45 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 invention belongs to the field of biology, discloses a variant of 7 alpha-hydroxysteroid dehydrogenase, and aims to improve the catalytic efficiency and stability of catalyzing chenodeoxycholic acid (CDCA) to be converted into UDCA precursor 7-ketolithocholic acid, and particularly, the variant is obtained by carrying out single mutation or multipoint combined mutation on the 93th site, the 94th site, the 96th site, the 146th site, the 150th site, the 155th site, the 188th site, the 189th site, the 190th site, the 195 site, the 195th site, the 196th site, the 196th site, the 195th site, the 195th site, the 195th site, the 196th site, the 199th site, the 200th site, the 204th site and the 249th site

The invention discloses a biomarker composition for predicting the biological age or aging state of an individual, and the biomarker composition comprises tetracosyl saturated fatty acid / tetracosyl monounsaturated fatty acid phosphatidylcholine (PC 24: 0 / 14: 1), cysteine-glycine-cysteine tripeptide (Cys-Gly-Cys), cysteine-glycine-cysteine tripeptide (Cys-Gly-Cys), cysteine-glycine-cysteine tripeptide (Cys-Gly-Cys), cysteine-glycine-cysteine tripeptide (Cys-Gly-Cys), cysteine-glycine-cysteine tripeptide (Cys-Gly-Cys), cysteine-glycine- The invention relates to a pharmaceutical composition for the preparation of a pharmaceutical composition, which comprises the following components in parts by weight: 20: 0 / 22: 5, 20 / docosapentaenoic acid monohexosyl sphingosine amide (HexCer 20: 0 / 22: 5), trigonelline, lithocholic acid glycine (Lithocholic acid glycine), and octadecanoic saturated fatty acid / octadecanoic monounsaturated fatty acid phosphatidylcholine (PC 18: 0 / 18: 1). The biomarker can be used for accurately characterizing the aging state of an organism, and provides a strategy for early screening, intervention evaluation, accurate health management and the like of related diseases of the elderly.

The present invention addresses the problem of providing a novel rodenticide. According to the present invention, there is provided a rodenticide comprising a compound represented by general formula (I), a salt thereof, or a prodrug thereof. (In the formula, R1 and R2 each independently represent a hydrogen atom or an alkyl group having 1-8 carbon atoms; n represents an integer of 1-3; R3, R4, R5, and R6 each independently represent a hydrogen atom or an alkyl group having 1-6 carbon atoms; X represents COOH, -C(=O)NH-Z, -CH(OH)-(Y)m-CH(OH)R7, -NH-CO-O-R10, -CO-O-R10 or -NH-CO-N(R11)-R10; Z represents a hydrogen atom, -CN, an alkyl group having 1-8 carbon atoms, an alkoxyl group having 1-8 carbon atoms, or a hydroxyl group; Y represents -C(R8)(R9)-, -C(=O)-, or -C(=CH2)-; m represents an integer of 0-3; R7, R8, and R9 each independently represent a hydrogen atom or an alkyl group having 1-8 carbon atoms; each of alkyl groups having 1-8 carbon atoms which are respectively represented by Z, R7, R8 and R9 may have a substituent selected from a carboxyl group and a hydroxyl group; and R10 and R11 each independently represent a hydrogen atom or an alkyl group having 1 to 8 carbon atoms which may 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 discloses a 7alpha-hydroxysteroid dehydrogenase mutant and application thereof in preparation of ursodesoxycholic acid, the enzyme mutant is obtained by mutating a wild type amino acid sequence as shown in SEQ ID NO: 1 through Q31A, H72Q, W111R or A178R, the mutated enzyme activity is high, 7-ketolithocholic acid can be prepared based on catalysis of a high-concentration substrate, and the 7alpha-hydroxysteroid dehydrogenase mutant can be applied to preparation of ursodesoxycholic acid. And the method has a significant meaning for industrial preparation of ursodesoxycholic acid under catalysis of the propulsor.

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 relates to a bile acid mixture in the field of food nutrition supplements and medicines, the bile acid mixture comprises Taurohycholic acid, Taurohycholic acid, Hyocholic acid, Taurohycholic acid, Taurohycholic acid, Taurohycholic acid, Glycholic acid, Chocholic acid, Glycholic acid, 7-Ketoithocholic acid, Glycholic acid and Lithocholic acid, and the bile acid mixture can be used for preventing and treating obesity.

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.

The application discloses a cytochrome P450 enzyme mutant derived from Streptomyces and application of the cytochrome P450 enzyme mutant in synthesis of ursodeoxycholic acid, wherein the cytochrome P450 enzyme mutant is obtained by single mutation or multiple mutations of positions 181, 192, 249 or 288 of the amino acid sequence shown in SEQ ID NO. 2. The cytochrome P450 enzyme mutant has higher activity and regional selectivity, and can use cheap lithocholic acid as a substrate, and hydroxylate 7beta of the substrate by using the high-efficiency cytochrome P450 enzyme to synthesize ursodeoxycholic acid in one step, thereby greatly reducing the industrial production cost, and having a good application prospect in industrial production of ursodeoxycholic acid.

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 utility model relates to the field of 7-ketolithocholic acid, in particular to 7-ketolithocholic acid filtering equipment which comprises a filtering box body, a filtering cavity is formed in the filtering box body, a mounting box body is arranged in the filtering cavity, an L-shaped connecting rod is arranged on one side of the mounting box body, and a limiting groove is formed in one side of the interior of the filtering box body. A clamping groove is formed in the inner side edge of the mounting box body, and a containing box is arranged in the clamping groove of the mounting box body. According to the ketolithocholic acid and sulfuric acid filtering device, firstly, the containing box is arranged in the mounting box body through the sealing clamping block, then the mounting box body is clamped in the filtering box body through the L-shaped connecting rod, a ketolithocholic acid solution and a sulfuric acid solution are poured into the filtering cavity, and the ketolithocholic acid and the sulfuric acid solution are filtered out through dislocation of the liquid leakage holes and the liquid seepage holes; the filter screen is arranged in the filter box body, so that a mixed solution can be quickly fused to generate precipitate, the mixed solution can be quickly discharged through the drain hole in the side edge of the filter box body, and the precipitate is left on the filter screen, so that the precipitate is convenient to collect and subsequent filtering and refining operation is facilitated.

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.

To provide new lithocholic acid derivatives with sufficient vitamin D3 activity.SOLUTION: The invention provides a compound represented by the general formula (I) in the figure, a salt thereof, or a prodrug thereof. (In the formula, R1 and R2 each independently denote a hydrogen atom or an optionally substituted C1-8 alkyl group; X denotes -O- or -NR4-; R3 and R4 each independently denote a hydrogen atom or an optionally substituted C1-8 alkyl group.)SELECTED DRAWING: None

The invention discloses application of bacteroides fragilis in preparation of a medicine for preventing and / or treating porcine intestinal coronavirus infection. The research finds that bacteroides fragilis hydrolyzes bound bile acid through bile salt hydrolase (BSH) to generate free bile acid (such as lithocholic acid LCA and deoxycholic acid DCA), so that an antiviral effect is generated. The bacteroides fragilis can regulate bile acid metabolism through BSH enzyme activity to inhibit virus infection, which indicates that the bacteroides fragilis can be used for preventing or treating porcine intestinal coronavirus infection.