92results about How to "Good inhibition rate" patented technology

The invention provides a nanometer capsule of a macromolecule adriamycin bonding medicine with a targeting function and a preparation method thereof. The nanometer capsule is mixed assembled with two block copolymers of poly ethylene glycol-polylactic acid, wherein the polylactic acid chain end of one block copolymer is connected with adriamycin, with a molar ratio of 98-70 percent in the nanometer capsule, while the poly ethylene glycol chain end of the other block copolymer is connected with lactose, with a molar ratio of 2-30 percent in the nanometer capsule. The adriamycin connected with the polylactic acid chain end is located in the capsule inner core, which is double protected by polylactic acid and poly ethylene glycol and has sustained release function; while the lactose connected with the poly ethylene glycol chain end is located in the outer layer of the capsule, which has targeting function and leads the nanometer capsule preferentially enter the cells carrying the lactose receptors.

The invention relates to a surface material with protein adsorption resistant property and a preparation method thereof, belonging to the technical field of biological materials. The surface material is an organic silicon surface material polymerized by monomer molecules with diionic property and organic silicon, has good protein adsorption resistant property and can be extensively applied to the fields of marine antifouling materials and biomedical materials. The surface material which has the protein adsorption resistant property through surface modification is prepared by carrying out graft polymerization on the monomer molecules with the diionic property on the surface of an organic silicon substrate; the surface material is combined with water molecules in a marine environment to form a water film on the surface of the material and can prevent the adsorption of proteins on the surface of the material because the water molecules contained in the water film are compactly arranged, thereby inhibiting the further adhesion of marine fouling organisms on the surface of the material and achieving the effect of effectively preventing and removing the fouling of marine organisms; in addition, the invention has wide application prospect.

The invention discloses a new compound, N1,N4-di(3-hydroxyphenyl)-3,6-dimethyl-1,2,4,5-tetrazine-1,4-dicarbonamide shown in formula (I), and preparation and application thereof. The preparation of the compound comprises the steps of using 3,6-dimethyl-1,6-dihydro-1,2,4,5-tetrazine and bis(trichloromethyl) carbonate as raw materials to react with m-hydroxyaniline in an organic solvent in the presence of alkaline catalyst. The compound provided by the invention is applied for preparing medicines for treatment and prevention of human gastric cancer, ovarian cancer, liver cancer, breast cancer or lung cancer. According to the invention, the compound is rational in design, easy in operation, low in production cost and easy to obtain raw materials, and is suitable for industrialized application, and a new choice for screening anti-tumor medicines is provided.

The invention relates to an alpha-naphthalenesulfonamide base quintuple heterocyclic compound and application thereof in anti-tumor treatment. Shown as research results, the alpha-naphthalenesulfonamide base quintuple heterocyclic compound, an isomer thereof, a stereomer or a mixture of the stereomer and a pharmaceutically acceptable salt or a precursor all have suppression effects on tumor cells, wherein the suppression ratios of about half compounds on the cell level are superior to that of ML-7 positive control medicine. The invention is expected to lay the foundation for developing anti-tumor medicaments.

The present invention relates to a kind of hypnone oxime derivative, its preparation and application. The tests show that said derivative has the good bactericidal activity and control effect for common diseases of vegetable, melon and fruit crops, such as powdery mildew, anthracnose and sclerotium disease, specially, for powdery mildew it can obtain better control effect.

The invention relates to the biological medicine field, and concretely relates to an application of DHM in the preparation of anti-hepatoma medicines. The DHM has a strong anticancer characteristic as a flavonoid compound. Tests prove that the DHM plays a positive role in hepatoma carcinoma cell propagation inhibition, hepatoma carcinoma cell apoptosis induction, hepatoma carcinoma cell adhesion capability reduction and hepatoma carcinoma cell invasion and transfer prevention, and can substantially reduce the contents of peroxides, glutathione and ATP in the hepatoma carcinoma cells.

The invention relates to a diheterocyclic compound as well as a synthesis method, which belongs to the organic synthesis field, and particularly relates to a pyrazol-pyrrole heterocyclic compound as well as a synthesis method, and aims at further improving the sterilizing activity of a nitrogen-containing heterocyclic sterilizing agent. The structural formula of the diheterocyclic compound is shown in the specification. The preparation method comprises the following steps of synthesizing an acyl-ethyl-ester compound and a hydrazine compound into a 5-pyrazolone compound, synthesizing by utilizing DMP (dimethyl formamide) and phosphorus oxychloride to obtain 5-chloride-4-formylpyrazole, adding potassium hydroxide and phenol compound to prepare five-replaced formylpyrazole, then carrying out the condensation reaction to form the acrylamide compound, and finally facilitating the ring-closing reaction of the formylpyrazole and p-toluenesulfonyl methylisocyanide to obtain the diheterocyclic compound. When used as a sterilizing agent, the diheterocyclic compound has the bacteriostatic activity for the rice sheath blight disease, cucumber gray mold and cucumber downy mildew.

The invention relates to the field of DC-CIK (Dendritic Cell-Cytokine-Induced Killer) cell culture and particularly relates to a culture method of DC-CIK cells loaded with tumor cell exosomes. The culture method comprises the following steps of: commonly culturing CIK cells and peripheral blood DC cells loaded with the tumor cell exosomes, after culturing for 65-75 hours, adding IL-2 with the amount of 1000-1500 IU/mL by volume of culture solution, and continuously culturing for 65-75 hours to obtain the DC-CIK cells; culturing by a CIK culture medium comprising the components of GT-T581 culture medium, autologous plasma and IL-2, wherein the autologous plasma is 5%+/-0.5% of the volume of the GT-T581 culture medium and the concentration of the IL-2 is 1000+/-100 IU/mL. The culture methodhas the beneficial effects that by culturing the CIK cells and the peripheral blood DC cells loaded with the tumor cell exosomes in a certain mode, the obtained DC-CIK cells loaded with the tumor cellexosomes have good killing capability.

The invention relates to 5-(1H-indolyl-3-methylene)-1,3-thiazolidinyl-4-one derivatives, and a synthesis method and application thereof. By using ethanol and/or water as a solvent, substituted 2-substituted-imino-1,3-thiazolidinyl-4-one and 1H-indolyl-3-formaldehyde are subjected to reflux reaction under the catalytic condition of piperidine through intermolecular dehydration condensation reaction to form methylene linking group, thereby obtaining the 5-(1H-indolyl-3-methylene)-1,3-thiazolidinyl-4-one derivatives. The intermediate 2-substituted-iminothiazolidinyl-4-one is prepared by carrying out cyclization reaction on various monosubstituted ethyl thiocarbamide chloroacetates or chloroacetic acids in a low-boiling solvent under reflux conditions, and the intermediate 2-substituted-imino-3-substituted-1,3-thiazolidinyl-4-one is prepared by carrying out a green environment-friendly synthesis technique on various disubstituted symmetric thiocarbamides and chloroacetic acids. The bioactivity preliminary screening experiment result of all the target compounds on the enzyme molecular level indicates that the target products have certain inhibition activity on PTP1B and CDC25B to different degrees.

The invention relates to a method for preparing a Gymnodinium breve inhibitor and belongs to the field of treatment of marine red tide. The method comprises the following preparation steps: firstly, a large-scale alga ulva pertusa material is pulverized and leached through anhydrous ethanol, usually, each kilogram of the ulva pertusa material uses 2 to 5 liters of the anhydrous ethanol to obtain an extract; secondly, cream obtained through condensation of the extract is dissolved in water; a supernatant fluid is taken out, is extracted through petroleum ether and is delaminated to obtain a water phase substance; and the water phase substance is extracted with n-butyl alcohol and is delaminated to obtain a water phase substance; and finally, the water phase substance is extracted with acetic ether; and the obtained acetic ether phase is the Gymnodinium breve inhibitor. The inhibitor with the concentration of between 8 and 10 milligram/litre has optimal inhibition ratio on Gymnodinium breve. The preparation method has a simple process, low preparation cost and no organic pollution; and the used reagent has low price and lower toxicity.

The invention discloses novel antibacterial application of NPS-2143. The systematic name of NPS-2143 is 2-chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthyl)ethyl]amino]-2-hydroxypropoxy]benzonitrile. Theinvention provides application of NPS-2143 in inhibition of Gram-positive bacteria and persistent bacteria thereof. According to the results of determination of inhibitory activity against the growthof a plurality of Gram-positive bacteria, NPS-2143 has good inhibitory activity against common Gram-positive bacteria such as MSSA strains (ATCC 25923), MSSA strains (ATCC 6538) and MRSA strains (ATCC33591). NPS-2143 has superiority in inhibition of sensitive Gram-positive bacteria and drug-resistant Gram-positive bacteria and in resistance of persistent bacteria compared with ciprofloxacin (CPFX), and shows good application prospects in the development of novel antibacterial drugs.

The invention provides a double-promoter and double-expression specific shRNA (Short Hairpin Ribonucleic Acid) lentiviral vector and application thereof. The double-promoter and double-expression specific shRNA lentiviral vector comprises an U6 promoter with a nucleotide sequence shown as SEQ ID NO: 1, and an H1 promoter with the nucleotide sequence shown as SEQ ID NO: 2. The experiment results show that the lentiviral vector can express two types of shRNA at the same time, can inhibit the expression of a vpr (Viral Protein Regulatory) gene and/or reduce the expression level of a tat (Transactivator) gene, and can be used for developing and preparing a medicine for preventing HIV (Human Immunodeficiency Virus) infection from occurring.

The invention provides a Marsdenia tenacissima saponins H and a preparation method thereof. According to the preparation method, traditional Chinese medicine Marsdenia tenacissima is used as raw material, Marsdenia tenacissima saponins H with good antineoplastic activity and high content is obtained through a series of steps such as extraction, separating, crystallization, recrystallization and the like, and a high efficiency liquid phase chromatography is adopted to determine that the content of the marsdenia tenacissima saponins H is in a range of 60-99.8%. Proper pharmaceutically acceptable carriers can be added to the Marsdenia tenacissima saponins H to prepare certain dosage form, so as to be used for clinic treatment of tumour. The Marsdenia tenacissima saponins H and the preparation method thereof of the invention employ traditional Chinese medicine modernization separating and purifying technology, the technology is innovative, is suitable for industrialization production, and has strong practicality.

The invention discloses a retinoic acid compound, and a preparation method, an intermediate and application thereof. The retinoic acid compound I provided by the invention has better inhibition ratio on tumor cells. (The formula (I) is shown in the description).

The invention discloses a preparation process of an acylated derivative of genistein. The preparation process comprises the following process steps: (1) taking genistein, dissolving the genistein in an organic solvent, dripping a catalyst, controlling the pH value to be 2-7, and controlling the temperature of the solution to be 0-5 DEG C; (2) dissolving chloroacetyl chloride into the organic solvent, adding into a constant pressure funnel, dripping into the solution in (1), and producing solids after dripping; monitoring the reaction process by TLC (Thin-Layer Chromatography), raising the temperature to be 10 DEG C, continuously reacting, and stopping the reaction within 17 hours; (3) standing the reaction solution for an hour, performing suction filtration, performing vacuum drying on thefilter cake at the temperature of 40 DEG C, thereby obtaining the acylated derivative of genistein. The preparation process has the advantages that the compound has excellent solubility in water, thein-vivo oavailability of the compound can be greatly improved, the compound has excellent inhibition rate on hepatoma carcinoma cell HepG2, and a novel drug with excellent water solubility and an anti-tumor effect is expected to be developed.

The invention provides a preparation method for a chlorella antibacterial peptide. According to the invention, chlorella is adopted as the raw material, ultralow temperature freezing and low temperature ultrahigh pressure continuous flow cell disruption are combined with an ultrasonic treatment process, effective wall-breaking is carried out on chlorella to obtain soluble protein, and then a biological enzyme method is utilized to obtain the antibacterial peptide with obvious antibacterial effect. The chlorella has the characteristics of extremely solid cell wall and high intramural protein content, and the technical key points of the invention lie in that ultralow temperature freezing and low temperature ultrahigh pressure continuous flow cell disruption are combined with the ultrasonic treatment process to treat chlorella, effective wall-breaking on chlorella is realized, and the content of soluble protein is increased. Through selection of appropriate enzyme and control of hydrolysis degree, the antibacterial peptide with a good antibacterial effect can be obtained.

The invention provides a novel nitrogen-atom double-substitution hydroxamate histone deacetylase inhibitor with an oxadiazole structure. The novel nitrogen-atom double-substitution hydroxamate histonedeacetylase inhibitor is synthesized by taking a nitrogen-atom double-substitution structure with oxadiazole as a CAP zone and combining the nitrogen-atom double-substitution structure with a hydroxamic acid structure. The invention also provides application of the compound used as a novel histone deacetylase inhibitor. The invention further discloses application of the compound or pharmaceuticalcompositions thereof to preparation of medicines for treating diseases such as growth, metastasis and recurrence of various malignant tumors caused by histone acetylation disorder.

The invention provides a small interfering ribonucleic acid-containing pharmaceutical composition and application thereof in preparation of medicines for preventing and/or treating hepatitis B. The small interfering ribonucleic acid-containing pharmaceutical composition contains two small interfering ribonucleic acids specified at different genotypes of the hepatitis B virus and serving as activeingredients, can achieve an effect of extensively covering multiple genotypes of HBV, has a synergistic effect in the aspect of inhibiting the multiple genotypes of the HBV, can simultaneously lower the level of HBsAg, and has the clinical application potential.

The invention relates to the field of DC-CTL cell culture, in particular to a culture method for DC-CTL cells loaded with tumor cell exosomes. The culture method for the DC-CTL cells loaded with tumorcell exosomes comprises the following step: carrying out co-culture on CTL cells and peripheral blood DC cells loaded with the tumor cell exosomes to obtain DC-CTL cells loaded with the tumor cell exosomes. A culture medium is a CTL culture medium, the CTL culture medium comprises the following components: an AIM-V culture medium, autologous plasma and IL-2, the content of the autologous plasma is 5%+/- 0.5% of the volume of the AIM-V culture medium, and the final concentration of the IL-2 is 1000+/- 100 IU/mL. Components of the culture medium are optimized, and the obtained DC-CTL cells loaded with the tumor cell exosomes have good killability.

The present invention relates to applications of Chinese herb plants, particularly to a portulaca oleracea l extract and applications thereof. The preparation method of the portulaca oleracea l extract comprises: crushing portulaca oleracea l herb, screening, and extracting the total flavone from the portulaca oleracea l herb by using an ultrasonic extraction method. According to the present invention, the portulaca oleracea l extract can inhibit pathogenic bacteria, kill bacteria, and induce apoptosis of pathogenic bacteria.

The invention relates to annonaceous acetogenins nanoparticles, which are prepared by taking cyclodextrin and lecithin as vectors, as well as a preparation method and an application of annonaceous acetogenins nanoparticles. The annonaceous acetogenins (annonaceous acetogenins total lactone or monomer ingredients thereof) nanoparticles are prepared by virtue of a solvent precipitation method; the mass ratio of the annonaceous acetogenins to the cyclodextrin to the lecithin is at 1 to (0.02-20) to (0.02-20); and in accordance with an optimal prescription, the combining proportion of the annonaceous acetogenins to the cyclodextrin to the lecithin is at 4 to 2 to 1 (in percentage by mass). The average grain size of the annonaceous acetogenins nanoparticles is 20-1000nm, and the annonaceous acetogenins nanoparticles are good in dispersity; the annonaceous acetogenins nanoparticles are stable in both gastrointestinal fluid and plasmid, and the annonaceous acetogenins nanoparticles are suitable for both oral administration and intravenous injection; with the application of the nanoparticles, the inhibitory effect of the annonaceous acetogenins on tumor cells can be significantly improved, and meanwhile, in vivo anti-tumor efficacy can be enhanced; and the annonaceous acetogenins nanoparticles have a broad development prospect.

The invention belongs to the technical field of cosmetics, and particularly relates to an extracting method and application of traditional Chinese medicine extracts in whitening cosmetics. A traditional Chinese medicine classic famous formula, namely a Simiaoyong'an decoction formula, is regarded as the research object for the first time, mixed liquid of acetone, ethyl acetate and water serves asan extraction agent for extracting a high-tyrosinase-inhibition-rate extract traditional Chinese medicine source whitening agent from a mixture of flos lonicerae, radix scrophulariae, radix angelicaesinensis and licorice root, and the traditional Chinese medicine source whitening agent can be used for preparing whitening lotions, whitening creams, whitening toners and other forms of cosmetics. The traditional Chinese medicine source whitening agent is provided for overcoming the defect that a chemical whitening agent has cytotoxicity and is harmful to human bodies.

The invention discloses a 3-benzothiazole-1-(3-dimethylamino)propyl quinoline-4-ketone derivative with a general formula (I). The general formula (I) is shown in the description, wherein R is H, halogen, alkyl, an alkoxy group or halogen alkane element. The invention discloses a preparation method of the 3-benzothiazole-1-(3-dimethylamino)propyl quinoline-4-ketone derivative and application to preparation of an antitumor medicament. Experiments show that the 3-benzothiazole-1-(3-dimethylamino)propyl quinoline-4-ketone derivative has high suppression activity for liver tumor cells HepG2, Bel-7402 and Bel-7404, a relatively high suppression rate for the HepG2 liver tumor and relatively good antitumor application prospect, the cycle of the cell HepG2 can be arrested in a G2/M period and the cell HepG2 can be induced to apoptosis.

The present invention belongs to the technical field of research on moisture evaporation inhibitor preparation processes, and more particularly relates to a novel heterogeneous moisture evaporation inhibitor preparation method. The inhibitor comprises 0.8-1.4% of even carbon fatty alcohol or 0.6-1% of odd carbon fatty alcohol, 4-10% of short-chain alcohol, 40-65% of petroleum ether, 0.7-1.1% of a fatty alcohol polyoxyethylene ether series emulsifier AEO-3 and/or AEO-5 and/or AEO-7, and the balance of distilled water. The preparation method comprises: (1) according to the ratio, weighing even carbon fatty alcohol or odd carbon fatty alcohol and short-chain alcohol, completely dissolving in petroleum ether at a room temperature, adding a fatty alcohol polyoxyethylene ether series emulsifier, and completely and uniformly mixing so as to be used as a moisture evaporation inhibitor oil phase system; and (2) weighing distilled water, adding to the obtained oil phase system, placing the oil phase system into an ultrasonic wave treatment apparatus, and carrying out intermittent shaking so as to prepare the stable water-in-oil type heterogeneous moisture evaporation inhibitor. The moisture evaporation inhibitor of the present invention has the significant technical effect in the water resource protection field.

The invention discloses piperidine alkyl phthalide compounds (I), pharmaceutically acceptable salt, a preparation method, a pharmaceutical composition and an application thereof in preparing drugs fortreating and/or preventing neurodegeneration related diseases, including but not being limited by neurodegenerative diseases such as vascular dementia, Alzheimer's disease, Parkinsonism, Huntington disease, HIV related dementia, multiple sclerosis, progressive lateral sclerosis spinal cord, neuropathic pain and glaucoma. The formula is as shown in the description.

The invention discloses Beauveria bassiana and application thereof in the prevention and treatment of tobacco brown spot and belongs to the technical field of plant protection. Beauveria bassiana is numbered HFBb009 and collected in China General Microbiological Culture Collection Center under 14158. Beauveria bassiana is used herein for the first time in the prevention and treatment of tobacco brown spot; data shows that Beauveria bassiana (numbered HFBb009) can well inhibit tobacco brown spot; the inhibitory action of Beauveria bassiana upon the pathogenic fungus tobacco brown spot pathogengrows stronger overtime, and the inhibitory action is most significant when Beauveria bassiana spore suspension having the concentration of 1.0*107 is used.