CN105497039A - Application of Trigonoliimines C in preparing drugs for treating or preventing acute heart failure - Google Patents
Application of Trigonoliimines C in preparing drugs for treating or preventing acute heart failure Download PDFInfo
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- CN105497039A CN105497039A CN201510930910.4A CN201510930910A CN105497039A CN 105497039 A CN105497039 A CN 105497039A CN 201510930910 A CN201510930910 A CN 201510930910A CN 105497039 A CN105497039 A CN 105497039A
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- heart failure
- trigonoliiminesc
- acute heart
- trigonoliimines
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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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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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 the application of Trigonoliimines C in preparing drugs for treating or preventing acute heart failure. The application of Trigonoliimines C in preparing drugs for treating or preventing acute heart failure is disclosed for the first time, a novel framework type is adopted, the acute heart failure curative activity of Trigonoliimines C is surprisingly high, the possibility of inspiration of other compounds is completely avoided, prominent substantive features are realized, and remarkable progress is made in treating acute heart failure by means of Trigonoliimines C.
Description
Technical field
The present invention relates to the novelty teabag of compound TrigonoliiminesC, particularly relate to the application of TrigonoliiminesC in preparation treatment or prevention acute heart failure medicine.
Background technology
Heart failure (hearfailure, HF) refers to that cardiac function is abnormal and causes heart pump blood volume can not meet a kind of pathological and physiological condition of tissue metabolism's needs.Cause of disease inducement causes structure function low and Progressive symmetric erythrokeratodermia morbidity because cardiac overload, cardiac muscle itself, the limited any reason of diastole cause initial myocardial damage; And infect, anemia, gestation, childbirth, cardiac arrhythmia, pulmonary infarction, hyperthyroidism, diabetes, suppression heart medicine bring out and increase the weight of HF.Pathogeny thinks that the mechanism that HF occurs to develop is abnormal hemodynamics in the past; The later stage eighties 20th century recognizes that the activation of nerve-endocrine hormone plays an important role (sympathetic ↑ NE ↑ RAS ↑ wait activation); Specify that after the nineties that " Myocardial Remodeling " (remodelling) is the fundamental mechanism causing the generation of heart failure to develop gradually.
The compound TrigonoliiminesC that the present invention relates to is one and delivers (PengjuFeng in 2013, etal., AnApproachtotheHexacyclicSkeletonofTrigonoliimines.ORGAN ICLETTERS, 2013, 13 (21): 5827 – 5829.) noval chemical compound, this compound has brand-new framework types, current purposes only relates to anti AIDS virus, (PengjuFeng, etal., AnApproachtotheHexacyclicSkeletonofTrigonoliimines.ORGAN ICLETTERS, 2013, 13 (21): 5827 – 5829.), the purposes of the TrigonoliiminesC that the present invention relates in preparation treatment or prevention acute heart failure medicine is belonged to first public.
Summary of the invention
The present invention proposes the application of TrigonoliiminesC in preparation treatment or prevention acute heart failure medicine.Find out from pharmacological evaluation, TrigonoliiminesC has the effect for the treatment of preferably or prevention acute heart failure.Due to the pharmacological action of the first public TrigonoliiminesC of the present invention in treatment or prevention acute heart failure.
Described compound TrigonoliiminesC structure is as shown in formula I:
The application of described TrigonoliiminesC in treatment or prevention acute heart failure medicine, the SW of TrigonoliiminesC increase Heart Failure Dogs, LVW ,+dp/dt, cardiac output.
A kind for the treatment of or prevention acute heart failure medicine, be that active component interpolation adjuvant is prepared from by TrigonoliiminesC, preparation method, for getting 5 g of compound TrigonoliiminesC, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
A kind for the treatment of or prevention acute heart failure medicine, be that active component adds adjuvant and is prepared from by TrigonoliiminesC, preparation method, for getting 5 g of compound TrigonoliiminesC, adds starch 195 grams, mixing, encapsulatedly makes 1000.
Technical scheme of the present invention is: the application of TrigonoliiminesC, is specifically applied to preparation treatment or prevention acute heart failure medicine.
The present invention finds by carrying out NS group contrast test to dog, and TrigonoliiminesC can increase the SW of Heart Failure Dogs, LVW ,+dp/dt, cardiac output.Therefore, TrigonoliiminesC for the preparation of the medicine of prevention heart failure, can have good development prospect.
The purposes of the TrigonoliiminesC that the present invention relates in preparation treatment or prevention acute heart failure medicine belongs to first public, because framework types belongs to brand-new framework types, and the activity of its treatment or prevention acute heart failure is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, be used for the treatment of simultaneously or prevent acute heart failure obviously to have significant progress.
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.
Detailed description of the invention
The preparation method of compound TrigonoliiminesC involved in the present invention is see document (PengjuFeng, etal., AnApproachtotheHexacyclicSkeletonofTrigonoliimines.ORGAN ICLETTERS, 2013,13 (21): 5827 – 5829.)
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 TrigonoliiminesC tablet involved in the present invention:
Get 5 g of compound TrigonoliiminesC, add 195 grams, dextrin, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound TrigonoliiminesC capsule involved in the present invention:
Get 5 g of compound TrigonoliiminesC, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: adopt NS method assessing compound TrigonoliiminesC to the therapeutical effect of dog acute heart failure
1, method: dog is divided at random NS group (waiting capacity solvent), gastric infusion TrigonoliiminesC2.0mg/kg group, 1.0mg/kg group, 0.2mg/kg group, often organizes 6.Fasting is after 12 hours, and intravenous injection pentobarbital sodium 40mg/kg anaesthetizes, tracheal intubation, artificial respiration, monitoring aortic pressure (AP) and electrocardiogram.Breast is opened in left side, plugs in conduit to left room pressure and rate of pressure change (± dp/dt thereof from the apex of the heart
max).Waltan-Brodie strain bow is implanted left ventricle antetheca, measures myocardial contraction.With electromagnetic flowmeter determination ascending aorta blood flow.Using ascending aorta flow as cardiac output (CO), calculate cardiac index (CI), index (SI) of often fighting, work done (SW) of often fighting, left heart work done (LVW).Parameters record and BIC physiograph.Postoperative half an hour, parameters reaches stable.From femoral vein constant speed gasing injection pentobarbital sodium (0.5mL/kgmin), with ± dp/dt
maxdropping to about 1000mHg/s is that leading indicator forms acute heart failure.After acute heart failure model stability, each treated animal duodenum gives relative medicine.Between group, T inspection, carries out statistical procedures.
2, result:
Table 1TrigonoliiminesC is on the impact (n=6, X ± s) of heart failure canine dp/dt
Compare with NS group, * * P<0.01*P<0.05
Table 2TrigonoliiminesC is on the impact (n=6, X ± s) of heart failure canine cardiac work
Compare with NS group, * * P<0.01*P<0.05; Compare with before administration,
##p<0.01
#p<0.05
Result is as shown in table 1,2, and instillation various dose TrigonoliiminesC can increase SW, the LVW ,+dp/dt (comparing with model group matched group, p<0.05orp<0.01) of Heart Failure Dogs.Gavage various dose TrigonoliiminesC can increase SW, the LVW ,+dp/dt (comparing with model group matched group, p<0.01orp<0.05) of Heart Failure Dogs.
Table 3TrigonoliiminesC is on the kinemic impact of heart failure canine (n=6, X ± s)
Compare with NS group, * * P<0.01*P<0.05; Compare with before administration,
##p<0.01
#p<0.05
Result is as shown in table 3, and instillation various dose TrigonoliiminesC can increase the cardiac output (comparing with model control group, p<0.01orp<0.05) of Heart Failure Dogs.Gavage various dose TrigonoliiminesC can increase the cardiac output (comparing with model control group, p<0.01orp<0.05) of Heart Failure Dogs.
Shown by above-described embodiment, TrigonoliiminesC of the present invention can increase the SW of Heart Failure Dogs, LVW ,+dp/dt, cardiac output.Prove thus, TrigonoliiminesC of the present invention significantly can improve acute heart failure, can be used for preparing the medicine for the treatment of or preventing heart failure.
Claims (4)
- The application of 1.TrigonoliiminesC in treatment or prevention acute heart failure medicine, described compound TrigonoliiminesC structure is as shown in formula I:
- 2. the application of TrigonoliiminesC in treatment or prevention acute heart failure medicine as claimed in claim 1, is characterized in that the SW of TrigonoliiminesC increase Heart Failure Dogs, LVW ,+dp/dt, cardiac output.
- 3. a treatment or prevention acute heart failure medicine, it is characterized in that by TrigonoliiminesC described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound TrigonoliiminesC, adds 195 grams, dextrin, mixing, Conventional compression makes 1000.
- 4. a treatment or prevention acute heart failure medicine, it is characterized in that by TrigonoliiminesC described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound TrigonoliiminesC, adds starch 195 grams, mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510930910.4A CN105497039A (en) | 2015-12-14 | 2015-12-14 | Application of Trigonoliimines C in preparing drugs for treating or preventing acute heart failure |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510930910.4A CN105497039A (en) | 2015-12-14 | 2015-12-14 | Application of Trigonoliimines C in preparing drugs for treating or preventing acute heart failure |
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| CN105497039A true CN105497039A (en) | 2016-04-20 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106727583A (en) * | 2016-12-12 | 2017-05-31 | 范旭升 | A kind of pharmaceutical composition for treating diastolic heart failure |
-
2015
- 2015-12-14 CN CN201510930910.4A patent/CN105497039A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106727583A (en) * | 2016-12-12 | 2017-05-31 | 范旭升 | A kind of pharmaceutical composition for treating diastolic heart failure |
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Application publication date: 20160420 |
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