262 results about "Purine-Xanthine Oxidase" patented technology

The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I):wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.

(Aza)indolizine derivatives represented by Formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In Formula (I), 0 to 2 of X1, X2, X3 and X4 are a nitrogen atom and the others are CR1; one of T1 and T2 represents cyano and the other represents a group represented by Formula (A), with the proviso that when T1 is cyano, at least one of X1 to X4 is a nitrogen atom; R1 independently represents a hydrogen atom, a halogen atom, a hydroxy group, C1-6 alkyl, C1-6 alkoxy or the like; ring U represents a benzene ring or the like; m represents integral number from 0 to 2; R2 independently represents a fluorine atom, a hydroxy group or the like.

The invention belongs to the chemical field of natural products and particularly relates to a preparation method and use of moringa oleifera leaf polysaccharides. The preparation method comprises the steps of carrying out combined microwave-ultrasound extraction, hydrochloric acid method deproteinization, hydrogen peroxide method decoloration and AB-8 macroporous adsorption resin column separation, so as to prepare the moringa oleifera leaf polysaccharides. The preparation method of the moringa oleifera leaf polysaccharides has the advantages of short extraction time, low extraction temperature, low energy consumption and high extraction rate and purity. Besides, an animal experiment proves that the prepared moringa oleifera leaf polysaccharides have remarkable treatment effect to hyperuricosuria; by decreasing the content of cholesterol, triacylglycerol, urea nitrogen, creatinine and xanthine oxidase, the production of uric acid is achieved; meanwhile, by directly decomposing uric acid, renal functions are improved, the excretion of uric acid is promoted, and blood vessels are protected, thereby being favorable to the recovery of patients with the hyperuricosuria. The preparation method has a wide medical application prospect.

The invention relates to application of celery seed extract to preparation of medicine or health-care food for resisting to hyperuricemia and gout and further provides medicine or health-care food for treating hyperuricemia and gout. Celery seed extract serves as the active constituent, and an appropriate number of medical carriers or auxiliary constituents are added, so that a preparation is obtained. The medicine for health-care food is simple in preparation process, the celery seed extract can obviously lower serum uric acid of model mice suffering from hyperuricemia caused by oteracil potassium salt, lower the activity of xanthine oxidase to different degrees, achieve an obvious inhibition effect on arthritis of the mice, prevent and treat hyperuricemia or gout and be applied to preparation of the medicine or health-care food for resisting to hyperuricemia and gout.

The present invention discloses oxygenic oxygenic oxysterols. Also disclosed, agents and methods for protecting, blocking or rescuing marrow stromal cells from the inhibitory effects of oxidative stress on their osteoblastic cellular differentiation. Exemplary agents include oxysterols, rhBMP2, alone or in combination which are demonstrated to specifically combat oxidative stress caused by inflammatory oxidized lipids, such as xanthine / xanthine oxidase and minimally oxidized LDL. The synergistic effects of oxysterols and bone morphogenic proteins are disclosed.

The invention disclosed an aryl nitrile group thiazole derivative for inhibiting the activity of xanthine oxidase, a method for preparing the same and application thereof. In the aryl nitrile group thiazole, R1 is methyl, ethyl, propyl, isopropyl, isobutyl, methyl cyclopropane, methyl cyclobutane, isoamyl, methyl cyclopentane, methyl cyclohexane or aromatic ring methyl, R2 is methyl or trifluoromethyl, and R3 is formic acid, sodium formate, potassium formate, lithium formate, methyl formate, or ethyl formate. Simultaneously, the invention discloses a method for synthesizing the aryl nitrile group thiazole derivative by using inexpensive raw materials, which has the advantages of simple operation, high yield, easy purification of products, application to industrial production and the like, and can obtain an efficient compound with low toxicity through screening; besides, the effective compound is expected to be widely applied to inhibit the activity of the xanthine oxidase required on animals and humans, and to become a new generation of antigout drugs and hyperuricemia drugs with special effect.

The invention discloses lactobacillus gasseri and application thereof in relieving and treating hyperuricemia, and belongs to the technical field of microorganisms. According to the lactobacillus gasseri CCFM1133 disclosed by the invention, the serum uric acid level of hyperuricemia mice and the xanthine oxidase (XOD) activity of serum and a liver can be reduced, and the occurrence of hyperuricemia and gout is reduced; the blood glucose and serum triglyceride (TG) level of a patient with hyperuricemia can be regulated, and the activity of liver catalase (CAT) and glutathione peroxidase (GSH-Px) is improved; expression of ileum ABCG2 is improved, and excretion of intestinal uric acid is promoted; and the intestinal short-chain fatty acid level is improved, and the health is promoted. The lactobacillus gasseri CCFM1133 disclosed by the invention can be used for preparing foods, functional foods or medicines, and has a wide application prospect.

The invention discloses lactobacillus rhamnosus NX-2 and an application thereof in preparation of uric acid reducing drugs, and belongs to the technical field of microorganisms. The lactobacillus rhamnosus NX-2 disclosed by the invention has a preservation number of CGMCC No.20110. Non-inactivated and inactivated fermentation supernate, bacterial suspension and cell disruption material supernate of the lactobacillus rhamnosus NX-2 have uric acid reducing effects on a zebrafish high-uric-acid model, and can inhibit the activity of xanthine oxidase in the body of a high-uric-acid zebrafish. Thelactobacillus rhamnosus NX-2 disclosed by the invention has a huge potential application prospect in the aspect of preparing medicines for treating and / or preventing hyperuricemia.

A method for inhibiting xanthine oxidase and for reducing uric acid levels using a composition obtained by culturing Lactobacillus rhamnosus in a medium. Also disclosed is a composition including a metabolite of Lactobacillus rhamnosus for reducing uric acid levels in a subject and a method for producing the composition.

An object of the present invention is to provide an agent for treating or preventing digestive ulcer that is effective even to ulcer of small intestine and others, for which gastric acid secretion inhibitors such as proton pump inhibitors are ineffective, and is superior to allopurinol in the efficaciousness and the safety.The pharmaceutical composition of the present invention comprising a non-purine xanthine oxidase inhibitor as the active ingredient is useful as an agent for treating or preventing ulcer that forms in digestive tracts by the attack of gastric acid, pepsin, stress, Helicobacter pylori bacteria, NSAID, etc. In particular, it is useful as an ulcer remedy heretofore unknown in the art as it is effective even for ulcer in small intestine for which gastric / duodenal ulcer remedies that inhibit gastric acid secretion such as proton pump inhibitors are ineffective.

The invention provides an Arthrobacter and an application of the Arthrobacter for generating xanthine oxidase and a preparation method thereof. The Arthrobacter XL2006 derives from nature and the16S rRNA sequence of the Arthrobacter XL2006 is shown in a sequence table SEQ ID NO.1. The Arthrobacter XL2006 is applied to producing, extracting and purifying the xanthine oxidase and preparing a diagnostic kit. The Arthrobacter XL2006 is characterized by the production of the xanthine oxidase and can adopt hypoxanthine or xanthine as a unique source of carbon and nitrogen and a unique energy source. The fermentation and the production of the xanthine oxidase are characterized by simple nutritional requirements, easy culture and short fermentation time; the produced xanthine oxidase has quite high activity, and strains provided by the invention are utilized to ferment and extract the xanthine oxidase and the prepared diagnostic kit can be applied to clinically testing the levels of hypoxanthine and xanthine in blood serum of patients.

The invention relates to a polypeptide with a function of reducing uric acid and an application of the polypeptide. The polypeptide with the function of reducing uric acid has an amino acid sequence as follows: Tyr-Glu-Gly. The polypeptide is synthesized with a solid-phase synthesis method by the use of a polypeptide synthesizer. In-vitro uric acid reduction activity detection is performed on the polypeptide with an HPLC method, and a result proves that the polypeptide has a good inhibition effect on xanthine oxidase and has excellent uric acid reduction activity. The polypeptide can be used as an adjuvant therapy drug for the gout disease or used in functional health-care food or medicines with the function of reducing uric acid.

1-Phenylpyrazole compounds of the formula (1): which is exemplified by 5-amino-1-(3-cyano-4-isobutoxyphenyl)pyrazole-4-carboxylic acid, an optical isomer thereof and a pharmaceutically acceptable salt thereof. These compounds have a xanthine oxidase inhibitory activity and are useful as therapeutic agents for diseases such as hyperuricacidemia and gout.

The invention discloses an application of a folium eucalypti extractive serving as an active ingredient in preparation of medicines for treating hyperuricemia, and also provides a preparation method of the folium eucalypti extractive. Main active ingredients of the folium eucalypti extractive are 6-12% of scabish essence B, 1-2% of tellimagrandin I, 1-1.5% of quercetin-3-O-glucoside acid, 0.8-1.2% of ellagic acid, 0.2-0.5% of tellimagrandin II, 0.1-0.15% of 1,2,3,4,6 pentagalloylglucose and 25-50% of total phenols. The pharmacological experiment shows that the folium eucalypti extractive has an inhibiting effect on xanthine oxidase and relatively strong effects of reducing uric acid, protecting renal injury caused by the hyperuricemia and the like in bodies.

The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I):wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.

The invention belongs to the chemical field of natural products and in particular relates to an extraction method and an application of moringa oleifera leaf total flavones. The extraction method adopts microwave and ultrasound to synergistically extract the moringa oleifera leaf total flavones, and has the advantages of high efficiency, time saving, energy conservation, low energy consumption, simple operation and good repeatability. Besides, an animal test proves that the extracted moringa oleifera leaf total flavones have a significant treatment effect on hyperuricosuria and Alzheimer's disease. The total flavones provided by the invention can reduce uric acid, and can also reduce cholesterol, triacylglycerol, urea nitrogen, creatinine and xanthine oxidase, reduce the generation of uric acid, directly decompose uric acid, improve the renal function, promote uric acid excretion, and protect multiple levels of blood vessels to reduce uric acid, so that the moringa oleifera leaf total flavones are beneficial for healing of lithemia patients and have a broad medical application prospect.

The invention discloses 2-arylselenazole compounds and a medicinal composition thereof. The 2-arylselenazole compounds are compounds represented by formula (I) or pharmaceutically acceptable salts thereof. The 2-arylselenazole compounds have a xanthine oxidase inhibition activity. The compounds or pharmaceutically acceptable salts thereof can be applied to prepare medicines for preventing or treating hyperuricemia, gout, diabetic nephropathy, inflammatory diseases and neurological system diseases.

The invention provides an allopurinol derivative as shown in Formula I, and a preparation method and application thereof. Tumor growth can be effectively suppressed by the allopurinol derivative provided by the invention, the activity of the allopurinol derivative is equivalent to that of 17-AGG (17-allylamide-17-demethoxygeldanamycin) to which phase III clinical trial is performed, and the allopurinol derivative has a good antitumor effect. The activity of xanthine oxidase can be effectively suppressed by the allopurinol derivative, and the allopurinol derivative can be used for treating gout and provides a new drug choice for clinically treating cancer and gout. Additionally, the preparation method of the compound provided by the invention has the advantages of simplicity, lower cost, high yield and good industrial application prospect.

The invention discloses lactobacillus fermentum for preventing and treating hyperuricemia as well as a composition and application thereof, wherein the lactobacillus fermentum GF1800 for preventing and treating hyperuricemia has the preservation number of CCTCC NO:M 2021984. The lactobacillus fermentum GF1800 is high in biological activity and strong in acid production capacity, can effectively inhibit the activity of pathogenic microorganisms and xanthine oxidase, can tolerate gastric acid and cholate, has a remarkable degradation effect on nucleoside substances, uric acid, cholesterol, nitrite and the like, can efficiently inhibit intake of exogenous uric acid and increase of endogenous uric acid, can obviously reduce the blood uric acid level of hyperuricemia, and meanwhile, improves intestinal and kidney structural injury and inflammatory response. The invention further discloses a composition containing the lactobacillus fermentum GF1800 and a strain metabolite and postbiotics of the lactobacillus fermentum GF1800 and an application of the lactobacillus fermentum GF1800 and the postbiotics of the lactobacillus fermentum GF1800 to preparation of functional food or medicine for preventing and treating hyperuricemia or / and gout, degrading nucleoside, inhibiting xanthine oxidase, reducing cholesterol, degrading nitrite and inhibiting pathogenic bacteria.

The invention discloses application of a gallate derivative which has a formula (I) and a pharmaceutically acceptable salt thereof to preparation of a medicine for treating hyperuricemia. The gallate derivative has a strong effect of inhibiting xanthine oxidase in vitro, can be used for reducing the level of serum uric acid of a mouse with hyperuricemia significantly, is dose dependent and can be used for treating hyperuricemia and gout or gout complications caused by hyperuricemia as a potential xanthine oxidase inhibitor and a potential uric acid lowering medicine. The formula (I) is as shown in the specification.

The invention particularly relates to a xanthine oxidase inhibitory peptide. The amino acid sequence of the xanthine oxidase inhibitory peptide is Glu-Glu-Ala-Lys (EEAK). The IC50 value of the tetrapeptide EEAK on xanthine oxidase inhibitory activity is 173.00+ / -0.06 [mu]M, the tetrapeptide EEAK has a continuous and stable inhibitory effect on xanthine oxidase, and the tetrapeptide EEAK has the outstanding advantages of safety, no toxic or side effect, easiness in absorption, industrialization and the like. The active tetrapeptide EEAK or the derivative thereof can be used for preparing gout treatment / prevention medicines or used as a functional food additive for long-term treatment and health care of gout patients, and has a wide application prospect and very important significance.

The invention provides a pharmaceutical composition for treating gout. The pharmaceutical composition consists of, by weight, pharmaceutical raw materials including butyl phthalide 25-35 parts, sedenenolide 15-25 parts and neocnidilide 40-55 parts. The invention further provides application of the pharmaceutical composition and phthalide compounds, namely the butyl phthalide, the sedenenolide and the neocnidilide in preparation of drugs for treating the gout. The pharmaceutical composition has the advantages that the pharmaceutical composition has the effect of promoting uric acid excretion and abirritation, three phthalide compounds, namely the butyl phthalide, the sedenenolide and the neocnidilide have certain xanthine oxidase inhibiting activity, and a novel source is provided for preparation of the drugs for inhibiting the xanthine oxidase activity or preventing and treating the gout.

The invention discloses a kidney bean bioactive peptide. The kidney bean bioactive peptide is prepared by the following method: 1) extracting proteins from kidney beans by adopting an alkali extraction and acid precipitation method; 2) dissolving the extracted proteins with water, then adding protease for enzymolysis, performing heating for inactivation, then performing centrifuging, and taking supernatant; and 3) filtering the supernatant with an ultrafiltration membrane, and performing freeze-drying to obtain the bioactive peptide. The kidney bean bioactive peptide provided by the inventionhas an inhibition effect on xanthine oxidase, and the in-vitro inhibition rate can reach 50% at most, so that the kidney bean bioactive peptide can be used for preparing xanthine oxidase inhibitors for in-vitro or in-vivo use or can be used for preparing uric acid reducing drugs for treating diseases such as hyperuricemia and gout.

The invention discloses a deuterium-substituted 2-phenylthiazole compound and a pharmaceutical composition thereof, and specifically relates to a deuterium-substituted 2-phenylthiazole compound with a general formula represented by formula (I), and a pharmaceutically acceptable salt thereof. At least one of R<3>, R<4>, and R<5> are used for representing deuterium or a substituent group containing deuterium. The deuterium-substituted 2-phenylthiazole compound is capable of inhibiting activity of xanthine oxidase. The deuterium-substituted 2-phenylthiazole compound or the pharmaceutically acceptable salt of the deuterium-substituted 2-phenylthiazole compound can be used for preparation of medicines used for preventing or treating hyperuricemia, gout, diabetic nephropathy, inflammatory diseases, and nervous system diseases.

The invention relates to aryl benzofuran amidated derivatives and a pharmaceutical use and a preparation method thereof; the derivatives have the antioxidant activity, have xanthine oxidase inhibitory activity, and can be used in preparation of compositions, drugs and health care products for resisting oxidation and treating gout and hyperuricemia.

The invention belongs to the technical field of medicaments, relates to 5-substituted phenyl-3-isoxazole carboxylic acid with xanthine oxidase inhibitory activity shown as in general expression I and ester compounds, tautomer, a pharmaceutical salt and a pharmaceutical solvate thereof and pharmaceutical compositions containing the components and a preparation method of the components, and also relates to application of the compounds and the compositions in preparing a medicament for treating hyperuricemia and gout (wherein R independently is substituted or unsubstituted linear and branched C1-C10 alkyl, C2-C10 alkenyl, C3-C7 naphthenic base, C3-C7 cycloalkenyl groups, an aromatic group, an aralkyl group, a heterocyclic group, heteroaryl, heterocyclic-alkyl, heteroarylalkyl, C3-C7 cycloalkyl-alkyl, aminoalkyl, primary alkyl aminoalkyl, dialkyl aminoalkyl, alkoxyl-alkyl, aryl-oxyalkyl, aralkoxy-alkyl and fully halogenated alkyl; R is a cyano-group, a nitro group, halogen and unsubstituted, monosubstituted or disubstituted aminocarbonyl; R is a hydrogen atom or ethyl; and A is an oxygen atom, a sulphur atom and a nitrogen atom).

The invention discloses a traditional Chinese medicine composite with a function of inhibiting alpha-glucuroide and xanthine oxidase and a preparation method and applications thereof. The bulk pharmaceutical chemical of the traditional Chinese medicine composite comprises drynaria rhizome, and also can comprise tuber fleeceflower stem, wherein, the weight ratio of drynaria rhizome to tuber fleeceflower stem is (0.5-2): 1, the preferential weight ratio is 1:1. The traditional Chinese medicine composite is based on two enzyme inhibitors of alpha-glucuroide and xanthine oxidase, and has double functions of reducing postprandial plasma glucose and blood uric acid. The invention has rich resource and low price, is safe and non-toxic, and has consistent function with Glucobay and allopurinol, thus the invention can be used for treating the diseases of glucose tolerance defect, diabetes, obesity, hyperuricemia and gout and the like.

The invention discloses a medicine for curing podagra, which is prepared by the raw materials with the weight proportions as follows: 15-25 parts of giant knotweed rhizome, 8-15 parts of salvia miltiorrhiza, 6-12 parts of rheum officinale, 12-17 parts of cuttlebone, 12-17 parts of isatis root, 12-17 parts of greater bunet root, 10-14 parts of herba scutellariae barbatae and 6-15 parts of radix bupleuri. The medicine for curing podagra provided by the invention has obvious effects on anti-inflammation and abirritation, can obviously lower the blood uric acid content and the activity of xanthine oxidase in livers, also can protect kidney and improve the organism condition, has excellent therapeutic effect on podagra; the therapeutic effect is excellent, the adverse reaction is little, the toxic side effect is not obvious, and the medicine is obviously better than the anti-podagra medicines clinically used at present.

The invention discloses lactobacillus rhamnosus CCFM1131 for relieving hyperuricemia, and belongs to the technical field of microorganisms. The lactobacillus rhamnosus CCFM1131 can reduce the serum uric acid level of a hyperuricemia mouse, inhibit the xanthine oxidase (XOD) activity of serum and the liver, and reduce the occurrence of hyperuricemia and gout; the lactobacillus rhamnosus CCFM1131 can be used for down-regulating serum blood sugar, down-regulating serum total triglyceride (TG), down-regulating serum total cholesterol (TC) level and inhibiting serum alkaline phosphatase (ALP) activity; in addition, the lactobacillus rhamnosus CCFM1131 can promote the expression of the ileum uric acid transporter ABCG2. Besides, the lactobacillus rhamnosus CCFM1131 can tolerate gastrointestinaltract environment, can be used for preparing functional microbial inoculants, foods and medicines for relieving hyperuricemia and gout, and has a wide application prospect.