33 results about "Hl60 cells" patented technology

The invention discloses a type of amino acid modified curcumin, a synthesis method thereof, and an application thereof. According to the invention, structural modification is carried out upon curcumin by using natural amino acid, such that 1-(4-hydroxy-3-methoxyphenyl)-7-(4-oxyacetyl amino carbobenzoxy-3-methoxyphenyl)-1,6-heptadiene-3,5-diketone which is represented by a general formula (I) is obtained. With an MTT method, evaluation is carried out upon the compound represented by the general formula (I) in the inhabitance of proliferation activities of four cells which are K562, H22, HL60 and S180. IC50 values of the compound represented by the general formula (I) in inhibiting the proliferations of the four tumor cells are calculated. As a result of experiments, with the compound represented by the general formula (I), proliferations of tumor cells can be substantially inhibited. The compound has excellent anti-tumor activity, and can be prepared into anti-tumor medicines.

The present invention discloses 10-alkoxy camptothecinie derivatives and its preparation process and application in treating tumor. The compounds have extraneous antitumor activity in different degree to P388 human leukemia cell, A649 human lung cancer cell, PC-3 human prostate cancer cell, HO-8910 human oophoroma cell, and K562 and HL60 human leukemia cell. The experiment of inoculating naked mouse with transplanted PC-3 human prostate cancer cell and inoculating mouse with S180 malignant solid tumor shows that partial compounds possess powerful tumor inhibiting activity.

The invention provides 2-arylamine pyrimidine derivatives containing hydroxamic acid fragments shown in the formulas I and II. 2-arylamine pyrimidine containing carboxyl fragments is mainly used as a parent nucleus and is subjected to single-step condensation and related modification with hydroxylamine protected by THP to obtain a target compound. An experiment proves that the derivatives has the remarkable anti-proliferative effect on tumor cells (an overexpression EGFR human epidermal carcinoma cell line A431 and a human pulmonary carcinoma cell line H1975 resisting Gefitinib) related to EGFR tyrosine kinase activity on the cellular level, and tumor cells (a human cervical carcinoma cell line Hela, a human hepatoma cell line HepG2, a human promyelocytic acute leukemia cell line HL60, a human oral epidermoid carcinoma cell line KB, a human colon cancer cell line SW620) related to the HDAC histone acetylase activity, and the corresponding medicine for resisting cancer cells can be prepared. The general structural formula is shown in the description.

The invention relates to the fields of marine organism and medical technology, and provides an aaptamine alkaloid compound which is obtained by extraction, separation and purification from marine Aaptos aaptos produced in sea areas nearby the Paracel Islands, wherein the chemical structure of the alkaloid compound is as shown in the formula (I) (in the specification). In-vitro activity tests prove that the alkaloid compound has remarkable inhibitory activity on various different tumor cells such as human acute leukemic cells HL60, human chronic leukemic cells K562, human breast cancer cells MCF-7, human nasopharyngeal carcinoma cells KB, human liver cancer cells Hep G2 and human colon cancer cells HT-29, and the alkaloid compound can be used for preparing anti-tumor medicines.

The invention relates to the field of genetic engineering, in particular to a novel fungal immunomodulatory protein FIP-NHA with antineoplastic activity and a gene thereof. The fungal immunomodulatory protein FIP-NHA according to the invention has an amino acid sequence as shown in SEQ ID NO. 1, and the gene fip-nha for coding the fungal immunomodulatory protein has a nucleotide sequence as shownin SEQ ID NO. 2. The fungal immunomodulatory protein FIP-NHA provided by the invention has the effects on promoting splenic lymphocyte division, increasing synthesis of interleukin 2, and obviously inhibiting proliferation of three tumor cells including hepatoma cell HepG2, gastric cancer cell MGC823 and leukemia cell HL60, therefore, the fungal immunomodulatory protein FIP-NHA as a novel antineoplastic biological agent can be widely used in the fields of health products and biological medicines.

The invention belongs to the technical field of medicine, particularly discloses a ciprofluoroquinolone C3 / C7 dithizone Schiff base, and meanwhile discloses a preparation method of the ciprofluoroquinolone C3 / C7 dithizone Schiff base and application of the ciprofluoroquinolone C3 / C7 dithizone Schiff base in pharmaceuticals. The chemical structural formula of the ciprofluoroquinolone C3 / C7 dithizone Schiff base is shown in a general formula I, wherein Ar is selected from phenyl, substituted phenyl, heterocyclic aromatic aryl alkyl and substituted heterocyclic aromatic aryl alkyl. Tests show that the ciprofluoroquinolone C3 / C7 dithizone Schiff base provided by the invention has strong in vitro cytotoxic activity to L1210, CHO (Chinese hamster ovary) and HL60 cancer cell strains, has strong antitumor activity, can be used for preparing antitumor drugs with human body acceptable pharmaceutical carrier, and can be further made into human body acceptable pharmaceutical salts for preparing antitumor drugs.

The invention provides application of ZDHHC21 genes in preparation of leukemia induced differentiation therapy drugs, and application of polypeptides targeting the DHHC21 genes, small molecule inhibitors and interfering siRNAs in preparation of leukemia induced differentiation agents. Research shows that as the ZDHHC21 amount is reduced by the RNA interfering technology, the proliferation of leukemia HL60 and NB4 cells is significantly inhibited, the expression of cell surface differentiation-specific antigens CD11b is significantly increased, the reduction ability of NBT of the cells is enhanced, and the ratio of nucleus to cytoplasm in the cells is reduced, the shapes of cell nuclei are changed into U shapes or half-moon shapes. Down-regulation of ZDHHC21 can effectively induce the differentiation of the human leukemia cells, a new direction is provided for the development of treatment drugs for leukemia, a new therapeutic target is provided for induction differentiation therapy of leukemia, and a new research field is opened up for the treatment of leukemia, the improvement of the treatment effect and the improvement of drug resistance.

The invention relates to the technical field of marine organisms and medicines and provides an aaptamine alkaloid compound extracted, separated and purified from a marine animal aaptos originating from surrounding waters of the Xisha Islands. The chemical structure of the aaptamine alkaloid compound is shown in a formula (I) as shown in the specification. In-vitro activity tests prove that the compound has obvious inhibitory activity on various tumor cells such as human acute leukemic cells HL60, human chronic leukemic cells K562, human breast cancer cells MCF-7, human nasopharyngeal cancer cells KB, human liver cancers Hep G2, human colon cancer cells HT-29 and the like and can be used for preparing antitumor medicines.

The invention relates to the fields of marine organism and medical technology, and provides an aaptamine alkaloid compound which is obtained by extraction, separation and purification from marine Aaptos aaptos produced in sea areas nearby the Paracel Islands, wherein the chemical structure of the alkaloid compound is as shown in the formula (I) (in the specification). In-vitro activity tests prove that the alkaloid compound has remarkable inhibitory activity on various different tumor cells such as human acute leukemic cells HL60, human chronic leukemic cells K562, human breast cancer cells MCF-7, human nasopharyngeal carcinoma cells KB, human liver cancer cells Hep G2 and human colon cancer cells HT-29, and the alkaloid compound can be used for preparing anti-tumor medicines.

The invention discloses the application of a As2O3 combined TSA in preparing drugs to induce the change of leukemia HL60 cells from partial differentiation to terminal differentiation. The concentration of the As2O3 combined TSA in preparing drugs to induce the change of leukemia HL60 cells from partial differentiation to terminal differentiation is: 0.25 to 0.5 Mu M of As2O3; 0.1 to 0.2 Mu M of TSA. In the aspect of drug combination to induce the change of leukemia HL60 cells from partial differentiation to terminal differentiation, the drug laid basis for clinical drug combination therapy to induce leukaemia differentiation.

The invention provides an amide bond containing heterocyclic compound, a preparation method and application thereof. Specifically, the amide bond containing heterocyclic compound has a structural general formula shown as the specification. Cellular level experiments find that the amide bond containing heterocyclic compound provided by the invention can inhibit proliferation of K562-3d, HL60, and KG1a cells, especially the example 1-5 compounds (compounds 7a to 7e) also can realize the effect of inhibiting the proliferation of K562-3d, HL60, and KG1a cells under a drug concentration lower than that of the positive control drug imatinib. Therefore, the amide bond containing heterocyclic compound provided by the invention can be used for treating leukemia.

The invention discloses an anti-tumor Chinese medicine extract, a preparation method and an application thereof; pulverized clematis terniflora is used or a clematis terniflora decoction piece is directly adopted, added with water or ethanol, heated, treated with reflux extraction for 2-5 times and then filtered; extract is merged, filtered or centrifugated, and then passes through macroporous resin; then water is firstly used for washing the resin, the water eluent is removed, then hydrous ethanol with the volume percentage of 30-95% is used for eluting, and the ethanol eluent is collected and concentrated into thick paste under reduced pressure, the thick paste undergoes decompressed concentration or spray drying so as to obtain the clematis terniflora extract which contains flavone and rutin no less than 20% and 0.1% respectively. The extract of the invention shows good in vitro inhibiting effect on the proliferation of leukemia Molt-4 cell strain, leukemia cell HL60, cerebral cancer U251 cell strain, esophagus cancer Eca-109 cell strain as well as liver cancer BEL-7402 cell strain. The anti-tumor Chinese medicine extract can be used for preparing the medicines for treating tumor, especially digestive system malignant tumor and the like diseases.

The invention discloses a GM-CSF target-direction drug liposome and preparing method of anti acute leukemia myelomatosis, which is composed of cytokine guiding matter with initiative target-tropism connecting to the surface of liposome and anti acute leukemia myelomatosis drug in liposome. The external model MTT of the invention experiments and checks the toxic effect on the cell of acute leukemia myelomatosis cell strain HL60 and the effect on cell death. The method improves the curative effect, which reduces the cost.

The invention provides 2,4-diarylamine pyrimidine derivatives containing hydroxamic acid fragments shown in formulas I and II. 2,4-diarylamine pyrimidine containing carboxyl fragments is mainly used as a parent nucleus and is subjected to single-step condensation and related modification with hydroxylamine protected by THP to obtain a target compound. An experiment proves that the remarkable anti-proliferative effect is achieved for tumor cells (a human lung adenocarcinoma cell line H1975 and an overexpression EGFR human epidermal carcinoma cell line A431) related to EGFR tyrosine kinase activity on the cellular level, and a human cervical carcinoma cell line Hela, a human oral epidermoid carcinoma cell line KB, a human promyelocytic acute leukemia cell line HL60, a human hepatoma cell line HepG2, a human colon cancer cell line SW620 and other tumor cells related to the HDAC histone acetylase activity, and the corresponding medicine for resisting cancer cells can be prepared. The general structural formula is shown in the description.

The invention provides a preparation method of an anticancer polysaccharide composition with an excellent anticancer effect. The polysaccharide composition prepared from a flammulina velutipes and radices lithospermi mixture by ultrasonic enzymolysis, and water extraction and alcohol precipitation disclosed by the invention shows excellent inhibiting rate on S180, HL60, A546 and H22, and excellent anticancer effect; the inhibiting rate is obviously superior to that when the flammulinan and lithosperman are independently used; and the anticancer polysaccharide composition can be applied to prevention and treatment of solid tumors and / or blood tumors.

The invention relates to a novel amino / acyl substituted β-carboline compound, a preparation method and application of antitumor activity. The invention transforms the structure of the gamma-carboline mother core to obtain the beta-carboline derivatives with basic side chain substitution. The compound of the present invention shows good antitumor activity through pharmacodynamic HL60 human leukemia and P388 mouse leukemia cell line antitumor activity tests, and can prepare novel antitumor drugs.

The invention provides sulfonyl piperazine containing coumarin pyrazole compounds. The compounds have a general formula shown in the specification, wherein R is shown in the specification. Experiments prove that the sulfonyl piperazine containing coumarin pyrazole compounds have different levels of inhibiting effects on human colon carcinoma cell lines HCT-116, human lung cancer cell lines A549, liver cancer cells Huh7 and human spinal cord leukemia M3 cell lines HL60, so that the compounds can be possibly used for preparing anti-cancer drugs. The invention discloses a preparation method of the sulfonyl piperazine containing coumarin pyrazole compounds.

The invention provides 2,4-diarylamine pyrimidine derivatives containing hydroxamic acid fragments shown in formulas I and II. 2,4-diarylamine pyrimidine containing carboxyl fragments is mainly used as a parent nucleus and is subjected to single-step condensation and related modification with hydroxylamine protected by THP to obtain a target compound. An experiment proves that the remarkable anti-proliferative effect is achieved for tumor cells (a human lung adenocarcinoma cell line H1975 and an overexpression EGFR human epidermal carcinoma cell line A431) related to EGFR tyrosine kinase activity on the cellular level, and a human cervical carcinoma cell line Hela, a human oral epidermoid carcinoma cell line KB, a human promyelocytic acute leukemia cell line HL60, a human hepatoma cell line HepG2, a human colon cancer cell line SW620 and other tumor cells related to the HDAC histone acetylase activity, and the corresponding medicine for resisting cancer cells can be prepared. The general structural formula is shown in the description.

An oral biology model which comprises biofilm, oral epithelial tissue and a suspension of neutrophil-like cells in media is disclosed. The biofilm, which comprises oral bacteria, is produced by culturing oral bacteria on a solid substrate. The oral epithelial tissue may be gingival epithelial tissue to model the gingival crevice or buccal epithelial tissue to model the oral check. The suspension of neutrophil-like cells in media comprises neutrophil-like cells that are differentiated HL60 cells induced to a neutrophil-like phenotype by treatment with retinoic acid. Methods of using the oral biology model to test and compare compounds and formulations or to screen compounds and formulations for their effect on release of inflammatory signals, their effect on biofilm and oral bacteria and / or their effect on the cellular components are disclosed.

The invention discloses 14 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters shown in the general formula I. In the general formula I, AA represents L-Ser residue, L-Glu (OBzl) residue, L-Phe residue, L-Val residue, L-Arg residue, L-Tyr residue, L-Ala residue, L-Trp residue, L-Asn residue, L-Met residue, L-Ile residue, Gly residue, L-Asp (OBzl) residue or L-Leu residue. The invention discloses a preparation method of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters, discloses HT-29, K562, A549 and HL60 tumor cell growth inhibition effects of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters, further discloses S180-loading mice tumor growth inhibition effects of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters, and also discloses use of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters as antitumor drugs.

The invention provides a heterocycle compound containing triazole, as well as a preparation method and application of the heterocycle compound. The heterocycle compound containing the triazole has a general formula in the following structure (as shown in the description). Cellular level experiments indicate that the heterocycle compound containing the triazole provided by the invention can restrain the proliferation of K562-3d cells, HL60 cells and KG1a cells, and particularly under the situation that the medicine concentration is lower than that of a positive control medicine namely Imatinib, a compound (compound 15c) in an example 3 can also realize the effect of restraining the proliferation of the K562-3d cells, the HL60 cells and the KG1a cells, so that the heterocycle compound containing the triazole provided by the invention can be used for treating leukaemia.

The invention discloses targeting antineoplastic fusion protein LPO. An artificially synthesized target gene segment LHRH-PEA wiped membrane peptide-ONC (LPO for short) is inserted in PET28a plasmids, and the fusion protein is expressed after the LPO inserted the plasmids are conveyed in escherichia coli BL21(DE3). Experiments prove that the fusion protein LPO has obvious inhibiting effect to tumor cell lines with LHRH receptors such as colon cancer LOVO cells, lung cancer A549 cells, oral cancer KB cells and prostatic cancer PC-3M cells rather than lymphoma Hut 102 and leukemia HL60 without LHRH receptors, and has targeting specificity, and is safe and reliable.

The invention provides oxadiazole-containing heterocyclic compounds, and a preparation method and an application thereof. The oxadiazole-containing heterocyclic compounds have a structural general formula shown in the description. Cell level experiments find that the oxadiazole-containing heterocyclic compounds can inhibit proliferation of K562-3d, HL60 and KG1a cells, and especially the compound (compound 10c) in the embodiment 11 also realize K562-3d, HL60 and KG1a cell proliferation inhibition effects when the concentration of the compound 10c is lower than a that of a positive control medicine imatinib, so the oxadiazole-containing heterocyclic compounds can be used for treating leukemia.

The invention provides 2-arylamine pyrimidine derivatives containing hydroxamic acid fragments shown in the formulas I and II. 2-arylamine pyrimidine containing carboxyl fragments is mainly used as a parent nucleus and is subjected to single-step condensation and related modification with hydroxylamine protected by THP to obtain a target compound. An experiment proves that the derivatives has the remarkable anti-proliferative effect on tumor cells (an overexpression EGFR human epidermal carcinoma cell line A431 and a human pulmonary carcinoma cell line H1975 resisting Gefitinib) related to EGFR tyrosine kinase activity on the cellular level, and tumor cells (a human cervical carcinoma cell line Hela, a human hepatoma cell line HepG2, a human promyelocytic acute leukemia cell line HL60, a human oral epidermoid carcinoma cell line KB, a human colon cancer cell line SW620) related to the HDAC histone acetylase activity, and the corresponding medicine for resisting cancer cells can be prepared. The general structural formula is shown in the description.

The invention provides a preparation method of a polysaccharide composition with excellent anticancer effect. The polysaccharide composition extracted from the mixture of Flammulina velutipes and Zicao by ultrasonic enzymolysis, water extraction and alcohol precipitation of the present invention shows significantly better inhibition rates to S180, HL60, A546 and H22 when the polysaccharides of Flammulina velutipes and Zicao polysaccharides are used alone, showing Excellent anti-cancer effect, can be used for the prevention and treatment of solid tumors and / or hematological tumors.

The invention relates to the technical field of medicines, in particular to a novel dinaphthaline spiro bruguiera gymnorrhiza 5 (BG5) compound separated from bruguiera gymnorrhiza in China, a preparation method of the novel dinaphthaline spiro bruguiera gymnorrhiza 5 (BG5) compound and application of the novel dinaphthaline spiro bruguiera gymnorrhiza 5 (BG5) compound to tumor treatment. The bruguiera gymnorrhiza 5 (BG5) disclosed by the invention has a structural formula shown in the description. Verified by tests, the compound has remarkable inhibitory activities for HL60 human leukemia cells and MCF (Macrophage Chemotatic Factor)-7 human breast cancer cells.

The invention discloses a GM-CSF target-direction drug liposome and preparing method of anti acute leukemia myelomatosis, which is composed of cytokine guiding matter with initiative target-tropism connecting to the surface of liposome and anti acute leukemia myelomatosis drug in liposome. The external model MTT of the invention experiments and checks the toxic effect on the cell of acute leukemia myelomatosis cell strain HL60 and the effect on cell death. The method improves the curative effect, which reduces the cost.