CN105919997A - Medicine for preventing or treating acute heart failure and application of medicine - Google Patents
Medicine for preventing or treating acute heart failure and application of medicine Download PDFInfo
- Publication number
- CN105919997A CN105919997A CN201610249259.9A CN201610249259A CN105919997A CN 105919997 A CN105919997 A CN 105919997A CN 201610249259 A CN201610249259 A CN 201610249259A CN 105919997 A CN105919997 A CN 105919997A
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- compound
- heart failure
- medicine
- acute heart
- composition
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61K31/12—Ketones
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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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention belongs to the field of medicine, and in particular relates to a pharmaceutical composition for preventing or treating acute heart failure. The composition is characterized in that an active ingredient of the composition consists of a compound I and a compound II, wherein the mass percentages of the compound I and the compound II in the composition are 70% and 30%; the compound is Naamidine G; and the compound II is Maristachones C. The medicine is disclosed for the first time, and the skeleton type of the medicine is a completely new skeleton type; moreover, the the medicine is strong in activity of preventing or treating the acute heart failure; the medicine has prominent substantive features; and meanwhile, the medicine has obviously made remarkable progress in preventing or treating the acute heart failure.
Description
Technical field
The invention belongs to field of medicaments, be specifically related to a kind for the treatment of or prevention acute heart failure medicine and application thereof.
Background technology
Heart failure (hear failure, HF) refers to that cardiac function is abnormal and causes heart pump blood volume can not meet tissue metabolism's needs
A kind of pathological and physiological condition.Cause of disease inducement is because cardiac overload, cardiac muscle itself, the limited any reason of diastole cause initial cardiac muscle
Damage causes structure function low and Progressive symmetric erythrokeratodermia morbidity；And infect, anemia, gestation, childbirth, cardiac arrhythmia, pulmonary infarction, first
High, diabetes, suppression heart medicine induction increases the weight of HF.Pathogeny is it is considered that the mechanism that HF occurs development is hemodynamics
Abnormal；The later stage eighties 20th century recognize the activation of nerve-endocrine hormone play an important role (sympathetic ↑ NE ↑ RAS ↑ etc.
Activate)；Gradually specify that after the nineties " Myocardial Remodeling " (remodelling) be cause heart failure occur development basic
Mechanism.
The compound N aamidine G that the present invention relates to is one and within 2012, delivers (Jayanta Das, et al., Total
Syntheses of Kealiinines A-C.Org Lett., 14 (24) 6,210 6213.) noval chemical compound, compound
Maristachones C is one and within 2013, delivers (Almeida C, et al., Unprecedented polyketides
From a marine sponge-associated Stachylidium sp.J Nat Prod, 2013,76 (3): 322-326.)
Noval chemical compound, both compounds have brand-new framework types, the Naamidine G that the present invention relates to and
Maristachones C in combination thing purposes in preparation treatment or prevention acute heart failure medicine belongs to first public.
Summary of the invention
Proposition one treatment that the present invention the is or prevention acute heart failure medicine and application thereof.
A kind for the treatment of or prevention acute heart failure pharmaceutical composition, it is characterised in that the active component of said composition by compound I and
Compound II forms, and in said composition, the mass percent of compound I and compound II is respectively 70% and 30%, described
Compound I is Naamidine G, and shown in structure such as formula (I), described compound II is Maristachones C, structure
As shown in formula (II):
Described treatment or prevention acute heart failure pharmaceutical composition, preparation method is by the powder of compound I and the powder of compound II
End is sufficiently mixed according to mass percent respectively 70% and 30%, adds adjuvant, makes preparation.
Described treatment or prevention acute heart failure pharmaceutical composition, adjuvant is dextrin or starch.
Described treatment or the application in treatment or prevention acute heart failure medicine of the prevention acute heart failure pharmaceutical composition.
Find out from pharmacological evaluation, Naamidine G and Maristachones C in combination thing have preferably treat or prevent acute
The effect of heart failure.Owing to the present invention first public Naamidine G and Maristachones C in combination thing are in treatment or prevention
Pharmacological action in terms of acute heart failure.The technical scheme is that Naamidine G and Maristachones C in combination thing
Application, specifically be applied to preparation treatment or prevention acute heart failure medicine.The present invention by carrying out NS group contrast test to dog
Finding, Naamidine G and Maristachones C in combination thing can increase the SW of Heart Failure Dogs, LVW ,+dp/dt, heart output
Amount.Therefore, Naamidine G and Maristachones C in combination thing can be used for preparing the medicine of prevention heart failure, have good
Development prospect.The Naamidine G that the present invention relates to and Maristachones C in combination thing are in preparation treatment or pre-
Purposes in anti-acute heart failure medicine belongs to first public, owing to framework types belongs to brand-new framework types, and its treatment or
The activity of prevention acute heart failure is strong, possesses prominent substantive distinguishing features, is simultaneously used for treatment or prevention acute heart failure obviously has aobvious
The progress write.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by specific embodiment
Any restriction, but be defined in the claims.
Detailed description of the invention
The preparation method of compound N aamidine G involved in the present invention sees document (Jayanta Das, et al., Total
Syntheses of Kealiinines A-C.Org Lett., 14 (24) 6,210 6213.) noval chemical compound, compound
The preparation method of Maristachones C sees document (Almeida C, et al., Unprecedented polyketides
From a marine sponge-associated Stachylidium sp.J Nat Prod, 2013,76 (3): 322-326.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by specific embodiment
Any restriction, but be defined in the claims.
Embodiment 1: the preparation of compound composition tablet involved in the present invention:
Take 7 g of compound Naamidine G and 3 grams of Maristachones C, add 195 grams of dextrin, mixing, conventional pressure
Sheet makes 1000.
Embodiment 2: the preparation of compound composition capsule involved in the present invention:
Take 7 g of compound Naamidine G and 3 grams of Maristachones C, add starch 195 grams, mixing, fill glue
Capsule makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1: use NS method to evaluate compound N aamidine G and the Maristachones C in combination thing heart acute to dog
The therapeutical effect of force failure
1, method: dog is randomly divided into NS group (waiting capacity solvent), gastric infusion 2.0mg/kg of the present invention group, 1.0mg/kg
Group, 0.2mg/kg group (preparing by embodiment 1 method), often group 6.After fasting 12 hours, intravenous injection pentobarbital
Sodium 40mg/kg anaesthetizes, tracheal intubation, artificial respiration, monitoring aortic pressure (AP) and electrocardiogram.Breast is opened, from the heart in left side
Point plugs in conduit extremely left chamber pressure and rate of pressure change (± dp/dt thereofmax).Before Waltan-Brodie strain bow is implanted left ventricle
Wall, measures myocardial contraction.With electromagnetic flowmeter determination ascending aorta blood flow.Using ascending aorta flow as cardiac output
(CO), cardiac index (CI), index (SI) of often fighting, work done (SW) of often fighting, left heart work done (LVW) are calculated.Parameters
Record and BIC physiograph.Postoperative half an hour, parameters reaches stable.From femoral vein constant speed gasing injection pentobarbital sodium (0.5
ML/kg min), with ± dp/dtmaxDropping to about 1000mHg/s is that leading indicator forms acute heart failure.Treat the acute heart
After failure model is stable, each treated animal duodenum gives relative medicine and (prepares sample according to above-described embodiment 1 method, the most separately
If individually oriented compound I and individually oriented compound II matched group).Between group, T inspection, carries out statistical procedures.
2, result:
Table 1 present invention impact (n=6, X ± s) on heart failure canine dp/dt
Compare with NS group, * * P < 0.01 * P < 0.05
Table 2 present invention impact (n=6, X ± s) on heart failure canine cardiac work
Compare with NS group, * * P < 0.01 * P < 0.05；Compare before being administered,##P<0.01 #P<0.05
Result is as shown in table 1,2, and the instillation various dose present invention can increase the SW of Heart Failure Dogs, LVW ,+dp/dt (with model group
Matched group compares, p < 0.05or p < 0.01).Gavage various dose Trefolane A can increase the SW of Heart Failure Dogs, LVW ,+dp/dt
(comparing with model group matched group, p < 0.01or p < 0.05), and effect is significantly better than individually oriented compound I and individually oriented compound
II matched group.
Table 3 present invention impact kinemic on heart failure canine (n=6, X ± s)
Compare with NS group, * * P < 0.01 * P < 0.05；Compare before being administered,##P<0.01 #P<0.05
Result is as shown in table 3, and the instillation various dose present composition can increase the cardiac output of Heart Failure Dogs (with model control group
Relatively, p < 0.01or p < 0.05).The gavage various dose present composition can increase the cardiac output of Heart Failure Dogs (with model pair
Compare according to group, p < 0.01or p < 0.05), and effect is significantly better than individually oriented compound I and individually oriented compound II matched group.
Being shown by above-described embodiment, the present composition can increase the SW of Heart Failure Dogs, LVW ,+dp/dt, cardiac output.Thus
Proving, the present composition can significantly improve acute heart failure, can be used to preparation treatment or the medicine of prevention heart failure, and imitates
Fruit is significantly better than individually oriented compound I and individually oriented compound II matched group.
Claims (4)
1. a treatment or prevention acute heart failure pharmaceutical composition, it is characterised in that the active component of said composition is by changing
Compound I and compound II composition, in said composition, the mass percent of compound I and compound II is respectively 70%
With 30%, shown in the structure such as formula (I) of described compound I, shown in the structure such as formula (II) of described compound II:
2. treat as claimed in claim 1 or prevention acute heart failure pharmaceutical composition, it is characterised in that: preparation method is
The powder of compound I and the powder of compound II are sufficiently mixed according to mass percent respectively 70% and 30%, add
Add adjuvant, make preparation.
3. treat as claimed in claim 2 or prevention acute heart failure pharmaceutical composition, it is characterised in that: adjuvant is dextrin
Or starch.
4. treatment or prevention acute heart failure pharmaceutical composition in treatment or prevent acute heart failure medicine as claimed in claim 1
In application.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610249259.9A CN105919997A (en) | 2016-04-19 | 2016-04-19 | Medicine for preventing or treating acute heart failure and application of medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610249259.9A CN105919997A (en) | 2016-04-19 | 2016-04-19 | Medicine for preventing or treating acute heart failure and application of medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105919997A true CN105919997A (en) | 2016-09-07 |
Family
ID=56839853
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610249259.9A Pending CN105919997A (en) | 2016-04-19 | 2016-04-19 | Medicine for preventing or treating acute heart failure and application of medicine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105919997A (en) |
-
2016
- 2016-04-19 CN CN201610249259.9A patent/CN105919997A/en active Pending
Non-Patent Citations (4)
| Title |
|---|
| CELSO ALMEIDA ET AL.: "Unprecedented Polyketides from a Marine Sponge-Associated Stachylidium sp.", 《J. NAT. PROD.》 * |
| JAYANTA DAS ET AL.: "Total Syntheses of Kealiinines A-C", 《ORG. LETT.》 * |
| 孙明等: "丁苯酞抑制大鼠急性心肌缺血导致的心肌损伤", 《安徽医科大学学报》 * |
| 葛建国: "《心血管疾病用药指导》", 30 April 2014, 人民军医出版社 * |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
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| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160907 |