58 results about "Nci h460" patented technology

The invention discloses a new platinum (II) complex of 6-amino oxoisoaporphine, namely monochloro.dimethyl sulfoxide.6-amino oxoisoaporphine platinum (II), and a synthesis method and an application thereof. The complex is synthesized by the steps of dissolving 6-amino oxoisoaporphine and dichloro.di(dimethyl sulfoxide) platinum (II) in a polar solvent, and heating or carrying out a reflux reaction to obtain the target product; specifically the complex can be synthesized by a solution method, and can also be synthesized by a solvothermal method. Through investigation of proliferation inhibitory activity of the complex against HepG2, BEL-7404 and NCI-H460 and other human tumor cell strains, the complex is found to have significant in-vitro antitumor activity against the 3 kinds of tumor strains and have relatively good potential medicinal value, and is expected to be used in preparation of various antitumor medicines. The complex has the chemical structure represented by the following formula as described in the specification.

The invention discloses a platinum (II) metal complex for specifically inhibiting proliferation of a lung carcinoma cell, and a synthesis method and an application thereof. The structural formula of the platinum (II) metal complex for specifically inhibiting the proliferation of the lung carcinoma cell is as shown in formula (I). The synthesis method of the platinum (II) metal complex for specifically inhibiting the proliferation of the lung carcinoma cell includes: fetching a compound as shown in following formula (II) and dichlorodi(dimethyl sulfoxide)platinate(II), dissolving the compound and the dichlorodi(dimethyl sulfoxide)platinate(II) in polar solvent, reacting under a heating or non-heating condition, and then obtaining reaction liquid containing the target product. The metal complex can specifically inhibit the proliferation of the lung carcinoma cell NCI-H460, and IC50 (half maximal inhibitory concentration) value is up to 5.01+/-0.54 microns, and the metal complex embodies good potential pharmaceutical value, and is hopefully used in preparation of specific lung cancer resisting pharmaceuticals. The formula (I) and the formula (II) show structures as follows.

The invention relates to an application of a flavonoid compound, the flavonoid compound is 3, 3', 4', 5, 7-pentahydroxyflavone dihydrate, the ELISA and protein fluorescence quenching experiments provethat the compound can effectively inhibit interaction of PD-1/PD-L1 proteins, and has a strong affinity for PD-L1 protein. Cell clone number formation and ELISA detection of IL-2 secretion assay prove that the compound can effectively enhance the tumor killing activity of T lymphocyte Jurkat cells against MDA-MB-231 and NCI-H460 tumor cells as well as the expression level of IL-2, and then reverse T cellular immunosuppression. The research results of the application provide a drug for tumor immunotherapy targeting the PD-1/PD-L1 immunological test site.

The invention discloses a marine bacillus polypeptide and a preparation and an application thereof and belongs to the technical field of marine microorganism medicines. The marine bacillus polypeptide is from metabolites of antarctic marine bacillus N11-8 subjected to fermentation cultivation; 15 amino acid sequences at N-ends of the active polypeptide are ASTGSQKVTVYAVAD; the active polypeptide has relatively high cytotoxicity to a plurality of tumor cells such as human hepatoma carcinoma cell BEL-7402, human ovarian carcinoma cells NIH:OVCAR-3, human renal clear cell carcinoma cells 786-0 and human large cell lung cancer cells NCI-H460, and has relatively good research and application value. The polypeptide can be applied to medicines for preventing and/or treating the cancers.

The invention discloses a compound Chinese actinidia root Chinese medicinal composition and a preparation method and application thereof, belonging to the technical field of traditional Chinese medicines. The Chinese medicinal composition is characterized by comprising the following traditional Chinese medicines in parts by weight: 40-80 parts of Chinese actinidia root, 20-40 parts of salvia chinensis, 20-40 parts of herba scutellariae barbatae, 20-40 parts of herba oldenlandiae and 20-40 parts of giant knotweed. The compound Chinese actinidia root Chinese medicinal composition has remarkable proliferation inhibition effects on various cancer cells such as a hepatoma cell line Hep-G2, a lung cancer cell line NCI-H460, a gastric cancer cell line MGC-803, a breast cancer cell line MCF-7, a colon cancer cell line HCT-116 and the like, and can be used for reducing physical and psychological pains of a cancer patient in the chemo-treatment process and solving the problems of difficult and expensive administration.

The invention discloses two novel ruthenium and rhodium metal complexes taking lysicamine as ligands as well as a synthetic method and application of the two novel ruthenium and rhodium metal complexes. The synthetic method of the ruthenium and rhodium metal complexes comprises the following steps: dissolving dichloro.tetra(dimethyl sulfoxide) ruthenium (II) or rhodium trichloride and lysicamine into a polar solvent, and performing complexation reaction to prepare the ruthenium and rhodium metal complexes, wherein the ruthenium and rhodium metal complexes can be synthesized by virtue of solution methods or solvothermal methods. After the applicants investigate the proliferation inhibition activity of the ruthenium and rhodium metal complexes on human tumor cell lines such as NCI-H460, HepG-2, DLD-1 and MGC80-3 and the toxicity of the ruthenium and rhodium metal complexes to human normal liver cells HL-7702, results show that the ruthenium and rhodium metal complexes have significant in-vitro anti-tumor activity, and the activity of a rhodium metal complex is equal to that of cis-platinum; moreover, the ruthenium and rhodium metal complexes have relatively low cytotoxicity to normal cells, have good potential medicinal values, and are expected to be applied to the preparation of various anti-tumor medicines; and structural formulas of the complexes are respectively shown in the following formula (I) and formula (II) in the specification.

The invention discloses an acridine-1,2,4-triazole-5-thioketone compound and a preparation method and applications of the acridine-1,2,4-triazole-5-thioketone compound. The preparation method of the compound comprises the following steps: 1) by taking an o-bromobenzoic acid and p-methoxyaniline as raw materials, taking potassium carbonate and copper powder as catalysts, and taking isopentyl alcohol or n-amyl alcohol as a solvent, reacting so as to obtain a compound 1; 2) carrying out cyclization on the compound 1 by using phosphorus oxychloride so as to obtain a compound 2; 3) after the compound 2 is dissolved by using an organic solvent, in the presence of tetrabutylammonium bromide, reacting the dissolved compound 2 with sodium sulfocyanate so as to obtain a compound 3; 4) after the compound 3 is dissolved by using an organic solvent, reacting the dissolved compound 3 with m-nitrobenzoylhydrazine so as to obtain a compound 4; and 5) reacting the compound 4 with sodium carbonate, carrying out suction filtration on a reactant, collecting filter liquor, adjusting the pH value of the filter liquor to be less than 4, separating out precipitates, and carrying out suction filtration on the precipitates. In-vitro antitumor test results show that the compound has a significant in-vitro antitumor activity to tested MGC80-3, NCI-H460 and T24.

The invention belongs to the field of chemical pharmaceutical technology, particularly relates to drug design of the traditional Chinese medicine extract shikonin serving as a lead compound and related research of anti-tumor activity. Carbohydrates are led into the framework molecule of the shikonin by means of chemical synthesis so as to obtain carbohydrate derivative with novel structure, and the research of in-vitro anti-tumor activity shows that the inhibition activity of the glycosyl shikonin on tumor cell A549 is obviously better than that of NCI-H460. From the activity result, the glycosyl shikonin can be prepared into anti-tumor medicament with high effect and low toxicity.

The invention discloses a monocarbonyl curcumin analogue, a preparation method and application thereof. The analogue has the structural features of general formula (I), wherein R is fluorine, the substitution positions of R are 2, 3, and 4-positions, and the two benzene rings pass through 1,4-pentadien-3-one connect. The invention uses o-, m-, p-fluorine substituted benzaldehyde as raw materials to generate monocarbonyl curcumin analogs through condensation with acetone. The stability of 2,2'-fluoromonocarbonyl curcumin in medium containing 10% serum is better than that of natural product curcumin. The results of pharmacological experiments showed that the anti-proliferation activity of fluorine-substituted monocarbonyl curcumin on human lung cancer NCI-H460 cells was significantly superior to that of natural product curcumin, and 2,2'-fluoro monocarbonyl curcumin could lead to cell proliferation by promoting the production of reactive oxygen species. Redox imbalance, lipid peroxidation, breakdown of mitochondrial membrane potential, and apoptosis in the body can be used as curcuminoid leads for the treatment of lung cancer.

The invention discloses a preparation method for isochromophilone VIII and application of the same in preparation of antineoplastic drugs. According to the invention, isochromophilone VIII with antineoplastic activity is isolated from a liquid fermentation culture of the marine fungus Penicillium sp. FS60. According to results of experiments, it is found that the IC50 values of isochromophilone VIII in inhibiting SF-268 cells, MCF-7 cells and NCI-H460 cells are 7.17, 6.36 and 22.27 mu g/mL, respectively; and isochromophilone VIII has significant antineoplastic activity. The invention providesa candidate drug for research and development of novel antineoplastic drugs and scientific bases for development and utilization of marine microbial resources.

The invention discloses a phthalizine [1,2,b] quinazoline-8-ketone compound, which is characterized in that the structural general formula of the compound is shown in the description, and phthalizine [1,2,b] quinazoline-8-ketone derivatives disclosed by the invention have very strong inhibiting effect on common cancer cells such as human gastric carcinoma cells (MGC-803), human lung cancer cells (NCI-H460), human hepatoma cells (HepG-2), cervical carcinoma cells (Hela), human bladder cancer cells (T-24) and the like, can induce apoptosis of the cancer cells, hence the phthalizine [1,2,b] quinazoline-8-ketone and derivatives thereof have potential application in preparation of antitumor drugs.

The invention provides a preparation method for a Sanhuang tablet. The Sanhuang tablet is prepared from the bulk drugs consisting of 300 g of rhubarb root and rhizome, 5 g of berberine hydrochloride and 80 g of baical skullcap root extract through supercritical extraction, so the content of Sanhuang tablet is greatly increased, and the dose of the Sanhuang tablet is reduced. The invention further provides application of the Sanhuang tablet in preparation of drugs used for inhibiting cell proliferation of human large cell carcinoma NCI-H460.

The invention discloses application of Lycojaponicumin A in preparation of medicaments for treating lung cancer. The compound shows good anti-lung cancer activity, can be used for preparing anti-lung cancer medicaments, and belongs to the technical field of new application of medicaments. The Lycojaponicumin A can prominently inhibit non-small cell lung cancer cells A549, large cell lung cancer cells NCI-H460, lung squamous cancer cells HTB-8 and human lung flat epithelial cancer cells QG-5 cultured in vitro, has a low inhibiting effect on human normal liver cells LO2 and peripheral blood lymphocytes, and shows obvious selectivity. The application of the Lycojaponicumin A in preparation of the medicaments for treating the lung cancer is made public for the first time; and because the skeleton type is completely novel, the Lycojaponicumin A has an unexpectedly strong lung cancer cell inhibiting activity.

The invention discloses an application of Lycojaponicumin B in preparation of a medicine for treating lung cancer. The compound, namely the Lycojaponicumin B shows high lung cancer resisting activity, can be used for preparing a lung cancer resisting medicine and belongs to the technical field of new applications of medicines. The Lycojaponicumin B can obviously inhibit the non-small-cell lung cancer cell A549, maxicell lung cancer cell NCI-H460, squamous cell lung cancer cell HTB-8 and human lung squamous epithelium cancer cell QG-5 cultured in vitro while realizing a relatively low effect on inhibiting the human normal liver cell LO2 and the peripheral blood lymphocyte cell, thereby showing obvious selectivity. The application of the Lycojaponicumin B in preparation of the medicine for treating lung cancer is disclosed for the first time; the skeleton type of the Lycojaponicumin B belongs to a brand new skeleton type, and the inhibitory activity of the Lycojaponicumin B on lung cancer cells is unexpectedly strong.

The invention discloses application of Chukrasone A in preparation of medicaments for treating lung cancer. The compound shows excellent activity for resisting lung cancer, can be used for preparing medicaments for resisting lung cancer, and belongs to the technical field of novel application of medicaments. Chukrasone A can remarkably inhibit in vitro cultured non-small cell lung cancer cells A549, large cell lung cancer cells NCI-H460, squamous cell lung carcinoma cells HTB-8 and human lung epidermoid carcinoma QG-5, but hardly has inhibition effects on human normal hepatocytes LO2 and peripheral blood lymphocytes, and shows a remarkable selectivity. The application of Chukrasone A in preparation of medicaments for treating lung caner is disclosed for the first time, and the frame type belongs to a brand-new frame type, so that the inhibition activity of the Chukrasone A to lung cancer cells is unexpectedly strong.

The invention discloses an application of polyflavanostilbene A in preparation of medicaments for treating lung cancer. The compound shows good anti-lung cancer activity, can be used for preparing anti-lung cancer medicaments and belongs to the technical field of new uses of the medicaments. The polyflavanostilbene A can significantly inhibit non-small cell lung cancer cells A549, large cell lung cancer cells NCI-H460, lung squamous carcinoma cells HTB-8 and human lung squamous cell carcinoma cells QG-5, which are cultured in vitro, realize a smaller inhibition effect against human normal liver cells LO2 and peripheral blood lymphocytes and show obvious selectivity. The use of the polyflavanostilbene A in the preparation of the medicaments for treating the lung cancer, disclosed by the invention, belongs to the first disclosure, the framework type belongs to the brand new framework type, and the strong inhibition activity against the cells of the lung cancer is further unexpected.