460results about How to "Has antitumor activity" patented technology

The invention discloses a 4-tertiary butyl-2-(nitrobenzyl imino) thiazole derivative (I) which has the following chemical structural formula, in the formula I, Xi is selected from hydrogen, methoxy group, trifluoro-methyl, ethyoxyl or chlorine; X2 is selected from hydrogen, methoxy group, trifluoro-methyl, ethyoxyl or chlorine; X3 is selected from hydrogen, methoxy group, trifluoro-methyl, ethyoxyl or chlorine; X4 is selected from hydrogen, methoxy group, trifluoro-methyl, ethyoxyl or chlorine; and NO2 is selected from 2-nitryl, 3-nitryl, 4-nitryl or 2,4-dinitryl. The 4-tertiary butyl-2-(nitrobenzyl imino) thiazole derivative (I) has favorable inhibition activity on human cervical cancer cells, human liver cancer cells, human nasopharyngeal carcinoma cells and the like and can be used for preparing medicaments for resisting tumors.

The present invention relates to an antibody which has a therapeutic effect on tumors. Namely, the present invention relates to an antibody which binds to B7-H3 and exhibits antitumor activity. The objective of the present invention is to provide a pharmaceutical product which has a therapeutic effect on tumors. An anti-B7-H3 antibody which binds to B7-H3 and exhibits antitumor activity is obtained, and a pharmaceutical product for treating tumors, which contains the antibody, or the like is obtained.

The invention discloses 5-benzyl-4-alkyl-2-aminothiazole as shown in a chemical structure formula I and pharmaceutically acceptable salts of the 5-benzyl-4-alkyl-2-aminothiazole as shown in the specification. A preparation method of the 5-benzyl-4-alkyl-2-aminothiazole is as follows: heating 2-haslogen-1-aryl alkyl ketone, alkyl thiourea and ethanol, stirring, and reacting for a certain time; filtering, drying to obtain5-benzyl-4-alkyl-2-aminothiazole salts; and filtering the obtained filter cake and neutralizing with ammonia water, and then obtaining 5-benzyl-4-alkyl-2-aminothiazole. The invention also discloses application of the 5-benzyl-4-alkyl-2-aminothiazole or salts thereof in preparing antitumor medicaments.

The invention belongs to the technical field of biopharmacy, particularly relates to a PD-L1 IgV targeted affinity peptide product with antineoplastic activity, and a preparation method and application of the affinity peptide product. According to the invention, the affinity peptide is specifically bonded in the PD-L1 IgV area, the amino acid sequence of the affinity peptide is ANGSRLV (Ala-Asn-Gly-Ser-Arg-Leu-Val), and the molecular weight of the affinity peptide is 715.4; the affinity peptide can be artificially synthesized by adopting the Fomc solid-phase polypeptide synthesis, and can be adopted as the mainly active ingredient in preparing colon cancer (CT26) resistance medicines. Bacteriophages are adopted to display the peptide bank screening technique, the PD-L1 IgV is adopted as the target for high-flux screening, and the affinity peptide with the antineoplastic activity is artificially synthesized; the inventor further proves that the affinity peptide has the better antineoplastic activity, can remarkably inhibit growth of tumors in rats, and provides the novel thinking and theoretical basis for the research and development of PD-L1-based medicines.

The invention discloses a method for comprehensively extracting various kinds of biologically active ingredients from mushroom dry powder; the technical proposal is as follows: firstly, extracting alcohol soluble substances; secondly, extracting mushroom proteins; thirdly, extracting water soluble polysaccharide of mushroom, fourthly, extracting alkali extraction water-insoluble polysaccharide and alkali extraction water soluble polysaccharide; fifthly, preparing mushroom fiber. The extracted constituents have different biological activities, for example, the alcohol soluble substances have strong antioxidation activity; the mushroom proteins are rich in essential amino acid; the lentinan has antineoplastic activity; and the mushroom fiber has the physiological function of a dietary fiber. Therefore, the extracted constituents can be used respectively.

The invention relates to a method for hydrolyzing oyster protein by enzyme method and extracting oyster active peptide by column chromatography including: rinding the oyster, washing, homogenate, adding distilled water to extract the oyster liquid at a low temperature; flocculating, centrifugal deslagging, taking the supernatant fluid, freeze-dry the supernatant fluid, separateing with the Sephacryl s-100 HR column or enzymolysis, inactivating, centrifugal deslagging, freeze-dry the oyster liquid to get coarse extract, gel column chromatography of the coarse extract; collecting the respective peak, purifying with ion-exchange column chromatography, collecting the respective peak having activity, desalting with the gel column after freeze out and getting the oyster natural purified activity peptide. The oyster natural activity peptide has a high purity and has an anti-tumor activity. The active peptide is natural-extracted and is protected in the extraction process and may be a medicine to use.

The invention relates to 4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole shown as a chemical structural formula I and a salt thereof. The chemical structural formula I is shown in the specifications, wherein R is selected from H, alkyl with 1-2 carbon atoms, or straight chain alkyl or branch chain alkyl with 3-4 carbon atoms; and X1, X2, X3, X4 and X5 is selected from hydrogen, alkyl with 1-2 carbon atoms, hydroxyl, methoxyl, oxethyl, trifluoromethyl, fluorine, chlorine, bromine, nitro or amino. A preparation method of the 4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole comprises the following steps of: feeding 2-(1,2,4-triazol-1-yl)-2-bromoalkylketone and aryl thiourea in the molar ratio of 1:1, and carrying out a reflux reaction in ethanol; and after reacting, distilling under reduced pressure to remove a solvent, adding ethyl acetate for washing, filtering, drying to obtain 4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole hydrobromide, neutralizing the hydrobromide with ammonia water, extracting with ethyl acetate, drying, and distilling under reduced pressure to obtain 4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole. The 4-alkyl-2-aryl amino-5-(1,2,4-triazol-1-yl)thiazole has high antitumor activity, and can be applied to preparation of an anticancer medicament.

The invention discloses 5-(4-chlorophenylmethyl)-4-tertiary butyl thiazole derivatives (I), which has the following structural formula as shown in the specification of the invention, wherein X1 in a formula I is selected from hydrogen, hydroxyl group, methoxy group, nitro group, amino group and chlorine; X2 is selected from hydrogen, nitro group, amino group, methoxy group, chlorine, bromine and iodine; X3 is selected from hydrogen, methyl group, ethyl group, nitro group, methoxy group, chlorine, bromine, amino group and dimethylamino group; and X4 is selected from hydrogen, nitro group, amino group, methoxy group, chlorine, bromine and iodine. The 5-(4-chlorophenylmethyl)-4-tertiary butyl thiazole derivatives (I) have favorable inhibition activity on human cervical cancer cells, human liver cancer cells, human nasal and oral cancer cells and the like and can be used for preparing anti-tumor medicines.

The invention discloses a method for preparing walnut polypeptide nano-selenium with anti-tumor activity. The method comprises the following steps: (1) performing limited enzymatic hydrolysis on walnut dreg; (2) concentrating, and spray-drying to obtain walnut polypeptide; (3) adding an inorganic selenium source and vitamin C into the walnut polypeptide solution to prepare functional nano-selenium sol; (4) dialyzing the sol; and (5) carrying out freeze drying to obtain the walnut polypeptide nano-selenium. The dissolved walnut polypeptide nano-selenium is orange sol, and the morphology of the polypeptide nano-selenium is observed by a scanning electron microscope, and nano-particles with uniform particle size can be observed. The walnut polypeptide nano-selenium disclosed by the invention can be used for preparing selenium supplement agent healthy products and medicines. Cell experiments prove that the sol has a remarkable anti-tumor bioactivity, and is expected to become a high-efficiency low-toxicity preparation for treating cancers, in particular breast cancer.

The invention provides a novel immunomodulatory protein FIP-ppl derived from a fungus by applying a genetic engineering means for the first time. According to the invention, a gene which codes the protein is provided and synthesized. The protein FIP-ppl has immunomodulatory and anti-tumor effect. Experiments verify that the protein has a catalytic splitting effect on splenic lymphocyte and can add synthesis of interleukin 2; the protein has remarkable suppress proliferation and apoptosis-inducing effects of the protein on hepatoma carcinoma cell HepG2 and gastric carcinoma cell MCG823 are further verified. The protein FIP-ppl provided by the invention is lowly homological with almost found immunomodulatory proteins of fungi and is a novel immunomodulatory and anti-tumor biological preparation.

The invention discloses a breeding method for antitumor chrysomyia megacephala larvae. The breeding method comprises the following steps of: disinfecting chrysomyia megacephala, acclimating for over two generations, and preparing seed chrysomyia megacephala; placing a culture medium in an incubator, fermenting for 3 to 5 hours, and putting the seed chrysomyia megacephala into the incubator for egg laying, wherein the concentration of ammonia in the incubator is controlled to be between 50 and 200 ppm, the temperature in the incubator is controlled to be between 26 and 35 DEG C after eggs are incubated, and the ammonia concentration is between 500 and 1,000 ppm; and continuously breeding for 24 to 120 hours. By the method, each protein expression is changed at the developmental stage of the larvae by controlling the concentration and the temperature of the ammonia in all the stage environments of larva breading, and proteins which are abnormally expressed have antitumor activity. The culture medium used in the method has simple components and is convenient to operation, large-scale breeding is easy to realize, and the breeding method has a better industrialization prospect.

The invention relates to the technical field of extraction of active ingredients of edible mushrooms, and particularly relates to a method for simultaneously extracting polysaccharide and polyphenol from needle mushrooms. The method comprises the steps: preparing an extraction solution, extracting an alkaline solution by assistance of ultrasonic wave, performing enzymolysis on residue, extracting polyphenol from ethyl acetate and extracting polysaccharide after ultrafiltration and desalination. According to the method, operations such as auxiliary extraction, enzymolysis and membrane filtration are organically combined, and the polysaccharide and the polyphenol are simultaneously extracted, so that the production process is simplified, the safety and reliability are achieved, the yield is high, the physiological and pharmacological activities of the polysaccharide and the polyphenol in a needle mushroom sporocarp are well reserved, and a larger economic value is achieved.

The invention discloses a 2-indolone derivative with tyrosine kinase inhibition activity, geometric isomers and medicinal salts thereof, and a preparation method and an application of the above compounds. Tyrosine kinase inhibition activity evaluation confirms that the derivative is a compound with good tyrosine kinase activity, so the derivative has potential antitumor activity, and can be used to prepare tumor disease prevention and treatment medicines (antitumor medicines) as an active component. The derivative provides research and enforcement foundation for tumor treatment, and has a wide application prospect.

The invention relates to polyphenols substances, a synthesis method thereof and the use thereof, in particular to a flavonoid derivative, a preparation method thereof and the use thereof, and solves the problem that the conventional natural flavonoids compounds are difficult to extract and obtain and cannot be widely used. The structural formula (I) of an intermediate and the structural formula (II) of a final product are shown below, wherein R1, R2 and R3 are respectively selected from hydrogen, C1-C8 alkyl, halogen, nitro, C1-C8 alkoxy and amino; and R1, R2 and/or R3 can be fused with a benzene ring to form a substituted or unsubstituted fused ring compound; R4 and R5 are respectively selected from C1-C8 alkyl, C1-C8 alkoxy and alkylene; R may be H, methoxy-methoxy or methoxy; and b ring is a benzene ring or a heterocyclic compound. The derivative can be used for preparing medicaments for resisting tumors and cardiovascular and cerebrovascular diseases and inhibitors of protein tyrosine kinases, opens up a new way for preparing the medicaments and brings a new breakthrough to the medicament field; and the synthesis method has the advantages of mild condition and convenient operation.

The invention discloses an edible and medical fungi blackening agent and specifically relates to the technical field of biological fermentation. Natural components with a blackening effect are fermented by edible and medical fungi so as to obtain zymogeneous bacteria. The bacteria contain higher nutrients than natural raw materials, and contain effective ingredients as well as amino acid, vitamin, trace elements and natural plant melanin which are necessary for the hair growth. The edible and medical fungi blackening agent has a more ideal effect for hair dyeing and blackening than general plant hair dyes, has a wide source of raw materials, requires low price, and can bring benefit for common people. The product provided by the invention contains no chemical hair dye component, is safe and reliable to use, has no toxic and side effect, and is a product which has a health-care function and also can be used to fundamentally treat leukotrichia and alopecia.

The invention discloses a method for preparing active polypeptides from deep-sea fish meat, and the method includes degreasing, first deodorization, enzymolysis, second deodorization, ultrafiltration,decolorization, desalting and freeze-drying. 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide is used to activate chitosan, and coupled with glutaraldehyde to form a lipase immobilized carrier, an active short peptide is used to improve the physical and chemical adsorption force between a carrier and lipase, the lipase stability, activity, heat resistance and use frequency are improved; through useof the complementary effect and synergistic effect of thermolysin and chymotrypsin hydrolysis sites, the protein hydrolysis degree and enzymatic hydrolysis speed of minced deep-sea fish meat can be improved, terminal group type can be changed, and the active polypeptides with antitumour activity can be obtained by hydrolysis.

The invention discloses a copper compound adopting 2-acetyl-3-ethyl pyrazine thiosemicarbazone as ligand as well as a synthetic method and application thereof. The synthetic method of the copper compound comprises the following steps: measuring 2-acetyl-3-ethyl pyrazine and thiosemicarbazide, reacting by using methanol as a solvent, after the reaction, transferring into a beaker, volatilizing, crystallizing, obtaining ligand 2-acetyl-ethyl pyrazine thiosemicarbazone crystals, filtering the crystals, and washing the crystals by using methanol; enabling the ligand 2-acetyl-ethyl pyrazine thiosemicarbazone to react with CuCl2 or CuBr2 in the mixed solvent of acetonitrile and methanol, transferring the reactant into the beaker, standing, cooling, volatilizing and crystallizing, collecting thecrystals, and obtaining the target compound. By researching the in-vitro glioma resistance and drug-resistant strain activity of the synthesized copper compound, the result shows that the compound forms thiosemicarbazone ligand with the metal copper, the activity is greatly improved, the glioma resistant activity is excellent, and the drug resistance can be overcome to certain extent.

The invention provides a preparation method for spirulina antitumor polypeptide. According to the invention, spirulina protein is extracted mainly by using a process of combined multigelation and ultrasonication, then is hydrolyzed by papain and finally filtered with an ultrafiltration centrifuge tube so as to obtain spirulina polypeptide with a molecular weight in ranges of 0 to 3 KD, 3 to 5 KD, 5 to 10 KD and more than 10 KD. The spirulina polypeptide prepared in the invention has antitumor activity and is beneficial for development and utilization of antitumor health food and medicinal products.

The invention provides taxus fruit wine, comprising the following components in parts by weight: 90 to 110 parts of sticky rice, 10 to 15 parts of red yeast rice, 2 to 15 parts of taxus flesh and 90 to 110 parts of water. The fruit wine has the following advantages: 1) the fruit wine has simple manufacture process, short procedure, and is advantageous to popularization; 2) the alcohol content is between 1 and 38 percent, so the taxus fruit wine can be used as health-care wine; 3) the wine contains oligosaccharides, gamma-aminobutyrate, natural lovastatin, 10-DAB and other components, has the functions of reducing blood sugar, blood fat and blood pressure, preventing and resisting cancers, removing residual free radicals in the body, contains functional oligosaccharides, promotes value addition of bifidobacterium, improves immunity and disease resistance, has antitumor activity, and can directly inhibit tumors; 4) the fermented product is proved to have not toxicity after toxicity inspection; and 5) the wine is mellow and sweet and has excellent taste.

The invention relates to an extract capable of resisting tumor activity, which is analyzed from centipede (a traditional Chinese medicine). The extract is obtained as follows: crushing the centipede at low temperature, conducting enzymolysis on the centipede at low temperature, separating and freeze-drying the centipede, and separating the centipede by a sephadex G-25 gel column, thereby obtaining an active ingredient which mainly comprises an effective ingredient, water-solubility micromolecule active peptide. By being tested by MTT, the extract has better anti-tumor activity. The extract avoids the defects that in the clinical application of a macromolecule protein medicine, certain allergenicity exists, and the quality control is not easy in industrialization caused by using the centipede (which is adopted as a crude drug), and has the advantages of a micromolecule activity peptide medicine, including high production efficiency, work procedure saving, quality control convenience and the like.

The invention discloses a resveratrol dimer derivative containing a Combretastin A-4 structure and preparation and application methods thereof, belonging to the technical field of medical engineering. By analyzing and researching reported anti-tumor activity and structure-activity relationship related to resveratrol and a derivative of the resveratrol, a series of derivatives with novel structures formed by polymerization of Combretastin A-4 and the resveratrol can be obtained through design and preparation. Through preliminary anti-tumor pharmacological tests, the prepared new compound is confirmed to have broad-spectrum tumor inhibitory activity to cancer cells.

The invention discloses polypeptide separated from centipede toxin, and determination on anti-tumour activity thereof is carried out. Ultrafilteration and reversed-phase chromatography separation methods are adopted to separate and purify one polypeptide composed of twelve amino acids from centipede toxin, the sequence thereof detected by applying edman degradation method is Phe-Thr-Gly-Gly-Asp-Glu-Ser-Arg-Ile-Gln-Glu-Gly, and the molecular weight thereof measured by applying mass-spectrometric method is 1296.05Da. The anticancer cell viability of the polypeptide is determined by applying MTT method. The polypeptide in the invention has anti-tumour activity, has inhibition action on propagation and growth of human umbilical vein endothelial cell, is in dose-response relationship and can be applied to treatment and auxiliary treatment of various cancers.

The invention discloses a pyrazolopyrimidine-type compound. The structural general formula of the pyrazolopyrimidine-type compound is shown as formula (I). The invention further discloses a preparation method of the pyrazolopyrimidine-type compound and application of the pyrazolopyrimidine-type compound in preparation of antitumor drugs. The provided pyrazolopyrimidine-type compound can effectively inhibit multipletumor cells, including human breast cancer cells, human lung cancer cells, human hepatoma carcinoma cells, human neuroblastoma cells and the like, has high antitumor activity and canbe applied to preparation of the antitumor drugs.