Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0001418 (adenocarcinoma)
 68,496 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The antitumor constituents were isolated from Pteris semipinnata L. (PsL), a Chinese traditional herb, and screened using tetrazolium salt (MTT) method. Their cytotoxic effects in vitro on several human tumor cell lines were studied. Compounds 5F, 6F, A and the ethanolic extract of PsL (PSE) were shown to have strong cytotoxicity against five cell lines: human liver adenocarcinoma cell line (HePG II), human lung adenocarcinom a cell line (SPC-A-1), human gastric adenocarcinoma cell line (MGC-803), human nasopharyngeal carcinoma cells in low differentiation (CNE-2Z) and human liver adenocarcinoma cell line (BEL-7402) in different degrees in a dose-dependent manner; compound 6F was the most active one, whose IC50 after 72 h treatment for the above five cell lines were 0.343 +/- 0.003, 0.115 +/- 0.022, 0.590 +/- 0.032, 0.328 +/- 0.066 and 0.221 +/- 0.058 microgram.ml-1, respectively. Compounds A and 5F were less active; no cytotoxicity of compounds 4F and B were detected on the five cell lines. Analysis of the relationship between structure and activity revealed that the antitumor activity portion in the structure is the alpha, beta-methylene cyclopentanone moiety, and the site and number of the hydroxy groups affect the cytotoxicity of these agents significantly.
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PMID:[Comparison of the cytotoxicity of five constituents from Pteris semipinnata L. in vitro and the analysis of their structure-activity relationships]. 1201 65

This in vitro feasibility study has assessed a number of techniques and their applicability when looking at the role of multidrug resistance (MDR) in solid tumours. Fresh tumour material was obtained from 34 patients, (11 previously treated, 23 untreated) with ovarian adenocarcinoma. Doxorubicin sensitivity was measured using the MTT assay +/- the cyclosporins, Pgp expression was assessed by immunocytochemistry with the MRK-16 MoAb and flow cytometry was used to assess intracellular drug accumulation +/- PSC 833. 85% of samples showed some evidence of modest chemosensitisation by the cyclosporins (median 1.74-fold). We saw a marked variation in the number of Pgp positive cells between patients (1-87%, median 31%). 63% of samples tested showed an enhancement of DNR accumulation in the presence of PSC 833, with a median increase of 7% (sample range 0-29%). The present study highlights some of the technical difficulties encountered when working with fresh tumour material ex vivo. We conclude that screening of patients for their suitability to enter clinical trials incorporating MDR modulating agents is technically demanding, but feasible.
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PMID:Assessment of the classical MDR phenotype in epithelial ovarian carcinoma using primary cultures: a feasibility study. 1201 36

Among 25 3-aryl-2-quinolone derivatives synthesized, the antitumor activity of some of them was characterized both in vitro and in vivo. In this series, no compound appeared to be cytotoxic in vitro, as was known by the colorimetric MTT assay carried out on 12 distinct human cancer cell lines obtained from the American Type Culture Collection. Indeed, the concentration values decreasing the growth of the 12 cell lines by at least 50% (IC(50) index) were always higher than 10(-5) M. We then made use of a computer-assisted phase-contrast videomicroscopy system to quantitatively determine in vitro the level of migration of living MCF-7 human breast cancer cells. For example, at 10(-7) M, compounds 7, 13, 16, and 28 markedly decreased the migration level of these MCF-7 human breast cancer cells. The in vivo determination of the maximum tolerated dose showed that all compounds tested were definitively nontoxic. When the nontoxic, antimigratory compound 16 was combined with either doxorubicin or etoposide, two cytotoxic compounds routinely used in the clinic, this led to additive in vivo benefits from this treatment (as compared to individual administrations of the drugs) when the MXT mouse mammary adenocarcinoma was used. Thus, nontoxic antimigratory compounds, including the 2-quinolone derivatives synthesized here, can actually improve the efficiency of antitumor treatment when combined with conventional cytotoxic agents.
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PMID:3-Aryl-2-quinolone derivatives: synthesis and characterization of in vitro and in vivo antitumor effects with emphasis on a new therapeutical target connected with cell migration. 1203 63

Caffeic acid phenethyl ester (CAPE, 2) and its twenty analogues (1, 3-21) were prepared. These esters were tested by MTT assay on growth of murine colon 26-L5 carcinoma, murine B16-BL6 malonoma, murine Lewis lung carcinoma, human HT-1080 fibrosarcoma, human lung A549 adenocarcinoma, and human cervix HeLa adenocarcinoma cell lines. It was found that CAPE analogues possessed selective antiproliferative activity toward highly liver-metastatic murine colon 26-L5 carcinoma cell line. Among them, 4-phenylbutyl caffeate (4), (Z)-8-phenyl-7-octenyl (10a) and (E)-8-phenyl-7-octenyl (10b) caffeate showed the most potent antiproliferative activity (EC50 value, 0.02 microM). In addition, CAPE (2) induced DNA fragmentation at concentrations of 1 to 10 microg/mL towards murine colon 26-L5 carcinoma cells.
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PMID:Selective antiproliferative activity of caffeic acid phenethyl ester analogues on highly liver-metastatic murine colon 26-L5 carcinoma cell line. 1215 Aug 82

Thymoquinone (TQ) is likely responsible for the chemotherapeutic effects of N. sativa extract; however, the cellular mechanisms remain ill-defined. TQ-induced cytotoxicity was investigated using canine osteosarcoma (COS31), its cisplatin-resistant variant (COS31/rCDDP), human breast adenocarcinoma (MCF7), human ovarian adenocarcinoma (BG-1) and Madin-Darby canine (MDCK) cell lines. TQ-induced cytotoxicity was determined using a proliferation assay (MTT assay) and apoptosis assays. Effects of TQ on the cell cycle were determined using flow cytometry. COS31/rCDDP resistant cells were the most sensitive cell line to TQ and MDCK cells were the least sensitive. TQ (25 micro M) induced apoptosis of COS31 cells 6 h after treatment and decreased the number of COS31 cells in S-phase and increased cells in G1-phase, indicating cell cycle arrest at G1. These results suggest that TQ kills cancer cells by a process that involves apoptosis and cell cycle arrest. Non-cancerous cells are relatively resistant to TQ.
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PMID:In vitro inhibition of growth and induction of apoptosis in cancer cell lines by thymoquinone. 1246 92

Although cellular experiments have elucidated a number of active principles in the study of the multidrug resistance (MDR) phenomena, most of the drug resistant tumor cells were derived from different parental cell lines. This fact limits generalization of some experimental data and conclusions, and therefore we selected and characterized cell lines resistant to various anti-cancer agents derived from four parental cell lines: CEM (human T-lymphoblastic leukemia), K562 (human myeloid leukemia), A549 (human lung adenocarcinoma) and MDAMB 231 (human breast adenocarcinoma). In total we obtained a set of 42 resistant sublines, which is an excellent tool for the future studies of different aspects of MDR. In this study we report on some basic characteristics of these sublines, namely, cross-resistance to other anti-cancer drugs investigated by in vitro MTT assay, expression of MDR associated proteins (Pgp, MRP1, LRP, GST-pi and Topo IIalpha) as well as the functional activity of Pgp and MRP.
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PMID:In vitro chemoresistance profile and expression/function of MDR associated proteins in resistant cell lines derived from CCRF-CEM, K562, A549 and MDA MB 231 parental cells. 1258 92

Recently we synthesized new drugs, diazenecarboxamides (shortly diazenes), that were cytotoxic for several tumour cell lines. Because the solubility and biological activity of these drugs was relatively low, new compounds have been synthesized. In the present study we examined the cytotoxic effect of nine compounds: an imidazolidin-2-one (SB-282: methyl 5-benzoyl-3-(2-chloroethyl)-2-oxo-4-phenyl-2,3-dihydro-1H-imidazol-1-ylcarbamate), two diazenecarboxamides (UP-140: N-phenyl-2-(2-quinolinyl)diazenecarboxamide; JK-1090: N-(4-iodophenyl)-2-(2-pyridinyl)diazenecarboxamide), two aminocarbonyl substituted diazenecarboxylates (SB-178: methyl 2-[(cyclohexylamino)carbonyl]diazenecarboxylate; SB-166: methyl 2-[[(2-chloroethyl)amino]carbonyl]diazenecarboxylate) and four diazenedicarboxamides (SB-410: N(1)-(2-chloroethyl)-N(2)-(2-pyridinylmethyl)-1,2-diazenedicarboxamide; SB-472: N(1)-(2-chloroethyl)-N(2)-(4-isopropylphenyl)-1,2-diazenedicarboxamide; SB-503: N(1)-(4-sec-butylphenyl)-N(2)-(2-chloroethyl)-1,2-diazenedicarboxamide; SB-474: N(1)-(4-tert-butylphenyl)-N(2)-(2-chloroethyl)-1,2-diazenedicarboxamide). Using a modified colorimetric MTT assay, their cytotoxicity was determined on eight human cell lines: laryngeal carcinoma parental and two drug-resistant cell lines, glioblastoma parental and drug-resistant cell lines, cervical carcinoma parental and drug-resistant cell lines and breast adenocarcinoma cells. Results show that diazene SB-166 was very effective, reducing significantly the cell survival of all eight examined cell lines, including four drug-resistant cell lines. Compound SB-410 was cytotoxic for all examined cell lines, but mostly only in the highest concentration. Other compounds were not significantly cytotoxic to any of the treated cell lines. Our results, especially those obtained on drug-resistant cells, encourage further research on compound SB-166 as a potential anticancer drug.
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PMID:Methyl 2-(2-chloroethylaminocarbonyl)diazenecarboxylate SB-166 inhibits the growth of different tumour cell lines, including drug-resistant sublines. 1265 Jun 69

Chitosan has the potential for DNA complexation and is useful as a non-viral vector for gene delivery. Highly purified low molecular weight chitosan (LMWC) was prepared. Lactobionic acid (LA) bearing galactose group was coupled with LMWC for liver-specificity. A series of galactosylated-LMWC (gal-LMWC) samples covering a range of galactose group contents were prepared. The chitosan/DNA complexes were obtained using a complex coacervation process. Gal-LMWCs were used to transfer pSV-beta-galactosidase reporter gene into human hepatocellular carcinoma cell (HepG2), L-02, SMMC-7721, and human cervix adenocarcinoma cell line (HeLa) cell lines in vitro. Transfection efficiency of gal-LMWCs was evaluated by beta-galactosidase assay and compared with those of lipofectin, calcium phosphate (CaP), high molecular weigh chitosan (HMWC) and LMWC. Gal-LMWC/DNA complex shows a very efficient cell selective transfection to hepatocyte. The transfection efficiency of gal-LMWCs increased with the improvement of the galactosylation degree. Cytotoxicity of gal-LMWC was determined by 3-(4,5-dimethylthiazd-2-yl)-2,5-diphenyltentrazolium bromide (MTT) assay and the results show that the modified chitosan has relatively low cytotoxicity, giving the evidence that the modified chitosan vector has the potential to be used as a safe gene-delivery system.
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PMID:Galactosylated low molecular weight chitosan as DNA carrier for hepatocyte-targeting. 1267 2

Investigation has been conducted to delineate the action of some phenolic compounds of natural origin in four human tumor cell lines: acute myeloblastic leukemia (HL-60), chronic myelogenic leukemia (K-562), breast adenocarcinoma (MCF-7) and cervical epithelial carcinoma (HeLa). In cells grown in appropriate media the phenolics curcumin, yakuchinone B, resveratrol and capsaicin exhibited growth inhibition as assessed by trypan blue dye exclusion. It was evident from the results of the MTT reduction assay and [(3)H]thymidine incorporation into nuclear DNA that the phenolics were cytotoxic and inhibited cell proliferation. Dose response studies indicated curcumin to be most cytotoxic towards HL-60, K-562 and MCF-7 but did not show much activity in HeLa cells. On the other hand, yakuchinone B, although less active than curcumin, displayed cytotoxicity towards all four cell lines. Resveratrol was cytotoxic only in leukemic cells, while capsaicin was marginally cytotoxic. All these phenolics did not elicit any cytotoxic activity as judged by the above parameters towards lymphocytes purified from normal human blood. When cells treated with phenolics were stained with propidium iodide and examined under a fluorescent microscope, characteristic apoptotic features such as chromatin condensation and nuclear fragmentation were observed. Scoring of cells with apoptotic and non-apoptotic features showed positive correlation of apoptotic index with dose of phenolic, and fragmented DNA extracted free of genomic DNA displayed on gel electrophoresis a typical ladder pattern. These phenolics which have human exposure are known cancer chemopreventive agents and their action as inducers of apoptosis in tumor cells suggest their potential use in a strategy for cancer control.
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PMID:Induction of Apoptosis in Tumor Cells by Natural Phenolic Compounds. 1271 10

The effects of all trans retinoic acid and hyperthermia were studied in the human colon adenocarcinoma cell line HT29. Cell cytotoxicity after exposure to ATRA or heat-shock, alone or in association, was evaluated by the MTT assay while cell surface and ultrastructure modifications and actin fibre assembly changes were investigated by electron microscopy and by the FITC-phalloidin method. Apoptosis was evaluated by flow cytofluorimetry and electron microscopy. Reverse transcriptase-polymerase chain reaction was employed to study mRNA expression of genes involved in apoptosis, differentiation and growth arrest. Joint treatments were more effective in reducing the vital cell yield, being this effect only partially due to apoptosis. A marked up-regulation of the cyclin-dependent kinase inhibitor p21WAF1/Cip1 expression, not followed by any differentiation process, was responsible for growth arrest. Modulation of Hsp-70 expression, involved in cell response to treatments, was considered. Our results demonstrate that cell treatment with ATRA followed by heat-shock may elicit useful effects to treat tumours, which are responsive to retinoids, as well as those malignant cells which may be constitutively thermotolerant.
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PMID:All trans retinoic acid sensitizes colon cancer cells to hyperthermia cytotoxic effects. 1279 92


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