106 results about "Myocardial hypertrophy" patented technology

The invention belongs to the technical field of biological medicines, and particularly relates to application of oxibenzophenone in preparation of a medicine for treating pathological cardiac hypertrophy and / or heart failure. Research results in myocardial cells of primary newborn rats show that Exibenzophenone can inhibit pathological hypertrophy of myocardial cells induced by phenylephrine (PE). Animal experiments show that the epoxybenzophenone can improve cardiac dysfunction induced by aortic arch constriction (TAC) and reduce cardiac hypertrophy and cardiac tissue fibrosis. The invention provides a new drug research and development approach and a drug action target for treating pathological cardiac hypertrophy and heart failure, and has very important medicinal value.

Disclosed in the present invention is a use of alisol-B23-acetate (AB23a) in the preparation of a drug for preventing or treating hypertrophic cardiomyopathy and diseases caused by the hypertrophic cardiomyopathy. The present invention provides for the first time a use of AB23a in the prevention or treatment of hypertrophic cardiomyopathy. According to the present invention, use of AB23a in direct in vitro treatment of cardiomyocytes derived from directed differentiation of human embryonic stem cells revealed that AB23a-based in-vitro treatment can significantly inhibit hypertrophic phenotypes of the human embryonic stem cells-cardiomyocytes; using an AB23a-containing feed to feed mice with hereditary hypertrophic cardiomyopathy caused by a gene mutation revealed that AB23a prominently relieves pathological myocardial hypertrophy of the mice and improves the cardiac function; AB23a can be used for preparing a drug for resisting hereditary hypertrophic cardiomyopathy, offering a novel way and means for treating hypertrophic cardiomyopathy; and AB23a is the main medicinal ingredient in the traditional Chinese medicinal herb-Rhizoma Alismatis, is safe to organisms, and has good clinical application prospects.

The invention relates to 3-quinoxalinyl imidazoline thioketone derivatives, a synthesis method and application technical contents. The structural general formula of the derivative is formula 1 or formula 2. The invention provides a preparation method of the derivative. The invention proves that the developed 3-quinoxalinyl imidazoline thioketone derivative has an anti-myocardial hypertrophy effect and can be applied to preparation, research and development of anti-myocardial hypertrophy drugs.

The invention provides an application of liquiritin in preparation of a PPAR gamma receptor partial agonist. Through a structure-based high-throughput virtual screening technology, it is found that liquiritin can be used as a partial agonist of a PPAR gamma receptor, and the relative activation efficiency of liquiritin is 35.9% of that of rosiglitazone; in-vitro experiments prove that liquiritin can remarkably promote glucose uptake and consumption of HepG2 cells and does not induce adipocyte differentiation; in-vivo experiments prove that liquiritin can effectively improve the blood glucose level of an insulin resistance mouse model induced by high fat diet and reduce the level of serum proinflammatory factors. Compared with thiazolidinedione compounds, liquiritin not only can relieve and treat insulin resistance or related metabolic diseases, but also does not cause adverse reactions such as weight gain, fat accumulation and myocardial hypertrophy, provides a new candidate compound for developing safe and effective anti-diabetic drugs, and has a wide application prospect.

The invention belongs to the technical field of biological medicine, and particularly relates to diagnosis and pharmaceutical application of SMOC2. Compared with normal people, the expression level of the SMOC2 gene in the heart of a clinical heart failure patient is increased, and the SMOC2 as a marker has clinical value in the diagnosis of cardiac hypertrophy and heart failure; in addition, by inhibiting the expression of the SMOC2 gene, the cardiac hypertrophy progress of the pressure overload model mouse can be delayed, and then the occurrence of heart failure is prevented. Therefore, a reagent for detecting the expression level of the SMOC2 gene can be used for preparing a reagent for detecting cardiac hypertrophy or heart failure, and an SMOC2 gene expression inhibitor can be used for preparing a medicine for preventing, relieving and / or treating cardiac hypertrophy.

The application discloses application of a BLM helicase inhibitor in treating myocardial hypertrophy. The application firstly finds that the BLM helicase inhibitor ML216 can significantly inhibit cardiac hypertrophy and myocardial cell fibrosis, thereby providing a new drug for treating myocardial cell hypertrophy diseases in the field, and providing practical experimental evidence and scientific basis for treating myocardial cell hypertrophy diseases, and having a good application prospect in treating myocardial hypertrophy and / or cardiac hypertrophy.

This invention discloses the application of alismazone B acetate in the preparation of drugs for the prevention or treatment of hypertrophic cardiomyopathy and its related symptoms. This invention is the first to propose the use of alismazone B acetate (AB23a) for the prevention or treatment of hypertrophic cardiomyopathy. The invention utilizes AB23a to directly treat cardiomyocytes obtained from directed differentiation of human embryonic stem cells in vitro, finding that AB23a treatment significantly inhibits the hypertrophic phenotype of human embryonic stem cell-cardiomyocytes. Feeding mice with hereditary hypertrophic cardiomyopathy caused by gene mutations to a diet containing AB23a showed that AB23a significantly alleviated pathological myocardial hypertrophy and improved cardiac function in mice. AB23a can be used to prepare drugs against hereditary hypertrophic cardiomyopathy, providing a new approach and method for treating hypertrophic cardiomyopathy. AB23a is the most important medicinal component of the traditional Chinese medicine Alisma plantago-aquatica, is safe for organisms, and has good clinical application prospects.

The invention belongs to the technical field of gene therapy, and particularly relates to application of an inhibitor of a targeted Connexin43 gene in preparation of a medicine for preventing or treating myocardial fibrosis. In order to define the effect of connexin43 in the cardiac hypertrophy process caused by myocardial cell hypertrophy induced by pathological matrix stiffness and pressure overload, the invention provides application of an inhibitor of a targeted Connexin43 gene in preparation of a medicine for preventing or treating myocardial fibrosis. According to the application disclosed by the invention, the Connexin43 gene is found to be used as a potential target for preventing or treating myocardial fibrosis for the first time, and a myocardial cell hypertrophy process induced by pathological matrix hardness and a myocardial hypertrophy process caused by overload of pressure can be relieved by knocking down the expression of the Connexin43 gene or inhibiting the semi-channel activity of the Connexin43. Therefore, the inhibitor targeting the Connexin43 gene can be used for preparing the medicine for preventing or treating the myocardial fibrosis, and a new way is provided for treating the myocardial fibrosis.

The invention discloses application of an HIF1A inhibitor in preparation of a medicine for preventing and / or treating hypertrophic cardiomyopathy, and belongs to the field of biological medicine. For a rat model of spontaneous hypertrophic cardiomyopathy caused by MYH7B gene knockout, hypertrophic cardiomyopathy can be significantly relieved by intraperitoneal injection of the HIF1A inhibitor LW6, heart remodeling can be relieved, heart functions can be improved, and myocardial hypertrophy caused by silent MYH7B genes can be effectively resisted by using siRNA of mRNA transcribed by the HIF1A gene. The key mechanism of the HIF1A inhibitor for treating the hypertrophic cardiomyopathy is that the hypertrophic cardiomyopathy is prevented and treated by reducing the expression level of glycolysis key enzymes GLUT1, HK2 and the like, inhibiting the formation and accumulation of cardiac lactic acid and improving the ventricular remodeling of the hypertrophic cardiomyopathy. The results show that the HIF1A inhibitor can be used for treating and / or preventing the human hypertrophic cardiomyopathy and has the potential of being developed into the medicine for clinically preventing and treating the hypertrophic cardiomyopathy.

The invention belongs to the technical field of biological medicine, and particularly provides application of flufenidone in preparation of a medicine for preventing or treating left heart failure. The research finds that the flufenidone has the effects of relieving myocardial cell hypertrophy under a heart failure cell model and relieving myocardial hypertrophy, fibrosis and heart function deterioration of an aortic constriction animal model. According to the present invention, further research results show that fluorofenidone is directly combined with SERCA2a through Q758, D812 and E917 residues of SERCA2a so as to inhibit recognition, combination and polyubiquitination effects of WWP1 on SERCA2a, such that the protein level and the activity of SERCA2a are stabilized so as to achieve the chronic left heart failure treatment purpose. Therefore, the flufenidone serving as an active ingredient has good application prospect and application value in research and development of novel medicines for treating chronic left heart failure.

The invention discloses a method for preventing and treating myocardial hypertrophy through calcium steady-state regulation and control of cassia twig and liquorice decoction, and belongs to the technical field of traditional Chinese medicine pharmacy and nano medicine. The nano-system has a core-shell structure, and a core of the nano-system wraps monarch and minister effect components composed of cassia twig and licorice fat-soluble components and is composed of an ATP responsive polymer; a shell of the pH-responsive adjuvant drug delivery system wraps an adjuvant effect component group composed of liquorice water-soluble components, the pH-responsive adjuvant drug delivery system is composed of a pH-responsive polymer, the surface of the pH-responsive polymer is modified with AT1R targeting peptide, and a preparation method of the pH-responsive adjuvant drug delivery system comprises the following steps: respectively preparing MMG and AEG; two-step self-assembly is carried out through a microfluidic technology, and AEG is used as a molecular template in the second step to guide the shell polymer to coat the core. The nano system disclosed by the invention can actively target hypertrophic myocardial cells, preferentially release AEG in a focus subacid environment, and then release MMG in a high ATP environment in the cells, so that materialization of a monarch, minister, assistant and guide compatibility theory is realized, and the targeting property, bioavailability and synergistic treatment effect of drugs are remarkably improved.

The invention relates to the technical field of traditional Chinese medicine preparations, in particular to an anti-heart-failure traditional Chinese medicine composition and a pharmaceutical preparation. The traditional Chinese medicine composition comprises sun-dried ginseng, radix ophiopogonis, schisandra chinensis, American ginseng, pseudo-ginseng and poria cocos. The traditional Chinese medicine composition for resisting heart failure and the medicinal preparation provided by the invention can relieve myocardial damage and load of patients with heart failure and relieve myocardial hypertrophy and fibrosis, so that the heart function of the patients with heart failure is effectively improved.

The application discloses application of a lipoic acid analogue in preparation of a product for relieving myocardial cell hypertrophy, and the lipoic acid analogue DMAE-LA is N -(2-(dimethylamino)ethyl)-5-(1,2-dithiopentyl-3-yl)valeric amide. DMAE-LA can effectively reduce ISO-induced myocardial hypertrophy of mice, reduce heart weight index and ANP and BNP expression, and significantly improve heart function. A small dose (2-10 μM) of a lysosome-targeting lipoic acid analogue DMAE-LA can effectively improve Ang II-induced myocardial hypertrophy and oxidative stress in H9c2 cells, and the protective effect is better than that of a high dose (200-400 μM) of LA. As a new substitute of traditional LA, DMAE-LA shows great potential for prevention and treatment of cardiovascular diseases.

The application relates to the technical field of medicines, and discloses application of gymnemon and a medicine thereof.According to the application, the gymnemon can be used for preparing medicines related to cardiovascular diseases, including medicines for improving heart failure, inhibiting myocardial hypertrophy, improving vascular endothelial function and reducing blood pressure, and further used for preparing medicines for reducing expressions of vascular cell adhesion molecule 1 and intercellular adhesion molecule 1 and / or increasing serum NO level; the gymnemon can also be used for preparing medicines for regulating abnormal lipid metabolism, including medicines for reducing triglyceride and total cholesterol level; the gymnemon can also be used for preparing medicines for relieving liver injury, including medicines for reducing glutamic-pyruvic transaminase and glutamic-oxalacetic transaminase level; and the gymnemon can also be used for preparing medicines for improving systemic inflammation and / or platelet and thrombin dysfunction.

This invention discloses a class of pyrazolopyridine compounds linked by an aza-four-membered ring, or pharmaceutically acceptable salts thereof, and their applications. These compounds can serve as novel, highly selective PDE10A inhibitors for the treatment of peripheral tissue diseases, including: myocardial hypertrophy and cardiac dysfunction (heart failure), diabetes, hypertension, renal impairment and renal fibrosis, pulmonary inflammation and pulmonary fibrosis, immune dysregulation, and cancers (colon cancer, ovarian cancer, and lung cancer). Two strategies are employed to achieve high selectivity for PDE10A inhibition while simultaneously reducing the inhibitory effect on the central nervous system. First, molecular structure modification: structural optimization of the aza-four-membered ring-linked pyrazolopyridine compounds, such as increasing the ratio of N, O, and S atoms in the molecular structure to increase the polar surface area and reduce lipophilicity; and introducing hydrophilic groups to increase water solubility, thereby reducing the permeability of the compound to the blood-brain barrier (BBB). Second, targeted drug delivery to lung tissue via pharmaceutical formulation.

The present application relates to the application of CircRAB3IP in the preparation of a drug for promoting angiogenesis, and belongs to the technical field of biological medicine; the present application provides the application of CircRAB3IP in the preparation of a drug for preventing or treating heart failure; in the preparation of a drug for promoting angiogenesis; in the preparation of a heart failure prognosis diagnosis kit; and in the preparation of a myocardial hypertrophy prognosis diagnosis kit; the present application proves through in-vivo and in-vitro experiments that circRAB3IP can promote angiogenesis, and can effectively improve heart function disorder caused by high blood pressure mechanical stress, slow down cardiac remodeling, myocardial fibrosis, and reduce cardiac inflammation. The present application provides a new target and theoretical basis for the treatment of hypertensive cardiac remodeling.

The invention provides a potential therapeutic target for cardiac hypertrophy and heart failure, finds that the cardiac hypertrophy caused by pressure load can be obviously relieved by using adeno-associated virus (AVV9) as a carrier myocardial cell specific overexpression Ces1d gene, and finds that the Ces1d relieves the cardiac hypertrophy by promoting fatty acid oxidation; and a potential target and a new strategy are provided for heart failure treatment. According to the invention, Ces1d is taken as a regulation target, and the expression level of Ces1d is regulated, so that the fatty acid oxidation of myocardial cells can be obviously promoted, and the expression of fatty acid oxidation related genes such as Cpt1a, Cpt1b, Cpt2, Acadm, Acadvl and Acox1 can be up-regulated, thereby optimizing the utilization mode of a myocardial energy metabolism substrate; meanwhile, mitochondrial dysfunction and mitochondrial generation damage induced by pressure load can be improved. Therefore, the regulation strategy taking the Ces1d as the action target and the AVV9 as the carrier provides a new gene therapy technical approach for prevention and treatment of cardiac hypertrophy and related cardiovascular diseases, and has a good application prospect and a remarkable clinical potential value.

This invention relates to the field of congenital heart disease treatment technology, and discloses the application of sapropterin in the prevention and treatment of bisphenol fluorene-induced congenital heart disease in fetuses. The congenital heart disease includes cardiac structural defects, heart failure, or cardiomyocyte lesions, specifically selected from ventricular septal defects, atrial septal defects, tetralogy of Fallot, myocardial hypertrophy, decreased cardiac ejection fraction, decreased short-axis contraction rate, cardiomyocyte ferroptosis, myocardial tissue inflammatory infiltration, or myocardial collagen fibrosis. Sapropterin is used as a direct supplement to biological tetrahydropterin (BH4). Through exogenous intervention, it precisely reverses the endogenous BH4 deficiency caused by bisphenol fluorene exposure, restores the expression of GTP cyclase 1 (GCH1) and the dynamic balance of RNA m6A, and upregulates the level of YTH domain family protein 2 (YTHDF2), thereby blocking ferroptosis signal transduction, reducing oxidative stress and inflammatory response, and inhibiting the process of myocardial tissue fibrosis at the molecular level.

This invention belongs to the field of biomedical technology, specifically involving Trmt61a The application of genes in the preparation of drugs for treating pathological myocardial hypertrophy. This invention provides... Trmt61a The application of genes in the preparation of drugs for treating pathological myocardial hypertrophy, the aforementioned Trmt61a The nucleotide sequence of the gene is shown in SEQ ID NO.1. Animal experiments have shown that knocking down... Trmt61a Gene knockdown can significantly improve cardiac contractile function after aortic arch coarctation surgery, alleviate cardiomyocyte hypertrophy, reduce the degree of cardiac fibrosis, and effectively treat pathological myocardial hypertrophy. This invention is the first to demonstrate knockdown... Trmt61a Genes can effectively improve pathological myocardial hypertrophy, providing a new drug development path and target for the prevention and treatment of this disease, and have important medicinal value and clinical application prospects.

The invention discloses an application of a disulfiram medicine in improving sepsis induced cardiomyopathy. The disulfiram drug is administered in a sepsis mouse model, and the disulfiram drug is proved to have obvious anti-inflammatory effect and myocardial protection effect. The disulfiram medicine can relieve myocardial hypertrophy of mice, relieve the degree of myocardial fibrosis and reduce myocardial interstitial inflammatory exudation, ZO-1 reconstructs continuous linear distribution after administration, and the degree of myocardial edema is obviously relieved. The invention provides a new application of the disulfiram medicine in improving sepsis-induced cardiomyopathy, and provides a new strategy for myocardial protection of sepsis.

The application discloses a kind of short peptides simulating RhoE C end, derivative and its pharmaceutical use in treating ventricular remodeling, belong to biological medicine technical field.The short peptide and derivative contain RhoE C end 200-240 linear function domain, can be combined and activated WWP2, remove HGS self-inhibition, start endosome-lysosome degradation pathway.Short peptide sequence is as SEQ ID NO.1, derivative can be coupled with TAT, T7 or RVG membrane penetrating peptide (SEQ ID NO.2-4), and endocytosed to myocardial cell by caveolin high efficiency delivery.The application solves the defects that existing anti-ventricular remodeling drug inhibits protective autophagy flow, and the ability of eliminating toxic protein is limited, can efficiently eliminate damaged mitochondria and misfolded protein, inhibits myocardial hypertrophy, fibrosis, improves cardiac remodeling, provides safe and effective treatment strategy for related diseases.

The present invention discloses the use of a traditional Chinese medicine composition in the preparation of a drug for preventing or treating diabetic cardiomyopathy. The traditional Chinese medicine composition of the present invention is composed of notopterygium root, angelica dahurica, Poria cocos, saposhnikovia root, schizonepeta tenuifolia, ligusticum wallichii, chuanxiong rhizome, platycodon grandiflorum, bupleurum root, peucedanum chinense, fructus aurantii, and liquorice. Pharmacodynamic experimental results show that the traditional Chinese medicine composition of the present invention can reduce serum creatine kinase isoenzyme (CK-MB) and lactate dehydrogenase (LDH) levels, and can significantly improve diabetic myocardial cell damage; reduce cardiac index, improve myocardial hypertrophy and left ventricular remodeling, and has the effect of preventing and treating diabetic cardiomyopathy.

This invention belongs to the field of biomedical engineering and relates to the application of SnoRNA Gm26330 as a biomarker and therapeutic target for myocardial hypertrophy. This invention provides a biomarker for myocardial hypertrophy, snoRNA Gm26330, the nucleotide sequence of which is shown in SEQ ID No. 1. In vitro and in vivo experiments have shown that SnoRNA Gm26330 can inhibit myocardial hypertrophy and has a protective effect against myocardial damage caused by myocardial hypertrophy. SnoRNA Gm26330 has potential value in the preparation of drugs for the prevention and treatment of related heart diseases.

Use of darutoside in preparing a drug for preventing and treating hereditary hypertrophic cardiomyopathy. The darutoside is used for directly treating hypertrophic cardiomyocytes in vitro. It is found that the darutoside significantly reduces the area of cardiomyocytes, and reduces the increase of myocardial hypertrophy marker expression caused by angiotensin II; meanwhile, feed containing the darutoside is applied to feed Tnnt2R109Q mice, such that the weight of the left ventricle and heart of the mice is reduced, the heart volume and the thickness of the myocardial wall during diastole and systole are reduced, and myocardial tissue fibrosis of the mice with hypertrophic cardiomyopathy is effectively inhibited. The darutoside can be used for preparing a drug for preventing and treating hereditary hypertrophic cardiomyopathy and provides a new way and means for treating hypertrophic cardiomyopathy.

The invention provides an application of up-regulated human enoyl coenzyme A delta isomerase 2 (ECI2) in preparation of a medicine for protecting a cardiac function. It is found for the first time that up-regulation of ECI2 promotes degradation of crotonyl coenzyme A by consuming a crotonyl donor (crotonyl coenzyme A) and effectively inhibits crotonyl modification, so that the heart function and myocardial hypertrophy can be effectively improved, and then the heart function protection effect on pressure overload heart diseases and heart failure is achieved. The above findings indicate a huge potential of upregulating ECI2 in the prevention and / or treatment of pressure overload heart diseases and heart failure.

The application discloses a plant extraction compound for reducing blood pressure, a preparation method and application thereof. The compound is composed of high-purity silybin extract and a specific fusion polypeptide through molecular self-assembly. The sequence of the fusion polypeptide is shown in sequence SEQ ID NO:1, which innovatively integrates cell membrane penetration function, angiotensin II receptor 1 antagonism function and hydrophobic drug binding function. The core of the application is that through polypeptide-mediated active targeting, silybin is accurately delivered to the diseased blood vessel area, and the double synergistic mechanism of upstream ACE inhibition and downstream receptor blocking of the renin-angiotensin-aldosterone system is realized. In-vivo pharmacodynamic experiments prove that compared with single components, the compound can produce more significant and persistent antihypertensive effect, and can effectively reverse myocardial hypertrophy and fibrosis caused by hypertension, and show excellent synergistic therapeutic effect and target organ protection ability.

This invention belongs to the field of pharmaceutical technology, and relates to diphenylmethane derivatives, their preparation methods, and applications. The diphenylmethane derivative is a compound represented by Formula I, its optical isomer, or a pharmaceutically acceptable salt thereof: wherein X is CH2; Y is selected from: -NH-, -CO-, -NHCONH-. The diphenylmethane derivative of this invention is stable, easy to store, and readily prepared, exhibiting good feasibility. It demonstrates outstanding in vitro and in vivo efficacy and good safety profile when used to prepare anticardioprotective drugs (for heart failure and myocardial hypertrophy).

The invention relates to a viral vector carrying a Prrg3 gene expression cassette and application thereof in treating diseases. Specifically, the invention relates to a Prrg3 gene expression cassette, a virus vector carrying the Prrg3 gene expression cassette and application of the virus vector in treatment of heart failure, cardiac hypertrophy, hypertension, overweight, obesity, diabetes, fatty liver, hyperlipidemia and other diseases, and the virus vector is especially suitable for ejection fraction retention heart failure patients with one or more diseases. The application provides a new thought and strategy for clinical treatment of ejection fraction retention heart failure and complications thereof, and has a wide application prospect.

The application relates to application of siRNA-OTUB1 in preparation of drugs for preventing or treating myocardial cell hypertrophy, and belongs to the biomedical technical field.The nucleotide sequence of the OTUB1 gene is shown as SEQ ID NO.1, and the targeted nucleotide sequence of the siRNA-OTUB1 for specifically interfering with the expression of the OTUB1 gene is shown as SEQ ID NO.2 or SEQ ID NO.3.The application innovatively proposes a strategy for preventing or treating myocardial cell hypertrophy by taking deubiquitinase OTUB1 as a core target point and by interfering with the expression thereof.In a myocardial cell experiment of a milk rat, the application of the designed siRNA-OTUB1 can effectively reduce the expression levels of OTUB1 mRNA and OTUB1 protein, and further reduce the degree of myocardial cell hypertrophy.Based on the finding, the OTUB1 gene can be developed as a novel treatment target point for myocardial cell hypertrophy, is used for designing a targeted drug, and provides a new technical thought for precise treatment of myocardial hypertrophy.

The invention discloses application of TRPML1 or an agonist thereof in preparation of a medicine for inhibiting myocardial cell hypertrophy and heart failure. According to the application disclosed by the invention, it is found through an in-vitro cell experiment and an in-vivo animal experiment that the TRPML1 (TRPML1) has a remarkable effect of resisting myocardial cell hypertrophy and heart failure. In addition, a mechanism of TRPML1 resisting heart failure is explored by adopting a proteomics technology and a molecular docking means, and the application basic theory is firm. On the basis, the invention provides a new strategy for treating myocardial cell hypertrophy and heart failure based on TRPML1 for the first time, the application of TRPML1 in clinical treatment of heart failure is promoted, the time from drug discovery to clinical transformation is greatly shortened, and the application has important clinical significance in treatment of myocardial cell hypertrophy and heart failure.