149 results about "Colon carcinoma cell" patented technology

The invention discloses a compound with an MEK (Mitogen-activated and Extracellular signal-regulated Kinase) inhibiting function as well as a preparation method and application of the compound. The structure of the compound disclosed by the invention is as shown in a formula (I). The preparation method of the compound disclosed by the invention comprises the steps of forming a coumarin ring by adopting a Pechmann reaction mainly and carrying out structural modification of different sites. In the binding experiment of the compound disclosed by the invention and MEK, the binding activity is up to 54.57nM; the anti-proliferation effect IC50 (half maximal inhibitory concentration) value on the melanoma cell A375 is up to 1.23 micrometers; the anti-proliferation effect IC50 value on the colon cancer cell HT-29 is up to 2.13 micrometers; and the activity is higher than that of a positive control U0126. The novel structure type coumarins compound with the MEK inhibiting function shows good MEK binding activity, MEK inhibiting activity, ERK (Extracellular signal Regulated Kinase) pathway inhibiting activity, anti-tumor effect and antiviral effect and has broad application value. The formula (I) is as shown in the specification.

The invention discloses a Caco-2 cell surface specific binding polypeptide. Four polypeptide fragments are screened by phage display of a random dodecapeptide library, and the amino acid sequences of the four polypeptide fragments are respectively as follows: SPSIDTRYSRLG, CVSVGMKPSPRP, SVSVGMKPSPRP and MVSMDSSPRDRL. According to the screening method disclosed by the invention, colorectal carcinoma Caco-2 cell binding polypeptide sequences are screened by a phage polypeptide display technology, the affinity of phage clones with colorectal carcinoma cells is judged by enzyme-linked immunosorbent assay (ELISA), ten phage clones are obtained, and four polypeptide sequences are obtained by sequencing. The consensus amino acid sequence is XXSXXXXXXXRXX; homology analysis indicates that the polypeptide motif is likely to be the amino acid determinant on the tumor cell surface receptor binding ligand protein; by further judgment of cell immunofluorescence, the targeting result of the phage positive clones implicates that the phage positive clones can be specifically bound with Caco-2 cells; and the colorectal carcinoma Caco-2 cell specific polypeptide acquired by screening provides a preliminary experiment basis for early diagnosis of colorectal carcinoma, targeted delivery of antitumor drugs and development of targeted small peptide drugs.

The invention relates to colon and prostate tumor associated antigen peptides obtainable from prostate specific G protein-coupled receptor (PSGR), six-transmembrane epithelial antigen of prostate (STEAP) and proteins encoded by genes found overexpressed in colon carcinoma cells, such as human 1-8D interferon induced transmembrane protein 2. The invention further relates to a polynucleotide encoding the tumor associated antigen peptides and to pharmaceutical compositions, which are preferably anti-tumor vaccine compositions, containing a tumor associated antigen, at least one tumor associated antigen peptide thereof, or encoding polynucleotide thereof as an active ingredient. The pharmaceutical compositions can be administered to a patient in need thereof to treat or inhibit the development of colon or prostate cancer.

The present invention describes a newly discovered human G-protein coupled receptor and its encoding polynucleotide. Also described are expression vectors, host cells, agonists, antagonists, antisense molecules, and antibodies associated with the polynucleotide and/or polypeptide of the present invention. In addition, methods for treating, diagnosing, preventing, and screening for disorders associated with aberrant cell growth, neurological conditions, and diseases or disorders related to the pituitary gland, colon, breast, lungs, and prostate are illustrated.

The invention provides a 2-aminoimidazopyridine derivative shown as a formula I, a formula II, a formula III or a formula IV and further provides a preparation method and application of the 2-aminoimidazopyridine derivative. An experiment shows that the 2-aminoimidazopyridine derivative has a remarkable proliferation inhibition effect on tumor cells (including an over-expressed wild type EGFR (Epidermal Growth Factor Receptor) human epidermal carcinoma cell line A431 and a Gefitinib drug-resisting human lung adenocarcinoma cell line H1975) related to the activity of EGFR tyrosine kinase in the aspect of a cell level, especially has a relatively good inhibition effect on the drug-resisting cell line H1975, has relatively weak inhibition activity on a low-expression EGFR human colon cancer cell line SW620 and can be applied to preparation of corresponding anti-tumor cell medicines. A general formula is shown in the description.

Phage display was used to screen peptide libraries that distinguish between well-differentiated (HCT116) and poorly-differentiated colon carcinoma cells (HT29). The screening protocol used selection and subtraction on intact, viable cells, resulting in phage libraries exhibiting high binding selectivity for the poorly-differentiated HT29 cells. A nine amino acid, disulfide-constrained peptide (RPM) was identified that selectively bound and was internalized into colon cancer cells. The peptide may be used to detect colon cancer cells and also may be used to selectively deliver therapeutic agents to the cells.

The invention relates to ursolic acid derivatives with anticancer activity and a preparation method thereof. In the method, a carbonoxyl group at the C-28 position of ursolic acid is connected with natural alpha-amino acid through ethanediamine in a mode of forming an amido bond to synthesize a series of ursolic acid derivatives with anticancer activity. In-vitro pharmacological experiments indicate that the ursolic acid derivatives chemically modified by amino acid have obvious in-vitro inhibition effect on human liver cancer HepG2 cells, human colon cancer HT-29 cells, human gastric cancer AGS and BGC-823cells, and human prostatic cancer PC-3 cells.

The invention discloses tetrandrine derivatives and a preparation method thereof. The structural general formula of the compounds is as shown in the specification. The method comprises the following steps: dissolving bisbenzylisoquinoline compounds used as raw materials in a certain solvent, adding a reactant Y, mixing, reacting for 0.1-72 hours at a temperature ranging from minus 20 to 300 DEG C and under a neutral or alkaline condition, adding an acid to a solution obtained after reacting and neutralizing, and then carrying out separation and purification to obtain target products. The tetrandrine derivatives prepared by the method have an outstanding inhibition effect on the proliferation of the human hepatocarcinoma cell line HepG2 and the human colon cancer cells HT29, and thus can be applied to preparing anti-tumor medicines.

The invention provides a preparation method of a colon cancer cell strain expressed by stabilized silent PKM2 gene. The preparation method comprises the steps of constructing of shRNA lentiviral expression vector of human PKM2 gene, packaging and obtaining of lentivirus, DLD1 colon cancer lentivirus infecting, stabilized cell strain puromycin screening and Real-time PCR, Western blot identification. The experimental results show that the shRNA nucleotide sequence can be successfully inserted into the pLKO.1-puro expression vector, and the inhibitory effect on the expression of PKM2 gene is remarkable, endurable and stable. The prepared cell strain can be used as the experimental material for researching the regulating effect of PKM2 in malignant characteristics such as colon cancer cell energy metabolism, cell proliferation, cell migration and inflammation.

The invention relates to an antitumor application of penicillium enol A2 from penicillium citrinum. Penicillium citrinum IBPT-5 is preserved at the China Center for Type Culture Collection on December 25, 2013; the address is Wuhan University; and the preservation number is CCTCC NO:M 2013713. An experiment proves that the compound has relatively good antitumor activity on a plurality of tumor cells, and can be used for preparing cell proliferation inhibition drugs or antitumor drugs to carry out antitumor research; and the tumor cells comprise human colon cancer cells SW620, human hepatoma carcinoma cells Huh7, human colon cancer cells SW480, human esophageal squamous cancer cells KYSE450, human esophageal carcinoma cells EC9706 and human hepatoma cells PLC.

The invention provides a gene inhibitor for promoting apoptosis of colon cancer cells and inhibiting migration of the colon cancer cells, and belongs to the technical field of biomedicine. Experimentsprove that the LINC02360 gene inhibitor can promote apoptosis of colon cancer cells, and migration and invasion of the colon cancer cells can be inhibited by regulating protein expression of E-cadherin and N-cadherin. Therefore, the siRNA of the LINC02360 can be used for preparing a medicine for promoting apoptosis of colon cancer cells and can also be used for preparing a medicine for inhibitingmigration and invasion of the colon cancer cells.

The invention discloses a series of amino acid derivatives prepared by using diosgenin as a lead compound through corresponding chemical reaction. Solubility test finds that the solubility of derivatives is increased compared with the raw material medicine of diosgenin; and the pharmacological experiments prove that the diosgenin amino acid derivatives have in vitro antitumor activity, have different degrees of growth inhibition on human colon cancer cell Caco-2, human gastric carcinoma cell MGC-709, human lung adenocarcinoma cell SPC-A-1 and human neuroblastoma cell SH-SY5Y, and have anti tumor activity similar to that of a nuclear parent compound diosgenin.

The invention provides a traditional Chinese medicine fermented beverage having efficacy of resisting tumors and a preparation method of the traditional Chinese medicine fermented beverage. The beverage consists of effective components of a Chinese wolfberry fruit and honeysuckle flower co-extract, a sugar solution, lactic acid bacteria, microzyme and acetic acid bacteria, wherein 300mL of the sugar solution, 1*10<3>-1*10<13>CFU of the lactic acid bacteria, 1*10<3>-1*10<13>CFU of microzyme and 1*10<3>-1*10<13>CFU of the acetic acid bacteria are added for every 500mL of the Chinese wolfberry fruit and honeysuckle flower co-extract. The lactic acid bacteria, the microzyme and the acetic acid bacteria are added to a mixed solution of the Chinese wolfberry fruit and honeysuckle flower co-extract and the sugar solution so that the traditional Chinese medicine fermented beverage is prepared. In vitro tests prove that the in vitro 72h suppression ratio of the beverage for HT29 (human colon cancer cell strains), S180 (mouse ascitic type sarcoma cell strains) and HpG2 (human liver cancer cell strains) is notable.

The invention relates to an uvaria macrophylla bisamide derivative and a preparation method and application thereof. The invention has the advantages that: the uvaria macrophylla bisamide derivative is subjected to chemical synthesis and research, and a series of novel uvaria macrophylla bisamide derivatives are synthesized; a novel source is provided for the search of anti-cancer medicaments; as proved by a cytotoxin activity experimental result, the varia macrophylla bisamide derivative has a remarkable inhibiting effect on the growth of human lung adenocarcinoma cells and human colon cancer cells; and in particular, uvaria microcarpa neomycin, 4,4'-di-p-dinitrlbinzene formyl-1,4-butanediamine and 4,4'-di-p-methoxy benzoyl-1,6-hexanediamine have remarkable inhibiting effects on the growth of human lung adenocarcinoma cells, so that application to preparation of anti-cancer medicaments is available.

The invention relates to diterpenoid alkaloid compounds in Aconitum naviculare as well as a preparation method and an application of the diterpenoid alkaloid compounds. According to the method, crude Aconitum naviculare medicine is taken as a raw material and is extracted with a solvent, an extract is subjected to acid dissolution and alkali precipitation, a product is processed with gel Sephadex LH-20 chromatography and reversed-phase RP-18 column chromatography separation, three diterpenoid alkaloid compounds including C40H50N2O4 (1), C47H56N2O5 (2) and C29H37NO3 (3) are obtained after analysis with thin-layer chromatography, in-vitro cytotoxic activity of the three compounds is determined, and test results prove that C47H56N2O5 (2) has anti-tumor activity in human promyelocytic leukemia cells, human hepatoma cells, human lung cancer cells, human breast cancer cells and human colon cancer cells, and can be used for preparing anti-tumor drugs.

The present invention describes a newly discovered human G-protein coupled receptor and its encoding polynucleotide. Also described are expression vectors, host cells, agonists, antagonists, antisense molecules, and antibodies associated with the polynucleotide and/or polypeptide of the present invention. In addition, methods for treating, diagnosing, preventing, and screening for disorders associated with aberrant cell growth, endocrine conditions, neurological conditions, and diseases or disorders related to the pituitary gland, colon, breast, lungs, and prostate are illustrated.

The invention provides a preparation method and application of sea anemone polypeptide toxin, and the preparation method comprises the following steps: 1, extraction of sea anemone crude venom: after live sea anemone is hungry, extracting an aqueous solution containing sea anemone crude toxin by using a manual extrusion method or/and an electrical stimulation method, freeze-drying the aqueous solution containing sea anemone crude toxin, and dialyzing and desalting by using a biological CE membrane dialysis bag; 2, filtering sea anemone crude toxin molecules: centrifuging the extracted sea anemone crude toxin by using an ultrafiltration tube to obtain a filtered component; and 3, purification of the sea anemone toxin: filtering the filtered component obtained in the step 2 through a microfiltration membrane, carrying out gradient elution through a reversed-phase high performance liquid chromatograph to obtain F1-F3 components, collecting the F1 component, and carrying out freeze drying to obtain the purified sea anemone polypeptide toxin, The sea anemone polypeptide toxin prepared by the invention not only can inhibit the activity of colon cancer cells HCT-116, but also can promote the apoptosis of the colon cancer cells HCT-116.

The invention relates to pyridopyrimidine ketones derivatives and application of the pyridopyrimidine ketones derivatives in preparing antitumor drugs, belongs to the chemical pharmaceutical area, particularly relates to application of a compound with a structure shows as formula (I), wherein Ar represents a substituted benzene ring or a heterocyclic ring Het; R1 represents H or CH3; and R2 represents a substituted benzene ring, a heterocyclic ring or alkane. Experiments show that compound with a structure shown as formula (I) has varying degrees of inhibitory activity in vitro to A549 (human lung adenocarcinoma cell), HepG2 (human hepatocellullar carcinoma cell), SKOV-3 (human ovarian neoplasm), Hela (human cervical carcinoma cell) and SW620 (human colonic cancer cell), and in particular has good inhibitory activity to SW620, so that a new choice is provided for preparation of the antitumor drugs.

The invention relates to the technical field of medicines, in particular to linear chain polyketone compounds separated from marine poriferans and application thereof in preparation of medicines for treating tumors, diabetes and obesity or inhibitors for protein tyrosine phosphatase-1B(PTP1B). The in vitro anti-tumor tests and the PTP1B inhibition tests show that the compound C17H32O4 has obvious inhibiting activity on human colon cancer cells HCT-116 and PTP1B, so that the compound can be used for preparing anti-tumor medicines or PTP1B inhibitors and medicines for treating diabetes, obesity and complications caused by diabetes and obesity. The invention provides novel lead compounds for developing new anti-tumor medicines or medicines for treating diabetes and obesity, and has great significance for the development and the utilization of Chinese marine medical biological resources.

The invention discloses application of anti-human immunodeficiency virus (HIV) drug amprenavir in preparation of an antitumor drug. The anti-HIV drug amprenavir identified by food and drug administration (FDA) is taken as a material; the killing effect of the amprenavir on a tumor cell is detected by adopting a microwave theory and techniques (MTT) method. An experiment proves that the amprenavir has a significant inhibiting effect on multiplication of a plurality of tumor cells, such as a breast cancer michigan cancer foundation (MCF-7) cell, a non-small cell lung cancer A549 cell, a mouse embryonic fibroblast glioblastoma multiforme L929 cell, a colon cancer HT29 cell, a brain glioma U87 cell and the like, so as to clarify new use of an old drug. Therefore, foundation is provided for development of a novel anti-tumor drug.