38 results about "Elastase activity" patented technology

Compounds of formula (I) and multimers thereof are inhibitors of human neutrophil elastase activity, and of utility in the treatment of, e.g., COPD:

wherein A is aryl or heteroaryl; D is oxygen or sulphur; R¹, R² and R³ are independently each hydrogen, halogen, nitro, cyano, C₁-C₆-alkyl, C₂-C₆-alkenyl, C₂-C₆-alkynyl, hydroxy or C₁-C₆-alkoxy or C₂-C₆-alkenyloxy, wherein C₁-C₆-alkyl and C₁-C₆-alkoxy can be further substituted with one to three identical or different radicals selected from the group consisting of halogen, hydroxy and C₁-C₄-alkoxy;

R and R⁴ each independently represent a radical of formula

—[X]_m-[Alk¹]_p-[Q]_n-[Alk²]_q-[X¹]_k-Z wherein k, m, n, p and q are independently 0 or 1; Alk¹ and Alk² each independently represent an optionally substituted C₁-C₆ alkylene, or C₂-C₆ alkenylene radical which may optionally contain an ether (O—), thioether (—S—) or amino (—NR^A—) link wherein R^A is hydrogen or C₁-C₃ alkyl; Q represents (i) O—, —S—, —S(═O)—, —S(═O)₂—, —S⁺(R^A)—, —N(R^A)—, —N⁺(R^A)(R^B)—, —C(═O)—, —C(═O)O—, —OC(═O)—, —C(═O)NR^A—, —NR^AC(═O)—, —S(O₂)NR^A—, —NR^AS(O₂)—, —NR^AC(═O)NR^B—, —NR^AC(═NR^A)NR^B—, —C(═NR^D)NR^E, —NR^EC(═NR^D), wherein R^A, R^B, R^D and R^E are independently hydrogen, C₁-C₆ alkyl, or C₃-C₆ cycloalkyl, or R^A and R^B, or R^D and R^E taken together with the nitrogen to which they are attached form a monocyclic heterocyclic ring of 5 to 7 ring atoms which my contain a further heteroatom selected from N, O and S, or (ii) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 3-6 ring members; X represents —(C═O)—, —S(O₂)—, —C(═O)O—, —(C═O)NR^A—, or —S(O₂)NR^A—, wherein R^A is hydrogen, C₁-C₆ alkyl, or C₃-C₆ cycloalkyl; X¹ represents —O—, —S—, or —NH; and Z is hydrogen or an optionally substituted mono- or bicyclic carbocyclic or heterocyclic radical having 3-6 ring members.

The present invention relates to a composition comprising a bamboo plant extract for the prevention and treatment of inflammatory or blood circulation disease. The extracts of bamboo plant has potent anti-inflammatory activity by inhibiting NO production and blood circulation-improving activity by inhibiting elastase activity and healing the wound of vascular endothelial cell, activating u-PA expression and inhibiting PAI-1 expression, lowering cholesterol deposit and inhibiting neointima formation, therefore it can be used as a therapeutic or health care food for treating and preventing inflammatory or blood circulation diseases.

The present invention relates to compositions for inhibiting elastase activity, enhancing collagen biosynthesis and improving skin wrinkle, comprising Mallotus japonicus extract as active ingredient. The present compositions exhibit the inhibition effect on elastase activity and promotion effect on collagen biosynthesis at a molecular level, and as a result, excellent efficacy in improvement of skin wrinkles.

The invention provides coumarin derivatives. The coumarin derivatives are shown in the formula (1), and in the formula (1), R1 represents one of pentafluoroethyl and heptafluoropropyl and R2 represents one of trifluoromethyl, methyl, cyano group, pyridine ring and benzothiazole ring. The invention also provides a use of the coumarin derivatives in detection of elastase activity, and an elastase activity detection method and kit. The coumarin derivatives as fluorescent probes have high sensitivity, high enzyme affinity and high atom utilization rate in elastase activity detection. The coumarin derivatives are non-peptide fluorescent probes. Compared with the peptide fluorescent probes, the coumarin derivatives have higher stability, better use convenience and lower price.

The invention discloses an anti-aging composition, which relates to the technical field of cosmetics. The anti-aging composition is prepared from the following components in parts by weight: 1-10 parts of 3-glycerol ascorbic acid, 1-10 parts of coconut oil acyl hydrolyzed collagen potassium, 1-10 parts of hydrolyzed conchiolin and 1-10 parts of vitamin C. The anti-aging composition provided by the invention is non-irritant and good in moisture retention, and can be used for directly supplementing collagen to the skin. Besides, the invention further provides essence containing the anti-aging composition, and the essence has the effects of inhibiting elastase activity, improving skin vitality and elasticity, inhibiting nonuniform cuticle shedding caused by abnormal keratinization, increasing collagen density and effectively inhibiting and eliminating skin wrinkles.

The invention discloses a skin aging-resistant tetrapeptide and a use thereof. The amino acid sequence of the tetrapeptide is Gly-Lue-Pro-Tyr(GLPY), the molecular weight is 449.2393 Da, and the tetrapeptide is synthesized through a chemical synthesis method in the prior art. The tetrapeptide GLPY can bind to elastase in order to inhibit the activity of the elastase and reduce fibroblast apoptosiscaused by photodamage, so the tetrapeptide has skin aging resistance, and can be used for preparing healthcare products and skincare products with an anti-aging effect.

To provide a DNA damage repair promoter for oral application and an elastase activity suppressor for oral application.

The invention provides a DNA damage repair promoter and an elastase activity suppressor for oral application each containing, as an active ingredient, a bacterium belonging to the genus bifidobacterium.

The invention is designed based on the elastinase deactivation research for phytosterols and relates to the new application of a phytosterol functioning as an elastinase activity inhibitor, and an external-use agent composition containing the same and capable of improving the skin elasticity and healing skin wounds. The phytosterol-containing combination can be used safely without any side effect on the skin. Meanwhile, by means of the composition, the skin elasticity is improved through deactivating the elastase, so that the skin anti-aging effect and the skin wound healing effect are greatly enhanced.

The invention discloses an eye mask with anti-wrinkle and skin-tightening effect, which is prepared from, by weight, 0.3-0.5 part of composite microsphere; the composite microsphere comprises butanediol, water, peony root extract, and polygonum cuspidatum extract. The eye mask displays the active effect through butanediol, water, peony root extract, and polygonum cuspidatum extract; the skin wrinkle is inhibited through inhibiting the elastic proteinase activity, so as to prevent wrinkle and delay senescence; thus the skin elasticity is recovered and the skin is tightened; besides, the eye mask can retain water and humidity, keep the eye part being moistened, and avoid dark, fine wrinkles and the like caused by the accelerated aging of the eye part.

The invention provides application of a nitraria tangutorum extract and a skin externally applied preparation containing the nitraria tangutorum extract. The application specifically means one or moreapplications of the nitraria tangutorum extract in preparation of antioxidants, melanin biosynthesis inhibitors, elastic fiber hydrolysis inhibitors and skin-aging resistant protein expression up-regulators. The nitraria tangutorum extract, especially a nitraria tangutorum seed extract, has the effects of scavenging the activity of free radicals, inhibiting the activity of tyrosinase, inhibitingthe activity of elastase and improving expression of anti-aging protein in human fibroblasts, can regulate synthesis of collagen in dermis and has the effect of delaying senescence.

The invention relates to the field of activity detection of elastinase, in particular to a quantum dot fluorescence probe, a preparation method and application thereof, and a method and a kit for detecting activity of elastinase. The quantum dot fluorescence probe comprises a semiconductor quantum dot of a nucleus-shell structure, a Rhodamine derivative and an elastinase specific polypeptide connected between the semiconductor quantum dot and the Rhodamine derivative; and the semiconductor quantum dot takes CdSe as a nucleus and takes ZnS as a shell. The preparation method includes the steps:EDC and NHS make contact with the semiconductor quantum dot so as to activate carboxyl on the surface of the semiconductor quantum dot; a reaction of the activated carboxyl on the surface of the semiconductor quantum dot and amidogen of the proteolytic enzyme specific polypeptide connected with the Rhodamine derivative is obtained to obtain the quantum dot fluorescence probe. When being used for detecting the activity of a proteolytic enzyme, especially the elastinase, the quantum dot fluorescence probe has higher affinity with the proteolytic enzyme, and the effectiveness of detection is higher.

Mutants of the human PAI-1 protein are described which are inhibitors of neutrophil elastase or are inhibitors of vitronectin (Vn)-dependent cell migration. These mutants preferably comprise one or two amino acid substitutions in the reactive center loop of PAI-1, particularly at positions 331 and 346 of the mature protein. These mutants are notable in being resistant to inactivation by elastase, having high affinity for Vn, or both properties. These mutant proteins as pharmaceutical compositions are used to inhibit elastase in a subject, thereby treating a number of disorders associated with elastase activity, most notatably emphysema, ARDS, inflammatory lung injury and cystic fibrosis. The mutants which interact with Vn are used to inhibit cell migration in a subject, thereby treating diseases or conditions associated with undesired cell migration and proliferation, particularly of smooth muscle cells. Such conditions include atherosclerosis, post angioplasty restenosis, fibrosis associated with chronic inflammation or chemotherapy, tumor invasion and metastasis and conditions in which angiogenesis is pathogenic. Also disclosed are peptides of such mutant proteins, mutant-specific antibodies, nucleic acid molecules, particularly DNA, encoding the mutant protein and host cells transformed by such nucleic acids.

The present invention provides a crude extract from the bark of an Acer rubrum (AR) tree and/or Picea mariana (PM), method of preparation and its use for inhibiting the signs of skin aging (such as wrinkles and/or dehydration) caused by at least one of: increased elastase activity, increased collagenase activity, decreased elastin synthesis, decreased collagen synthesis or decreased involucrin synthesis, in skin fibroblast cells, particularly those of a human subject.

A novel alpha-1 antitrypsin variant, a method of preparing the same, and use thereof are provided. The alpha-1 antitrypsin variant has excellent stability in the body and maintains an inhibitory effect on elastase activities because the blood half-life (t_1/2) and the area under blood drug concentration vs. time curve (AUC) are remarkably increased by adding an N-glycosylation site in animal cells through amino acid mutation between 1^st and 25^th positions of the N-terminus of alpha-1 antitrypsin. Therefore, the alpha-1 antitrypsin variant can be useful in preventing or treating alpha-1 antitrypsin deficiency.

The present invention relates to pharmaceutical aerosols comprising a β-hairpin peptidomimetic of formula cyclo(-OctG-Glu-Thr-Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-^DPro-Pro-), or a pharmaceutically acceptable salt thereof, having inhibitory activity against human neutrophil elastase. It further relates to solid or liquid pharmaceutical compositions and kits for preparing and administering such aerosols. The invention can be used for the prevention, management or treatment of pulmonary diseases, such as alpha-1 antitrypsin deficiency (AATD), cystic fibrosis (CF), non-cystic fibrosis bronchiactasis (NCFB), or chronic obstructive pulmonary disease (COPD), or infections, or diseases, or conditions of the lungs, being mediated by or resulting from human neutrophil elastase activity. Thus, the invention further relates to a pharmaceutical composition or a pharmaceutical aerosol comprising the active compound cyclo(-OctG-Glu-Thr-Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-^DPro-Pro-), or any pharmaceutically acceptable salt thereof, for use in a method for the prevention, management or treatment of diseases or conditions of the lungs being mediated by or resulting from human neutrophil elastase activity in a subject.

The present invention relates to methods and kits for the diagnosis and confirmation of Chronic Fatigue Syndrome (CFS) by measuring elastase activity in a patient sample, preferably a PBMC sample. The assays of the invention can also be used to characterize CFS, to determine the disease stage, the disease progression, the efficiency of a therapeutic regime and/or to predict the recurrence of possible attacks. The assays of the invention advantageously allow CFS to be distinguished from other CICIDs like MS or RA.

A Basidiomycetes-X FERM BP-10011 dry powder or an extract composition thereof is used as an active ingredient.

A cosmetic material, cell growth promoting agent, elastase activity inhibiting agent and anti-aging agent containing sweet pea extract, formulated with the aim of preventing or slowing aging.