CN106344567A - Application of Ternatusine A in preparation of drugs for treating or preventing acute heart failure - Google Patents
Application of Ternatusine A in preparation of drugs for treating or preventing acute heart failure Download PDFInfo
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- CN106344567A CN106344567A CN201610818352.7A CN201610818352A CN106344567A CN 106344567 A CN106344567 A CN 106344567A CN 201610818352 A CN201610818352 A CN 201610818352A CN 106344567 A CN106344567 A CN 106344567A
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- Prior art keywords
- ternatusine
- heart failure
- acute heart
- treating
- preparation
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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)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides application of Ternatusine A in the preparation of drugs for treating or preventing acute heart failure. The application of Ternatusine A related herein in the preparation of drugs for treating or preventing heart failure is disclosed for the first time; since a framework is of brand-new type and the activity of Ternatusine A in treating acute heart failure is unexpectedly high, there is no chance for other compounds to give any indication and outstanding practical characteristics are provided; in addition, Ternatusine A has significant progress in treating acute heart failure.
Description
Technical field
The present invention relates to the new application of compound ternatusine a, more particularly, to ternatusine a are in preparation treatment
Or the application in prevention acute heart failure medicine.
Background technology
Heart failure (hear failure, hf) refers to that cardiac function leads to heart pump blood volume can not meet tissue metabolism's need extremely
A kind of pathological and physiological condition wanted.Cause of disease inducement is because cardiac overload, cardiac muscle itself, any reason limited by diastole cause initially
Myocardial damage causes structure function low and progressive morbidity；And infect, anemia, gestation, childbirth, cardiac arrhythmia, pulmonary infarction, first
High, diabetes, suppression heart medicine induce and increase hf.Pathogeny is it is considered that the mechanism that hf occurs development is that hemodynamics are different
Often；The later stage eighties 20th century recognizes that the activation of nerve-endocrine hormone plays an important role (sympathetic ↑ ne ↑ ras ↑ wait activation)；
Gradually specify that after the nineties that " Myocardial Remodeling " (remodelling) is the fundamental mechanism that development occurs leading to heart failure.
Compound ternatusine a according to the present invention be one deliver within 2013 (zhilai zhan, et al.,
ternatusine a,a new pyrrole derivative with an epoxyoxepino ring from
Ranunculus ternatus.organic letters, 2013,15 (8): 1970 1973..) noval chemical compound, this chemical combination
Thing has brand-new framework types, and current purposes merely relates to function of tumor inhibition, (zhilai zhan, et al.,
ternatusine a,a new pyrrole derivative with an epoxyoxepino ring from
Ranunculus ternatus.organic letters, 2013,15 (8): 1970 1973..), for according to the present invention
Purposes in preparation treatment or prevention acute heart failure medicine for the ternatusine a belongs to first public.
Content of the invention
The present invention proposes application in preparation treatment or prevention acute heart failure medicine for the ternatusine a.Real from pharmacology
Examine out, ternatusine a plays the role of preferable treatment or prevention acute heart failure.Because the present invention is first public
Pharmacological action in terms for the treatment of or preventing acute heart failure for the ternatusine a.
Shown in described compound ternatusine a structure such as formula ():
The technical scheme is that the application of ternatusine a, be specifically applied to preparation treatment or prevention is acute
Heart failure medications.
The present invention is found by dog is carried out with ns group contrast test, ternatusine a can increase the sw of Heart Failure Dogs, lvw,
+ dp/dt, cardiac output.Therefore, ternatusine a can be used for preparing the medicine of prevention heart failure, has good development and application
Prospect.
Purposes in preparation treatment or prevention acute heart failure medicine for the ternatusine a according to the present invention belongs to first
Open, because framework types belong to brand-new framework types, and the activity of its treatment or prevention acute heart failure is strong must expect not
Arrive, there is not the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for treatment or pre-
Anti- acute heart failure obviously has and significantly improves.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to concrete reality
Apply any restriction of example, but be defined in the claims.
Specific embodiment
The preparation method of compound ternatusine a involved in the present invention referring to document (zhilai zhan, et al.,
ternatusine a,a new pyrrole derivative with an epoxyoxepino ring from
ranunculus ternatus.organic letters,2013,15(8):1970–1973.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to concrete reality
Apply any restriction of example, but be defined in the claims.
Embodiment 1: the preparation of compound ternatusine a tablet involved in the present invention:
Take 5 g of compound ternatusine a, add 195 grams of dextrin, mix, conventional tablet presses make 1000.
Embodiment 2: the preparation of compound ternatusine a capsule involved in the present invention:
Take 5 g of compound ternatusine a, add 195 grams of starch, mix, encapsulated make 1000.
To further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: the therapeutical effect to dog acute heart failure for the compound ternatusine a is evaluated using ns method
1st, method: dog is randomly divided into ns group (waiting capacity solvent), gastric infusion ternatusine a 2.0mg/kg group,
1.0mg/kg group, 0.2mg/kg group, every group 6.After fasting 12 hours, intravenous injection pentobarbital sodium 40mg/kg anaesthetizes, trachea
Intubation, artificial respiration, monitoring aortic pressure (ap) and electrocardiogram.Breast is opened in left side, plugs in conduit to left chamber pressure and its pressure from the apex of the heart
Pace of change (± dp/dtmax).By waltan-brodie strain bow implantation left ventricle antetheca, measure myocardial contraction.Use electromagnetism
Effusion meter measures ascending aorta blood flow.Using ascending aorta flow as cardiac output (co), calculate cardiac index (ci), often fight
Index (si), work done (sw) of often fighting, left heart work done (lvw).Parameters record and bic physiograph.Postoperative half an hour, respectively
Item parameter reaches stable.From femoral vein constant speed gasing injection pentobarbital sodium (0.5ml/kg min), with ± dp/dtmaxDrop to about
1000mhg/s forms acute heart failure for leading indicator.After acute heart failure model stability, each group animal duodenum gives
Relative medicine.Between group, t inspection, carries out statistical procedures.
2nd, result:
The impact (n=6, x ± s) to heart failure canine dp/dt for the table 1 ternatusine a
Compare with ns group, * * p < 0.01*p < 0.05
The impact (n=6, x ± s) to heart failure canine cardiac work for the table 2 ternatusine a
Compare with ns group, * * p < 0.01*p < 0.05；Compare with before administration,##p<0.01#p<0.05
As shown in table 1,2, instillation various dose ternatusine a can increase the sw of Heart Failure Dogs, lvw ,+dp/dt to result
(comparing with model group matched group, p < 0.05or p < 0.01).Gavage various dose ternatusine a can increase Heart Failure Dogs
Sw, lvw ,+dp/dt (comparing with model group matched group, p < 0.01or p < 0.05).
Table 3 ternatusine a kinemic impact (n=6, x ± s) on heart failure canine
Compare with ns group, * * p < 0.01*p < 0.05；Compare with before administration,##p<0.01#p<0.05
As shown in table 3, instillation various dose ternatusine a can increase the cardiac output of Heart Failure Dogs (with model to result
Matched group compares, p < 0.01or p < 0.05).Gavage various dose ternatusine a can increase the cardiac output of Heart Failure Dogs
(comparing with model control group, p < 0.01or p < 0.05).
Shown by above-described embodiment, the ternatusine a of the present invention can increase the sw of Heart Failure Dogs, lvw ,+dp/dt, the heart
Output.Thus prove, the ternatusine a of the present invention can significantly improve acute heart failure, can be used to preparation treatment or
The medicine of prevention heart failure.
Claims (1)
1.ternatusine a is treating or is preventing the application in acute heart failure medicine, described compound ternatusine a knot
Shown in structure such as formula ():
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610818352.7A CN106344567A (en) | 2016-09-11 | 2016-09-11 | Application of Ternatusine A in preparation of drugs for treating or preventing acute heart failure |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610818352.7A CN106344567A (en) | 2016-09-11 | 2016-09-11 | Application of Ternatusine A in preparation of drugs for treating or preventing acute heart failure |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106344567A true CN106344567A (en) | 2017-01-25 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610818352.7A Pending CN106344567A (en) | 2016-09-11 | 2016-09-11 | Application of Ternatusine A in preparation of drugs for treating or preventing acute heart failure |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106344567A (en) |
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2016
- 2016-09-11 CN CN201610818352.7A patent/CN106344567A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170125 |
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| WD01 | Invention patent application deemed withdrawn after publication |