55 results about "Desoxycholic acid" patented technology

The invention discloses a synthesis method of N-goose deoxycholyl-L-aspartic acid and application of the N-goose deoxycholyl-L-aspartic acid in preparation of a medicine for improving metabolism-related fatty liver diseases. According to the method provided by the invention, chenodeoxycholic acid and L-dimethyl aspartate hydrochloride are taken as raw materials, and a chenodeoxycholic acid-dimethyl aspartate intermediate is synthesized, so that a target compound-N-chenodeoxycholyl-L-aspartic acid with a brand new structure is efficiently prepared. The compound shows a treatment effect superior to that of obeticholic acid (OCA) in an animal model, and can effectively improve multiple indexes such as fatty degeneration, inflammation and fibrosis of the liver. The invention provides a brand new solution for major clinical challenges of insufficient curative effect, large side effect, drug withdrawal rebound and the like of the current MAFLD treatment drug, and provides a candidate compound with a wide prospect for developing a novel efficient MAFLD treatment drug.

The invention relates to a metabolite marker for early diagnosis of colorectal cancer as well as application and a device of the metabolite marker. The marker comprises sulfate, ubiquinone-1, a deoxycholic acid glycine conjugate, demethylchlorophyllin, 3-(3, 5-diiodine-4-hydroxyphenyl) lactate, vitamin K1, O-decanoyl-L-carnitine, sedoheptulose 1, 7-diphosphoric acid, cholesterol-docosahexaenoic acid ester and acyl AMP (adenosine monophosphate). The marker combination has excellent performance in colorectal cancer detection, AUROC can reach 0.97, and noninvasive screening and early diagnosis of colorectal cancer can be accurately, quickly and simply realized.

The application provides a reduction-responsive nano delivery system and application thereof in preparation of a drug for treating drug-resistant tumors, and belongs to the pharmaceutical field. The application constructs a reduction-responsive branched copolymer functionalized by pegylation and deoxycholic acid (DA) (referred to as: pegylated branched poly(HPMA-DA)), which can effectively encapsulate small molecule drugs to form a nano delivery system. Experiments prove that the nano delivery system can be taken up by tumor cells, has good tumor targeting, and exhibits excellent anti-tumor effect in tumor xenografts (CDX) derived from non-small cell lung cancer (NSCLC) chemoresistant cell lines and patient-derived xenograft mouse models (PDX). The pegylated branched poly(HPMA-DA) provided by the application has wide application prospect in preparation of a drug carrier, and the nano delivery system provided by the application has wide application prospect in preparation of a drug for treating cancer.

The invention belongs to the technical field of biological medicine, and relates to a novel application of endogenous substances in alcohol related liver disease (ALD). The invention proposes for the first time that an endogenous substance with regular concentration change in the ALD process can be used as a biomarker for auxiliary diagnosis and / or stage evaluation of ALD, the exogenous supplement of the endogenous substance has a prevention and treatment effect on ALD, and the endogenous substance has double values of being used as an excellent biomarker and an effective therapeutic agent. The substances include but are not limited to taurochenodeoxycholic acid (TCDCA), dehydroepiandrosterone sulfate (DHEA-S) and the like. Wherein the serum concentration of TCDCA is obviously increased along with disease progression, and the concentration of DHEA-S is obviously reduced. The diagnostic value of the substance on ALD is remarkably superior to that of a traditional liver injury marker, and ethanol-induced liver cell injury and mouse liver pathological change can be remarkably improved through exogenous supplementation. The invention provides a brand new strategy for accurate diagnosis and prevention of ALD.

The invention belongs to the technical field of biological medicines, and particularly relates to application of chenodeoxycholic acid in preparation of drugs for treating allergic diseases. It is found that CDCA can effectively inhibit pyroptosis and secretion of proinflammatory factors, expression of complement inhibition proteins CD46, CD55 and CD59 is remarkably up-regulated, expression of the complement inhibition proteins CD46, CD55 and CD59 is finally promoted, and occurrence and development of allergic diseases are effectively relieved. In a mouse model, CDCA can significantly improve OVA-induced food allergy symptoms, and has application prospects in treatment of allergic diseases.

The invention provides two new applications of taurochenodeoxycholic acid (TCDCA) in the field of alcohol related liver diseases (ALD), and belongs to the field of biological medicines. First, the invention proposes that TCDCA is used as a biomarker for auxiliary diagnosis and / or staging evaluation of ALD for the first time. Clinical research finds that the level of TCDCA in human serum is in significant positive correlation with the severity of ALD, and the TCDCA has extremely high accuracy in ALD diagnosis and can effectively assist in distinguishing different stages of diseases. Secondly, the invention discloses an application of TCDCA in preparation of a medicine for preventing and / or treating ALD (Atomic Lymphosis Disease). Researches show that the TCDCA can save ethanol-induced liver cell activity decline in a concentration-dependent manner and improve liver pathological indexes of mice. The TCDCA has double values of being used as an excellent biomarker and an effective prevention and treatment component, and a brand new strategy is provided for accurate diagnosis and prevention and treatment of ALD.

The application discloses a synthesis method of N-chenodeoxycholyl-L-aspartic acid and application of the N-chenodeoxycholyl-L-aspartic acid in preparation of a medicine for improving metabolic associated fatty liver disease. The method provided by the application uses chenodeoxycholic acid and L-aspartic acid dimethyl ester hydrochloride as raw materials, synthesizes a chenodeoxycholic acid-aspartic acid dimethyl ester intermediate, and efficiently prepares a target compound, N-chenodeoxycholyl-L-aspartic acid, which is a novel structure, the compound exhibits a treatment effect superior to that of obeticholic acid (OCA) in an animal model, and can effectively improve multiple indexes such as liver steatosis, inflammation and fibrosis. The application provides a novel solution for major clinical challenges such as insufficient treatment effect, large side effect and rebound after drug withdrawal of current MAFLD treatment medicines, and provides a candidate compound with broad prospects for developing a new high-efficiency MAFLD treatment medicine.

The present invention relates to a lipolytic injection composition having excellent effects of alleviating pain during treatment, and improving solubility and maintaining stability of deoxycholic acid by comprising deoxycholic acid (DCA) and cyclodextrin in an optimal composition ratio and adjusting pH to a range of 7.0 to 7.7.

The present invention provides a fat-dissolving composition and a use thereof. The fat-dissolving composition of the present invention comprises a pharmaceutically active ingredient, an inclusion material, a pH regulator optionally selected from one or more of a buffer, a stabilizer, an osmotic pressure regulator, and a complexing agent, and optionally purified water, wherein the pharmaceutically active ingredient is selected from one or more of deoxycholic acid, a pharmaceutically acceptable salt of deoxycholic acid, and a deoxycholic acid derivative, and the amount of the inclusion material ranges from 4% to 35% on the basis of the total weight of the fat-dissolving composition. Compared with conventional formulations at the same dose, the fat-dissolving composition of the present invention can significantly reduce adverse effects at the administration site while having a good fat-dissolving effect, and has higher safety.

The invention provides a fat-dissolving composition and application thereof. The fat-dissolving composition comprises an active pharmaceutical ingredient, an inclusion material, a pH regulator, one or more optional components selected from a buffering agent, a stabilizing agent, an osmotic pressure regulator and a complexing agent, and optional purified water, the active pharmaceutical ingredient is selected from one or more of deoxycholic acid, pharmaceutically acceptable salts of deoxycholic acid and deoxycholic acid derivatives, and the dosage range of the inclusion material is 4-35% based on the total weight of the fat-dissolving composition. Compared with a conventional preparation with the same dosage, the fat-dissolving composition disclosed by the invention has the advantages that under the condition that a good fat-dissolving effect is achieved, the adverse reaction of an administration part can be obviously relieved, and the fat-dissolving composition has higher safety.

This invention belongs to the field of traditional Chinese medicine technology, and provides the application of Scutellaria baicalensis leaf aqueous extract in the preparation of drugs for improving or treating inflammatory bowel disease (IBD) with depression. The Scutellaria baicalensis leaf aqueous extract improves IBD with depression by increasing the abundance of Akkermansia myxophilus (AKK) bacteria, restoring disordered deoxycholic acid metabolism. The extract increases the abundance of AKK bacteria in the intestine, increases the content of deoxycholic acid (DCA) in the intestine, regulates Th17 / Treg homeostasis, reduces intestinal inflammation, maintains intestinal barrier integrity, reduces the entry of pro-inflammatory factors into the bloodstream and across the blood-brain barrier into the hippocampus, inhibits neuroinflammation, and improves depression. Scutellaria baicalensis leaves can improve IBD with depression by increasing the abundance of AKK bacteria in the intestine, increasing intestinal DCA levels, regulating Th17 / Treg balance, repairing the intestinal barrier, reducing LPS leakage and alleviating nerve damage, and inhibiting the inflammatory response of the gut-brain axis. This provides certain experimental evidence for the development and utilization of related traditional Chinese medicine resources.

This application discloses a lipid control solution, comprising a buffer solution, cholesterol or cholesterol and glycerol, cholic acid or deoxycholic acid and its salts, and cyclodextrin. The lipid control solution provided in this application uses cholic acid or deoxycholic acid and its salts and cyclodextrin as solubilizers to form a complex, allowing cholesterol to dissolve in a water-soluble matrix. It is prepared by direct stirring at room temperature, without the involvement of any organic flammable or harmful reagents. The process is simple, safe, reliable, and exhibits good stability with a shelf life of up to 12 months.

The invention provides application of ergosterol in preparation of a medicine for treating pulmonary arterial hypertension. The preparation method of the ergosterol comprises the following steps: cleaning, crushing and drying silkworm chrysalis cordyceps hainanensis sporocarp to obtain cordyceps militaris powder; the method comprises the following steps: mixing cholic acid, deoxycholic acid, methoxypolyethylene glycol and absolute ethyl alcohol to obtain ethanol mother liquor of a supramolecular solvent; carrying out gradient synergistic extraction on the cordyceps militaris extract; carrying out reduced pressure distillation and drying to obtain an extract, and carrying out chromatographic separation and drying; and recrystallizing, cleaning and drying to obtain the product. According to the invention, CO2 expanded ethanol liquid is adopted as a solvent, a cholic acid-deoxycholic acid-methoxypolyethylene glycol supramolecular solvent system technology and homologous adaptability of steroid nucleus structures of etocholic acid and deoxycholic acid and ergosterol are utilized to construct a multi-stage cavity recognition network, and C5-C6 double bonds and C22-C23 double bonds of ergosterol are specifically combined, so that the detection sensitivity of ergosterol is improved, and the detection sensitivity of ergosterol is improved. Meanwhile, the pore diameter of the cavity is regulated and controlled through methoxypolyethylene glycol, and the content of ergosterol in the extract is increased.

The application discloses a deoxycholic acid intermediate and application thereof, and belongs to the technical field of organic synthesis. The deoxycholic acid intermediate has a structural formula as shown in the specification, wherein R1 is -OH or -OAc; R2 is alpha-OH, beta-OH or =O; and R3 is =O or -CHCH3. In addition, the application further provides application of the deoxycholic acid intermediate in preparation of deoxycholic acid. The intermediate can be used for effectively and safely synthesizing deoxycholic acid.

The application provides application of ergosterol in preparation of a medicine for treating pulmonary arterial hypertension. A preparation method of the ergosterol is as follows: Cordyceps militaris Haining strain fruiting bodies are taken, washed, crushed, and dried to obtain Cordyceps militaris powder; cholic acid, deoxycholic acid, polyethylene glycol monomethyl ether and anhydrous ethanol are mixed to obtain an ethanol mother liquor of a supramolecular solvent; Cordyceps militaris extraction liquid is gradiently and cooperatively extracted; vacuum distillation, drying, chromatographic separation, drying, recrystallization, washing and drying are sequentially performed, and the ergosterol is obtained. In the application, CO2 expanded ethanol liquid is used as a solvent, and a cholic acid-deoxycholic acid-polyethylene glycol monomethyl ether supramolecular solvent system technology is used. Relying on the homologous adaptability of the steroid nucleus structure of cholic acid and deoxycholic acid and ergosterol, a multi-level cavity recognition network is constructed, the C5-C6 double bond and the C22-C23 double bond sites of ergosterol are specifically combined, and the content of ergosterol in the extract is improved by regulating the cavity aperture through the polyethylene glycol monomethyl ether.

The application belongs to the field of new adjuvants and new dosage forms of pharmaceutical preparations, and particularly relates to a type I and type II immunogenic cell death inducer ion pairing engineered nanoassemblies as well as construction and application thereof. The nanoassemblies are composed of type I ICD inducers, type II ICD inducers, hydrophobic auxiliary counterions and amphiphilic lipid ion pairing. The type I ICD inducer is selected from mitoxantrone, doxorubicin, oxaliplatin or cyclophosphamide; the type II ICD inducer is selected from hypericin; and the hydrophobic auxiliary counterion is selected from cholesteryl sodium sulfate, cholic acid, deoxycholic acid, chenodeoxycholic acid, lithocholic acid, glycolcholic acid, taurocholic acid, glycochenodeoxycholic acid, taurochenodeoxycholic acid, deoxycholic acid lysine derivative, oleanolic acid and ursolic acid. The type I and type II ICD inducers are combined in the application, and have a synergistic tumor treatment effect.

This application relates to the field of feed, specifically to the application of UDCA in the preparation of formulations that reduce the incidence of intrauterine growth retardation (IUGR) in pregnant sows. According to the technical solution of this application, by adding 0.05% ursodeoxycholic acid to the diet of sows during late gestation (85 days) to the farrowing stage, using a restricted feeding method, at a rate of 2 kg / head / day, twice daily, the incidence of IUGR in sows can be effectively reduced by up to 76.17%, while also increasing the average weaning weight of piglets at 28 days by 9.61%.

The application provides a traditional Chinese medicine composition for clearing vision and removing nebula and application thereof, and includes bear bile powder and borneol with a mass ratio of 1-5:1; the bear bile powder includes tauroursodeoxycholic acid and tauroursodeoxycholic acid arginine salt with a molar ratio of 0.4-0.9:0.1-0.6. The application converts tauroursodeoxycholic acid in bear bile powder into tauroursodeoxycholic acid arginine salt, so that the molar ratio of tauroursodeoxycholic acid and tauroursodeoxycholic acid arginine salt in bear bile powder is 0.4-0.9:0.1-0.6, and the bear bile powder is compounded with borneol to treat cataract. Experimental results show that when the molar ratio of tauroursodeoxycholic acid and tauroursodeoxycholic acid arginine salt in bear bile powder is 0.4-0.9:0.1-0.6, the effect of the bear bile powder compounded with borneol in treating cataract is significantly better than that of bear bile powder containing only tauroursodeoxycholic acid or bear bile powder containing only tauroursodeoxycholic acid arginine salt, for example, there is a significant difference in slowing down the degree and thickness of lens turbidity.

The present application relates to the technical field of nanomedicine, in particular to a β-cyclodextrin-carboxymethyl chitosan-deoxycholic acid nanoparticle carrying ginsenoside CK, a preparation method and application. A first esterification reaction is performed between a β-cyclodextrin solution and a carboxyl-activated carboxymethyl chitosan solution to obtain a β-cyclodextrin-carboxymethyl chitosan polymer; a second esterification or amidation reaction is performed by adding carboxyl-activated deoxycholic acid to the β-cyclodextrin-carboxymethyl chitosan polymer to obtain a β-cyclodextrin-carboxymethyl chitosan-deoxycholic acid polymer; an ethanol solution of ginsenoside CK is mixed with a water solution of the β-cyclodextrin-carboxymethyl chitosan-deoxycholic acid polymer to obtain a whole particle, and a freeze-drying protective agent is added for freeze-drying to obtain the β-cyclodextrin-carboxymethyl chitosan-deoxycholic acid nanoparticle carrying ginsenoside CK. The present application focuses on the design of an intelligent carrier, realizes the synergistic optimization of high drug loading and intelligent delivery, and overcomes the defects of the prior art.

The present application belongs to the field of aquaculture and nutrition regulation technology, and particularly relates to a ursodeoxycholic acid preparation for inducing the group behavior of juvenile fish, a preparation method and application. The ursodeoxycholic acid preparation for inducing the group behavior of juvenile fish is composed of ursodeoxycholic acid and additives equivalent to 0% to 2% of the mass of ursodeoxycholic acid; the additives are cholic acid or a mixed agent, and the mixed agent is a mixture of taurine and tryptophan in a mass ratio of 1:1. After the ursodeoxycholic acid preparation for inducing the group behavior of juvenile fish is used to feed large yellow croaker juveniles, the juvenile fish olfaction can be stimulated, the group behavior of the juvenile fish can be induced, the growth of the large yellow croaker juveniles can be promoted, the metabolism can be promoted, and the immunity can be improved.

The invention relates to a metabolite and methylation combined marker for early diagnosis of colorectal cancer as well as application and a device of the metabolite and methylation combined marker. The marker comprises sulfate, ubiquinone-1, a deoxycholic acid and glycine conjugate, demethylchlorophyllin, 3-(3, 5-diiodine-4-hydroxyphenyl) lactate, vitamin K1, O-decanoyl-L-carnitine, sedoheptulose 1, 7-diphosphoric acid, cholesterole-docosahexaenoic acid ester, acyl AMP, cg 19669457, cg 19181811, cg 18092474, cg 05452319, cg 06270401, cg 24911721, cg 07732037, cg 21805179, cg 25288194, cg 15845821 and cg 01649837, and is characterized in that the cg 19669457, the The marker combination has excellent performance in colorectal cancer detection, AUROC can reach 0.98, and noninvasive screening and early diagnosis of colorectal cancer can be accurately, rapidly and simply realized.

The present application relates to the technical field of diagnostic markers and diagnostic methods for intrahepatic cholestasis of pregnancy (ICP), and in particular to a combination of diagnostic or condition monitoring markers for intrahepatic cholestasis of pregnancy and application thereof. The biomarkers include diagnostic markers for diagnosis and screening, and condition monitoring markers for follow-up; the diagnostic markers include a diagnostic combination marker composed of tauroursodeoxycholic acid and glycochenodeoxycholic acid, and taurohyocholic acid; and the condition monitoring markers include glycochenodeoxycholic acid, glycolcholic acid, and taurohyocholic acid. The technical solution solves the technical problem of the prior art that there is a lack of sensitive and specific diagnostic markers for intrahepatic cholestasis of pregnancy, and has important significance for early diagnosis, auxiliary clinical diagnosis and treatment, and improvement of population quality, and provides a new strategy for the difficult diagnosis and treatment of ICP.

A method for treating or reducing localized fat, and a pharmaceutical composition for use in treating or reducing localized fat. The method comprises injecting the pharmaceutical composition into the localized fat of a subject in need, wherein the pharmaceutical composition comprises deoxycholic acid and a viscous agent, and wherein deoxycholic acid is present in the pharmaceutical composition in an amount of 1% to 5% w / v.

This invention discloses the application of *Gastrococcus xanthophylloides* in regulating intestinal bile acid metabolism disorders, including *Gastrococcus xanthophylloides* (… Ruminococcus flavefaciens The application of this invention in the preparation of compositions for regulating intestinal bile acid metabolism disorders, wherein the compositions promote the conversion of primary bile acids to secondary bile acids, wherein the primary bile acids include cholic acid and chenodeoxycholic acid, and the secondary bile acids include deoxycholic acid and lithocholic acid; wherein the intestinal bile acid metabolism disorders include metabolic disorders caused by antibiotics, wherein the antibiotics include one or more of moxifloxacin and metronidazole; wherein the compositions can be health products, pharmaceuticals, or feed; and wherein the active ingredient of the compositions includes xanthospirococcus flavus.

The invention relates to the field of medicines, and particularly discloses application of bile acid in preparation of a medicine for treating osteoporosis. Research finds that the content of hyodeoxycholic acid (HDCA) in an old individual is remarkably reduced, and the bone mineral density and the bone microstructure can be improved by supplementing the HDCA. Animal experiment results show that the HDCA can significantly inhibit bone mass loss and improve bone quality through oral administration and intragastric administration, and the effect of the HDCA depends on a bile acid receptor TGR5. HDCA is provided as an active component for treating osteoporosis for the first time, and a new drug candidate and an action mechanism can be provided for prevention and treatment of osteoporosis.

The invention belongs to the technical field of nano drug delivery systems, and particularly relates to an amphiphilic cascade response chitosan nano drug delivery system and a preparation method and application thereof. The nano drug delivery system is of a multi-layer structure composed of an enzyme response inner layer and a pH response outer layer; the enzyme response inner layer is formed by sulfobutyl ether-beta-cyclodextrin and protamine sulfate through electrostatic adsorption, and a hydrophobic anti-cancer drug is loaded in a hydrophobic cavity of the sulfobutyl ether-beta-cyclodextrin to form enzyme response supramolecular nanoparticles; the pH response outer layer is composed of amphiphilic chitosan which is hydrophilically modified by succinic anhydride and hydrophobically modified by deoxycholic acid, and the amphiphilic chitosan is coated on the surfaces of the enzyme response supramolecular nanoparticles. By utilizing the arrangement of the structure, the invention provides the nano drug delivery system based on the amphipathic chitosan, which is suitable for intestinal targeted delivery and controlled release therapy of hydrophobic anti-cancer drugs.

This invention relates to the field of pharmaceutical technology, specifically to the application of porcine deoxycholic acid (HDCA) in the preparation of a drug for alleviating colitis. The dosage of HDCA is 50-200 mg / kg body weight / day. The colitis referred to is DSS-induced colitis, inflammatory bowel disease, or ulcerative colitis. Administration is by gavage. The drug alleviates colitis by promoting the proliferation of intestinal stem cells and / or repairing intestinal barrier function. This method can reverse the decrease in food intake and body weight in mice under DSS, reduce their disease activity index, and alleviate the problem of DSS-induced colon shortening in mice; simultaneously, HDCA also promotes the proliferation of intestinal stem cells, repairs intestinal permeability, and alleviates DSS-induced damage to the intestinal mucosal barrier function in mice. It can inhibit the expression of intestinal inflammation-related genes in mice, alleviating inflammatory complications. It helps to reshape the intestinal flora of mice, especially promoting Akkermansia colonization and alleviating intestinal barrier damage.

Disclosed in the present invention are a kit for detecting 15 bile acid profiles and three bile acid precursors in serum simultaneously and a detection method therefor. The 15 bile acid profiles comprise: cholic acid, deoxycholic acid, chenodeoxycholic acid, ursodeoxycholic acid, lithocholic acid, glycocholic acid, glycodeoxycholic acid, glycochenodeoxycholic acid, glycoursodeoxycholic acid, glycolithocholic acid, taurocholic acid, taurodeoxycholic acid, taurochenodeoxycholic acid, tauroursodeoxycholic acid and taurolithocholic acid; and the three bile acid precursors comprise: 3α,7α-dihydroxycoprostanic acid, 3α,7α,12α-trihydroxycholestanoic acid and 7α-hydroxy-4-cholesten-3-one. The kit and detection method of the present invention enable the simultaneous and accurate detection of the 15 bile acid profiles and the three bile acid precursors, with a short detection time and a high detection accuracy. This, to a certain extent, meets the clinical need for assessing the enterohepatic cycle composed of the biliary system, intestines, portal venous circulation and hepatocytes.

The invention provides a method and a kit for diagnosing or identifying whether an individual suffers from liver cancer or not by detecting a metabolic biomarker, and the metabolic biomarker comprises 1-stearoyl-2-arachidonyl-sn-glycerol, NG, S-glycerol, S-glycerol, N-glycerol, N-glycerol, N-glycerol, N-glycerol, N-glycerol, N-glycerol, N-glycerol, N-glycerol and N-glycerol. The compound is selected from one or more of N, N-dimethyl-L-arginine, N, N-dimethyl-L-arginine (ADMA), taurochenodeoxycholic acid, proline-valine (Pro-Val) and 1-oleoyl-L-alpha-lysophosphatidic acid.

A method for treating or reducing localized fat, and a pharmaceutical composition for use in treating or reducing localized fat. The method comprises injecting the pharmaceutical composition into the localized fat of a subject in need, wherein the pharmaceutical composition comprises deoxycholic acid and a viscous agent, and wherein deoxycholic acid is present in the pharmaceutical composition in an amount of 1% to 5% w / v.