93 results about "Active metabolite" patented technology

The invention discloses a method for improving beef quality, an action mechanism and an experimental method, in a cattle body, vitamin A can activate the expression of EBF2 through an active metabolite RA of the vitamin A, and the EBF2 can inhibit the transcription process of CYP26B1 in a targeted manner to maintain the activity of a retinol signal channel, so that PPAR gamma and downstream lipid metabolism related genes thereof are activated, and the activity of the retinol signal channel is improved. Fatty acid transport and lipid accumulation in fat cells in the cattle muscle are promoted, fat deposition in the cattle muscle is promoted, and the beef quality is improved. By constructing the molecular network for regulating and controlling the formation of the fat in the cattle muscle, a complex regulation and control mechanism for controlling the fat deposition in the cattle muscle can be understood more deeply, a method for improving the beef quality based on regulating and controlling the vitamin A mediated key factor EBF2 is provided, and a new way is provided for improving the beef quality in a targeted manner.

The present application relates to a sustained release delivery composition of a vesicular monoamine transporter type 2 (VMAT2) inhibitor, a deuterated derivative thereof, a pharmaceutically acceptable salt thereof, an active metabolite thereof, or a prodrug thereof for treatment of hyperkinetic movement disorders including, but not limited to, tardive dyskinesia (TD), Huntington's disease (HD) chorea, tremors, dystonia, chorea, tics, myoclonus, stereotypies, restless legs syndrome, and various other disorders with abnormal involuntary movements. The present application also relates to a sustained release delivery composition of an antipsychotic agent, a pharmaceutically acceptable salt thereof, an active metabolite thereof, or a prodrug thereof for treatment of schizophrenia, bipolar disorder, and other psychiatric diseases or disorders. The method of making or using the composition is also disclosed.

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 discloses low-GI probiotic compound coarse cereal meal replacement powder and a preparation method thereof. The preparation method comprises the steps of raw material and auxiliary material treatment, starch enzymolysis, strain activation culture, fermentation, freeze drying, blending and packaging and the like. The black tartary buckwheat, the black beans, the black sesame, the black rice and the black mulberries are used as main raw materials, good growth conditions are created for lactic acid bacteria by means of an amylase enzymolysis technology, and further the cereals are subjected to synergistic fermentation by inoculating a strain suspension of lactobacillus reuteri and lactobacillus rhamnosus, so that the nutritional value is increased, bioactive metabolites are added, and the nutritional value is increased. And the flavor and taste of the grains are also improved. Compared with common commercially available meal replacement powder, the product realizes directional domestication fermentation of probiotics in a composite coarse cereal environment, so that the product has high viable organism stability, ensures the colonization ability of the probiotics in cereal powder, realizes synergistic improvement of nutrition and flavor, contains certain functional components, and has relatively good sugar controlling and stabilizing ability.

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.

To provide a novel tetracycline derivative having reduced antimicrobial activity for use in treating disorders of the central nervous system.SOLUTION: Provided are novel molecules comprising a modified tetracycline molecule including Deamino Diacetyl Minocycline, Methyl Ether Minocycline, Ethyl Ether Minocycline, Propyl Ether Minocycline, Butyl Ether Minocycline, Butyl Ether Monoacetyl Minocycline, Butyl Ether Diacetyl Minocycline, Butyl Ether Triacetyl Minocycline, or Butyl Ether Tetra Acetyl Minocycline, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, and tautomers thereof, and methods for using the same to treat Alcohol Use Disorder (AUD), Substance Use Disorder (SUD), tobacco use, pain, or proinflammatory disorders.SELECTED DRAWING: None

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.

Provided is a pharmaceutical composition comprising a sulfonamide derivative represented by the following formula (1), a pharmaceutically acceptable salt thereof, or an active metabolite thereof, and having improved absorbability when orally administered. Disclosed is a self-emulsifying composition comprising: a sulfonamide derivative represented by the following formula (1), a pharmaceutically acceptable salt thereof, or an active metabolite thereof; and at least two solubilizers.

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 relates to application of uridine in the development process of a medicine for preventing and treating diabetic nephropathy and in the medicine. Clinical metabonomics identification and animal experiment verification prove that uridine is a key active metabolite of DKD, the treatment effect of uridine has the characteristics of multiple targets and tissue specificity, and a new solution for research and development of metabolic drugs based on DKD is provided; through pharmacodynamic research of uridine and exploration of a protection mechanism, various application scenes of uridine in the research and development process of medicines for preventing and / or reducing diabetic nephropathy patients are further explored, so that the application of uridine in DKD medicines and the research and development process of the medicines is wider, and a wider prospect is provided for later research and development of the DKD medicines.

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.