CN102885836A - Application of Gypensapogenin B in medicament for treating or preventing acute heart failure - Google Patents
Application of Gypensapogenin B in medicament for treating or preventing acute heart failure Download PDFInfo
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- CN102885836A CN102885836A CN2012104177020A CN201210417702A CN102885836A CN 102885836 A CN102885836 A CN 102885836A CN 2012104177020 A CN2012104177020 A CN 2012104177020A CN 201210417702 A CN201210417702 A CN 201210417702A CN 102885836 A CN102885836 A CN 102885836A
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Abstract
The invention provides an application of Gypensapogenin B in the preparation of a medicament for treating or preventing acute heart failure. The application of Gypensapogenin B in the preparation of the medicament for treating or preventing acute heart failure is firstly disclosed; since the skeleton type belongs to an entirely new skeleton type and the activity for treating acute heart failure is previously unimagined high without any possibility of giving out revelation by other compounds, the application has outstanding substantial characteristics; and simultaneously, the application for treating acute heart failure is obviously advanced.
Description
Invention field
The present invention relates to the application of Gypensapogenin B in the medicine of preparation treatment or prophylaxis of acute heart failure.
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 chemical 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 chemical 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 preparation treatment acute heart failure medicine, because framework types belongs to brand-new framework types, and its treatment acute 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 acute heart failure and obviously have significant progress.
Summary of the invention
The invention provides the application of Gypensapogenin B in the medicine of preparation treatment or prophylaxis of acute heart failure.
Described chemical compound Gypensapogenin B structure is shown in formula I:
The purposes of the Gypensapogenin B that the present invention relates in preparation treatment acute heart failure medicine belongs to open first, because framework types belongs to brand-new framework types, and its treatment acute 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 acute heart failure and obviously have significant progress.
The specific embodiment
The preparation method of chemical 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 chemical compound Gypensapogenin B tablet involved in the present invention:
Get 20 and digest compound Gypensapogenin B, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of chemical compound Gypensapogenin B capsule involved in the present invention:
Get 20 and digest compound Gypensapogenin B, 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: Gypensapogenin B is to the therapeutical effect of dog acute heart failure
1 material animal health adult dogs body weight, 12.5 ~ 13.5 kg.Pentobarbital sodium (Sigma, import packing, specification: 25g); Instrument U.S. BIC16 leads physiograph (production of U.S. BIC Corp.); Electromagnetic flowmeter (MFV-3200 type): Japanese photoelectricity company produces.
2 test methods and result
Dog is divided into NS group (waiting the capacity solvent) at random, gastric infusion Gypensapogenin B 2.0 mg/kg group, 1.0 mg/kg group, 0.2 mg/kg group, 6 every group.After the fasting 12 hours, intravenous injection pentobarbital sodium 40 mg/kg anesthesia, tracheal intubation, artificial respiration, monitoring aortic pressure (AP) and electrocardiogram.The left side opening breast is plugged in conduit to left constant pressure and rate of pressure change (± dp/dt thereof from the apex of the heart
Max).Waltan-Brodie strain bow is implanted the left ventricle antetheca, measure myocardial contraction.With electromagnetic flowmeter determination ascending aorta blood flow.As cardiac output (CO), calculate cardiac index (CI), the index (SI) of whenever fighting, the work done (SW) of whenever fighting, left heart work done (LVW) with the ascending aorta flow.Parameters record and BIC physiograph.Postoperative half an hour, it is stable that parameters reaches.From femoral vein constant speed gasing injection pentobarbital sodium (0.5 mL/kgmin), with ± dp/dt
MaxDropping to approximately, 1000 mHg/s are that leading indicator forms acute heart failure.Behind the acute heart failure model stability, each treated animal duodenum gives relative medicine.Statistical procedures is carried out in the T check between group.
Table 1 Gypensapogenin B is on the impact of heart failure canine dp/dt (n=6, X ± s)
Compare with the NS group,
@P＜0.05,
@@P＜0.01
Table 2 Gypensapogenin B is on the impact of heart failure canine cardiac work (n=6, X ± s)
With comparison * p＜0.05 before the administration, * * p＜0.01; Compare with the NS group
@P＜0.05,
@@P＜0.01
The result shown in table 1,2, instillation various dose Gypensapogenin B can increase Heart Failure Dogs SW, LVW ,+dp/dt(and model group matched group relatively, p＜0.05or p＜0.01).Gavage various dose Gypensapogenin B can increase Heart Failure Dogs SW, LVW ,+dp/dt(and model group matched group relatively, p＜0.01or p＜0.05).
Table 3 Gypensapogenin B is on the kinemic impact of heart failure canine (n=6, X ± s)
With comparison * p＜0.05 before the administration, * * p＜0.01; Compare with the NS group
@P＜0.05,
@@P＜0.01
The result is as shown in table 3, and instillation various dose Gypensapogenin B can increase the cardiac output (comparing p＜0.01or p＜0.05 with model control group) of Heart Failure Dogs.Gavage various dose Gypensapogenin B can increase the cardiac output (comparing p＜0.01or p＜0.05 with model control group) of Heart Failure Dogs.
Conclusion: Gypensapogenin B can significantly improve acute heart failure, can be used for preparing the medicine for the treatment of or prevention heart failure.
Claims (1)
1.Gypensapogenin the application of B in treatment or the medicine of prophylaxis of acute heart failure, described chemical compound Gypensapogenin B structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210417702.0A CN102885836B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in medicament for treating or preventing acute heart failure |
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| CN201210417702.0A CN102885836B (en) | 2012-10-26 | 2012-10-26 | Application of Gypensapogenin B in medicament for treating or preventing acute heart failure |
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| CN102885836A true CN102885836A (en) | 2013-01-23 |
| CN102885836B CN102885836B (en) | 2014-04-16 |
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- 2012-10-26 CN CN201210417702.0A patent/CN102885836B/en active Active
Non-Patent Citations (1)
| Title |
|---|
| NING LI, ET AL: "Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》 * |
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