100 results about "Cell Proliferative Activity" patented technology

IL-10 sequence variants are disclosed that retain the therapeutically desirable anti-inflammatory properties of wild-type IL-10 but do not retain the hemoatopoeitic cell regulatory and cell proliferative activities. The mutant IL-10 polypeptides of the invention are used in methods of treating diseases involving inflammatory response, including neuropathic pain and other neurological disorders.

The invention discloses an N-alkyl-1,2,3,4,5,6-hexahydro-1,1,5,5-tetramethyl-7H-2,4 alpha-methanonaphthalene-7-amine compound as well as a synthetic method and an application thereof. Longifolene serving as a heavy oil main component is relatively rich terpenoid in numerous natural extracts. The synthetic method comprises the following steps: obtaining isolongifolene through longifolene isomerization, obtaining isolongifolenone through allylic oxidation of the isolongifolene, carrying out dehydration condensation on the isolongifolenone and primary amine so as to obtain imine and obtaining the chiral N-alkyl-1,2,3,4,5,6-hexahydro-1,1,5,5-tetramethyl-7H-2,4 alpha-methanonaphthalene-7-amine compound after reduction. The compound has vey good inhibition activity on candida albicans, aspergillus niger, candida tropicalis, escherichia coli, staphylococcus aureus, pseudomonas fluorescens, bacillus subtilis and the like, a part of compound has good cancer cell proliferation inhibition activity on human breast cancer cells MCF-7, human lung adenocarcinoma cells A549, hepatoma cells HepG2 and SMMC-7721, and the N-alkyl-1,2,3,4,5,6-hexahydro-1,1,5,5-tetramethyl-7H-2,4 alpha-methanonaphthalene-7-amine compound is a potential antibacterial and bactericidal and anti-tumor compound.

The invention discloses gynostemma pentaphyllum extract compounds (I) with inhibiting actions on human liver cancer HepG2 cells and a preparation method thereof, and application of the compounds in medicine, belonging to the field of phytochemistry. The preparation method of the compounds disclosed as Formula (I) comprises the following steps: carrying out high-temperature high-pressure treatment on whole gynostemma pentaphyllum, extracting with ethanol under reflux, and concentrating the extracting solution under reduced pressure to obtain an extractum; adding distilled water into the extractum to form a suspensoid, and extracting sequentially with dichloromethane and ethyl acetate; concentrating under reduced pressure to obtain an ethyl acetate extract; passing the extract through an HP20 resin, eluting sequentially with 20%, 50% and 70% ethanol, and concentrating the 70% ethanol eluate under reduced pressure to obtain an elution product; and treating the elution product with silica gel column chromatography, eluting with dichloromethane / methanol in a ratio of 20:1-10:1 (v / v), sectionally collecting the eluates to obtain 6 components, and eluting the component 3 with acetonitrile / water in a ratio of 53:47 (v / v) at the flow rate of 3 mL / minute in a semipreparative chromatographic column (250*10mm, 5 mu m). The pharmacodynamical test indicates that the compounds disclosed as Formula (I) have obvious activities for inhibiting cancer cell proliferation.

The invention relates to tetralin isoquinoline compounds and synthesis thereof as well as applications of the tetralin isoquinoline compounds in the aspect of inhibiting tumor cell proliferation. In the invention, the structure of natural (-)-alpha-(1R, 9S)-narcotine is modified, so as to synthesize a series of novel tetralin isoquinoline compounds (I). In vitro antitumor activity screening indicates that the tetralin isoquinoline compounds have activities of inhibiting the tumor cell proliferation, thus the compounds can be further developed into novel antitumor medicaments.

The invention discloses a triazole gold compound as well as a preparation method and application thereof. The structural general formula of the compound is shown as the description, wherein R1 is phenyl, p-methylphenyl, p-Chlorophenyl, a methoxyl group, methoxycarbonyl or p-fluorophenyl; R2 is triphenylphosphine, dimethyl -phenyl phosphine, 35 fluorine Phenyl phosphine or triethylphosphine; R3 is hydrogen, methyl or phenyl; R4 is hydrogen, methyl or phenyl; X is boron tetrafluoride negative ions or trifluoromethyl sulfonic acid negative ions. The inhibitory activity IC50 of the triazole gold compound disclosed by the invention (in nanomoles) indicates that the triazole gold compound is strongly combined with thioredoxin reductase active centers. The triazole gold compound disclosed by the invention has high anticellularity reproductive activity, is a thioredoxin reductase inhibitor adopting a novel structure, is good in physico-chemical property, is good in water solubility, and can be utilized as a lead compound of antitumor drugs.

The invention discloses application of aripiprazole in preparation of an antineoplastic drug. According to the application, it is found for the first time that the aripiprazole can inhibit the proliferative activity of colorectal cancer cells, reduce the clone formation number of the colorectal cancer cells, and inhibit growth of tumors of colorectal cancer. The colorectal cancer proliferative activity inhibiting effect of the aripiprazole is more remarkable along with the increase of the concentration of the aripiprazole and prolonging of the medication time, and has concentration dependencyon the cycle arrest function and in-vivo inhibiting function on the colorectal cancer cells. Meanwhile, the aripiprazole is a drug ratified by FDA for sale; compared with new medicine development, thecost is low, no obvious toxic or side effect exists, the aripiprazole is used for assisting in treatment of colorectal cancer, and a new drug source can be provided for adjuvant therapy of cancer.

The invention discloses a fibronectin composition freeze-dried micro-core with a skin barrier repairing effect and a preparation method thereof. The freeze-dried micro-core is prepared from the following raw materials in percentage by weight: 10 to 15 ppm of fibronectin, 10 to 15 ppm of platelet-derived growth factors, 10 to 15 ppm of metallothionein type IV, 10 to 15 ppm of elastin, 20 to 40 ppm of fibroin, freeze-drying protection liquid and the balance of water. The pharmaceutical composition is a biological functional product, has cell proliferation promoting activity and cell migration promoting activity, shows the effect of relieving stabbing pain in lactic acid stabbing pain experiments, is free of preservatives and artificial chemical components during preparation, and is non-irritant to skin.

The invention discloses G1 / G0-phase blocked pentacyclic indol-quinolizidine which is (6S)-3-acetyl-6-(N-phenylacetyl amino acyl)-oxidative methyl-4,6,7,12-tetrahydro-4-oxoindole-[2,3-1] quinolizidine, and discloses a compound, cell proliferation resistance activity, antineoplastic activity and application thereof.

The invention discloses a heteroaromatic amide compound and a preparation method and application thereof. According to the heteroaryl amide compound provided by the invention, a preliminary activity research shows that the compound has selectivity to STAT3 and also has very strong tumor cell proliferation inhibition activity; the compound can be used as a series of novel STAT3 inhibitors and can be used for preparing drugs for treating corresponding diseases. The compound has obvious killing effect on human cancer cells, especially human breast cancer cell line MDA-MB-231, human prostate cancer cell line PC-3 and human prostate cancer cell line DU-145, has the potential of being prepared into novel antitumor drugs, and has better market prospect.