61 results about "Choleic Acid" patented technology

The invention belongs to the technical field of microorganisms, and particularly relates to bacillus cereus as well as a culture and application thereof. The preservation number of the bacillus cereus AK-LY1 is CCTCC (China Center For Type Culture Collection) NO: M 2025756. The bacillus cereus AK-LY1 disclosed by the invention is excellent in trypsin resistance, good in cholate resistance, acid resistance and high temperature resistance, good in inhibition performance on antibiotics such as strong penicillin and chloramphenicol, and relatively good in adhesion capacity in intestinal tracts, and provides a relatively good microecological preparation reference basis for expanding a bacillus cereus resource library and applying the bacillus cereus.

The application belongs to the field of neuropharmacology and medicine, and particularly relates to application of taurine cholic acid in preparation of a drug for preventing or treating Alzheimer's disease. Through animal model experiment verification, the A beta lateral ventricle injection is used to prepare an AD mouse model, and after oral administration of TCA for 2 weeks, cognitive behavior and pathological indexes are significantly improved.

The invention belongs to the technical field of detection and analysis, and provides an HPLC detection method for taurocholic acid in snake gall bulbus fritilariae liquid, which comprises the following steps: collecting chromatograms of a test sample and a reference substance through HPLC, and judging whether a co-outflow phenomenon exists or not; if the co-outflow phenomenon occurs, interference proportion analysis is carried out, and main interferents are identified; the judged main interferents are removed; carrying out retention analysis to obtain a taurocholic acid retention rate, judging whether the taurocholic acid retention rate accords with expectation or not based on the taurocholic acid retention rate, and if not, judging whether a trailing signal is triggered or not; if the trailing signal is triggered, performing cause analysis to determine the cause of triggering the trailing signal; when the optimal methanol proportion is obtained, a comprehensive detection signal is triggered; if the comprehensive detection signal is triggered, performing comprehensive adaptation analysis of the HPLC detection method to obtain an adaptation index, and evaluating the comprehensive performance of the HPLC detection method according to the adaptation index; and the accuracy of HPLC taurocholic acid detection is effectively improved.

The application provides a preparation method and application of a near-infrared two-region fluorescent sensor, and chiral single-walled carbon nanotubes are separated by using a double water phase extraction method; materials in the separation process include deionized water, polyethylene glycol, dextran, sodium dodecyl sulfate, sodium deoxycholate and cholic acid sodium hydrate; the chiral single-walled carbon nanotubes are dispersed and mixed with 4-nitrobenzene tetrafluoroboric acid diazonium salt to obtain the fluorescent sensor; high-purity (6,5)-SWCNT is efficiently and simply separated by using the double water phase extraction technology, the prepared SWCNT-NBD nanomaterial has good optical performance, including bright light emission in the near-infrared two-region, has good penetration capacity on biological tissues, the fluorescent detector (SWCNT-NBD) has low detection line, wide linear range, good selectivity on DA, and is convenient to prepare and low in cost.

The invention belongs to the technical field of biomedicine synthesis, and particularly relates to the technical field of chemical synthesis of natural drugs / prodrugs for controlling metabolic abnormalities such as blood sugar and blood fat. The invention provides a preparation method of a cholic acid derivative. The preparation method comprises the following steps: adding benzyl bromide into an alkaline solution containing cholic acid to obtain benzyl cholate; the method comprises the following steps: adding a dichloromethane solution containing acyl chloride into a dichloromethane solution containing benzyl cholate and 4-dimethylaminopyridine under protective gas to obtain a colorless oily product; and introducing hydrogen into the absolute ethyl alcohol in which the colorless oily product is dissolved to obtain the cholic acid derivative. The chemical synthesis of the cholic acid derivative is realized.

The invention belongs to the technical field of biochemical pharmacy, and particularly relates to a compound bezoar composition, decoction piece type compound bezoar and a preparation method of the decoction piece type compound bezoar. The compound calculus bovis composition provided by the invention comprises 94-96% by mass of main agents and 8 kinds of calculus bovis intermediates, the mass content of the auxiliary agent is 4-6%, and the auxiliary agent is six commercially available finished product combined cholic acid. The bilirubin content of the bezoar intermediate used in the invention is increased by more than 30% and the yield is increased by more than 25% compared with the existing biochemical reaction process of oxgall. The DPPH free radical scavenging rate of the compound bezoar composition reaches 89.6% + / -2.1% and is increased by 25.7-36.9% compared with 58.3% + / -3.5% of a product prepared from ox bile, and through t inspection, p is smaller than 0.01 (n is equal to 5). Free cholic acid intervention is strictly prohibited, lithocholic acid addition is completely eradicated, and the composition has the advantages of being high in bilirubin content, high in oxidation resistance and high in biological activity and adapts to the physiological characteristics of the human body.

The invention belongs to the technical field of fish and shrimp breeding feed additives, and particularly relates to a bile acid composition for fish and shrimp feed and a preparation method of the bile acid composition, and the composition comprises the following components in parts by weight: 50-60 parts of hyocholic acid, 40-55 parts of chenodeoxycholic acid, 40-60 parts of hyodeoxycholic acid, 30-45 parts of methionine glycine dipeptide and 60-115 parts of a compound plant extract. According to the invention, the methionine glycine dipeptide is used for improving the lipid metabolism capability of fishes and shrimps; the composite plant extract is used for enhancing the immunity and the anti-stress capability of the fish and the shrimps.

The application discloses a kind of 3-(cholic acid pentanoyl amide) cyclobutane-1,1-dicarboxylic acid purification method, belong to the technical field of pharmaceutical chemistry intermediate purification.The method includes: (1) its precursor diethyl ester is hydrolyzed in methanol and / or acetonitrile, concentrated after dissolving with water, with organic solvent extraction is discarded organic phase, water phase is adjusted to 2-4 to pH, again with organic solvent extraction, concentrated and obtained crude product;(2) the crude product is dissolved in alcohol solvent, after filtration, ester solvent is added to crystallize, alcohol ester volume ratio 1:2-1:10, filtration, washing, drying.The application removes unreacted ester, monocarboxylic acid byproduct and cholic acid analogue amide and other impurities by alkaline hydrolysis combined with "alkali dissolving acid extracting" and "alcohol dissolving-ester crystallizing" recrystallization.The product obtained by the method has HPLC purity ≥98.2%, yield ≥80%, and the process is stable, simple to operate, suitable for large-scale production.

The application provides a paclitaxel molecular umbrella delivery system prodrug, a preparation method and application thereof. The paclitaxel molecular umbrella delivery system prodrug comprises a molecular umbrella target head part composed of two surface amphiphilic molecules connected by spermidine, a paclitaxel drug part, and a connecting group connecting the molecular umbrella target head part and the paclitaxel drug part through a disulfide bond; wherein the surface amphiphilic molecule is selected from cholic acid, deoxycholic acid or a sodium sulfonate thereof. Compared with paclitaxel, the paclitaxel molecular umbrella delivery system prodrug has significantly improved water solubility, lower toxicity to normal cells than free paclitaxel, and significantly improved safety; and the paclitaxel molecular umbrella delivery system prodrug has the following characteristics in a physiological environment: releasing active drugs in the high GSH / ROS microenvironment of tumor cells; and maintaining a prodrug state in normal cells.

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.

This invention discloses an evaluation method for bile acids in alleviating intestinal inflammation in grouper, belonging to the field of aquaculture technology. Addressing the intestinal inflammation problem caused by feed oxidation, pathogen infection, or water quality deterioration in intensive grouper farming, this invention proposes to achieve efficient regulation of intestinal health by adding a compound bile acid composition to the feed. The core technical solution of the method is as follows: a compound bile acid is formed by compounding porcine deoxycholic acid, chenodeoxycholic acid, and porcine cholic acid in a specific ratio, combined with a carrier premixing process to prepare a bile acid premix, which is then added to the basal feed at 0.15%-0.60% of the total feed mass. This invention effectively alleviates enteritis symptoms in grouper by enhancing the integrity of the intestinal epithelial structure, repairing damaged mucosal barriers, regulating inflammatory responses, and optimizing intestinal flora composition. It provides a safe and efficient technical solution for replacing feed antibiotics in aquaculture, with significant economic and ecological benefits.

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 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 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.

The invention provides an identification method of a compound Pien Tze Huang ointment, and belongs to the technical field of medicines. According to the method, the preparation method of the test solution is improved, the concentration operation after filtration in the existing method is omitted for the first time, the operation steps are simplified, and the defects that in the prior art, when cholic acid and deoxycholic acid in the compound Pien Tze Huang ointment are identified, sample application is not prone to occurring, spots are smeared, and judgment is affected are overcome. The improved method is easy in sample application, good in map separation degree, clear and easy in spot distinguishing, feasible through methodology verification, and capable of being used for identifying cholic acid and deoxycholic acid in the compound Pien Tze Huang ointment. The product quality control level is improved, the positive influence on the product quality guarantee is achieved, and the positive effect on the safety and effectiveness of clinical medication is achieved.

The present disclosure provides a liquid formulation comprising: (a) RK-33, (b) cholic acid or derivative thereof, (c) a water-soluble polyvinyl polymer, and (d) water. The disclosure also provides a method of making a liquid formulation comprising RK-33. The disclosure further provides a method of treating cancer in a subject in need thereof, the method comprising (a) diluting the formulation of the present disclosure to form a diluted formulation, and (b) intravenously administering to the subject the diluted formulation.

The invention provides a liver cancer early warning and risk assessment method based on intestinal microbiome, and relates to the technical field of medical auxiliary analysis, by collecting excrement and plasma samples of high-risk groups and combining 13C-cholic acid dynamics, functional gene abundance and intestinal barrier indexes, a multi-modal risk score is calculated, and dynamic monitoring is realized through longitudinal CUSUM. When the risk index exceeds a threshold value, the system can give out an early warning to assist iconography review and personalized intervention. According to the method, high-risk individuals of liver cancer can be identified in serum AFP and iconography unabnormal stages, early intervention and follow-up visit optimization are achieved, prediction sensitivity is high, interpretability is high, and the method is suitable for high-risk groups of HBV / liver cirrhosis and metabolic liver diseases and has remarkable clinical application value and generalizability.

The present application relates to an exosome fusion liver-targeting liposome drug delivery system and its preparation method and application, and belongs to the field of polymer materials and pharmaceutical preparations. The present application discloses an exosome fusion liver-targeting liposome drug delivery system, which uses high-concentration PEG 8000 and Nycodenz in combination to synergistically improve the exosome and liposome fusion efficiency, form biomimetic vesicles with uniform size and high drug loading. The exosome not only can play the characteristics of anti-inflammatory and antioxidant, but also plays a role in resisting harsh gastrointestinal environment and crossing biological barriers. In addition, the liposome is modified by cholic acid derivative by using EDC / NHS mediated amidation reaction, which realizes precise targeting of liver and sufficient accumulation in liver. The above-mentioned effects synergistically realize the treatment of type II diabetes and non-alcoholic fatty liver disease.

The invention discloses an injectable gel-state composition with local fat reduction and drug sustained release effects as well as preparation and application of the injectable gel-state composition. The injectable gel-state composition consists of the following components in percentage by mass: 5-50% of phospholipid, 0.4-10% of cholic acid derivatives and / or salts thereof, 0-5% of divalent metal salt, 0-10% of amino acid and / or salts thereof, 0-10% of cholesterol and the balance of water, the stable hydrogel is formed by constructing a three-dimensional network structure by using phospholipid, cholic acid derivatives and / or salts thereof and water. The injectable gel-state composition is prepared by mixing a simple lipid and a water phase, and is simple to operate and environment-friendly. The injectable gel-state composition can be used as a gel-state carrier for delivering active substances (various fat-soluble and water-soluble drugs) or used for preparing injectable gel-state composition preparations loaded with the active substances, and can also be used as or used for preparing drugs with local fat reduction effects for local fat reduction for medical and / or cosmetic purposes. The application range is wide.

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 application discloses a method for reducing the lipid content of oocytes or improving the cryopreservation survival rate of oocytes, and comprises the following steps: (1) preheating an incubation solution; and incubating oocytes in the preheated incubation solution; (2) freezing and thawing the incubated oocytes; wherein the incubation solution is prepared by adding bezafibrate and cholic acid to a culture medium 199 containing 10wt% fetal bovine serum. The incubation solution used in the method provided by the application can significantly reduce the lipid content of oocytes or improve the cryopreservation survival rate of oocytes, compared with the conventional culture medium 199 containing 10wt% fetal bovine serum, because the added bezafibrate and cholic acid have a synergistic lipid-lowering effect. The application has application prospects in reducing the lipid content of oocytes or improving the cryopreservation survival rate of oocytes.

The invention discloses application of a compound rohdea japonica capsule in preparation of a medicine for preventing pulmonary fibrosis, belongs to the technical field of medicines, and finds that the compound rohdea japonica capsule can inhibit a TGF-beta / Smad3 / Arg-1 signal channel, reduce the content of proinflammatory factors IL-6, TNF-alpha and pulmonary hydroxyproline and increase an anti-inflammatory factor IL-10; meanwhile, according to the invention, the intestinal flora structure is remodeled, key metabolites such as 6-ketoprost, 1-oleoyl-SN-glycerol-3-phosphorylcholine and cholic acid are callback, and core pathways such as arachidonic acid metabolism, glycerophospholipid metabolism and bile acid metabolism are involved; the mechanism of preventing and treating pulmonary fibrosis by improving the metabolic homeostasis of the host is clarified from the microorganism-metabolic axis level.

The application belongs to the technical field of pharmaceutical preparations, and particularly relates to a cholic acid oral composition and a preparation method and application thereof. According to weight parts, the cholic acid oral composition comprises the following components in parts by weight: cholic acid 90-110 parts, a polymer carrier 100-300 parts, a stabilizer 60-200 parts, a filling agent 100-200 parts, a disintegrating agent 10-30 parts and a lubricant 1-5 parts; the stabilizer comprises vitamin E polyethylene glycol succinate and sulfobutyl ether-beta-cyclodextrin. The application significantly improves the dissolution effect by adopting polymer solid dispersion, cyclodextrin inclusion and surfactant micelle solubilization, and the dissolution rate can reach more than 85% in 30 minutes.

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.

This invention belongs to the fields of medicinal chemistry and organic synthesis, specifically relating to a stable 3-aminocyclobutane-1,1-dicarboxylic acid diethyl oxalate and its application in the preparation of 3-(cholate-valerate)cyclobutane-1,1-dicarboxylic acid. This invention effectively solves the technical bottlenecks of poor stability, difficulty in purification, and storage by converting unstable free 3-aminocyclobutane-1,1-dicarboxylic acid diethyl oxalate into a specific organic acid salt form. More importantly, this invention discovers that this organic acid salt can be directly used as a reaction intermediate, and can be used efficiently in subsequent amide condensation reactions with cholic acid or its active derivatives without the separation of free amines. This method significantly improves the purity and yield of the key intermediate and its downstream product 3-(cholate-valerate)cyclobutane-1,1-dicarboxylic acid. The process is stable and simple to operate, providing a stable, controllable, and economical preparation route for the industrial production of 3-(cholate-valerate)cyclobutane-1,1-dicarboxylic acid, a key active pharmaceutical ingredient in the liver cancer prodrug LLC-202.

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 application provides a Qingkailing composition, Qingkailing tablets, a preparation method and application thereof, and belongs to the technical field of traditional Chinese medicine preparations.The Qingkailing composition provided by the application comprises the following components: cholic acid, hyodeoxycholic acid, a Scutellaria baicalensis Georgi-Cortex Ilicis Latani extract, a nacre extract, an elephant-foot coral extract, Isatidis radix, Honeysuckle, dextrin, magnesium stearate and corn starch.Through optimization of the extraction process of Scutellaria baicalensis Georgi and Cortex Ilicis Latani, the anti-inflammatory effect of the obtained Scutellaria baicalensis Georgi-Cortex Ilicis Latani extract is significantly improved.The Qingkailing tablets prepared by the application have good tablet stability and uniformity of baicalin content.

The invention discloses mink gallbladder eye drops and preparation thereof. The eye drops comprise a composition for protecting cornea, and the preparation method of the eye drops comprises the following steps: adding a mink bile total cholic acid extract and carnosine powder into an ethanol water solution, heating for dissolving, filtering, and concentrating and drying the obtained filtrate to obtain the eye drops. According to the eye drops, corneal epithelial cell injury is repaired, corneal epithelial cell hyaluronic acid secretion is promoted, and therefore eye dryness and fatigue can be relieved, and cornea can be effectively protected.

The present application provides a kind of micro tablet, it includes the compound shown in formula I, filler and optionally pharmaceutically acceptable adjuvant, wherein, the diameter of the micro tablet is 1 ~ 3mm, the ratio of diameter and thickness is 0.6 ~ 1.2, the tablet weight is 2.5 ~ 10mg, and includes 1 ~ 5mg compound shown in formula I.The present application also provides the preparation method and pharmaceutical use of the micro tablet.The micro tablet of the present application can realize small dose direct precision dosing, easy to use;It is easy to swallow, can effectively improve the problem of poor palatability of cholic acid drugs, improve medication compliance;It can realize the effect of consistent dissolution characteristics of different doses, ensure the stability of treatment effect under different doses;It can reduce the use of adjuvant, avoid the safety problem of children medication;High stability, conducive to storage and transportation, improve the safety of use;High bioavailability, can more effectively realize in vivo absorption and utilization;Effectively solve the content uniformity problem, reduce the difficulty of process, more suitable for industrial production.