CN103316028A - Application of Polyflavanostilbene A in preparation of drug for treating or preventing chronic heart failure - Google Patents
Application of Polyflavanostilbene A in preparation of drug for treating or preventing chronic heart failure Download PDFInfo
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- CN103316028A CN103316028A CN2013103044740A CN201310304474A CN103316028A CN 103316028 A CN103316028 A CN 103316028A CN 2013103044740 A CN2013103044740 A CN 2013103044740A CN 201310304474 A CN201310304474 A CN 201310304474A CN 103316028 A CN103316028 A CN 103316028A
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- heart failure
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- chronic heart
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Abstract
The invention provides an application of a drug for treating or preventing chronic heart failure and specifically brings forward the therapeutical effect of Polyflavanostilbene A on acute and chronic heart failure. The application of Polyflavanostilbene A in the preparation of a drug for treating chronic heart failure is disclosed for the first time. A matrix type belongs to a brand new matrix type, and the activity for treating chronic heart failure is unexpectedly strong. There is no possibility for any revelation of other compounds. The drug has protrude substantive features, and is a remarkable progress for treating chronic heart failure.
Description
Technical field
The present invention relates to the new purposes of Compound P olyflavanostilbene A, relate in particular to the application of Polyflavanostilbene A in preparation treatment or preventing chronic heart failure medicine.
Background technology
Heart failure (hear failure, HF) refers to that cardiac function causes the heart pump blood volume can not satisfy a kind of pathological and physiological condition of tissue metabolism's needs unusually.Cause of disease inducement causes initial myocardial damage because of cardiac overload, cardiac muscle itself, the limited any reason of diastole and causes structure function lowly and the morbidity of carrying out property; And infect, anemia, gestation, childbirth, cardiac arrhythmia, pulmonary infarction, hyperthyroidism, diabetes, inhibition heart medicine bring out and increase the weight of HF.Pathogeny thinks that in the past the mechanism of HF genesis is abnormal hemodynamics; The later stage eighties 20th century is recognized the activation of nerve-endocrine hormone play an important role (sympathetic ↑ NE ↑ RAS ↑ wait activation); Clear and definite gradually " Myocardial Remodeling " is the fundamental mechanism that causes the genesis of heart failure (remodelling) after the nineties.
The Compound P olyflavanostilbene A that the present invention relates to is one and delivered (Fushuang Li in 2013, et al., Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum.Organic Letters, 2013,3 (15), 674 – 677.) noval chemical compound, this chemical compound has brand-new framework types, present purposes only suppresses alpha-glucosidase activity (Fushuang Li, et al., Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum.Organic Letters, 2013,3 (15), 674 – 677.), the purposes of the Polyflavanostilbene A that the present invention relates in preparation treatment or preventing chronic heart failure medicine belongs to open first.
Summary of the invention
The object of the invention is to provides the application of Polyflavanostilbene A in preparation treatment or preventing chronic heart failure medicine according to not finding that it has the present situation of the report for the treatment of or preventing chronic heart failure activity in the existing Polyflavanostilbene A research.
Described Compound P olyflavanostilbene A structure is shown in formula I:
The purposes of the Polyflavanostilbene A that the present invention relates in preparation treatment chronic heart failure belongs to open first, because framework types belongs to brand-new framework types, and its treatment chronic heart failure is unexpectedly active strong, there is not the possibility that is provided any enlightenment by other chemical compounds, possess outstanding substantive distinguishing features, be used for the treatment of simultaneously chronic heart failure and obviously have significant progress.
The specific embodiment
The preparation method of Compound P olyflavanostilbene A involved in the present invention is referring to document (Fushuang Li, et al., Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum.Organic Letters, 2013,3 (15), 674 – 677.)
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 P olyflavanostilbene A tablet involved in the present invention:
Get 5 and digest compound Polyflavanostilbene A adding dextrin 195 grams, mixing, conventional tabletting are made 1000.
Embodiment 2: the preparation of Compound P olyflavanostilbene A capsule involved in the present invention:
Get 5 and digest compound Polyflavanostilbene A and add starch 195 grams, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Experimental example 1:Polyflavanostilbene A is on the impact of chronic heart failure rat
Test method and result:
100 of rats, Nanjing Medical University's Experimental Animal Center, male and female half and half are got 100 lumbar injection doxorubicin hydrochloride 2mg/kg, and 1 time weekly, totally 6 weeks.Be divided at random 10 groups, be the NS group, Captopril tablets 12.5mg/kg group, gastric infusion Polyflavanostilbene A0.2mg/kg group, gastric infusion Polyflavanostilbene A2.5mg/kg group, gastric infusion Polyflavanostilbene A5.0mg/kg group.Play giving every day Polyflavanostilbene A gavage each group the 5th week, administration 21 days.20% urethane 1.1g/kg intraperitoneal injection of anesthesia, peeling operation trachea and intubate, the total tremulous pulse in right side that dissociates simultaneously inserts homemade ventricle intubate (diameter 1mm is full of 1% heparin) through it, traces blood pressure curve; Continue again to insert, make it enter left ventricle by the left side arterial valve, trace the intraventricular pressure curve, Automatic analysis left ventricular systolic pressure (LVSP), the maximum climbing speed of intraventricular pressure (+dp/dtmax), the intraventricular pressure maximum falling speed is (dp/dtmax) and the data such as the myocardium maximal velocity of contraction of actual measurement (Vpm).Other gets 10 rats as Normal group, does not give doxorubicin hydrochloride, and all the other operate with above-mentioned, and statistical procedures is carried out in the T check between group.
Table 1Polyflavanostilbene A is on the impact (n=10) of chronic heart failure Cardiac Function in Rat
Compare △: p<0.05, △ △: p<0.01 with the NS group
Table 1 result of the test shows can the raise LVSP of the Heart Failure Wistar Rats that caused by doxorubicin hydrochloride of Polyflavanostilbene A gastric infusion 0.2mg/kg group ,+dp/dtmax, the reduction of-dp/dtmax and Vpm (organizing comparison, P<0.05 with NS); Can significantly the raise LVSP of the Heart Failure Wistar Rats that caused by doxorubicin hydrochloride of Polyflavanostilbene A gastric infusion 2.5mg/kg, 5.0mg/kg ,+dp/dtmax, the reduction of-dp/dtmax and Vpm (with the NS group relatively, P<0.01).
Conclusion: Polyflavanostilbene A has the effect of significant treatment or preventing chronic heart failure, can be used for preparing the medicine for the treatment of or preventing chronic heart failure.
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CN2013103044740A CN103316028A (en) | 2013-07-17 | 2013-07-17 | Application of Polyflavanostilbene A in preparation of drug for treating or preventing chronic heart failure |
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Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
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CN102480951A (en) * | 2009-04-17 | 2012-05-30 | 卡迪罗治疗公司 | Methods and compositions for treatment of ischemic conditions and conditions related to mitochondrial function |
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Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
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CN102480951A (en) * | 2009-04-17 | 2012-05-30 | 卡迪罗治疗公司 | Methods and compositions for treatment of ischemic conditions and conditions related to mitochondrial function |
Non-Patent Citations (1)
Title |
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FUSHUANG LI ET AL: "Polyflavanostilbene A, a New Flavanol-Fused Stilbene Glycoside from Polygonum cuspidatum", 《ORGANIC LETTERS》 * |
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Application publication date: 20130925 |