58 results about "Active metabolite" patented technology

The invention discloses application of a plant lactobacillus CCFM1357 to conversion of anthocyanin to generate various active metabolites, inhibition of a cGAS-STING pathway and enhancement of improvement of brain aging, and belongs to the technical field of microorganisms and the technical field of medicines. The phytobacterium plantarum CCFM1357 fermented anthocyanin and the compound preparation thereof provided by the invention have the following effects: (1) a marker for relieving D-gal induced mouse brain senescence and a marker for relieving D-gal induced mouse brain senescence; (2) promoting and relieving D-gal induced mouse histopathologic characterization; (3) relieving D-gal induced mouse neuroinflammation; (4) relieving behavioral characterization of the D-gal induced aging mouse; and (5) a cGAS-STING signal channel is inhibited. The phytobacterium plantarum CCFM1357 fermented anthocyanin and the compound preparation thereof provided by the invention can be used for a product for relieving brain aging, and have a huge application prospect.

The invention relates to the technical field of medicines, and discloses an application of combination of bufalin and heme in preparation of a cancer treatment medicine. According to the invention, by means of an active metabonomics means, a key active metabolite-heme is locked through exogenous library screening and endogenous analysis, and the drug effect of bufalin is regulated by means of the active metabolite. Through verification, it is found that heme can cooperate with the synergistic drug effect in various cancer cell lines, and a new technical normal form based on an active metabolome for improving the drug effect of bufalin is provided. The pharmaceutical composition can improve the apoptosis induction ability of bufalin to different cancer cells, and provides powerful guiding significance for developing a novel treatment scheme in clinical medicine.

The present application relates to the field of traditional Chinese medicine, in particular to a composition, eye patch and preparation method thereof for preventing and treating eye dryness, blurred vision fatigue and dry eye, comprising a carrier vehicle and a matrix layer, selecting medicinal materials with the effects of improving eyesight and resisting oxidation, fermenting the medicinal materials with plant lactic acid bacteria, bacillus or yeast to decompose macromolecules into small molecule active substances and possibly produce new active metabolites, adopting temperature control during the fermentation process to avoid high temperature from destroying heat-sensitive components, compounding the fermented medicinal material extract with hyaluronic acid, menthol, carboxymethyl cellulose and glycerol to form an intelligent rheological regulation body, hyaluronic acid synergistically enhances the moisturizing effect with the fermented extract, carboxymethyl cellulose serves as a film-forming agent to ensure the stability of the matrix layer, and glycerol improves the moisturizing performance, adopting a green process of activation, fermentation, mixing, loading and sterilization, selecting plant fibers as the carrier vehicle, cutting and packaging after loading the matrix layer, and then sterilizing to ensure the safety and effectiveness of the product.

This invention provides a method for treating a pulmonary arterial hypertension with reduced incident of side effect using a controlled release pharmaceutical composition of selexipag or its active metabolite, wherein the controlled release pharmaceutical composition of selexipag or its active metabolite following oral administration with an alcoholic beverage reduces incidence of at least one side effect associated with the selexipag or its active metabolite compared to the immediate-release dosage form comprising the same amount of the selexipag or active metabolite thereof.

The invention discloses a strain of parateratomycosis aveosphaeroides and application thereof, and belongs to the technical field of microorganism and biological prevention and control. In order to screen new species of fungi and provide alternative strains for application of plant beneficial bacteria in agriculture, a fungus SGSF1293 is separated, and the fungus SGSF1293 is identified to be a new species of the cystis clavatum and is named as the parateratosis aveoensis, and the new species of the cystis clavatum is named as the parateratosis aveoensis. According to the present invention, the activity research results show that the strain SGSF1293 has rice root-knot nematode killing activity, plant pathogen resistance (Brassica oleracea black rot xanthomonas, Pseudomonas syringae, Ralstonia solanacearum and Fusarium oxysporum) resistance, oxidation resistance and phosphorus solubilizing activity; besides, the secondary metabolite of the strain is separated and identified, two active compounds, namely, wintergreen ambrotic acid and brefeldin A, are separated, and the wintergreen ambrotic acid has the activity of killing rice root-knot nematode. The discovery of the strain SGSF1293 and the active metabolite thereof has certain application value in the agricultural fields of plant disease control and the like.

Fatty acids with one or more unsaturations and an odd-numbered hydrocarbon chain are described, wherein these fatty acids have the chemical structure of the therapeutically active metabolites of alpha-hydroxylated mono- or polyunsaturated fatty acids with an even-numbered chain. The compositions comprising these fatty acids, their medical uses, and their use as indicators of a patient's efficacy and / or response to treatment with the alpha-hydroxylated mono- or polyunsaturated fatty acids with an even-numbered chain from which they are derived are also described.

The invention belongs to the technical field of medicines, and relates to a compound as shown in a formula I, a stereoisomer, a prodrug and a pharmaceutically active metabolite thereof, pharmaceutically acceptable salt, a solvate and a hydrate thereof, a pharmaceutical composition containing the compound, and application of the compound in preparation of medicines for preventing and / or treating diseases or symptoms related to virus infection.

The invention discloses a lactobacillus paragasseri strain capable of converting anthocyanin to generate various active metabolites, inhibiting NF-kappa B and cGAS-STING signals and enhancing inflammatory response relieving, and belongs to the technical field of microorganisms and the technical field of medicines. The lactobacillus paragasseri CCFM1499 provided by the invention can be used for converting anthocyanin into various active substances such as homovanillic acid, cyanidin, 3 ', 4'-dihydroxyphenylacetic acid and the like; fermentation supernate obtained by fermenting anthocyanin through the lactobacillus paragasseri CCFM1499 has the following effects: (1) the capability of reducing inflammatory factors of cells is achieved; (2) the cell senescence phenotypic capability is relieved; (3) the cGAS-STING signal channel capability is inhibited; and (4) inhibiting the NF-kappa B signal path capability. The lactobacillus paragasseri CCFM1499 fermented anthocyanin provided by the invention can be used for preparing a product for relieving inflammatory response, and has a huge application prospect.

This disclosure provides the use of valbenazine, its active metabolites, or pharmaceutically acceptable salts thereof in the preparation of megakaryocytes, wherein the preparation of megakaryocytes is carried out in vitro. The valbenazine, its active metabolites, or pharmaceutically acceptable salts thereof in this disclosure can promote megakaryocyte proliferation and platelet production, providing a promising strategy for megakaryocyte proliferation and platelet production.

The present invention provides compounds of formula (I) and / or salts thereof and / or biologically active metabolites thereof and / or prodrugs thereof and / or solvates thereof and / or hydrates thereof and / or polymorphs thereof having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 and act as GABAA α5 positive allosteric modulators, thereby useful in the treatment or prevention of diseases related to the GABAA α5 receptor, process for the preparation and intermediates of the preparation process thereof, pharmaceutical compositions comprising them alone or in combination with one or more other active ingredients and their use as medicaments.

The invention discloses a lactobacillus paracasei capable of converting anthocyanin to generate various active metabolites and enhancing the effect of relieving cognitive impairment and neuroinflammation, and belongs to the technical field of microorganisms and the technical field of medicines. The lactobacillus paracasei CCFM1497 obtained through screening is combined with anthocyanin intake in animal experiments, and by inhibiting a cGAS-STING signal channel, brain inflammatory response of senescence individuals is effectively relieved, senescence-related cognition and behavior degeneration performance is improved, and brain senescence is delayed. The lactobacillus paracasei CCFM1497 fermented anthocyanin and the compound preparation thereof provided by the invention can be used for products for relieving cognitive impairment and neuroinflammation, and have a huge application prospect.

The present invention provides compounds of formula (I) and / or salt thereof and / or biologically active metabolite thereof and / or prodrug thereof and / or solvate thereof and / or hydrate thereof and / or polymorph thereof having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 and act as GABAA α5 negative allosteric modulators, thereby useful in the treatment or prevention of diseases related to the GABAA α5 receptor, process for the preparation and intermediates of the preparation process thereof, pharmaceutical compositions comprising them alone or in combination with one or more other active ingredients and their use as medicaments.

The invention discloses a two-way positioning release sustained-release pharmaceutical composition and a preparation method thereof, the pharmaceutical composition is a double-layer tablet, and the double-layer tablet comprises an upper-layer tablet and a lower-layer tablet. The upper-layer tablet is a slow-release intragastric positioning release preparation part and contains 1 / 3 marked amount of active ingredients; the lower-layer tablet is a quick-release gastrointestinal tract release preparation part and contains 2 / 3 labeled amount of active ingredients. A new preparation technology and a new dosage form are adopted, the lower-layer tablet in the double-layer tablet can enable the medicine to be rapidly disintegrated in the stomach, the disintegrated medicine forms a particle dispersion, and the particle dispersion can be rapidly emptied by the stomach to enter the intestinal tract, so that the absorption of the medicine is promoted; the upper-layer tablet floats in the stomach after absorbing water, then the medicine is slowly dissolved out, the medicine dissolved out of the preparation can be metabolized into active metabolite OP-1118 in an acid environment in the stomach, then the active metabolite OP-1118 is absorbed through the gastrointestinal tract, and part of the medicine can be absorbed immediately after uniformly and slowly entering the intestinal tract, so that the bioavailability is improved.

The present invention relates to a composition comprising a) at least one biological control agent which is a fungicidally active bacterium and / or a fungicidally active metabolite produced by the respective bacterium and b) one or more fatty acids or derivatives thereof selected from unsaturated and saturated C12-24 fatty acids, salts thereof, esters thereof or mixtures of any of the foregoing as well as methods of using this composition and related uses.

The invention discloses a Lactobacillus paracasei 1029 and application thereof, the preservation number of the Lactobacillus paracasei 1029 is CCTCC (China Center for Type Culture Collection) NO: M20251441, and the Lactobacillus paracasei 1029 is preserved in the China Center for Type Culture Collection on June 23, 2025. The fermentation product contains a plurality of active metabolites, such as pyruvic acid, pantothenic acid, proline and leucine, and the components synergistically enhance the effects of oxidation resistance, bacteriostasis and cell melanin inhibition. Compared with the prior art, the fermented product disclosed by the invention realizes integration of multiple effects, is high in safety (free of cytotoxicity) and simple in preparation process (standing for 6 days at 30 DEG C, filtering, centrifuging, freezing and drying), has wide application prospects including food additives, health-care products, cosmetics and pharmaceutical preparations, and can remarkably improve the bioavailability and market competitiveness of products.

The present application relates to the technical field of probiotic composition, and discloses a bacterial agent for regulating vaginal microbial flora and a preparation method thereof, which comprises the following steps: preparing Lactobacillus paracasei KFY202407 powder into a seed solution; performing segmented fermentation culture on the seed solution; obtaining bacterial slurry after centrifugal enrichment of the fermentation product; mixing the bacterial slurry with a composite freeze-drying protective agent and then performing freeze-drying to obtain freeze-dried bacterial powder; and performing gelatinization treatment on the freeze-dried bacterial powder to obtain the bacterial agent. The present application realizes rapid proliferation of bacterial cells and promotes accumulation of active metabolites by adopting a two-stage fermentation process of liquid-state fermentation followed by solid-state fermentation, thereby solving the technical problems of low active bacterial proliferation efficiency and insufficient metabolites in the prior art. Meanwhile, the present application adopts a freeze-drying process of two-stage pre-freezing and drying sublimation, so that ice crystals are removed in the form of sublimation instead of melting, thereby solving the technical problem of bacterial cell damage and uncontrollable inactivation due to ice crystals in the traditional freeze-drying technology.

A method for treating patients with NOTCH3 mutations using a rho kinase inhibitor has been disclosed. Abnormal NOTCH3 signaling is a pathological factor in cerebral small vessel diseases, including CADASIL. A preferred embodiment relates to treating patients orally with the rho kinase inhibitor fasudil or its active metabolite hydroxyfasudil.

The present invention relates to a thioether compound having soft drug properties, and a pharmaceutical composition and use thereof. The compound has a structure of formula I. The thioether structure of the compound of the present invention has pharmacological activity, and after exerting pharmacological effects, it is rapidly converted into sulfoxide and sulfone metabolites that do not have pharmacological activity according to an established metabolic pathway, so that it can be achieved that the toxicity of prototype drugs, active metabolites and reactive metabolites to a body is avoided while exerting therapeutic effects, and the safety is relatively higher

The invention discloses lactobacillus paracasei AUQAVATE-5, and the preservation number of the lactobacillus paracasei AUQAVATE-5 is CGMCC (China General Microbiological Culture Collection Center) No.36510. The lactobacillus paracasei The invention also discloses a method for preparing the camellia oil by using the lactobacillus paracasei AUQAVATE-5. The invention also discloses an application of the lactobacillus paracasei AUQAVATE-5 in preparation of a skin repair product. The invention also discloses an application of the lactobacillus paracasei AUQAVATE-5 in fermentation of oils to increase the content of monoglyceride. According to the invention, the camellia oil is directly fermented by using a single lactobacillus strain so as to increase the content of monoglyceride and enhance the repairing function, the process is simple, the strain is safe, and the method is easy to control and realize large-scale production; monoglyceride is increased to an effective functional concentration, and active metabolites such as lactic acid and the like are synergistically enriched; food-grade raw materials and safe strains are used in the whole process, and the product is mild.

The invention provides an antimycotic polyene-alginate oligomer conjugate comprising an antimycotic polyene connected covalently to at least one alginate oligomer, wherein one or other terminal uronic acid residues of each alginate oligomer in the conjugate is connected to the antimycotic polyene via a direct covalent bond or a covalent molecular linker, or a pharmaceutically acceptable salt, solvate, hydrate, diastereoisomer, tautomer, enantiomer, or active metabolite thereof. Also provided are methods for the preparation of said conjugate, pharmaceutical compositions comprising said conjugate and the use thereof in a method for the treatment or prevention of a fungal infection in a subject with, suspected to have, or at risk of, a fungal infection.

The invention relates to the technical field of biology, in particular to application of Erythritol in preparation of a medicine for treating diabetic retinopathy. According to the application, angiogenesis in the diabetic retinopathy process is relieved by a method of inhibiting ferroptosis through the active metabolite Erythrotol, and from the perspective of metabonomics, it is found for the first time that the metabolite Erythrotol inhibits ferroptosis by regulating the activity of ACSL4, the angiogenesis is relieved, and the DR process is delayed. The Erythritol is convenient to extract, high in stability, remarkable in pharmacological action, small in molecular weight and high in stability, has the characteristics of good bioavailability, effective antioxidant activity, easiness in clinical transformation and the like, and is expected to become an ideal choice for treating many diseases. Based on the various advantages, new treatment thinking and targets can be provided for diagnosis and treatment of DR.

The invention discloses a formula of a fermented feed for enhancing animal immune function, and relates to the technical field of fermented feeds. The formula comprises the following components in parts by mass: a basic raw material, an immune enhancement extract, a functional additive, 0.3-0.6 part of a composite microbial agent and 2-4 parts of composite mineral substances. Wherein the ganoderma lucidum extract and the folium cortex eucommiae extract activate immune cells through the synergistic effect of polysaccharide and chlorogenic acid; the complex microbial inoculant is composed of lactobacillus acidophilus, bacillus licheniformis and candida utilis according to a ratio of (5-6): (3-4): 2, efficiently degrades antinutritional factors and generates immunocompetence metabolites. The preparation process comprises the following steps: supercritical extraction of plant active components, mixing and humidifying of base materials, segmented stirring and fermentation after microbial inoculum activation, and then addition of functional components and drying. Through synergistic combination of the raw materials and process optimization, the animal immunity is remarkably improved, and the feed additive has the advantages of low cost and multiple immune enhancement mechanisms.

The invention discloses application of a miR-6809-5p inhibitor, and belongs to the technical field of biological medicine.The inventor finds that expression of miR-6809-5p in plasma of a PD patient is abnormally increased in the research of PD pathogenesis, and further cell experiments find that the expression of miR-6809-5p is abnormally increased in the plasma of the PD patient. By inhibiting the expression of the miR-6809-5p, the adverse effects of MPP + on cell viability, apoptosis, ROS, p-alpha-syn and TH protein can be effectively improved, and the miR-6809-5p has a remarkable treatment effect on PD. MPP + is an active metabolite of neurotoxin MPTP, can be selectively absorbed by dopaminergic neurons through dopamine transporter (DAT) protein to trigger degeneration death of the dopaminergic neurons, and is widely applied to construction of PD cell models to research pathogenesis of PD and drug evaluation. The miR-6809-5p inhibitor disclosed by the invention is used for preparing a medicine for treating the Parkinson's disease, and the nucleotide sequence of the miR-6809-5p inhibitor is as follows: UGAUCCUUUCUUUCCUUGCCA.

Compositions and methods are disclosed herein for inducing (up-regulating) the expression of sulfotransferases in the hair follicles, e.g., the scalp. Increasing sulfotransferase is beneficial for metabolizing pro-drugs that require sulfonation to be activated, e.g., minoxidil sulfate is the active metabolite of minoxidil. A method for combining the compositions described herein with topical minoxidil to enhance minoxidil treatment for androgenetic alopecia is described. Additional methods and compositions include the use of retinoid X receptor agonists, retinoic acid receptor agonists, and nuclear receptor agonists in an RXR-NR heterodimer. Additional methods and compositions include the use of a topical solution containing an alkalinizing agent or an alkalinizing agent used with a penetration enhancer for up-regulating the sulfonating capacity of hair bearing skin, hair follicles, and / or keratinocyte cells. In addition, compositions and methods for increasing or decreasing the growth rate of hair follicles is disclosed by altering the intracellular pH. Additionally, methods for preparing a stable liposomal containing solution are described.

This invention belongs to the field of pesticide residue detection technology, specifically relating to a method for detecting flufenoxuron and its active metabolites in plant-derived foods. The detection method includes: mixing and shaking the plant-derived food to be tested with a formic acid-acetonitrile solution; mixing and shaking the resulting mixture with sodium chloride and magnesium sulfate, followed by solid-liquid separation to obtain an extract; purifying the extract by mixing it with 10-30 nm multi-walled carbon nanotubes, followed by solid-liquid separation to obtain a test solution; and performing liquid chromatography-mass spectrometry (LC-MS) on the test solution to determine the content of flufenoxuron and its active metabolites in the plant-derived food based on the obtained peak area and a predetermined standard curve. The detection method provided by this invention can simultaneously detect flufenoxuron and its active metabolites with high sensitivity. In the examples, two compounds showed good repeatability and reproducibility in five matrices, enabling simultaneous detection of flufenoxuron and its active metabolites in spinach, green peppers, lemons, sweet oranges, and tea.

The present invention relates to elafibranor or its active metabolite, for use in a method for the treatment of primary sclerosing cholangitis.

Embodiments of the present invention relate generally to the treatment of schizophrenia or bipolar I disorder, and more particularly to the administration of iloperidone, including escalating doses of iloperidone, a pharmaceutically acceptable salt of iloperidone, an active metabolite of iloperidone, or a pharmaceutically acceptable salt of a metabolite of iloperidone, in such treatment. A first aspect of the present invention provides a method of treating a patient suffering from bipolar I disorder, comprising administering to the patient an effective amount of iloperidone, a pharmaceutically acceptable salt of iloperidone, an active metabolite of iloperidone, or a pharmaceutically acceptable salt of a metabolite of iloperidone, wherein the effective amount is effective to improve at least one manic symptom in the patient.

This invention belongs to the field of drug metabolism and analytical chemistry, specifically relating to a method for the rapid determination of tigustastat and its active metabolite GD-MET-1 concentrations in a human liver microsome incubation system using liquid chromatography-tandem mass spectrometry (LC-MS / MS). The method first prepares stock solutions of tigustastat, GD-MET-1, and an internal standard, and prepares a series of standard curve solutions, quality control solutions, and precipitant solutions containing the internal standard. Next, the sample with the added precipitant solution undergoes vortexing and centrifugation pretreatment. Finally, chromatographic and mass spectrometric conditions are set, and the analysis is performed by LC-MS / MS. This method has been validated for specificity, accuracy, precision, matrix effects, recovery, residues, and stability, and can be reliably used for metabolic stability studies of tigustastat and GD-MET-1 in a human liver microsome incubation system, GD-MET-1 formation studies, metabolic enzyme identification, enzyme kinetic studies, and drug interaction studies.

The invention discloses heavy metal resistant bacillus coagulans as well as a soil remediation agent and application thereof, and relates to the field of special medicament materials for soil pollution treatment and remediation service and material environment pollution treatment. The bacillus coagulans is Bacillus coagulans DBS06, the preservation number of the strain is CCTCC NO: M 20252772, and the strain has the characteristics of multiple heavy metal synergistic resistance, strong acid resistance and high spore yield, and can be used for efficiently synthesizing functional enzymes and active metabolites. The repairing agent is prepared by regulating and controlling the C / N ratio of a culture medium, supplementing an accelerating nitrogen source, combining two-stage culture of proliferation at 35-37 DEG C and induction at 40-45 DEG C, and adding regulation and control factors such as manganese sulfate and nano carboxymethyl cellulose. The remediation agent is suitable for green in-situ remediation of acidic, barren and heavy metal compound contaminated soil, and has good application prospects and popularization value.

The application discloses a plant salt-tolerance promoting active metabolite separated from a rhizosphere growth-promoting Pseudomonas proteus and application thereof. The metabolite is dibutyl phthalate (DBP) with a molecular formula of C 16 H 22 O4, has the effect of improving the salt tolerance of rice, and obviously increases the plant height, root length, aboveground fresh weight and underground fresh weight of the rice, is stable in effect, and has a good application prospect; and can be used as a preparation for improving the salt tolerance of crops in agricultural green production.