10results about How to "Good development value" patented technology

The invention discloses a BimBH3 analogue containing D-type amino acid and N-terminal fatty acid acylation, a preparation method of the BimBH3 analogue and application of the BimBH3 analogue as a PTPN1 inhibitor to development of hypoglycemic drugs. The structural general formula of the novel BimBH3 mimic peptide analogue is shown as a formula I: # imgabs0 #, wherein Raa2 is equal to D-His, D-Leu, D-Pro, D-Ser, D-Arg, D-Gln, D-Lys, D-Trp, D-Val, D-Tyr, D-Ala, Raa3 is equal to D-Gln, Raa7 is equal to D-Arg, and Raa8 is equal to D-Allo-Ile. The mimic peptide compound is derived from a core region of a Bim-BH3 structural domain, different D-type amino acid site-specific replacement modification and N-terminal conjugated hexadecanoic acid modification are adopted for amino acids at the second, third, seventh and eighth sites respectively, the BimBH3 mimic peptide modified by the D-type amino acid is more stable and has higher metabolic stability, and the target binding capacity and inhibitory activity of the BimBH3 mimic peptide can still be reserved or even improved. The BimBH3 mimic peptide compound shows an excellent PTPN1 inhibitor, the ability of resisting protease hydrolase and various digestive enzymes is also remarkably improved, and the BimBH3 mimic peptide compound has longer pharmacological action time and can play a potential long-acting hypoglycemic role through subcutaneous injection or oral administration. The compound is completely prepared by a polypeptide solid-phase synthesis method, and an obtained crude product is subjected to semi-preparative liquid chromatography purification and freeze-drying to obtain a target compound.

The invention belongs to the field of chemical synthesis, and particularly relates to four acinetobacter baumannii cell wall oligosaccharide fragments as well as a synthesis method and application thereof. Four acinetobacter baumannii core oligosaccharide fragments are synthesized by adopting a divergent synthesis strategy, compounds 1-3 take orthogonally protected alpha-(2-> 5)-Kdo-Kdo disaccharide as key precursors, protecting groups at different sites are selectively removed, glycosyl is introduced through a stereoselective glycosylation reaction, and thus a target molecular skeleton is constructed. The method disclosed by the invention and the four finally prepared acinetobacter baumannii core oligosaccharide fragments have huge industrial application potential.

The invention relates to galactomannan tetrasaccharide with anti-tumor activity and application of the galactomannan tetrasaccharide, and belongs to the technical field of active oligosaccharide drugs. The galactomanninotetraose ACP-3 synthesized by the invention has a good anti-tumor effect, is effective and safe, and has a very good development value. The galactomanninotetraose ACP-3 can obviously inhibit tumor cell proliferation in vitro and has no obvious toxicity to normal cells, so that the antitumor effect of the galactomanninotetraose ACP-3 has selectivity. In-vivo anti-tumor experiments show that the immunologic function of a body can be improved and tumor growth can be inhibited by single administration of the galactomanninotetraose ACP-3, and the galactomanninotetraose ACP-3 and CTX or PTX are combined for use, so that the effects of enhancing effects and reducing toxicity are achieved. The invention is helpful for developing oligosaccharide drugs with anti-tumor effect, and has important significance for research and development of corresponding carbohydrate drugs.

The invention belongs to application of collocation synergism of agricultural biostimulant in fertilizer, and particularly relates to a composite synergism technology containing 5-ALA and GABA (gamma-aminobutyric acid), and the effective components are 5-ALA and GABA; the weight percentage of the 5-ALA in the composition is 0.0075%-1%, and the weight percentage of the GABA in the composition is 0.1%-5%. According to the invention, 5-ALA and GABA are compounded according to a combination ratio to prepare the functional fertilizer. On the other hand, the activity is greatly improved compared with that of a single agent. Field trials prove that the composition disclosed by the invention has good growth promoting and yield increasing effects on crops.

The invention discloses a BimBH3 mimic peptide analogue of double-site coupling fatty acid, a preparation method of the BimBH3 mimic peptide analogue and application of the BimBH3 mimic peptide analogue serving as a novel PTPN1 inhibitor to development of long-acting hypoglycemic drugs. The structural general formula of the Bim BH3 mimic peptide analogue is as shown in formula I: # imgabs0 # mimic peptide compound is derived from a core region of a BimBH3 structural domain, the second amino acid is replaced and modified by Fmoc-Lys (Dde)-OH, the N end of a peptide chain is conjugated and modified by fatty monoacid or fatty diacid, the amino group of a side chain of lysine is conjugated and modified by fatty diacid, and the amino group of the side chain of lysine is conjugated and modified by fatty diacid. The compound has better metabolic stability, membrane permeability, pharmacokinetic characteristics and longer pharmacological action time, and shows an excellent long-acting hypoglycemic effect in the body of a type 2 diabetes mellitus model mouse. The compound is prepared by adopting a polypeptide solid-phase synthesis method, and a crude product is purified and freeze-dried to obtain a target compound.

The application discloses a method for efficiently separating high-purity conjugated linoleic acid from Tetrastigma hemsleyanum, which takes stems and leaves of Tetrastigma hemsleyanum as raw materials, and sequentially carries out ethanol extraction, ethyl acetate extraction, normal-phase silica gel column chromatography, gel column chromatography and semi-preparative reverse-phase liquid chromatography coupling purification process, so that 10E, 12Z-CLA monomers with chemical purity of greater than or equal to 99% are efficiently prepared. Experiments prove that the compound can significantly inhibit the inflammatory reaction of macrophages induced by lipopolysaccharide, and the mechanism is that the compound down-regulates TLR4 protein expression and inhibits NF-kappa B p65 phosphorylation, so as to block the activation of the TLR4 / NF-kappa B signal pathway. The application realizes high-value utilization of the abandoned resources of Tetrastigma hemsleyanum, and the obtained product can be used as a definite active ingredient for developing anti-inflammatory drugs, functional foods or cosmetics.

OCR04PP The present invention involves an indolone derivative which is replaced by pyrrole, a method. The preparation thereto, the components comprising derivatives, and the applications of those. The indolone derivative which is replaced by -pyrrol has a structure which is shown in formula(I) below. The current invention also involves the use of indolone derivatives which are replaced by... Pyrrol is used for therapeutic purposes through tyrosine kinase receptor-mediated therapy, and its components are linked to other treatments. Pharmaceuticals containing compounds with that structure for the treatment of related diseases, such as: tumor (Chemical formula)(I)

The application discloses application of a BMP9 inhibitor in preparation of a medicine for treating hypertension. It is found for the first time that knocking out BMP9 can reduce the blood pressure rise, vascular dysfunction and vascular remodeling phenomenon induced by AngII, that is, the BMP9 inhibitor can be used in effective treatment of hypertension, has a good application prospect and medicine development value in the technical field of hypertension treatment, and provides a brand-new thought and strategy for research and development of a hypertension treatment medicine.

The present application relates to the technical field of supramolecular, in particular to a collagen supramolecule, a preparation method and application thereof, the collagen supramolecule is prepared by taking collagen, a stabilizer, an alcohol solvent, glycerol, an ionic liquid and water as raw materials, the preparation method of the collagen supramolecule is simple and easy to operate, and the prepared collagen supramolecule has high stability. Meanwhile, in the collagen supramolecule, the collagen can not only be used as one of active ingredients to improve the skin condition, but also be used as a carrier of active ingredients to improve the solubility and transdermal performance of various active ingredients including the collagen itself, so as to solve the defects in the prior art.

The application provides application of basic lanthanum oxide in preparation of a medicine for treating hyperphosphatemia or a disease related to hyperphosphatemia, and belongs to the technical field of medicines.The application provides application of basic lanthanum oxide in preparation of a medicine for treating hyperphosphatemia or a disease related to hyperphosphatemia, and the application adopts basic lanthanum oxide to prepare the medicine for treating hyperphosphatemia or the disease related to hyperphosphatemia; the basic lanthanum oxide has a higher lanthanum content, which can reach 80.8%, and is developed into the medicine for treating hyperphosphatemia or the disease related to hyperphosphatemia; the medicine has a smaller use amount or preparation specification in combination with the use amount of the medicine for the same amount of phosphate in blood of a hyperphosphatemia patient, is beneficial to improving the compliance of the patient, and has a better phosphorus-lowering effect.