593 results about "Human lung cancer" patented technology

The present invention relates to a pentacyclic triterpanoid derivative of multiple-oxide substitution of the A ring and the C ring and the medicine salt or solvate of the derivative, and the present invention also relates to the preparation method, the drug combination, and medical use of the derivative. The compound of the present invention has the functions of inhibiting the activity of six human tumor cell strains in vitro, such as human prostate cancer cell (PC-3), nasopharyngeal carcinoma cells (CNE), oral squamous carcinoma cell(KB), human lung cancer cell (A549), human hepatoma cell (BEL-7404), and human cervix cancer cell (Hela), and the function of the invention is at the same magnitude of the positive control of cisplatin, thereby the compound can be used as expected antitumor drug. The compound of the present invention also inhibits the alpha glucosidase strongly, and the inhibiting effect is greater than the positive control of acarbose, thereby the compound can be used as expected medicine for preventing and treating diabetes and the treatment of the virus diseases.

A 3-methoxy-flavone compound comprises 5,7-dihydroxy-8-(3,3-dimethyl diallyl)-3,3', 4'-trimethoxy flavone and 5, 7-2 dihydroxy-8- (3,3-dimethyl allyl)-3,4'-dimethoxy flavonoe. harmacological test results prove that: the 3-methoxy-flavone compound is an effective fatty acid synthase inhibitor, which shows the broad-spectrum anti-tumor effect in the cytotoxicity tests of various tumor cell lines and has strong tumor growth inhibiting effect on human prostate cancer cell LnCAP, human breast cancer cell ZR-75-1, human lung cancer cell NCI-H23 or human colon cancer cell HCT-116 when applied to human tumor transplant nude mice model tests. In addition, the 3-methoxy-flavone compound reveals no toxicity in mice acute toxicity tests, which then can be used as anti-tumor drug and is a new broad-spectrum anti-tumor drug with great development prospects.

The invention discloses a ganoderan extraction method and a ganoderan use. The ganoderan extraction method utilizes an ultrasonic enzyme method to realize ganoderan extraction and comprises ganoderma lucidum crushing, extraction, ultrafiltration, condensation and ethanol precipitation separation. The ganoderan extraction method has a ganoderan extraction rate of 3.14 to 4.21%. The ganoderan obtained by the ganoderan extraction method has molecular weight less than 10000 dalton and is light brown. The ganoderan extraction method has simple extraction separation processes and is suitable for industrial production. Ganoderan has strong antioxidant activity and anticancer activity. In a DPPH. free radical system, IC50 of ganoderan is in a range of 0.28 to 0.43mg / mL and an ORAC value of ganoderan is in a range of 1207.66 to 1777.90 micromole Trolox / g. When a concentration of ganoderan is 2mg / ml, ganoderan has a human lung cancer cell A549 inhibition rate of 53.04 to 68.37 and can be used for preparation of an anticancer drug.

The invention discloses polypeptide for specifically targeting a lung cancer cell and an application thereof. The polypeptide for specifically targeting the lung cancer cell has an amino acid sequence shown as SEQ ID NO.1, and is prepared by screening on the surface of the human lung cancer cell by an ex-vivo bacterial random polypeptide library exhibiting method and a flow cell sorting method. The polypeptide for specifically targeting the lung cancer cell can be applied to preparation of lung cancer diagnosing tracer, lung cancer cell detecting reagent and the like. The polypeptide for specifically targeting the lung cancer cell can be combined with a lung cancer A549 cell specifically, is not combined with a normal lung cell and other tumor cells; and the preparation method is simple, feasible and applicable to large-scale industrial production. The polypeptide for specifically targeting the lung cancer cell provides important theoretical and practical basis for early diagnosis, targeting therapy of the lung cancer and the like, and has a wide application prospect.

The invention discloses 4-alkyl-2-arylamino-5-(1,2,4-triazole-1-group) thiazole and salts thereof shown in a formula I, wherein R is selected from H, alkyl groups of C1-C2 and straight-chain alkyl groups or branched-chain alkyl groups of C3-C4; X1, X2, X3, X4 and X5 are selected from hydrogen, alkyl groups of C1-C2, hydroxide group, methoxy group, oxyethyl group, trifluoromethyl, fluorine, chlorine, bromine, nitryl, amino group, acetyl amino group, methanesulfamide, ethoxycarbonyl or carboxyl; and the salts of the 4-alkyl-2-arylamino-5-(1,2,4-triazole-1-group) thiazole are selected from hydrochloride, hydrobromide, nitrate, sulfate, phosphate, mesylate, p-toluene sulfonate, tartrate, lactate or malate. The 4-alkyl-2-arylamino-5-(1,2,4-triazole-1-group) thiazole is applied to preparation of medicaments for resisting cervical cancer or lung neoplasms.

The invention discloses 3-phenylcoumarin robustic acid as well as an extraction method and application thereof. 3-phenylcoumarin robustic acid has a structural formula as shown in the specification as well as a chemical name of 3-(p-methoxyphenyl)-4-hydroxy-5-methoxy-2', 2'-dimethyl-6,7-dihydropyrancoumarin, a molecular formula of C22H20O6, and relative molecular weight of 380. 3-phenylcoumarin robustic acid disclosed by the invention has anti-tumor and other biological activities, can be effectively applied in preparation of anti-tumor drugs and has very strong inhibition effect on human gastric cancer cells, liver cancer cell lines, human lung cancer cells, cervical cancer cells, ovarian cancer cells and the like, the extraction method is simple and feasible and the extraction efficiency is relatively high.

The invention discloses rubescensin A derivatives and a preparation method and applications thereof. The rubescensin A derivatives have structures represented by formulas (I), (II), (III), or (IV). Onthe premise that the active center of rubescensin A is not destroyed, the hydroxyl groups on the 1st, 6th, and 14th positions or the hydroxyl groups on the 6th and 7th positions are subjected to ringchange modification; and obtained rubescensin A derivatives have higher antitumor activity, higher intercellular selectivity, lower dosage, and lower toxicity. Compared with that of rubescensin A, the performance of rubescensin A derivatives on killing cancer cells of human liver cancer, human multiple myeloma, human lung cancer, and the like, is enhanced by 3 to 5 times; the optimal performancecan be strengthened by 11 times; and the rubescensin A derivatives can be used to prepare antitumor drugs for treating liver cancer, rubescensin A derivatives, lung cancer, and the like.

The invention provides a peripheral blood mRNA marker for predicting prognosis of patients with lung adenocarcinoma and a screening method and application thereof and belongs to the technical fields of medical molecular biology and clinical medicine. The screening method includes the steps of 1), comparatively analyzing gene expression profiles of wild-type human lung cancer cell lines and Nrf2 gene knockout human lung cancer cell lines to obtain Nrf2 target genes; 2), analyzing the relationship between Nrf2 target gene expression and the prognosis survival rate of lung adenocarcinoma by the aid of a discovery group database and screening out the genes with the Nrf2 target gene expression Wald statistics greater than 2 in the discovery group database to obtain the periphery blood MRNA marker for predicting prognosis of the patients with the lung adenocarcinoma. The marker obtained with the screening method is applied to predicting prognosis of the patients with clinical lung adenocarcinoma, good flexibility, stability and specificity are achieved, and spreading use can be realized.

The invention provides nucleic acids, peptides, and antibodies for use in applications including diagnosis and therapy. The peptides target neovasculature and were identified by in vivo phage display. One such peptide, SP5-52, recognized the neovasculature of multiple tumors in SCID mice, but did not target normal blood vessels. This peptide also binds to blood vessels of human lung cancer biopsy specimens. Liposomes comprising SP5-52 and doxorubicin enhanced the efficacy of the drug against multiple human cancer xenografts in SCID mice.

The invention discloses a raja porosa cartilage polypeptide angiogenesis inhibitory factor and a preparation method and application thereof. The amino acid sequence of the polypeptide angiogenesis inhibitory factor is Gly-Glu-Glu-Gly-Thr-Met-Gly-Leu (GEEGTMGL), and in ESI / MS detection, a molecular ion peak of m / z 793.11 Da ([M+H]<+>) is given out; the raja porosa cartilage polypeptide angiogenesis inhibitory factor Gly-Glu-Glu-Gly-Thr-Met-Gly-Leu (GEEGTMGL) can effectively inhibit angiogenesis of a chick chorioallantoic membrane (CAM) and proliferation of a human lung cancer cell A-549 and a human hepatoma cell line Bel-7402. The raja porosa cartilage polypeptide angiogenesis inhibitory factor Gly-Glu-Glu-Gly-Thr-Met-Gly-Leu (GEEGTMGL) can be used for preparation of drugs for inhibiting angiogenesis and preventing and treating tumors.

The invention discloses brefeldin A ester derivatives, and preparation and application thereof. The brefeldin A ester derivative compounds have antioxidation activity and antitumor activity, wherein the brefeldin A ester derivative compound disclosed as Formula (I-1), (I-3), (I-5) or (I-7) has favorable antioxidation effect and can remove DPPH, ABTS and super oxygen free radical (O2<->), and the compound (I-7) has better removal effect on DPPH, ABTS and super oxygen free radical (O2<->) than vitamin E; and the compound disclosed as Formula (I-1), (I-3), (I-5) or (I-7) has favorable inhibition activity for human lung cancer cells A549. Therefore, the result shows that the derivatives have wide application prospects in the drug development system, provide a new and broader idea for synthesizing and screening BFA (brefeldin A) derivative drugs and provide a more efficient way for treating related diseases.

The invention belongs to the field of drugs, and relates to an antineoplastic drug, particularly an indazole / azaindazole-based diarylcarbamide / thiocarbamide-structure antineoplastic drug. The structural general formulae of the indazole / azaindazole-based diarylcarbamide / thiocarbamide-structure antineoplastic drug are disclosed as Formula (Ia) and (Ib), wherein Z is an N or C atom; W is an atom or group, such as O, S, NH, NOH, NCH or the like; M is O, S, N, CH or the like; n is 1 or 2; and Y and R are respectively halogen atom, H, R1, CF3, OCF3, OH, OR2, OCOR3, NH2, NHR4, NR52, NHCOR6, carboxy group, ester group, cyano-group, sulfhydryl group, alkylthio group, sulfuryl group, sulfoxide group, sulfo-group, sulfonate group, sulfamide group, ketone group, aldehyde group, nitro-group or nitroso-group. The pharmacological experiment proves that the drug has favorable antineoplastic effect on human lung cancer, human kidney cancer, human colon cancer, human liver cancer, human stomach cancer and human breast cancer.

The invention belongs to the field of cell biology, and discloses a human lung cancer cell line. The present invention also discloses a construction method for the cell line and a use of the cell line. The human lung cancer cell line provided by the present invention has characteristics of high chromosome integration, high fluorescence intensity, stable genetic character and sensitivity to the lung cancer drug, and is an ideal study model for screening the lung cancer drugs.

The invention discloses shell-broken ganoderma spore powder and particle combination and a preparation method thereof. Shell-broken ganoderma spore powder is extracted, centrifuged, concentrated, dried and crushed to obtain the shell-broken ganoderma spore powder and particle combination, the content of crude polysaccharide in the shell-broken ganoderma spore powder and particle combination is 10-20g / 100g, and the content of total triterpene in the shell-broken ganoderma spore powder and particle combination is 4-10g / 100g. The shell-broken ganoderma spore powder and particle combination has the advantages that immunities are enhanced, radiation hazards are reduced in an auxiliary manner, the shell-broken ganoderma spore powder is treated by the aid of a special process, the content of effective components are increased, nutrient components in the effective components can be effectively absorbed by human bodies, functions of the shell-broken ganoderma spore powder are effectively played, the shell-broken ganoderma spore powder is conveniently carried and taken, the shell-broken ganoderma spore powder and particle combination has an inhibiting effect on zebra fish human stomach cancer transplantation tumors, human lung cancer transplantation tumors and human lymphocyte cancer transplantation tumors, and the shell-broken ganoderma spore powder and particle combination has a strong inhibiting effect on the zebra fish human stomach cancer transplantation tumors and the human lymphocyte cancer transplantation tumors.

The invention discloses a compound with antitumor activity and a preparation method and application of the compound and belongs to the technical fields of new compound synthesis and medicine application. According to the compound, the preparation and the application thereof disclosed by the invention, aromatic aldehyde and aromatic ketone are catalyzed by sodium hydroxide to synthesize 3,4,5-triethoxy-3',4'-dimethoxy chalcone for the first time, and the test of in vitro tumor cell inhibitory activity on the 3,4,5-triethoxy-3',4'-dimethoxy chalcone is realized; the result shows that the compound has higher inhibitory activity for human lung cancer cell A549, human colon carcinoma cell SW620 and human liver cancer cell HepG2. In addition, the antitumor activity of the 3,4,5-triethoxy-3',4'-dimethoxy chalcone for the human colon carcinoma cell SW620 and the human liver cancer cell HepG2 is superior to that of a reference drug 5-fluorouracil. The invention provides a new effective treatment means for tumor treatment and has a broad application prospect.

The invention relates to an organic hydridized tetra-core platinum complex having an anticancer activity. The structure general formula of the complex is shown in a formula (I), wherein in the formula (I), a bond (as shown in the specification) represents the same bridge ligand which is one of formulas (II), (III) and (IV). The compound has excellent antitumor activity, and especially, a methyl thiazolyl tetrazolium (MTT) test data of human lung cancer cell A549 / cisR shows that the antitumor activity of the compound is 10 times that of cisplatinum.

The present invention relates to an indirubin-3′-oxime derivative as potent cyclin dependent kinase inhibitor with anti-cancer activity. More particularly, this invention relates to an indirubin-3′-oxime derivative as potent cyclin dependent kinase inhibitor having excellent anti-cancer activity against human lung cancer cell, human fibro sarcoma cell, human colon cancer cell, human leukemia cell, human stomach cancer cell, human nasopharyngeal cancer cell and / or human breast cancer cell.

The invention discloses a 3-(3,4,5-trimethoxybenzoyl)-benzofuran microtubulin inhibitor as well as a preparation method and use thereof. A 3-(3,4,5-trimethoxybenzoyl)-benzofuran compound in the invention has an action mechanism similar to colchicine and is capable of inhibiting polymerization of microtubulins. The 3-(3,4,5-trimethoxybenzoyl)-benzofuran compound has very strong proliferation inhibition activity to human lung cancer cells A549, human gastric cancer cells MGC-803, human liver cancer cells HepG2, human colon cancer cells HCT-116, human cervical cancer cells HeLa and human breast cancer cells MCF-7.

Disclosed are methods and compositions for the selective manipulation of gene expression through the preparation of retroviral expression vectors for expressing antisense sequences, such as K-ras oncogene antisense sequences, or sequences encoding a desired product, such as wild type p53 sequences. Preferred retroviral vectors of the present invention incorporate the β-actin promoter in a reverse orientation with respect to retroviral transcription. Preferred antisense RNA constructs of the present invention employ the use of antisense intron DNA corresponding to distinct intron regions of the gene whose expression is targeted for down-regulation. In an exemplary embodiment, a human lung cancer cell line (NCI-H460a) with a homozygous spontaneous K-ras mutation was transfected with a recombinant plasmid that synthesizes a genomic segment of K-ras in antisense orientation. Translation of the mutated K-ras mRNA was specifically inhibited, whereas expression of H-ras and N-ras was unchanged. A three-fold growth inhibition occurred in H460a cells when expression of the mutated ras p21 protein was down-regulated by antisense RNA and cells remained viable. The growth of H460a tumors in nu / nu mice was substantially reduced by expressed K-ras antisense RNA.

Targeting metabolic enzymes in human cancer Abstract Lung cancer is a devastating disease and a major therapeutic burden with poor prognosis. The functional heterogeneity of lung cancer (different tumor formation ability in bulk of tumor) is highly related with clinical chemoresistance and relapse. Here we find that, glycine dehydrogenase (GLDC), one of the metabolic enzyme involved in glycine metabolism, is overexpressed in various subtypes of human lung cancer and possibly several other types of cancers. GLDC was found to be highly expressed in tumor-initiating subpopulation of human lung cancer cells compared with non-tumorigenic subpopulation. By array studies we showed that normal lung cells express low levels of GLDC compared to xenograft and primary tumor. Functional studies showed that RNAi inhibition of GLDC inhibits significantly the clonal growth of tumor-initiating cells in vitro and tumor formation in immunodeficient mice. Overexpression of GLDC in non-tumorigenic subpopulation convert the cells to become tumorigenic. Furthermore, over-expression of GLDC in NIH / 3T3 cells and human primary lung fibroblasts can transform these cells, displaying anchorage-independent growth in soft agar and tumor-forming in mice. Not only is GLDC is expressed human lung cancer, it is also up-regulated in other types of cancer, such as colon cancer. RNAi knockdown of GLDC in colon cancer cell line, CACO-2 cells, can also inhibit the tumor formation in mice. Thus GLDC maybe a new metabolic target for treatment of lung cancer, and other cancers.

The invention relates to a crocetin amides derivative. The crocetin amides derivative is characterized by having the following general formula: (img file='DSA00000789203800011.tif' wi='1009' he='177' / ), wherein R in the formula is (img file='DSA00000789203800012.tif' wi='1529' he='751' / ). The crocetin amides derivative has obvious inhibiting effect on human lung cancer cells A549 and human gastric carcinoma cells SGC7901. Therefore, the crocetin amides derivative can be applied to preparing anti-cancer drug. The invention also discloses a preparation method of the crocetin amides derivative.

The invention discloses tetrahydropalmatine derivatives and a preparation method and application thereof. The structural formula of the tetrahydropalmatine derivatives is shown as a formula II, wherein R is octyl, isopropyl or 3-methybutyl. The provided application is the application of the tetrahydropalmatine derivatives shown as the formula II or pharmaceutically acceptable salts thereof in the preparation of eukaryotic tumor cell antiblastics and medicaments for preventing and / or treating tumors. The results of in-vitro anti-tumor activity experiments prove that each tetrahydropalmatine derivative has the effect of inhibiting human lung cancer cells A-549, KB human nasopharyngeal carcinoma cells, and HL-60 leukemia cell strains to a certain extent. The results show that the tetrahydropalmatine derivatives shown as the formula II can be applied to preparing the medicaments for treating the tumors, and the pharmaceutical application of the tetrahydropalmatine derivatives is widened.

The present invention discloses a cyclic pentapeptide with anti-tumour activity, which is cyclic (leucyl-N-methylleucyl-leucyl-leucyl-N-methylleucyl) and the constitutional formula of which is shown in the formula (I). The cyclic pentapeptide of the present invention is separated from galaxaura filamentosa in the South China Sea, and in vitro experiments show that the cyclic pentapeptide has strong inhibiting effect on human hepatoma cell lines (HepG2), human hepatoma cell lines (BEL-7402), human mammary cancer cell lines (MCF-7), human colon cancer cell lines (LOVO), human lung cancer cell lines (PC84045) and human nasopharyngeal cancer (CNE) and can keep the mitotic cycle of BEL-7402 hepatoma cells in G2 / M phase. The present invention provides a pilot compound for the research and the development of new anti-tumour drugs and is valuable for the exploitation of the marine pharmaceutical resources of China.

A sorafenib antitumor platinum (II) complex targeted at human lung cancer drug-resistant cells is disclosed. The chemical structure of the complex is shown as follows in the description. The complex shows excellent antitumor activity in vitro, has potential medicine value and can be used for preparing various antitumor medicines.

The invention discloses a pyrazolopyrimidine-type compound. The structural general formula of the pyrazolopyrimidine-type compound is shown as formula (I). The invention further discloses a preparation method of the pyrazolopyrimidine-type compound and application of the pyrazolopyrimidine-type compound in preparation of antitumor drugs. The provided pyrazolopyrimidine-type compound can effectively inhibit multipletumor cells, including human breast cancer cells, human lung cancer cells, human hepatoma carcinoma cells, human neuroblastoma cells and the like, has high antitumor activity and canbe applied to preparation of the antitumor drugs.

The invention discloses a quinoline derivative as shown in the formula (I) in the specification and a salt of the quinoline derivative, wherein in the formula, Z is NH or O; R is selected from hydrogen, fluorine, chlorine, bromine, methyl, ethyl, tertiary butyl, trifluoromethyl, methoxyl or nitryl; n is an integer of 0, 1, 2 or 3. The invention relates to a preparation method and application of the compound as shown in the formula (I) in the specification and the salt of the compound. The compound or the salt has very high inhibition activity for a human lung cancer cell strain A549, a colorectal cancer cell strain HCT-116 and a breast cancer cell strain MCF-7. The compound has a broad-spectrum anti-cancer activity and can be used as a candidate medicine or a lead compound for treating diseases such as tumor and cancer.

The invention relates to a yellow mushroom standardized component manufacturing method. The method comprises the following steps: (1) drying and crushing yellow mushrooms, then performing water extraction, centrifugally collecting mushroom residues, extracting the mushroom residues with acetone, centrifugally collecting filtrate, and performing reduced pressure concentration on the filtrate to form paste, namely an acetone extract; (2) dissolving the acetone extract in an n-hexane-ethyl acetate mixed solution, then filtering to obtain a sample solution containing the acetone extract, and separating the sample solution containing the acetone extract on a preparation chromatogram to obtain 14 standardized component samples, namely Fr1, Fr2,..., Fr13 and Fr14; and (3) performing anti-lung cancer cell model screening on the 14 standardized component samples in vitro by an iCelligence real-time label-free cell analyzer, thus determining that the 7th, 8th and 14th standardized components have human lung cancer cell adherence and proliferation inhibition activity in vitro. The yellow mushroom standardized component manufacturing method provided by the invention has the advantages of simple process and easiness in implementation. Simultaneously, the obtained active components can be applied to treatment of lung cancer.

Spiro indolone compounds, a preparing method, a medicine composition and uses of the compounds are disclosed. In particular, the invention provide spiro indolone compounds shown as a formula I or II, a preparing method of the spiro indolone compounds and uses of the compounds in preparation of antitumor medicines. The compounds have a spiro indolinone skeleton, and the preparing method and potential uses of the compounds have not been reported before. The compounds have obvious killing functions for human cancer cells, particularly a human breast cancer cell strain MDA-MB-231, a human cervical cancer cell strain HeLa or a human lung cancer cell strain A549, have high selectivity, have potentials as novel antitumor medicines and have a good market prospect.

Disclosed are micro / nano composite drug delivery compositions for use in diagnosis, prophylaxis, treatment and / or amelioration of one or more symptoms of a mammalian disease, disorder, dysfunction, or abnormal condition. In illustrative embodiments, pharmaceutical formulations comprising these composites are provided that are useful in methods for targeting selected mammalian cells and tissues, particularly human lung tissue, and delivering one or more therapeutic agents, particularly in the treatment of human lung cancers, such as melanoma lung metastases.