umol/L) be derivant, measure platelet aggregation rate in 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 Gypensapogenin B can obviously suppress platelet aggregation in body, and drug effect and positive drug aspirin and clopidogrel maintain an equal level.
Table 1 Gypensapogenin B 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, Gypensapogenin B is anticoagulant significantly, maintains an equal level with positive drug, can be used for preparing medicament for resisting platelet aggregation.
Claims (1)
1.Gypensapogenin the application of B in medicament for resisting platelet aggregation, described compound Gypensapogenin B structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012104153613A CN103127153A (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in anti-platelet aggregation medicines |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012104153613A CN103127153A (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in anti-platelet aggregation medicines |
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| Publication Number | Publication Date |
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| CN103127153A true CN103127153A (en) | 2013-06-05 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN2012104153613A Pending CN103127153A (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in anti-platelet aggregation medicines |
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Cited By (2)
| 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 |
| CN105412099A (en) * | 2015-10-28 | 2016-03-23 | 淄博齐鼎立专利信息咨询有限公司 | Application of Denudatine-type diterpenoid in preparation of medicine for resisting platelet aggregation |
-
2012
- 2012-10-26 CN CN2012104153613A patent/CN103127153A/en active Pending
Non-Patent Citations (1)
| Title |
|---|
| NING LI ET. AL.: "《Triterpenes possessing an unprecedented skeleton isolated from hydrolyzateof total saponins from Gynostemma pentaphyllum》", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》 * |
Cited By (2)
| 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 |
| CN105412099A (en) * | 2015-10-28 | 2016-03-23 | 淄博齐鼎立专利信息咨询有限公司 | Application of Denudatine-type diterpenoid in preparation of medicine for resisting platelet aggregation |
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Application publication date: 20130605 |