32 results about "Fatty acid synthase" patented technology

The invention discloses an application of 2, 3-dihydroxybenzoic acid in preparation of an antitumor drug. Researches find that 2, 3-dihydroxybenzoic acid can inhibit proliferation, migration and invasion of colorectal cancer cells in vitro and promote cell cycle arrest and cell apoptosis, and 2, 3-dihydroxybenzoic acid can inhibit growth of mouse transplanted tumors in vivo and promote cell apoptosis; the 2, 3-dihydroxybenzoic acid has a remarkable treatment effect on mouse colon cancer and can improve the immunotherapy effect; moreover, the 2, 3-dihydroxybenzoic acid small molecule substance, as an inhibitor of fatty acid synthase (FASN), plays an important role in inhibiting colorectum.

The application belongs to the technical field of biological medicine, and specifically discloses a compound for targeted degradation of fatty acid synthase and application thereof, which has a structure shown in general formula I or a pharmaceutically acceptable salt thereof. The compound provided by the application is designed through a target ligand-connection bridge-E3 ligand structure, realizes efficient degradation, can significantly reduce the level of FASN in high-expression cells, and thus specifically targets cells related to abnormal lipid metabolism. The mechanism of action depends on the ubiquitin-proteasome pathway and is time-dependent. The compound provided by the application has good biological activity of degrading FASN, can be applied to the development of anti-liver cancer drugs, and has a wide application prospect.

The invention relates to the technical field of biological fermentation, and discloses sauced rosa roxburghii tratt and a preparation process and application thereof.The sauced rosa roxburghii tratt is prepared through a 1298 fermentation process, namely, the sauced rosa roxburghii tratt is prepared through nine procedures of steam processing, liquid fermentation, separation and juicing, material mixing and yeast stirring under eight fermentation environment parameters in a one-year fermentation period and a liquid-state and solid-state combined fermentation mode, and the sauced rosa roxburghii tratt is obtained. The inherent health attribute of the rosa roxburghii tratt is reserved to the maximum extent, and the sauce flavor is achieved. Efficacy verification tests show that the sauced roxburgh rose can activate phosphorylation expression of adenylate activated protein kinase in a mouse body, reduce fatty acid synthase and inhibit expression of a fat generation gene, so that de novo synthesis of fatty acid is inhibited, lipid accumulation in the liver is reduced, and the effect of preventing and treating liver cancer is achieved. The compound can regulate intestinal flora related to lipid accumulation and energy metabolism, realizes the effect of regulating the non-alcoholic fatty liver, and has a wide application prospect in preparation of large healthy food, health care products and medicines for regulating or improving the non-alcoholic fatty liver.

Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

The invention belongs to the technical field of biological medicines, and particularly relates to a daphniphyllum calycinum extract compound, an extraction method thereof and application of the daphniphyllum calycinum extract compound in preparation of a medicine for preventing or treating non-alcoholic fatty liver diseases. A natural compound with a novel structure is obtained from daphniphyllum calycinum for the first time, a preparation method of the compound is provided, activity research is carried out on the compound, and experimental data shows that the compound is low in cytotoxicity and has no obvious cytotoxicity to normal cells, and the compound can be used for preparing the compound by inhibiting expression of fatty acid synthetases ACC, ACLY and FAS. The compound inhibits the de novo synthesis of fatty acid in cells, thereby inhibiting the accumulation of lipid droplets in the cells and reducing the lipid level in the cells, and has wide application prospects in the field of preparation of drugs for preventing or treating non-alcoholic fatty liver diseases.

The invention relates to the field of biological medicines, in particular to application of fatty acid synthase (FASN) as a target spot in screening or preparing medicines for treating breast cancer, and particularly relates to targeted therapy for breast cancer stem cells (BCSCs). The invention discloses application of an FASN target spot in screening or preparing a medicine for treating breast cancer. Research finds that FASN is highly expressed in BCSCs, and stem cell characteristics of the BCSCs are maintained by activating a Wnt / beta-catenin pathway. By inhibiting the activity of FASN (such as using lansoprazole), the proliferation, self-renewal and tumor formation ability of BCSCs can be significantly reduced. The invention provides an FASN-based drug screening method and a drug composition, and provides a new strategy for breast cancer treatment.

The present invention provides the use of fatty acid synthase inhibitors for the prevention and treatment of drug-induced liver injury (DILI), relating to the field of biotechnology. This invention demonstrates that increased fatty acid synthesis mediated by FASN regulates macrophage inflammatory responses and migratory chemotactic behavior. Targeting macrophage fatty acid synthesis can alleviate acute liver injury and inflammatory responses. This discovery represents the first discovery of new targets and new efficacy for fatty acid synthase inhibitors, potentially resolving the current lack of specific treatments for acute liver injury.

The present invention provides a use of an inhibitor of fatty acid synthase (FASN) or its gene activity in the preparation of a drug for treating essential thrombocythemia (ET). The inventors have verified that the FASN small molecule inhibitor and the BASIN The therapeutic effects of gene editors or inhibitory nucleic acids in ET in vitro and in vivo models were evaluated, and the possibility of FASN or its gene as a new target for ET treatment was evaluated, providing new ideas for the clinical treatment of ET.

The application discloses a method for constructing a multi-enzyme complex engineering strain, and has the characteristics that the method comprises the following steps: S1, constructing a light decarboxylase FAP and an oil-producing yeast fatty acid synthase fusion expression vector; S2, electrically shocking and transforming the constructed target vector into an agrobacterium competent AGL1, and introducing the target vector into a starting strain through an agrobacterium-mediated transformation method to obtain an engineering strain that is back-supplemented with a fatty acid defect; the engineering strain that is back-supplemented with the fatty acid defect is obtained, the FAP-FAS2 fusion expression is realized at the same time as the self-assembly of the intracellular FAS1, and a FAP-FAS synthase complex is obtained. The complex not only back-supplements the fatty acid defect function, so that the strain grows normally, but also can synthesize alkanes in the process of blue light irradiation fermentation culture, and realizes the intracellular assembly of protein macromolecules.

Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds. Also described herein are methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

The invention relates to the field of gene engineering, and discloses a CRISPRi (clustered regularly interspaced short palindromic repeats i) system, a recombinant strain containing the CRISPRi system, a construction method and application of the recombinant strain, and a method for producing gibberellin. The CRISPRi system comprises a coding gene of a dCas9 mutant protein without cleavage activity, sgRNA and an induction regulation component, wherein the induction regulation component is used for regulating the expression of the dCas9 mutant protein coding gene; the sgRNA guides the dCas9 mutant protein to be combined to a target gene, so that the expression of the target gene is inhibited; the dCas9 mutant protein is obtained by mutation on the basis of a Cas9 protein, and mutation sites are D10A and H840A of the dCas9 protein; the target genes comprise squalene synthase encoding genes, fatty acid synthase encoding genes and the like, the CRISPRi system can accurately and efficiently regulate and control gibberellin gene expression, the gibberellin yield is remarkably increased, the influence on strain growth is small, regulation and control are reversible, specificity is high, and the CRISPRi system is matched with gibberellin and has good industrial prospects.

Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds. Also described herein are methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

The application belongs to the field of tumor diagnosis and treatment, and relates to a potential inhibitor of fatty acid synthase (FASN) and application of the potential inhibitor in treating various tumors such as colorectal cancer, breast cancer, ovarian cancer and the like. The small-molecule inhibitor is a compound shown in formula I or II, or a stereoisomer of the compound shown in formula I or II, or a pharmaceutically acceptable salt, a solvate, a hydrate, a polymorph, a co-crystal, a tautomer, an isotopically labeled derivative and a prodrug thereof. The compound is mainly used for inhibiting the enzyme activity of FASN and then inhibiting the proliferation of various tumors, for example, the growth and proliferation of colorectal cancer, breast cancer, ovarian cancer and the like, and is expected to become a novel broad-spectrum tumor treatment drug and has a wide application prospect.

The invention discloses application of a Reg4 gene in treatment of metabolism-related fatty liver, and relates to the technical field of biomedicine. The Reg4 gene is applied to the aspect of treating obesity and metabolism-related fatty liver; according to the application, by increasing expression of the Reg4 gene, liver lipid deposition, liver cell ballooning and inflammatory infiltration related to the metabolism-related fatty liver are inhibited; the application is realized by inhibiting the processes of de novo synthesis of fat in the liver, liver lipid uptake and fatty acid beta oxidation. The step of inhibiting the de novo synthesis of fat in the liver comprises the step of inhibiting the expression of genes of acetyl coenzyme A carboxylase 1, fatty acid synthase and / or stearoyl coenzyme A desaturase 1. The invention definitely proves that the Reg4 gene has an obvious effect of improving obesity and metabolism-related fatty liver, and can relieve hepatic fatty degeneration and inflammation.

Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and / or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatopepatitis (NASH).

The invention discloses functional feed for protecting liver and intestines of mandarin fish and a preparation method of the functional feed, and belongs to the technical field of feed. The functional feed for protecting the liver and the intestine of the mandarin fish comprises the following components: an intestine and liver protecting compound, an enteric coating material, an adsorbent, an anti-sticking agent, a protein source, a fat source, carbohydrate, compound vitamins and compound minerals. The preparation method comprises the following steps: firstly, preparing a coating solution, putting an intestine and liver protecting compound into a fluidized bed, spraying the coating solution at the bottom, curing, adding an adsorbent, and mixing to obtain a coated compound; then mixing a protein source, a fat source and carbohydrate to obtain a basic nutrient; and finally, mixing the coated compound, the basic nutrient mixture, the compound vitamins and the compound minerals, extruding and granulating, spraying an anti-sticking agent, and drying to obtain the feed. The functional feed for protecting liver and intestine of mandarin fish provided by the invention can inhibit fatty acid synthase in liver, reduce liver lipid deposition of mandarin fish, restore the liver-body ratio, improve the feed conversion rate and enhance the growth performance of mandarin fish.

The invention provides application of a dipsacus asper and radix cyathulae stem and leaf compound in a feed additive, and belongs to the technical field of feed. Dipsacus asper stem and leaf powder, radix cyathulae stem and leaf powder and corn flour are compounded, and the feed additive is prepared through double fermentation of bacillus subtilis and lactobacillus plantarum. The fatty acid synthase expression level of fattening pigs fed with the feed additive is remarkably reduced. The lean meat percentage of a control group is 62.75%, the lean meat percentage of a group fed with a conventional traditional Chinese medicine feed additive is 64.35%, the lean meat percentage of a group fed with a fermented traditional Chinese medicine feed additive is 67.87%, and the lean meat percentage is remarkably improved. The pig fattening period of the control group is 104 days, and the feed conversion ratio is 3.02: 1; the fattening period of the pigs fed with the conventional traditional Chinese medicine feed additive group is 101 days, and the feed conversion ratio is 2.94: 1; the fattening period of pigs fed with the fermented traditional Chinese medicine feed additive is shortened to 88 days, the feed conversion ratio is 2.57: 1, and the breeding efficiency is remarkably improved.

The invention relates to the technical field of feed additives. The invention provides a composition for producing selenium-enriched snowflake beef, a functional feed additive prepared from the composition and application of the functional feed additive. Comprising rapeseed oil, soybean oil, palm oil, linseeds, fructus perillae, semen raphani, platycladus orientalis kernels, fennel, fructus psoraleae, pumpkin seeds, semen cassiae, fructus arctii, semen plantaginis, common fenugreek seeds, semen cuscutae, fructus cnidii, cardamine violifolia powder, cortex magnoliae officinalis, cortex cinnamomi, haws, pericarpium citri reticulatae, pericarpium citri reticulatae viride, rhizoma atractylodis, cyrtomium fortunei, herba artemisiae scopariae, bile acid, soybean phospholipid, cellulase, fatty acid synthetase, vitamin E, vitamin D, zeolite powder and the like. Lipase, polyunsaturated fatty acid, phytoestrogen and the like contained in the traditional Chinese veterinary medicine seeds are utilized to regulate fat metabolism of an organism and increase the content of high-density lipoprotein, and traditional Chinese veterinary medicines for warming and nourishing liver and kidney and soothing liver-gallbladder are fused to enhance liver and kidney functions of the organism, increase biliary secretion and cooperatively promote digestion and absorption of lipid and formation of snowflake beef.

The invention relates to a fatty acid synthase inhibitor and application thereof. Particularly, the invention relates to a compound shown in a general formula (I), a stereoisomer or pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and application of the compound shown in the general formula (I) or the pharmaceutical composition thereof in preparation of drugs for preventing and / or treating fatty acid synthase (FASN) mediated diseases, and substituents in the general formula (I) are as defined in the specification.

Described herein are spiropiperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described spiropiperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described spiropiperidine compounds and synthetic intermediates that are useful in those syntheses.

The present invention relates to a composition and a method capable of predicting sulfonylurea dependence in diabetic patients by identifying the variants of: rs777077261(C>A) of KCNB2(Potassium Voltage-Gated Channel Subfamily B Member 2); rs202112906(C>T) of GHSR(Growth hormone secretagogue receptor); rs28944173(T>C) of NOS2(Nitric oxide synthase 2); rs3792268(C>A) of CAPN10(Calpain 10); rs199670165(C>A), rs17848945(C>T), rs755372392(G>A), rs200840955(G>A), rs200842352(C>A) or rs45489599(C>T) of FASN(Fatty acid synthase); rs185358392(G>A), rs769120237(G>A), rs201884071(G>A) or rs766766661(C>T) of KCNH6(Potassium Voltage-Gated Channel Subfamily H Member 6); rs14847401(G>A), rs37551700(G>A) or rs774656238(A>G) of DIS3L2(DIS3 like 3'-5' exoribonuclease 2); or rs74315349(G>A) or rs150546920(C>G) of NR0B2(Nuclear Receptor Subfamily 0 Group B Member 2).

The invention provides application of tauroursodeoxycholate in prevention or treatment of mitochondrial encephalopathy, and belongs to the technical field of medicine. The core of the invention lies in that the pathological mechanism of the mitochondrial encephalopathy is coped with by utilizing multiple biological effects of the TUDCA. In-vivo and in-vitro experiments find that after a cKO mouse is treated by TUDCA, the expression of an endoplasmic reticulum stress marker Atf4 and fatty acid synthase (Fasn) in the mouse can be remarkably reduced, and abnormal accumulation of lipid is reduced, so that the metabolic state of cells is improved. In animal models, treatment with TUDCA not only alleviates dyskinesia, but also promotes the neurogenesis process and extends the survival time of mice.

Method and compositions for treating glioblastoma (GBM) and other cancers is disclosed, involving the combination of radiation therapy (RT), fatty acid synthase (FASN) inhibitors, and programmed cell death protein 1 (PD-1) inhibitors or programmed death ligand 1 (PD-L1) inhibitors. The disclosed approach addresses the technical problem of RT-induced immunosuppression and resistance in cancers by targeting RT-induced lipid metabolism, which promotes immune escape. FASN inhibitors block fatty acid synthesis, enhancing immune cell infiltration and restoring anti-tumor immunity. PD-1 / PD-L1 inhibitors further counteract immunosuppressive pathways to improve therapeutic efficacy. This combination therapy prolongs survival, induces immune memory, and is applicable to other cancers, including those exhibiting increased lipid content post-RT or chemotherapy, including melanoma, breast cancer, and lung cancer.

When employed, a recombinant expression vector carrying a daptomycin production gene including a foreign fatty acyl AMP ligase (FAAL) gene, a thioesterase (TE) gene, and a fatty acid synthase (FAS) gene according to the present invention can enhance specificity for decanoic acid, and produce daptomycin without supplementation of lipopeptides, such as decanoic acid, from the outside of the strain. In addition, no by-products are generated during the production process, thereby enabling production of daptomycin with high purity and high yield.

The application provides an enzyme inhibiting supramolecular complex and application in cosmetics, and relates to the field of cosmetic raw materials.The supramolecular complex is a supramolecular structure formed by hydrogen bond connection of coriander glycoside and sodium phosphatide through high-pressure homogenization treatment and gradient freeze-drying treatment, and can inhibit key enzymes of sebaceous gland secretion, including aminoacylase N, 3beta-hydroxysteroid dehydrogenase and fatty acid synthase.The supramolecular complex can be added into different types of cosmetics, especially cosmetics with oil control and pore shrinking functions, so that the supramolecular complex can not only play a role of the composition itself, but also improve the transdermal rate by using the lipophilicity of phospholipid, and maximizes the cosmetic effect.

Methods of circulating Fatty Acid Synthase (cFAS) detection, assays, and kits thereof, as well as methods of diagnosis and treatment for cardiovascular-related diseases based on cFAS are provided. Exemplary embodiments of the methods, assays, and kits disclosed herein allow for improved, noninvasive, low-cost, and reliable diagnosis and treatment for cardiovascular-related diseases, particularly in subjects suffering from both symptomatic and asymptomatic Peripheral Arterial Disease (PAD), via detecting and measuring cFAS from LDL-associated cFAS captured from a biological sample.

Methods of circulating Fatty Acid Synthase (cFAS) detection, assays, and kits thereof, as well as methods of diagnosis and treatment for cardiovascular-related diseases based on cFAS are provided. Exemplary embodiments of the methods, assays, and kits disclosed herein allow for improved, noninvasive, low-cost, and reliable diagnosis and treatment for cardiovascular-related diseases, particularly in subjects suffering from both symptomatic and asymptomatic Peripheral Arterial Disease (PAD), via detecting and measuring cFAS from LDL-associated cFAS captured from a biological sample.

The invention relates to a fatty acid synthase inhibitor and application thereof. Particularly, the invention relates to a compound shown in a general formula (I), a stereoisomer or pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and application of the compound shown in the general formula (I) or the pharmaceutical composition thereof in preparation of drugs for preventing and / or treating fatty acid synthase (FASN) mediated diseases, and substituents in the general formula (I) are as defined in the specification.

The invention relates to a cornu cervi degelatinatum extract, in particular to a cornu cervi degelatinatum extract as well as a preparation method, a composition and application thereof. The preparation method of the cornu cervi degelatinatum extract comprises the following steps: S1, mixing cornu cervi degelatinatum with water, heating to boil, preserving heat, and cooling to obtain a mixture a; s2, adding alkaline protease into the mixture a, and stirring to obtain a zymolyte; s3, heating the zymolyte until the zymolyte is boiled, preserving heat, cooling, filtering or centrifuging, taking supernate, and carrying out vacuum concentration to obtain a concentrate; and S4, adding ethanol into the concentrate, carrying out alcohol precipitation treatment, filtering or centrifuging, taking the precipitate, and drying to obtain the cornu cervi degelatinatum extract. The cornu cervi degelatinatum extract is obtained by combining alkaline proteolysis of cornu cervi degelatinatum and alcohol precipitation treatment of ethanol, is a hydrolytic peptide, contains multiple amino acids, has a certain proliferation promoting effect on HaCaT cells, and has the effects of improving the activity of fatty acid synthase FAS in the cells and increasing the HA content.

The present invention relates to heterocyclic modulators of lipid synthesis. Compounds are provided as modulators of fatty acid synthesis. The compounds are useful in treating disorders characterized by dysregulation of fatty acid synthase function and / or the fatty acid synthase pathway by modulating fatty acid synthase function and / or the fatty acid synthase pathway. Methods for treating such disorders are provided, including viral infections, such as hepatitis C infection, cancer, and metabolic disorders, such as nonalcoholic steatohepatitis (NASH).