41 results about "Endothelin 1" patented technology

Chronic glaucoma, cataract, ocular and periocular aging are treated and prevented by the administration of agents that affect metabolic subsystems such as (i) mitochondrial bioenergetics, (ii) free radical moderation and glutathione maintenance, (iii) constitutive nitric oxide / endothelin-1 balance, and (iv) calcium wave signaling and associated neuronal excito-toxicity. Included among the agents are tetrahydrobiopterin, R-alpha-lipoic acid, coenzyme Q10, 17 alpha-estradiol, and glutathione.

The present invention relates to compositions comprising semi-crystalline beta-1-4-N-acetylglucosamine polymers (p-GlcNac) and methods utilizing such polymers modulation of vascular structure and / or function. The compositions and methods disclosed are useful for stimulating, in a p-GlcNac concentration-dependent manner, endothelin-1 release, vasoconstriction, and / or reduction in blood flow out of a breached vessel, as well as for contributing to or effecting cessation of bleeding. The methods of the present invention comprise topical administration of materials comprising semi-crystalline p-GlcNac polymers that are free of proteins, and substantially free of single amino acids as well as other organic and inorganic contaminants, and whose constituent monosaccharide sugars are attached in a beta-1-4 conformation.

The present application is directed to the identification of mutations and / or polymorphisms in the Dual Endothelin-1 / Angiotensin II Receptor (Dear) that indicate susceptibility to, or show current affliction with, hypertension. Additionally, the present invention discloses methods for the modulation of angiogenesis via the regulation of Dear.

The present invention provides antibodies that bind big-endothelin-1 (“big-ET-1”), and methods of using same. According to certain embodiments of the invention, the antibodies specifically bind human big-ET-1 but do not bind human small-ET-1 (i.e., the active form of endothelin-1 that results from proteolytic cleavage of big-ET-1 by endothelin-converting enzyme-1 [ECE-1]). According to certain embodiments of the invention, the anti-big-ET-1 antibodies are capable of blocking cleavage of big-ET-1 by ECE-1. The antibodies of the invention are useful for the treatment of big-ET-1-related disorders, including hypertension disorders, fibrotic disorders, neurodegenerative disorders, retinal disorders, pain and cancers.

The present invention relates to compositions comprising semi-crystalline beta-1-4-N-acetylglucosamine polymers (p-GlcNac) and methods utilizing such polymers modulation of vascular structure and / or function. The compositions and methods disclosed are useful for stimulating, in a p-GlcNac concentration-dependent manner, endothelin-1 release, vasoconstriction, and / or reduction in blood flow out of a breached vessel, as well as for contributing to or effecting cessation of bleeding. The methods of the present invention comprise topical administration of materials comprising semi-crystalline p-GlcNac polymers that are free of proteins, and substantially free of single amino acids as well as other organic and inorganic contaminants, and whose constituent monosaccharide sugars are attached in a beta-1-4 conformation.

Cell transplantation for constructing biological heart pacemaker is used embryo source dry / ancestral cell and adult mesogalia dry cell as cell sources. The process is carried out by oriented differentiation inducing for heart pacemaker cell by embryo source multifunctional dry cell, bone marrow adhering to obtain primary culture cell, clone culturing to obtain purifying system by diluting, applying paracrine factor endothelin-1 or nervous adjusting protein-1, extracellular matrix laminated adherent protein and fiber connecting protein etc. substrate glue, trans-dyeing pacemaker gene HCN4, and in-vitro inducing embryo source multifunctional dry cell. It is various and non-immunogenicity. It can be used to treat sick sinus syndrome.

The present invention relates to therapeutic protocols and pharmaceutical compositions designed to treat and prevent cancer. More specifically, the present invention relates to a novel method of treating cancer using antagonists to the endothelin B receptor (ETB) or inactive mimic forms of endothelin-1. The pharmaceutical compositions of the invention are capable of selectively inhibiting the early events associated with the development of cancer. The present invention further relates to screening assays to identify compounds which inhibit ETB activation.

Sequences in human preproendothelin-1 mRNA are described against which antisense oligonucleotides can be used to inhibit the synthesis of endothelin-1. This inhibition of endothelin-1 synthesis may be used to treat diseases where excess production of endothelin-1 is an underlying cause of the symptoms.

The present invention relates to methods and compositions for monitoring, diagnosis, prognosis, and determination of treatment regimens in subjects suffering from or suspected of having a renal injury. In particular, the invention relates to using a one or more assays configured to detect a kidney injury marker selected from the group consisting of Endothelin-1, Somatotropin, and Interleukin-13 as diagnostic and prognostic biomarkers in renal injuries.

The present application is directed to the identification of mutations and / or polymorphisms in the Dual Endothelin-1 / Angiotensin II Receptor (Dear) that indicate susceptibility to, or show current affliction with, hypertension. Additionally, the present invention discloses methods for the modulation of angiogenesis via the regulation of Dear.

The invention relates to novel pharmacological action of traditional Chinese medicine salvianolic acid A and application thereof in the preparation of products for preventing, relieving and / or treating pulmonary arterial hypertension and its complications. The salvianolic acid A has the advantages that the salvianolic acid A has the pharmacological action of relieving pulmonary circulation pressure rise, the pharmacological actions of relieving right heart failure due to pulmonary arterial hypertension, improving right ventricular hypertrophy and right ventricular enlargement, improving heart injury due to pulmonary arterial hypertension, and restoring from heart failure, and the pharmacological actions of lowering endothelin-1 level in pulmonary tissues, relieving pulmonary arterial remodeling and improving pathologic damage of pulmonary tissues; the salvianolic acid A is a monomer compound extracted from Salvia miltiorrhiza, has low toxicity, has a wide source range of material, has promising application and development prospect, is an ideal novel traditional Chinese medicine monomer for treating pulmonary arterial hypertension and its complications, and may be applied to prepare products for preventing, relieving and treating pulmonary arterial hypertension and its complications, such as chronic obstructive pulmonary emphysema, chronic pulmonary heart disease and heart failure.

The invention discloses an application of sodium butyrate in the preparation of hypoxic pulmonary hypertension control medicines. The sodium butyrate has an inhibition effect on the secretion of endothelin-1 of hypoxic endothelial cells and has a promotion effect on the secretion of NO in the hypoxic endothelial cells, so the hypoxic pulmonary hypertension disease is controlled. The sodium butyrate has the advantages of stable property, easy dissolving in aqueous solutions, direct oral taking after dissolving, convenient administration, convenient carrying, non-toxicity and harmlessness, and low price.

The invention provides an anti-alcohol drink used for protecting liver and gastric mucosa, and a preparation method of the drink. The method comprises the steps of mixing semen hoveniae, radix salviae miltiorrhizae, radix puerariae, radix codcnopsitis pilosulas, pericarpium citri reticulatae, fructus lycii, flos puerariae, fructus crataegi, radix glycyrrhizae and fructus ligustri lucidi according to a weight ratio, and decocting a mixture twice by using water with the weight 8 times that of the mixture; and combining filter liquors and performing reduced pressure concentration to prepare fluid extract. By building models of acute liver injury and gastric mucosal lesion of mice, tissue forms of the liver and the gastric mucosa are checked, and indexes such as ALT, AST, ALB and the like in serum are measured; an immunohistochemical method is used for detecting expression situations of MnSOD, BCL-2 and Caspase-3 of the liver; a fluorescent PCR method is used for detecting gene expression levels of Nrf2 and SOD of liver tissues; gastric mucosal lesion indexes, inhibition rates and content of endothelin-1 and the like of the gastric mucosa of each group of mice are measured; the protection effect of the drink on the liver and gastric mucosa of a mouse is comprehensively researched; and experimental data proves that the drink can improve oxidation resistance of the liver and inhibit liver cell apoptosis, and has the effect of protecting gastric mucosal lesion.

The invention discloses a preparation method and application of an RNA interfering medicine for treating a pulmonary hypertension syndrome and an efficacy validation method thereof. The preparation method comprises the following steps: firstly, establishing a slow virus expression vector, namely HIF-1alpha-shRNAi; secondly, packaging HIF-1alpha-shRNAi recombinant plasmids into a preparation; thirdly, injecting the plasmids into bodies of broilers, silencing an HIF-1alpha gene, inhibiting expressions of a vascular endothelial growth factor (VEGF), endothelin 1 (ET 1) and an insulin-like growth factor II (IGF - II) of a downstream gene and the like, controlling a pulmonary vascular remodeling (PVR) phenomenon, reducing damage of a cardiopulmonary function and ascites formation and finally achieving the clinical treatment to the pulmonary hypertension syndrome. The preparation method has the advantages of specificity, high efficiency and multifunctionality and the like on an aspect of treatment.

A method for diagnosing, or differentially diagnosing, interstitial cystitis (IC) involves detecting or measuring increased expression of a biomarker Endothelin 1 (ET-1) in a biological sample from a mammalian subject, particularly in the urine or urothelial tissue. An increased level of expression of ET-1 above the level of expression in the same sample of a healthy mammalian subject is an indication of a diagnosis of IC. Such diagnosis may further involve identify other clinical symptoms of IC. Additionally the method may use additional biomarkers, such as Hb-EFG, EGF, APF, IL-8, IL-6, and cGMP. Assay methods and diagnostic reagents and kits for such diagnosis are provided. Methods and compositions for treating IC by reducing the action, production or synthesis of ET-1 in the urine or urothelium and / or inhibiting its binding to its ETA and / or ETB receptors are also provided.

The invention discloses application of a scirpusin component C in common burreed rhizome in synthesis of anti-blood stasis syndrome drugs. The invention first proves that the scirpusin C has an obvious anti-blood stasis drug effect, and can be used for preparing a medicine for treating the blood stasis syndrome. Pharmacological experiments prove that the scirpusin C is capable of obviously reducing the levels of thromboxane B2 (TXB2), fibrinogen (FIB), active plasminogen activator inhibitor (PAI-1) and endothelin 1 (ET-1) in serum of blood stasis model mice and improving the thymus index (TI),spleen index (SI) and hepatic index (HI) of the mice, and has high clinical application value and development prospects in the aspect of treating the blood stasis syndrome.

The invention discloses polypeptide having effect of resisting tumors and use of the polypeptide. The polypeptide is named as TAT-ETA1, is polypeptide as shown as (1) or (2): (1) polypeptide of the 12-69th amino acid residues of an amino acid sequence as shown in SEQ ID NO:1; and (2) polypeptid of an amino acid sequence as shown in SEQ ID NO:1. The polypeptide TAT-ETA1 provided by the invention isfrom the carboxyl terminal of A type endothelin receptor 1(ETAR), when the TAT-ETA1 can act on ETAR in endothelin 1, the TAT-ETA1 can be combined with the carboxyl terminal of the Beta-arrestin 1 (ETAR) competitively to interfere interact between ETAR and beta-arrestin 1 so as to relieve cancer cell migration, invasion induced by the beta-arrestin 1, reverse tolerance during chemotherapy and thelike. The polypeptide TAT-ETA1 has clinical application potential for treatment of cancer.

The present invention provides methods of treating Alport syndrome in a subject by the administration of an agent that can block the activation of RAC1 / CDC42 members of the rho family of small GTPases. Such agents include, but are not limited to, the endothelin receptor antagonists such as bosentan and letairis and neutralizing antibodies to endothelin-1. Such administration prevents invasion of the glomerular capillary tufts by mesangial lamellipodial / filopodial processes, blocks mesangial process invasion abrogates the deposition of laminin 211 in the GBM, and prevents the activation of maladaptive expression of proteins known to contribute to glomerular disease progression.

The present invention relates to a composition containing a Scutellaria alpina extract as an active ingredient. The composition of the present invention exhibits effects of reducing the amount of endothelin 1 by containing a Scutellaria alpina extract, and reducing the overexpression of NK1R and EDN1 genes. Therefore, the Scutellaria alpina extract of the present invention can exhibit, by said effects, skin homeostasis maintenance and anti-stress effects, and thus can be widely used as a composition for maintaining skin homeostasis in the pharmaceutical or cosmetic field.

A method for diagnosing, or differentially diagnosing, interstitial cystitis (IC) involves detecting or measuring increased expression of a biomarker Endothelin 1 (ET-1) in a biological sample from a mammalian subject, particularly in the urine or urothelial tissue. An increased level of expression of ET-1 above the level of expression in the same sample of a healthy mammalian subject is an indication of a diagnosis of IC. Such diagnosis may further involve identify other clinical symptoms of IC. Additionally the method may use additional biomarkers, such as Hb-EFG, EGF, APF, IL-8, IL-6, and cGMP. Assay methods and diagnostic reagents and kits for such diagnosis are provided. Methods and compositions for treating IC by reducing the action, production or synthesis of ET-1 in the urine or urothelium and / or inhibiting its binding to its ETA and / or ETB receptors are also provided.

The present invention relates to a method for increasing the stemness of human mesenchymal stem cells and, more particularly, to: a method for increasing the stemness of human mesenchymal stem cells by means of endothelin-1 treatment; the human mesenchymal stem cells having increased stemness by using the method; and a composition for increasing the stemness of human mesenchymal stem cells, containing endothelin-1 as an active ingredient. In the present invention, it is confirmed that the expression of a stemness marker is increased and that a stem cell characteristic is improved such as the length of telomeres being extended, by treating human mesenchymal stem cells with endothelin-1, and thus cellular life span is extended, aging is inhibited, and the growth and viability of cells are increased, thereby enabling mass culturing of human mesenchymal stem cells such that human mesenchymal stem cells are expected to be used effectively in cell therapy or regenerative medicine.

Disclosed is a composition containing an extract of alpine wormwood (Artemisia Umbelliformis) as an active ingredient. The composition disclosed in the present specification has the effect of reducing the amount of endothelin 1 and reducing the overexpression of NK1R and EDN1 genes due to the composition containing the extract of an alpine wormwood (Artemisia Umbelliformis). Accordingly, due to such effects, the alpine wormwood (Artemisia Umbelliformis) extract of the present specification can exhibit benefits for maintaining skin homeostasis and an anti-stress effect, and thus can be widely used in the pharmaceutical or cosmetics fields as a composition for maintaining skin homeostasis.

Cell transplantation for constructing biological heart pacemaker is used embryo source dry / ancestral cell and adult mesogalia dry cell as cell sources. The process is carried out by oriented differentiation inducing for heart pacemaker cell by embryo source multifunctional dry cell, bone marrow adhering to obtain primary culture cell, clone culturing to obtain purifying system by diluting, applying paracrine factor endothelin-1 or nervous adjusting protein-1, extracellular matrix laminated adherent protein and fiber connecting protein etc. substrate glue, trans-dyeing pacemaker gene HCN4, andin-vitro inducing embryo source multifunctional dry cell. It is various and non-immunogenicity. It can be used to treat sick sinus syndrome.

The invention discloses application of a scirpusin component C in common burreed rhizome in synthesis of anti-blood stasis syndrome drugs. The invention first proves that the scirpusin C has an obvious anti-blood stasis drug effect, and can be used for preparing a medicine for treating the blood stasis syndrome. Pharmacological experiments prove that the scirpusin C is capable of obviously reducing the levels of thromboxane B2 (TXB2), fibrinogen (FIB), active plasminogen activator inhibitor (PAI-1) and endothelin 1 (ET-1) in serum of blood stasis model mice and improving the thymus index (TI),spleen index (SI) and hepatic index (HI) of the mice, and has high clinical application value and development prospects in the aspect of treating the blood stasis syndrome.

Disclosed is a composition comprising an extract of alpine wormwood (Artemisia umbelliformis) as an active ingredient. The composition disclosed in the present specification, which comprises the extract of alpine wormwood (Artemisia umbelliformis), exhibits an effect of reducing the amount of endothelin 1 and reducing the overexpression of NK1R and EDN1 genes. Accordingly, due to such effects, the alpine wormwood (Artemisia umbelliformis) extract of the present disclosure can exhibit benefits for maintaining skin homeostasis as well as an anti-stress effect, and thus can be widely used in pharmaceutical or cosmetic fields as a composition for maintaining skin homeostasis.

A process for testing the susceptibility of primary hypertension includes detecting if there are variations in endotheline (gene EDN1, transcript and protein of an individual and determining its high susceptibility if there are. Its reagent kit is also disclosed.

The invention provides a human oocyte in vitro maturation culture solution containing Endothelin-1. The human oocyte in vitro maturation culture solution comprises liquid A and liquid B, wherein the liquid A comprises ET-1, r-FSH and 10% SSS, the liquid B comprises ET-1, r-FSH, hCG and 10% SSS, and solvent is conventional basic culture solutions. Researches show that the culture solution and culture method are capable of promoting human oocyte in vitro maturation especially cytoplasmic maturation and can increase embryo development potential after human oocyte in vitro fertilization. The culture solution aiming at the current situation that development imbalance of cytoplast and cell nucleus during immature human oocyte in vitro culture affects embryo in vitro development potential is developed by utilizing the biological function and effect of ET-1 in cumulus cells. The culture solution has the advantages that the culture solution is applicable to human oocyte in vitro culture, an IVM process can be optimized favorably, and the culture solution is worthy of popularization and application.

A formulation comprises phenoxyacetic acid derivative or its salt. A formulation comprises phenoxyacetic acid derivative of formula (I) or its salt. [Image] X and Y : chiral carbon atom; R 1OH,1-6C alkoxy, aryl-1-6C alkoxy, primary amino or mono- / di-(1-6C alkyl)amino; R 2and R 3H, halo, 1-6C alkyl, trifluoromethyl or 1-6C alkoxy; and R 4H, 1-6C alkyl, halo(1-6C alkyl), hydroxy, 1-6C alkoxy, aryl-1-6C alkoxy, 1-6C alkoxy, cyano, nitro, amino, mono- or di(1-6C alkyl)amino, carbamoyl, mono- or di(1-6C alkyl)carbamoyl or NHCOR 5; R 5H or 1-6C alkyl. Provided that at least one of R 2and R 3is H. ACTIVITY : None given. MECHANISM OF ACTION : Adrenoreceptor-beta -3 agonist. Effect of (-)-2-[4-(2-{(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino}ethyl)-2,5-dimethylphenoxyl] acetic acid (A1) on the tone of monkey detrusor was studied. The detrusor of cynomolgus monkey was isolated and dissected. Tracheal, atrial and urethral dissections were also prepared. The results were as follows: EC 50value of (A1) / isoproterenol was 8.2X10 ->7>. (A1) Exhibited lesser effect on the trachea and atria. The detrusor selectivity of (A1) was 1200 times greater (compared with the trachea) and 80 times greater (compared with the atria). (A1) Showed no effect on endothelin-1-induced tonic contraction of the isolated urethra.

The invention discloses polypeptide having effect of resisting tumors and use of the polypeptide. The polypeptide is named as TAT-ETA1, is polypeptide as shown as (1) or (2): (1) polypeptide of the 12-69th amino acid residues of an amino acid sequence as shown in SEQ ID NO:1; and (2) polypeptid of an amino acid sequence as shown in SEQ ID NO:1. The polypeptide TAT-ETA1 provided by the invention isfrom the carboxyl terminal of A type endothelin receptor 1(ETAR), when the TAT-ETA1 can act on ETAR in endothelin 1, the TAT-ETA1 can be combined with the carboxyl terminal of the Beta-arrestin 1 (ETAR) competitively to interfere interact between ETAR and beta-arrestin 1 so as to relieve cancer cell migration, invasion induced by the beta-arrestin 1, reverse tolerance during chemotherapy and thelike. The polypeptide TAT-ETA1 has clinical application potential for treatment of cancer.

Subject of the present invention is an in vitro method for the alternative assessment of peak oxygen consumption (VO2) for a subject not having a heart failure by measuring Pro-Endothelin-1 (ProET-1) or fragments thereof.