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 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 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 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.