41 results about "Endothelin 1" patented technology

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.

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.

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.

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.