5 results about "Enzymes levels" patented technology

The present invention discloses a coumarin HDAC6 inhibitor and its preparation method and application, belonging to the field of chemical medicine technology. The present invention provides coumarin compounds shown in Formula I, Formula II and Formula III. Based on the structure of coumarin, the characteristic group of HDAC6 inhibitor hydroxamic acid is introduced to achieve good homologous selectivity for HDAC1 / 6; at the enzyme level, cell level and animal experiment level, it is verified that the compound has excellent target inhibition effect; by studying the example of HDAC6-NF-κB participating in the inflammatory response of colonic tissue, a new practical basis is provided for the treatment of ulcerative colitis. The compound provided by the present invention can be used as a new HDAC6 inhibitor to prevent and treat HDAC6-related diseases, especially it is expected to solve the shortcomings of some current small molecule drugs for the treatment of ulcerative colitis, such as poor relief effect and large side effects.

The invention discloses an MIF small-molecule inhibitor as well as a screening method and application thereof, and belongs to the technical field of medicinal chemistry. The inhibitor is composed of seven compounds with specific structures and pharmaceutically acceptable salts thereof, and the compounds and the pharmaceutically acceptable salts can effectively inhibit the tautomerase activity of MIF. The lead compounds are efficiently found from a large number of compounds through a computer-aided virtual screening method. In-vitro and in-vivo experiments show that the compound F3277-0933, especially the compound F3277-0933, shows remarkable MIF inhibitory activity and anti-tumor effect in enzyme level, cellular level and animal models, and the effect of the compound F3277-0933 is superior to that of an existing inhibitor ISO-1. The MIF small-molecule inhibitor disclosed by the invention provides a new candidate compound for developing medicines for treating MIF-related diseases such as colorectal cancer.

The invention discloses a preparation method of astaxanthin immobilized probiotic vesicles capable of resisting ionizing radiation liver injury, and belongs to the field of biological medicines. Preparing probiotic vesicles by taking lactobacillus rhamnosus as a raw material; the preparation method comprises the following steps: dissolving astaxanthin in absolute ethyl alcohol, dispersing vesicles in a phosphate buffer solution, mixing the two vesicles in a microreactor, and carrying out ultrasonic treatment to obtain astaxanthin-loaded probiotic vesicles; the immobilized probiotic vesicles loaded with the astaxanthin are obtained by incubating the immobilized probiotic vesicles with glutamine transaminase, so that the embedding rate and the loading rate of the astaxanthin are improved, and the immobilized probiotic vesicles have good biocompatibility and biological safety; the residence time of fat-soluble compounds in intestinal tracts is prolonged, and targeted enrichment of the liver is increased; x-ray induced active oxygen accumulation, mitochondrial dysfunction and DNA damage in cells are relieved, the antioxidant enzyme level is improved, and the lipid peroxide content is reduced; the liver injury caused by ionizing radiation is remarkably relieved by reducing oxidative stress and DNA injury of the liver and delaying cell apoptosis.

The present invention discloses a tuna swim bladder hypolipidemic and antioxidant oligopeptide and its application. The present invention uses tuna swim bladder as a raw material, and after enzymatic hydrolysis, ultrafiltration, gel chromatography purification, and RP-HPLC purification, the tuna swim bladder hypolipidemic and antioxidant oligopeptide His-Ser-Gly-Pro-Tyr-Met (HSGPYM) is prepared, and its molecular weight is 690.8 Da. The HSGPYM of the present invention can significantly reduce the contents of triglyceride (TG) and total cholesterol (TC) in the lipid accumulation model of HepG2 cells, showing good lipid-lowering activity; at the same time, it can significantly increase the antioxidant enzyme level in the cell model, effectively scavenge excessive reactive oxygen species, and reduce oxidative stress damage. The HSGPYM of the present invention has the advantages of being safe, non-toxic, and having strong lipid-lowering and antioxidant capabilities, and can be used for the development of functional products for the treatment of non-alcoholic fatty liver disease, and can also be used as an additive for health products and foods.

The application discloses a kind of for waste PET depolymerization system glycol directional efficient conversion of glycolic acid two enzyme level connection system and its application, belong to biological catalysis and resource recycling technical field.The system includes a kind of mutant alcohol dehydrogenase with high selectivity to glycol and a mutant aldehyde dehydrogenase ALDH-V7.Said mutant alcohol dehydrogenase is obtained in at least one combination mutation in 97 and 101 and / or 145 and 148 in the basis of ADH5 enzyme derived from acetic acid bacillus ( Gluconobacter oxydans ).The system can efficiently and directionally oxidize low-value glycol in waste PET chemical or biological depolymerization product to high-value-added product glycolic acid under mild conditions, effectively avoiding peroxidation and C-C bond rupture.The application provides an efficient and green biological catalysis solution for upgrading and recycling of waste PET, and realizes a circular economy path of "waste plastics-degradable plastic monomers".