33 results about "Lithocholic acid" patented technology

An object of the present application is to provide a novel rodenticide. According to the present application, a rodenticide comprising a compound represented by the following general formula (I), a salt thereof, or a prodrug thereof is provided. In the formula, R 1 and R 2 each independently represent a hydrogen atom or an alkyl group having 1 to 8 carbon atoms. n represents an integer of 1 to 3. R 3 , R 4 , R 5 and R 6 each independently represent a hydrogen atom or an alkyl group having 1 to 6 carbon atoms. X represents COOH, -C(=O)NH-Z, -CH(OH)-(Y) m -CH(OH)R7, -NH-CO-O-R 10 , -CO-O-R 10 or -NH-CO-N(R 11 )-R 10 . Z represents a hydrogen atom, -CN, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms or a hydroxyl group, Y represents -C(R8)(R9)-, -C(=O)- or -C(=CH2)-, and m represents an integer of 0 to 3. R7, R8 and R9 each independently represent a hydrogen atom or an alkyl group having 1 to 8 carbon atoms. The alkyl group having 1 to 8 carbon atoms represented by Z, R7, R8 and R9 can have a substituent selected from a carboxyl group or a hydroxyl group. R 10 and R 11 each independently represent a hydrogen atom or an alkyl group having 1 to 8 carbon atom which can have a substituent.

The application discloses a metabolic marker for distinguishing metabolic syndrome and simple obesity and application thereof. The marker comprises eight metabolites, i.e. glycocholic acid, lithocholic acid, linoleic acid, valine, leucine, alanine, serine and glycine. The application performs non-targeted metabolomics analysis on serum of metabolic syndrome and simple obesity patients by liquid chromatography mass spectrometry, finds eight metabolites with significant difference between the two, and finds that the eight metabolic markers have high AUC when used for diagnosing and distinguishing metabolic syndrome patients or simple obesity patients alone or in combination.

The invention provides a mutant R41D / S193N of 7beta-hydroxysteroid oxidative dehydrogenase, a gene sequence of the mutant enzyme, a recombinant expression vector containing the gene sequence of the enzyme and an engineering strain containing the vector. The invention also provides a construction method of a recombinant expression vector and an engineering strain, a method for preparing the mutant enzyme by using the engineering strain, and application of the mutant enzyme in in-vitro enzyme catalysis of 7-ketolithocholic acid to produce ursodeoxycholic acid. Compared with a wild type, the R41D / S193N mutant provided by the invention shows stronger preference on a cofactor NADH, is more economical than the traditional NADPH utilization, is simple and convenient in preparation process, high in yield and simple in downstream treatment process, does not involve other solvents except water in the preparation process, belongs to a green biosynthesis method, and is suitable for industrial production. Meanwhile, the method has relatively high atom economy and step economy.

The invention discloses an application of isolithocholic acid in preparation of a medicine for preventing or treating colorectal cancer induced by high fat diet. The invention proves that the isolithocholic acid can be accurately replenished by intragastric administration of 100g / kg of isoLCA at one time, and meanwhile, the isolithocholic acid can obviously inhibit the occurrence of obesity-related colon tumors, reduce the proliferation index of tumor cells and repair the intestinal barrier structure. Isolithocholic acid is endogenous secondary bile acid, can be chemically synthesized or semi-synthesized, is high in safety and good in patient compliance through oral administration, is expected to reduce the occurrence rate of colorectal cancer of obese people, and has important significance in treatment of colorectal cancer.

The invention relates to the technical field of functional polymer materials, in particular to preparation and sensing application of liquid metal composite slip ring hydrogel. The preparation method comprises the following steps: preparing a novel slip ring cross-linking agent by utilizing the host-guest recognition effect of lithocholic acid and beta-cyclodextrin, uniformly dispersing gallium-indium alloy in an aqueous solution through ultrasound, and then adding an acrylamide monomer and a photoinitiator to prepare the liquid metal composite slip ring hydrogel. The liquid metal composite slip ring hydrogel shows excellent toughness, high tensile strength and stable sensing performance under the cooperation of sliding cross-linking points and multiple non-covalent interaction, and can be applied to the fields of flexible sensors and wearable equipment.

The application discloses a 7-ketolithocholic acid molecularly imprinted polymer microsphere and application thereof in solid phase extraction, and belongs to the field of functional polymer materials and separation and analysis technologies. The microsphere is a hollow structure formed by dissolving a silica core, the overall particle size is 3-5 mu m, the particle size distribution index PDI is 0.05-0.08, the molecularly imprinted polymer shell is formed by taking lithocholic acid as a template molecule and through a thermal initiation free radical copolymerization reaction, and is copolymerized by the template molecule, a functional monomer 4-vinylphenylboronic acid and acrylamide, and a crosslinking agent ethylene glycol dimethacrylate in a molar ratio of 1:1:2:20. The application further provides a preparation method of the microsphere and a solid phase extraction column containing the microsphere. The molecularly imprinted polymer microsphere is used as a solid phase extraction adsorbent, can selectively enrich and purify 7-ketolithocholic acid from serum or bile samples, has high selectivity and high recovery rate, and completely avoids the template leakage problem.

This application discloses a biomarker for calcium oxalate kidney stones and its application, relating to the field of pharmaceutical technology. Specifically, it proposes a biomarker for calcium oxalate kidney stones, namely isolithocholic acid. It reveals that isolithocholic acid directly targets and activates the PARP1 protein, inducing parthanatos in renal tubular epithelial cells, leading to cell damage and a microenvironment conducive to crystal adhesion, ultimately driving kidney stone formation. Isolithocholic acid is specifically elevated in feces, serum, kidney, and urine in a calcium oxalate kidney stone model, and its spatial localization is associated with areas of renal tubular damage, indicating its high relevance as a diagnostic or risk warning biomarker.

Provided in the present invention is a method for synthesizing a 7-ketolithocholic acid intermediate, the method comprising preparing compound OB-1 in an amide solvent to obtain a 7-ketolithocholic acid intermediate OB. The method of the present invention has the advantages of readily available of raw materials, a high yield, simple and mild reaction conditions, and suitability for industrial production.

The present invention relates to the field of medicinal chemistry. Specifically disclosed is a use of oxime-based cholic acid (CA) analogs as allosteric agonists for TGR5. In the present invention, CA used as a raw material undergoes a series of reactions to obtain CA intermediates each having an oxime at either or both of positions 7 and 12, and a series of modifications are then carried out on positions 24 and the oximes of these intermediates to obtain CA analogs as represented by formula 1, formula 2, or formula 3. The present invention uses a GloSensor cAMP accumulation assay to test the functional activity and allosteric mechanism of all target compounds on TGR5. Pharmacological results have shown that all synthesized target compounds have relatively good agonistic activity on TGR5 and can positively allosterically regulate the functional activity of chenodeoxycholic acid (CDCA) or lithocholic acid (LCA), that is, the target compounds are all positive allosteric modulators or allosteric agonists for TGR5.

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 invention discloses the application of red ginseng polysaccharide in the preparation of pharmaceutical compositions for the prevention and treatment of inflammatory bowel disease, belonging to the field of medical formulation technology. It is the first to clearly demonstrate that red ginseng polysaccharide promotes the expression of bile salt hydrolase and 7α-hydroxysteroid dehydrogenase by targeting and upregulating the relative abundance of Bacteroides acidophilus and Clostridium lysate in the intestine, thereby driving the production of 7-ketolithocholic acid in the intestine. Through the TGR5 activation mediated by 7-ketolithocholic acid, it improves intestinal damage caused by inflammatory bowel disease, providing a solid experimental basis and theoretical support for the application of red ginseng polysaccharide in the preparation of drugs or functional foods for the prevention and treatment of inflammatory bowel disease.

The invention relates to the technical field of biomedicine, and particularly discloses an in-vitro diagnosis marker for gall-stone and application thereof.The in-vitro diagnosis marker is jointly composed of a metabolism marker and an inflammation marker, the metabolism marker is the concentration ratio of lithocholic acid to ursodesoxycholic acid (LCA / UDCA), and the inflammation marker is the concentration ratio of CD133 to lipopolysaccharide (CD133 / LPS); the invention further provides a kit containing the marker and a detection method of the kit. The kit integrates specific detection reagents for LCA, UDCA, CD133 and LPS, two specific value markers can be rapidly, sensitively and simultaneously detected through an optimized sample treatment and detection process, and result judgment is carried out based on a preset reference interval upper limit and a composite judgment rule.

The invention relates to the technical field of biological medicine chemical separation, and discloses a separation and purification process of high-purity ursodesoxycholic acid mother liquor, which comprises the following steps: adding alkaline amino acid into the mother liquor containing ursodesoxycholic acid, stirring and dissolving to obtain a water phase system; adding a neutral chiral hydrophobic deep-eutectic solvent formed by complexing L-menthol and long-chain fatty alcohol into the water-phase system, and carrying out mixed extraction; standing for layering, separating to remove an upper-layer oil phase, and collecting a lower-layer water phase; finally, acid is added into the water phase to adjust the pH value, and an ursodesoxycholic acid product is obtained through ultrasonic-assisted crystallization, cleaning and drying. According to the method disclosed by the invention, efficient separation of a target product from chenodeoxycholic acid and lithocholic acid is realized by utilizing the specific hydrophilic anchoring effect of the basic amino acid on ursodeoxycholic acid and cooperating with the chiral hydrophobic recognition effect of the eutectic solvent on impurities. The process is green and environment-friendly, the solvent can be recycled, and the obtained product is high in purity and suitable for industrial application.

The present invention provides a method for synthesizing 7-ketolithocholic acid intermediate, which comprises the step of obtaining 7-ketolithocholic acid intermediate OB from compound OB-1 in an amide solvent. The method of the present invention has easy availability of raw materials, high yield, simple and mild reaction conditions, and is suitable for industrial production.

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 subject matter of the invention is an isolitocholic acid for use in the prevention and / or treatment of inflammatory diseases of the respiratory system and / or prevention and / or treatment of cytokine storm-associated diseases.

The invention provides a composite antibacterial inclusion compound, a slow-release antibacterial surface sizing agent and a preparation method and application thereof, and belongs to the technical field of papermaking. Lithocholic acid and titanium dioxide are used as antibacterial agents, nitrogen-doped modified titanium dioxide and lithocholic acid are subjected to esterification to prepare a lithocholic acid grafted nitrogen-doped modified titanium dioxide antibacterial agent, and then the LCA-N / TiO2-beta-CD-HAM inclusion compound with slow-release antibacterial performance is obtained through host-guest recognition of the lithocholic acid grafted nitrogen-doped modified titanium dioxide antibacterial agent and alkenyl cyclodextrin. And finally, preparing the LCA-N / TiO2-beta-CD-HAM styrene-acrylic surface sizing agent with the slow-release antibacterial property. The slow-release broad-spectrum surface sizing agent with the slow-release antibacterial function is prepared through doping modification, grafting and polymerization.

The subject matter of the invention is a compound of the formula (I), or a salt, prodrug, solvate, hydrate, or stereoisomer thereof, wherein Rn represents groups for n=1, 2, or 3, as follows R1 represents -NHCH(CH3)2, R2 represents -CONH2, R3 represents -CH2NH2. Another subject matter of the invention is a compound according to the present invention for use in a prevention and / or treatment of inflammatory diseases of the respiratory system and / or prevention and / or treatment of cytokine storm-associated diseases.

This invention discloses a ferrugin mutant and its application in the synthesis of mouse deoxycholic acid, belonging to the field of biocatalytic enzyme technology. This invention uses *E. coli* as the chassis strain to express the P450 enzyme OleP and establishes a three-component redox chaperone library, screening for the most suitable redox chaperones PetH / PetF for OleP. A high-throughput method based on characteristic absorbance values ​​is developed, enabling rapid and efficient detection of lithocholic acid and mouse deoxycholic acid. Furthermore, through semi-rational design of ferrugin proteins, a ferrugin mutant, PetF, is screened. F64D This method can significantly improve the conversion rate of catalytic preparation of mouse deoxycholic acid. It provides a new strategy for improving the biosynthesis of hydroxylated steroidal substances.

The application discloses a combined biomarker combination and evaluation model for evaluating chronic low-grade inflammation of polycystic ovary syndrome, and belongs to the technical field of biomarkers. The combined biomarker combination comprises inflammation-related proteins and metabolites; the inflammation-related proteins comprise FURIN, CCL3, CCL8, CD38, NOS2, NOS3, IL18R1 and HGF; and the metabolites comprise lithocholic acid-3-O-glucuronide and taurine. The application provides a combined biomarker combination for diagnosing and evaluating the chronic inflammation state of polycystic ovary syndrome and an application method thereof. By jointly detecting specific inflammatory proteins and metabolites, the systemic chronic inflammation load of PCOS patients is quantitatively evaluated, and the combined biomarker combination has the beneficial effects of high stability, accurate discrimination, wide applicability and easy clinical transformation, and solves the problem that there is no objective evaluation method for the chronic inflammation state of PCOS.

Compositions and methods for preventing dental cavities are described. The compositions include, and the methods involve the use of, an anti-biofilm compound such as pranlukast or lithocholic acid.

This invention relates to the field of artificial bear bile powder preparation technology, specifically to a novel 7α-hydroxysteroid dehydrogenase gene R-α-1 and its application in the production and conversion of bear bile powder. This method isolates a novel gene catalyzing asymmetric carbonyl reduction reactions from the feces of Sichuan brown bears. This gene encodes a 7α-hydroxysteroid dehydrogenase, which catalyzes the formation of the intermediate tauroursodeoxycholic acid from tauroursodeoxycholic acid, which is further catalyzed by a 7β-hydroxysteroid dehydrogenase to produce tauroursodeoxycholic acid, the main component of bear bile powder. The nucleotide sequence of this gene is shown in SEQ ID NO.1, and its encoded amino acid sequence is shown in SEQ ID NO.2. This technical solution can solve the technical problem that existing types of 7α-hydroxysteroid dehydrogenases cannot meet the needs of large-scale production due to unsatisfactory enzyme activity and thermostability, and has ideal prospects for widespread application.

The invention belongs to the field of medicines for treating male infertility diseases, and discloses application of 12-ketolithocholic acid (12-keto-LCA) in the aspect of improving sperm quality decline, namely application of 12-keto-LCA in preparation of medicines for improving sperm quality decline. The invention provides a new application of 12-keto-LCA, reveals for the first time that 12-keto-LCA can support the spermatogenesis process, especially can improve the reproductive function of obese males, realizes the effects of improving testosterone secretion, repairing the spermatogenic function, improving the sperm quality and embryonic developmental ability and the like, and improves the condition that the sperm quality of mammals is reduced. The 12-keto-LCA can effectively relieve dyszoospermia of males, especially relieve damage of obesity to the reproductive function of males, and a new way is provided for developing drugs for improving the reproductive function of obese males.

The present invention provides a synthesis method for a 7-ketolithocholic acid or an intermediate thereof, which is prepared from a new intermediate I-1. According to the method, phytosterol degradation product bisnoralcohol is used as a starting material, and the 7-ketolithocholic acid or the intermediate thereof is obtained by means of an oxidation reaction, a Knoevenagel reaction (or wittig reaction), hydrogenation, a ketal protection reaction, an allylic oxidation reaction, ketal removal protection, and the hydrogenation. According to the method of the present invention, raw materials are easily available, the yield is high, reaction conditions are simple and mild, and the method is suitable for industrial production.

This invention provides a method for synthesizing 7-ketolithocholic acid or its intermediates, which is prepared via a novel intermediate I-1. The method uses phytosterol degradation product dichlorol as a starting material and proceeds through oxidation, Knoevenagel reaction (or Wittig reaction), hydrogenation, esterification, ketal protection, allylic oxidation, deketal protection, and hydrogenation to obtain 7-ketolithocholic acid or its intermediates. The method of this invention uses readily available raw materials, has high yield, and employs simple and mild reaction conditions, making it suitable for industrial production.

The utility model discloses a reaction kettle for producing lithocholic acid intermediates, which comprises a reaction shell, feeding pipes which are transversely and symmetrically distributed are arranged on the top wall of the reaction shell in a penetrating manner, and the reaction kettle further comprises a mixing mechanism, the mixing mechanism comprises a rotating shaft I, a connecting seat, a telescopic rod, a connecting frame, a stirring rod I, a rotating shaft II, a stirring rod II, a transmission assembly and a protection assembly. According to the device, the two groups of stirring elements are arranged in the device, so that the lithocholic acid intermediate raw material and the palladium-carbon catalyst in the device are uniformly mixed and stirred, and the mixing speed of the lithocholic acid intermediate raw material and the palladium-carbon catalyst is increased; the mixing speed of the lithocholic acid intermediate raw material and the palladium carbon catalyst is further improved, the generation of isomer impurities is reduced, and the preparation speed of the lithocholic acid intermediate is accelerated.

The invention discloses application of mussel plasmalogen in preparation of a product for improving activity of lithocholic acid synthase. The mussel plasmalogen comprises mussel plasmalogen phosphatidylethanolamine and / or mussel plasmalogen phosphatidylserine. The mussel plasmalogen comprises mussel plasmalogen phosphatidylethanolamine and The mussel plasmalogen promotes the biosynthesis of lithocholic acid by enhancing the activity of lithocholic acid synthetase, significantly reduces the content of a lithocholic acid synthesis precursor and significantly improves the lithocholic acid level.

The invention relates to an application of 7-ketolithocholic acid as a functional additive in stabilizing highly unsaturated grease, belongs to the technical field of grease antioxidation, and has the core technology that a known compound 7-ketolithocholic acid is developed into an efficient antioxidant for solving the industrial problem that highly unsaturated grease rich in DHA, EPA and the like is easy to oxidize. By utilizing the unique amphiphilic structure, the interface targeting anti-oxidation in an emulsion system is realized, and a synergistic interaction effect is generated with lecithin; meanwhile, the additive shows excellent stability under the conditions of microcapsule storage and 160-180 DEG C high-temperature frying, and can inhibit the generation of harmful aldehyde substances, thereby providing a brand new technical scheme for prolonging the shelf life of related grease products and improving the quality and safety.

The invention discloses a method for separating and identifying a microbial strain capable of catalyzing oxidation of 7-site hydroxyl of bile acid from animal intestinal tracts. The method comprises the following steps: carrying out multiplication culture on microorganisms separated from small intestines of pigs to obtain single colonies, and carrying out taxonomic identification on strains obtained by screening by utilizing 16S rRNA sequence alignment and genome sequencing analysis to determine that the strains are pseudomonas chlororaphis. The strain is applied to catalytic conversion of chenodeoxycholic acid, and 7-O-lithocholic acid is successfully obtained.