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Prophylactic agent for heart failure

a technology aprophylactic agent, which is applied in the field of systolic heart failure apophylactic agent, can solve the problems of cardiac hypertrophy, systolic heart failure, and inability to readily define diseases, etc., and achieve the effect of preventing cardiac hypertrophy

Inactive Publication Date: 2010-01-28
CALPIS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention provides a compound or composition that can prevent heart wall thickening and heart failure. This compound, called Xaa Pro Pro, has been found to have a suppressive action against heart wall thickening, and can be used in the production of pharmaceuticals and functional foods to prevent heart failure and cardiac hypertrophy. The invention also includes a method for administering Xaa Pro Pro to a subject to suppress heart wall thickening and prevent heart failure. The use of Xaa Pro Pro in producing a pharmaceutical is also described."

Problems solved by technology

Since the pathologic state, classification, and progression of heart failure varies, the disease cannot be readily defined.
Systolic heart failure occurs when the heart fails to contract normally.
The heart can take in blood but cannot fully pump out adequate blood due to weakened cardiac muscles.
As a result, the volume of the blood pumping out to the whole body and lungs decreases and the heart, in particular the left ventricle, can become hypertrophic.
On the other hand, diastolic heart failure occurs when the heart wall becomes too stiff to fill up the heart with blood.
As a result, blood dams up in the left atrium and lung blood vessels, which could cause congestion.
Thus, heart failure generally refers to a condition that heart's pump functions become impaired and hence the heart become incapable of pumping a sufficient amount of blood.
Heart failure could cause other changes which further deteriorate functions of the heart, including a decrease in blood volume and congestion of blood in the veins and lungs.
Also, agnogenic myocardiopathy of unexplained origins, such as myocardosis, may also cause heart wall hypertrophy.
Continuous mechanical load to the heart triggers a gradual decrease in the contractile power of the cardiac muscles, followed by reduction in cardiac performance, and eventually progresses to ventricular arrhythmia, heart ischemia, coronary artery disease, and congestive heart failure.
However, the action is not satisfactory and also some antihypertensive drugs have no effects (Am J. Hypertens. 1997 August; 10(8):913˜20).
Also, even when hypertension is improved, heart wall thickening remains unimproved in many cases.
In such cases there is still a risk for the onset of heart failure.
Yet on the other hand, for heart failure induced by various primary diseases, the ACE inhibitors are not effective for all cases.
Rather there is a risk of developing acute renal failure accompanying lowering blood pressure and therefore it has been pointed out that careful administration is required (Saishin Igaku, 48:1404 to 1409, 1993), That is, the antihypertensive drug can be insufficient for the prophylaxis of heart failure but also could rather induce renal failure.
However, whether they have a suppressive action against heart wall thickening or not has not been directly demonstrated (Japanese Patent Publication No. 2782142, J. Dairy Sci.
Additionally, as described above, since the prophylactic and therapeutic effect for heart failure mediated by ACE inhibition is limited, prophylaxis and treatment of the disease which are not dependent on the ACE inhibition are desired.

Method used

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Examples

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Example of Peptide Synthesis

[0083]The active ingredient according to the present invention Ile Pro Pro and Val Pro Pro were synthesized by the following chemical synthesizing method (Fmoc method). The synthesis was carried out by solid phase method using an automatic peptide synthesizer (PSSM-8type) manufactured by Shimadzu Corporation.

[0084]As a solid phase carrier, 50 mg of a resin (SynProPep Resin®, manufactured by Shimadzu Corporation) which is a 2-chlorotrityl(2-Chlorotrityl)type polystyrene resin in which proline protected its amino group with a fluorenylmethyloxy carbonyl group (hereinafter referred to as Fmoc for short) is bound, was used. According to the above described amino acid sequence, Fmoc-Ile, Fmoc-Pro, and Fmoc-Val (100 μmol each) which are protected their amino group with the Fmoc group were reacted in the order of the peptide sequence to obtain a peptide-bound resin in accordance with a conventional method.

[0085]This peptide-bound resin was then suspended in 1 ml...

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PUM

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Abstract

The present invention provides an agent having a suppressive action against the thickening of the heart wall, a prophylactic agent for heart failure containing the above described agent, and functional foods expected to have a prophylactic effect for heart failure. The agent for suppressing heart wall thickening comprises Xaa Pro Pro as an active ingredient.

Description

FIELD OF THE INVENTION[0001]The present invention relates to an active ingredient having a suppressive action on cardiac wall thickening, a prophylactic agent for cardiac hypertrophy and a prophylactic agent for heart failure containing the active ingredient, as well as functional foods containing the active ingredient, the functional foods being expected to have a prophylactic effect against cardiac hypertrophy and heart failure.[0002]Also, the present invention relates to a method for suppressing cardiac wall thickening. Further, the present invention relates to a method for preventing cardiac hypertrophy and heart failure.BACKGROUND OF THE INVENTION[0003]Recently, the number of those who have a risk factor considered to cause heart diseases, such as smoking, hypertension, hyperglycemia, and hyperlipidemia, have increased in some countries. There is an increasing trend in the number of patients suffering from heart failure. In addition, these pathologic states are not limited to h...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07K5/08A61P9/00A61P9/04A23L33/10A23L33/17A23L33/19A61K35/20A61K35/74A61K35/747A61K36/06A61K38/00A61K38/01A61K38/02A61K38/06A61K38/17A61P43/00C07K14/47C12P21/06
CPCA23L1/3053A23V2002/00A61K38/06A23V2200/326A23V2250/0654A23V2250/064A23V2200/32A23V2250/0626A23L33/18A61P1/16A61P7/00A61P9/00A61P9/04A61P9/10A61P13/12A61P43/00
Inventor HIROTA, TATSUHIKOOHKI, KOHJINAKAMURA, TEPPEITAKANO, TOSHIAKI
Owner CALPIS