35 results about "Cyclooxygenase" patented technology

The invention discloses a novel benzofuran component in eupatorium chinense and application of the benzofuran component in anti-inflammatory activity. The obtained compound is separated from an eupatorium chinense extract. The eupatorium chinense root extract is separated by using an extraction method, macroporous adsorption resin impurity removal, Sephadex LH-20 gel column chromatography, high performance liquid chromatography and other methods. According to the present invention, all the separated compounds and the analogues thereof have good inhibition activity on target cyclooxygenase-2 of inflammation-related diseases, and have good inhibition activity on COX-2 enzyme, and the molecular docking experiment results show that the compounds and the target proteins have good binding energy. Therefore, the compound can be used for preparing drugs for treating inflammatory related diseases, or anti-inflammatory and analgesic drugs, or tumor drugs by inhibiting COX-2 enzyme, such as drugs for rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, Alzheimer's disease and the like, and related natural lead compounds are provided.

The present invention relates to a composition for diagnosing diseases associated with cyclooxygenase 2 (COX2) overexpression and a screening method therefor and, more particularly, to: a composition for diagnosing diseases associated with COX2 overexpression, containing a compound with a structural feature of exhibiting strong binding activity to a COX2 protein; and a screening method therefor.

The invention discloses a benzofuran glycoside compound as well as a separation and extraction method, a pharmaceutical composition and application thereof. The compound 1 is separated from an eupatorium chinense extract. And separating and purifying chemical components of the n-butyl alcohol part of the eupatorium chinense root to obtain the benzofuran compound. The inhibition activity of target cyclooxygenase-2 of inflammatory related diseases of all the separated compounds 1 is tested, and the compounds 1 have good inhibition activity on COX-2 enzyme and have good binding energy with target protein. In addition, the compound also has a good NLRP3-related inhibition effect, can be independently used or combined with other medicines to regulate NLRP3-related proteins, and is used for treating NLRP3-related mediated diseases and / or diseases and preparing medicines for preventing or treating the diseases or diseases. The compound 1 also has a good inhibition effect on acetylcholin esterase, and can be used for treating Alzheimer's disease, myasthenia gravis, Parkinson's disease and other diseases.

The invention provides a functionalized magnetic bead modified by cyclooxygenase as well as a preparation method and application of the functionalized magnetic bead, and belongs to the technical field of mass spectrometric detection. According to the invention, the functionalized magnetic bead modified by cyclooxygenase is successfully constructed, and the functionalized magnetic bead has good physical properties, activity, specificity and stability, and can be repeatedly used. The functionalized magnetic bead can be used as a material for screening active ingredients, and is applied to screening of anti-inflammatory active ingredients in meconopsis quintuplina alkaloid. The method for screening the active components by using the cyclooxygenase-modified functional magnetic beads disclosed by the invention provides a certain thought and reference for screening the active components from Chinese herbal medicines, and has a wide application prospect.

The application belongs to the technical field of wound dressings, and discloses a water-based gel dressing with antibacterial and scar prevention effects and a preparation method, wherein 3-fluoro-4-carboxyphenylboronic acid is introduced to graft chitooligosaccharide, a large number of catechol structures in tannic acid solution are combined with the phenylboronic acid bond to form a dynamic boron ester bond, and a network gel structure is formed by responding to the supermolecular forces such as hydrogen bonds, wherein the boron ester bond can be broken in response to the high ROS level of the wound microenvironment and the acidic environment caused by bacterial infection, so as to efficiently release celecoxib, a selective non-steroidal anti-inflammatory drug of cyclooxygenase-2, and the liposome of verteporfin is limited in volume and stays in the dressing for a longer time, so that the sustained and stable release can be maintained in the whole wound healing process, thereby achieving the effects of on-demand inflammation regulation and long-acting mechanical response regulation.

The invention belongs to the technical field of biological medicines, and particularly relates to application of arctigenin (ATG) in preparation of a medicine for preventing and / or treating milk protein allergic enteritis, the prevention and treatment effect of the ATG on the milk protein allergic enteritis is found for the first time, and the clinical application range of the ATG is expanded; in-vivo and in-vitro experiments prove that ATG can significantly relieve intestinal inflammatory response by targeted inhibition of abnormal expression of cyclooxygenase-2 and heat shock protein 90; meanwhile, the expression of autophagy key proteins LC3B and Beclin-1 is down-regulated to inhibit abnormal autophagy, and the expression of Claudin-3, ZO-1 and other intestinal barrier related genes is up-regulated, so that the integrity of the intestinal barrier is maintained, the allergic enteritis induced by milk protein is effectively prevented or improved, and the intestinal barrier is prevented from being damaged. The invention provides new drug candidate molecules and action targets for clinical prevention and treatment of milk protein allergic enteritis, and has a good application prospect in clinical use.

Colorectal cancer (CRC) is one of the leading causes of cancer-related mortality in men and women. Uncontrolled proliferation of CRC cells is pivotal in colorectal tumorigenesis and cyclooxygenase-2 (COX-2) is an important regulatory enzyme in this process. Timely diagnosis is the key to life-saving management of CRC, which is under-diagnosed because colorectal aberrant crypt foci, hyper plastic polyps, micro edemas are often missed with conventional colonoscopy. Disclosed herein are imaging agents tagged to nanobodies specific for COX-2 protein that can selectively accumulate and retain in COX-2 expressing cells and colorectal adenomas, resulting in specific and sensitive of early detection, while reducing background and off-target systemic toxicity. The prospect of combining structural and functional imaging readouts obtained with fluorescence-aided colonoscopy measurements would provide powerful diagnostic information for improved management of colorectal carcinogenesis.

The invention belongs to the technical field of wound dressings, and discloses a hydrogel dressing with antibacterial and scar-preventing effects and a preparation method thereof.3-fluoro-4-carboxyphenylboronic acid grafted chitosan oligosaccharide is introduced, phenylboronic acid bonds are matched with a large number of catechol structures in a tannic acid solution to form dynamic boron ester bonds, and the dynamic boron ester bonds are grafted to the chitosan oligosaccharide; the preparation method comprises the following steps: carrying out joint response with supramolecular forces such as hydrogen bonds to form a network gel structure, enabling boron ester bonds to respond to a high ROS level of a wound microenvironment and an acidic environment caused by bacterial infection to break, so as to efficiently release cyclooxygenase-2 selective non-steroidal anti-inflammatory drug celecoxib, and enabling the vinipofen liposome to be limited by a relatively large volume, so that the vinipofen liposome has a good anti-inflammatory effect. The time of staying in the dressing is longer, and continuous and stable release can be maintained in the whole wound healing process range, so that the effects of on-demand inflammation regulation and control and long-acting mechanical response regulation and control are achieved.

The application discloses a preparation method of copper-azo salicylic acid nanosheet for cyclooxygenase-2 inhibition, which comprises the following steps: (1) dissolving copper nitrate trihydrate and azo salicylic acid in an N,N-dimethylformamide solution of ethanol, performing ultrasonic dissolution, and then performing hydrothermal reaction, cooling to room temperature after reaction, and centrifuging the reaction solution to collect the solid; (2) dispersing the solid in water again, obtaining uniform two-dimensional nanosheet after ultrasonic centrifugation, and washing and vacuum drying the nanosheet to obtain the product. The nanosheet is prepared by coordinating the multidentate ligand formed by 5-aminosalicylic acid through an azo bond and Cu 2+ The nanosheet avoids the toxic side effects brought by directly taking COX-2 inhibitors, and can efficiently deliver 5-aminosalicylic acid to a tumor site through enhanced permeability and retention effect, so as to be beneficial to inhibiting the expression of COX-2 / PGE2, and the released Cu 2+ Also can catalyze Fenton-like reaction to produce hydroxyl radicals to kill tumor cells.

The invention belongs to the technical field of biological medicine, and particularly relates to coriaria sinica lactone compounds, a preparation method thereof and application of the coriaria sinica lactone compounds in anti-inflammatory activity. The coriaria sinica lactone compound can significantly inhibit a TLR4 / NF-kappa B signal channel to inhibit downstream inflammatory protein nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and further inhibit inflammatory BV2 cells from generating nitric oxide, the inhibition rate can reach 65.5%, and it is indicated that the coriaria sinica lactone compound has an application prospect in treatment of neuroinflammatory diseases.

The invention provides an aggregation-induced emission (AIE) ionic probe (E)-4-(2-(5-(4-(diphenylamino) phenyl) thiophene-2-yl) vinyl)-1-(4-sulfanilamide acyl benzyl) quinoline-1-onium hexafluorophosphoric acid (V) salt of a targeted golf apparatus, namely a fluorescent probe TTQ-GA, a preparation method of the fluorescent probe TTQ-GA and application of the fluorescent probe TTQ-GA in the aspect of detection. The benzenesulfonamide group of the probe can be selectively combined with a Golgi apparatus protein cyclooxygenase 2 (COX-2) inhibitor SC-558 to realize Golgi apparatus targeting; due to the hydrophobic triphenylamine part and the hydrophilic quinoline cation part of the probe, the probe has amphipathy; the probe does not emit fluorescence in an aqueous solution, and can emit strong fluorescence when molecular movement is limited and excited, so that no-wash marking of the Golgi apparatus is realized; the probe generates a large amount of ROS under light excitation, promotes local lipid peroxidation increase of Golgi apparatus, and promotes cancer cell apoptosis.

The invention discloses a sesquiterpene compound as well as a preparation method and application thereof, and relates to the technical field of medicines. The invention provides a sesquiterpene compound and discloses new activity of the sesquiterpene compound, namely the sesquiterpene compound is used for remarkably inhibiting generation of inflammatory BV2 cell NO and remarkably inhibiting oxidative stress SH-SY5Y cell damage. The sesquiterpene compound can significantly inhibit TLR4 / NF-kappa B signal channels to inhibit expression of downstream inflammatory protein nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and has an application prospect in treatment of neuroinflammatory diseases. The invention can obtain the sesquiterpene compound as well as the preparation method and the application thereof.

The present invention discloses a class of divalent platinum complexes containing non-steroidal anti-inflammatory drug structural units, their derivatives, preparation methods, pharmaceutical compositions and applications. The structure of this class of divalent platinum complexes is as follows: The derivatives of this class of divalent platinum complexes refer to isomers of the said divalent platinum complexes or mixtures thereof. When this class of divalent platinum complexes and their derivatives act on cancer cells, they can cause apoptosis by inducing DNA damage and the production of reactive oxygen species, and can also effectively inhibit the growth of cancer cells by down-regulating the expression of cyclooxygenase 2 to reduce inflammation. At the same time, this class of divalent platinum complexes with C=N double bonds can also target tumors using the acidic microenvironment of tumors, reduce tissue toxicity, show the characteristics of high efficiency and low toxicity in anti-tumor, and can overcome cisplatin resistance to a certain extent, and can be prepared into anti-tumor drugs. In addition, the synthesis method of this class of divalent platinum complexes is simple and easy to operate.

The disclosure provides compounds of Formula 1, and the pharmaceutically acceptable salts thereof. The variables in Formula 1, e.g. X1-X5, A1, A2, and R1-R4 are described herein. Such compounds are useful as prostaglandin transport (PGT) inhibitors. The disclosure further includes pharmaceutical compositions comprising a compound of Formula 1 or salt thereof and methods of using compounds of Formula 1 and salts thereof to treat diseases and disorders mediated, at least in part, by prostaglandin levels or cyclooxygenase activity. Such diseases and disorders include painful and inflammatory conditions.

The application provides a whey protein hydrolysate and application thereof in preparation of anti-inflammatory, antioxidant or allergy relief related products. The preparation method has the advantages of high preparation efficiency, fast speed and sufficient hydrolysis. The whey protein hydrolysate obtained through the preparation method is of excellent quality, rich in nutrition, easy to be absorbed by the human body, and can improve the cyclooxygenase-2 inhibition rate, improve the free radical clearance rate, and relieve the kidney and liver damage caused by the body allergy, and thus has the effects of anti-inflammation, anti-oxidation and allergy relief.

The application discloses a benzofuran glycoside compound, a separation and extraction method thereof, a pharmaceutical composition and application, and the compound 1 is separated from a macleaya cordata extract. A benzofuran compound is obtained by separating and purifying a n-butanol part chemical component of a macleaya cordata root. The inhibitory activity of all separated compounds 1 on a target point cyclooxygenase-2 of an inflammatory related disease is tested, the compound 1 has good inhibitory activity on COX-2 enzyme, and the compound 1 has better binding energy with the target point protein. The compound also has good NLRP3 related inhibitory effect, can be used alone or in combination with other drugs to regulate NLRP3 related proteins, is used for treating NLRP3 related mediated diseases and / or diseases, and is used for preparing drugs for preventing or treating the diseases. The compound 1 also has better inhibitory effect on acetylcholinesterase, and can be used for treating diseases such as Alzheimer's disease, myasthenia gravis and Parkinson's disease.

Preparation method and application of diterpenoid, relate to the application technical field of diterpenoid.The present application separates two new compounds of diterpenoid A and diterpenoid B from a strain of Hericium fermentation extract, and discloses chemical structural formula of the two compounds, and corresponding nuclear magnetic, mass spectrum, infrared and ultraviolet data, and its function of significantly inhibiting the production of inflammatory BV2 cell NO.Diterpenoid B has 24% of the promotion rate of axon growth of PC-12 cell, and simultaneously has significant inhibition of TLR4 / NF-κB signal path to inhibit downstream inflammatory proteins of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and diterpenoid A and diterpenoid B both show significant anti-neuroinflammatory activity.The present application can obtain the preparation method and application of diterpenoid.

This invention discloses a 7-O-7' lignan (+) / (–)-7- epi -oryzativol, its preparation method, and its applications belong to the field of pharmaceutical chemistry technology. The 7-O-7' lignan (+) / (–)-7- epi -oryzativol has the structure shown in formula C. This class of compounds was first obtained from Artemisia bulbifera (… Laportea bulbifera The compound was isolated from (+) / (–)-7- epi -oryzativol exhibits significant inhibitory activity against cyclooxygenase-2 (COX-2), and compound (+)-7- epi -oryzativol has a high COX-2 selectivity index and exhibits significant anti-inflammatory effects, making it suitable for use in the preparation of anti-inflammatory drugs.

A topical cyclooxygenase (COX) inhibitor formulation comprising an inhibitor of COX-1 and / or COX-2, one or more long chain monounsaturated fatty acids, long chain monounsaturated fatty alcohols, terpenes, or combinations thereof; and a solvent mixture comprising ethanol, propylene glycol, 2-(2-Ethoxyethoxy)ethanol, and optionally dimethylsulfoxide.

The invention relates to the technical field of biology, in particular to novel application of sanguinarine (SAN), a method for inducing human amniotic mesenchymal stem cells (hAMSCs) to be differentiated into osteoblasts through COX2 protein and an osteogenic induction culture medium for the inducing method, and the method can be applied to the fields of bone disease treatment drug research and development and clinical transformation. It is proved for the first time that SAN mediates hAMSCs osteogenic differentiation through COX2 protein, SAN can significantly improve expression of COX2 gene (PTGS2) in hAMSCs, the osteogenic effect of SAN can be reversed by adding a COX2 inhibitor (such as celecoxib), and direct experimental evidence is provided for'COX2 serving as a small molecule drug to promote osteogenic differentiation '.

The invention provides methods for treating, suppressing, or preventing detrimental cytokine and / or lipid mediator surges that can result from a variety of different diseases, conditions, and therapeutic treatments, e.g., by inhibition of cyclooxygenase-2 (COX-2) and soluble epoxide hydrolase (sEH).

The present invention provides methods of female contraception, the methods comprising administering an effective amount of a combination of a progesterone receptor agonist and a cyclooxygenase-2 inhibitor in each of two doses, the first dose is administered within about 24 hours before or after a first act of sexual intercourse and the second dose is administered between about 36 hours and about 60 hours after the first dose.

Disclosed in the present invention is a synergistic phytomedical mind and body wellbeing formulation involving a botanical composition with a dual approach to inhibit Cyclooxygenase (COX) and Lipoxygenase (LOX) enzymes that enhances nervine function for therapeutic intervention encompassing phytoceutical compositions and methods for treating inflammatory conditions, neurological and gut microbiome disorders. The formulation integrates a selected blend of natural ingredients with main active ingredients, including Stabilized Flax Meal, Cynatine® FLX, Sunflower Lecithin, Boswellia Extract, Turmeric / Curcumin C-3 Reduct®, Egg Shell Membrane, Green Oat Extract-Neuravena®, Hyaluronic Acid, Manganese Chelate and AstaReal® Astaxanthin are carefully chosen for their documented efficacy in addressing various dimensions of chronic pain and inflammation, as well as promoting joint / tissue health, gut health and cognitive function. Through synergistic action, these ingredients work in tandem to provide holistic relief from chronic inflammation, thereby improving quality of life without reliance on harsh pharmaceutical interventions.

The present application relates to a kind of pentacyclic triterpenoids and its preparation method and application.The pentacyclic triterpenoids provided by the present application belong to methylsuccinic acylitans type triterpenoid compounds and analogs, the compound shows good inhibitory activity to cyclooxygenase-2 (COX-2), can be used for preparing anti-inflammatory drug;The present application takes oleanolic acid or ursolic acid as matrix, under the action of condensing agent, with organic diacid monomethyl ester or organic diacid monomethyl ester acyl chloride is reacted, so as to introduce specific organic diacid monomethyl ester acyl in the 3-position hydroxyl of matrix, reaction condition is mild, synthesis speed is fast, yield is high, the present application provides a kind of efficient, fast method for methylsuccinic acylitans type triterpenoid compounds and analogs.

The present disclosure relates to a cosmetic composition containing an extract of Cyperus rotundus extracted using warm microbubbles. The extract inhibits nitric oxide (NO) production and exhibits excellent anti-inflammatory efficacy by inhibiting the expression of interleukin 6 (IL-6), cyclooxygenase-2 (COX-2), interleukin-1β (IL-1β), and tumor necrosis factor-α (TNF-α), which are inflammatory expression factors. In addition, the extract enhances the expression of aquaporin-3 (AQP-3), hyaluronan synthase 2 (HAS-2), claudin-1 (CLDN-1), cadherin 1 (CDH1), filaggrin (FLG), and involucrin (IVL), which are genes related to the skin barrier and moisturizing. Thus, when using the extract for cosmetic products, excellent effects can be exhibited in skin soothing, moisturizing, enhancement of the skin barrier, relief of irritation such as erythema, relief of pruritus, and the like, so the extract can be usefully applied to multi-care products that improve skin conditions.

Compounds derived from celecoxib and valdecoxib, and methods of use thereof, are disclosed. The compounds are useful for, inter alia, identifying and localizing the site of pathology and / or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The compounds contain a radioactive agent which permits imaging. The compounds concentrate at sites of increased cyclooxygenase expression, such as areas of increased COX-2 expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and / or location. Identifying areas of increased COX expressing can also aid in screening for infections, assessing efficacy of diagnosis and treatment of rheumatoid arthritis, and assessing the need for treatment with opioid drugs.

The invention relates to the field of traditional Chinese medicine preparations, in particular to an analgesic and anti-inflammatory patch and a preparation method thereof.The patch comprises, by weight, 30 parts of gentiana macrophylla, 15 parts of frankincense, 15 parts of myrrh, 15 parts of ligusticum wallichii, 15 parts of angelica sinensis, 10 parts of notopterygium roots, 10 parts of radix angelicae pubescentis, 10 parts of garden balsam stems, 8 parts of ground beetles, 8 parts of carthamus tinctorius, 5 parts of borneol, 3 parts of menthol and 3 parts of liquorice. The radix gentianae macrophyllae is used as a monarch drug and is matched with the medicinal materials such as the frankincense, the myrrh and the ligusticum wallichii to form a scientific and reasonable compound compatibility, the components are in synergistic interaction, and the analgesic and anti-inflammatory effects of the application are remarkably improved. Gentiana macrophylla alkali A in gentiana macrophylla and boswellic acid and gallic acid in frankincense and myrrh have a synergistic effect, cyclooxygenase can be inhibited, prostaglandin synthesis can be reduced, capillary permeability can be reduced, inflammation exudation can be relieved, and therefore the multi-target analgesic and anti-inflammatory effects are achieved.

The invention belongs to the technical field of molecular breeding, and particularly relates to a syntrichia caninervis zeaxanthin epoxidase gene as well as an encoded protein and application thereof, under salt stress, transgenic syntrichia caninervis overexpressing the syntrichia caninervis ScZEP gene has the advantages that the growth speed, length and diameter of protonemata are obviously increased; and the survival rate of the transgenic syntrichia caninervis of the overexpressed ScZEP gene is obviously improved. The invention provides a gene resource capable of regulating and controlling the salt resistance of plants, provides an excellent candidate gene for cultivating salt-resistant plants, especially salt-resistant non-vascular plants, and provides gene resources and technical support for preventing and controlling soil salinization.

Present invention relates to aqueous compositions comprising cyclooxygenase-2 (COX-2) inhibitors, preferably Etoricoxib or Celecoxib or Valdecoxib or Paracoxib or salts thereof at least two solubilizers at 4.2% w / v to 19% w / v, preferably between 4.2% w / v to 18% w / v having viscosity in range of 1.0 cps to 3 cps, wherein the Etoricoxib and Celecoxib or salts thereof are present in amount ranging from 0.14 mg to 4 mg. The composition is suitable for the parenteral route of administration primarily for ready to dilute and ready to infuse which alternatively can be administered as intramuscular, intraarterial, intraocular, intraventricular, intravenous routes; also for subcutaneous, cutaneous delivery. The invention further provides a method for preparing the said composition.