CN105412081A - Application of Penicillactones A in preparing drugs for treating or preventing acute heart failure - Google Patents
Application of Penicillactones A in preparing drugs for treating or preventing acute heart failure Download PDFInfo
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- CN105412081A CN105412081A CN201510963779.1A CN201510963779A CN105412081A CN 105412081 A CN105412081 A CN 105412081A CN 201510963779 A CN201510963779 A CN 201510963779A CN 105412081 A CN105412081 A CN 105412081A
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- Prior art keywords
- heart failure
- penicillactonesa
- acute heart
- treatment
- application
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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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
-
- 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
-
- 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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention provides application of Penicillactones A in preparing drugs for treating or preventing acute heart failure, and is disclosed for the first time; due to the fact that a matrix type belongs to a new matrix type, and the activity on treating acute heart failure is high, the Penicillactones A has outstanding substantive features, and obviously has remarkable improvement for treatment of acute heart failure at the same time.
Description
Technical field
The present invention relates to the novelty teabag of compound PenicillactonesA, particularly relate to the application of PenicillactonesA 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 PenicillactonesA that the present invention relates to is one and delivers (YunbaoLiu in 2013, etal., StructuresandAbsoluteConfigurationsofPenicillactonesACfr omanEndophyticMicroorganism, PenicilliumdangeardiiPitt.ORGANICLETTERS, 2013, 15 (20) 5206 – 5209.) noval chemical compound, this compound has brand-new framework types (YunbaoLiu, etal., StructuresandAbsoluteConfigurationsofPenicillactonesACfr omanEndophyticMicroorganism, PenicilliumdangeardiiPitt.ORGANICLETTERS, 2013, 15 (20) 5206 – 5209.), the purposes of the PenicillactonesA that the present invention relates in preparation treatment or prevention acute heart failure medicine belongs to first public.
Summary of the invention
The present invention proposes the application of PenicillactonesA in preparation treatment or prevention acute heart failure medicine.Find out from pharmacological evaluation, PenicillactonesA has the effect for the treatment of preferably or prevention acute heart failure.Due to the pharmacological action of the first public PenicillactonesA of the present invention in treatment or prevention acute heart failure.
Described compound PenicillactonesA structure is as shown in formula I:
Formula I
The application of described PenicillactonesA in preparation treatment or prevention acute heart failure medicine, PenicillactonesA increases the cardiac output of Heart Failure Dogs.
A kind for the treatment of or prevention acute heart failure medicine, be that active component interpolation adjuvant is prepared from by PenicillactonesA, preparation method, for getting 5 g of compound PenicillactonesA, 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 PenicillactonesA, preparation method, for getting 5 g of compound PenicillactonesA, adds starch 195 grams, mixing, encapsulatedly makes 1000.
Technical scheme of the present invention is: the application of PenicillactonesA, 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 PenicillactonesA can increase the SW of Heart Failure Dogs, LVW ,+dp/dt, cardiac output.Therefore, PenicillactonesA for the preparation of the medicine of prevention heart failure, can have good development prospect.
The purposes of the PenicillactonesA 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 strong, 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 PenicillactonesA involved in the present invention is see document (YunbaoLiu, etal., StructuresandAbsoluteConfigurationsofPenicillactonesACfr omanEndophyticMicroorganism, PenicilliumdangeardiiPitt.ORGANICLETTERS, 2013,15 (20) 5206 – 5209.)
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 PenicillactonesA tablet involved in the present invention:
Get 5 g of compound PenicillactonesA, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound PenicillactonesA capsule involved in the present invention:
Get 5 g of compound PenicillactonesA, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1: adopt NS method assessing compound PenicillactonesA to the therapeutical effect of dog acute heart failure
1, method: dog is divided at random NS group (waiting capacity solvent), gastric infusion PenicillactonesA2.0mg/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 1PenicillactonesA 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 2PenicillactonesA 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 PenicillactonesA 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 PenicillactonesA can increase SW, the LVW ,+dp/dt (comparing with model group matched group, p<0.01orp<0.05) of Heart Failure Dogs.
Table 3PenicillactonesA 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 PenicillactonesA can increase the cardiac output (comparing with model control group, p<0.01orp<0.05) of Heart Failure Dogs.Gavage various dose PenicillactonesA can increase the cardiac output (comparing with model control group, p<0.01orp<0.05) of Heart Failure Dogs.
Shown by above-described embodiment, PenicillactonesA of the present invention can increase the SW of Heart Failure Dogs, LVW ,+dp/dt, cardiac output.Prove thus, PenicillactonesA 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.PenicillactonesA in treatment or prevention acute heart failure medicine, described compound PenicillactonesA structure is as shown in formula I:
- 2. the application of PenicillactonesA in treatment or prevention acute heart failure medicine as claimed in claim 1, is characterized in that PenicillactonesA increases the cardiac output of Heart Failure Dogs.
- 3. a treatment or prevention acute heart failure medicine, it is characterized in that by PenicillactonesA described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound PenicillactonesA, adds 195 grams, dextrin, mixing, Conventional compression makes 1000.
- 4. a treatment or prevention acute heart failure medicine, it is characterized in that by PenicillactonesA described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound PenicillactonesA, adds starch 195 grams, mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510963779.1A CN105412081A (en) | 2015-12-20 | 2015-12-20 | Application of Penicillactones A in preparing drugs for treating or preventing acute heart failure |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510963779.1A CN105412081A (en) | 2015-12-20 | 2015-12-20 | Application of Penicillactones A in preparing drugs for treating or preventing acute heart failure |
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| Publication Number | Publication Date |
|---|---|
| CN105412081A true CN105412081A (en) | 2016-03-23 |
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|---|---|---|---|
| CN201510963779.1A Pending CN105412081A (en) | 2015-12-20 | 2015-12-20 | Application of Penicillactones A in preparing drugs for treating or preventing acute heart failure |
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| CN (1) | CN105412081A (en) |
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Application publication date: 20160323 |