piperidines has been researched along with Carcinoma--Ehrlich-Tumor* in 20 studies
1 review(s) available for piperidines and Carcinoma--Ehrlich-Tumor
1 trial(s) available for piperidines and Carcinoma--Ehrlich-Tumor
19 other study(ies) available for piperidines and Carcinoma--Ehrlich-Tumor
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LQFM030 reduced Ehrlich ascites tumor cell proliferation and VEGF levels.
This study reports the biological properties of LQFM030 in vivo, a molecular simplification of the compound nutlin-1.. Ehrlich ascites tumor (EAT)-bearing mice were treated intraperitoneally with LQFM030 (50, 75 or 150mg/kg) for 10days to determine changes in ascites tumor volume, body weight, cytotoxicity and angiogenesis. Moreover, flow cytometric expression of p53 and p21 proteins and caspase-3/7, -8 and -9 activation were investigated in EAT cells from mice treated. Acute oral systemic toxicity potential of LQFM030 in mice was also investigated using an alternative method.. LQFM030 seems to be a promising antitumor candidate for combinatory therapy with typical cytotoxic compounds, reducing the toxicity burden while allowing a superior anticancer activity. Moreover, these data also open new perspectives for LQFM030 as an antiangiogenic agent for treatment of diseases involving VEGF overexpression. Topics: Angiogenesis Inhibitors; Animals; Apoptosis; Carcinoma, Ehrlich Tumor; Caspases; Cell Proliferation; Female; Injections, Intraperitoneal; Male; Mice; Neovascularization, Pathologic; Oncogene Protein p21(ras); Piperidines; Pyrazoles; Tumor Suppressor Protein p53; Vascular Endothelial Growth Factor A | 2018 |
Piper nigrum ethanolic extract rich in piperamides causes ROS overproduction, oxidative damage in DNA leading to cell cycle arrest and apoptosis in cancer cells.
Ayurvedic and Chinese traditional medicine and tribal people use herbal preparations containing Piper nigrum fruits for the treatment of many health disorders like inflammation, fever, asthma and cancer. In Brazil, traditional maroon culture associates the spice Piper nigrum to health recovery and inflammation attenuation.. The aim of the current work was to evaluate the relationship between reactive oxygen species (ROS) overproduction, DNA fragmentation, cell cycle arrest and apoptosis induced by Piper nigrum ethanolic extract and its antitumor activity.. The plant was macerated in ethanol. Extract constitution was assessed by TLC, UV-vis and ESI-IT-MS/MS spectrometry. The cytotoxicity, proliferation and intracellular ROS generation was evaluated in MCF-7 cells. DNA damage effects were evaluated through intercalation into CT-DNA, plasmid DNA cleavage and oxidative damage in CT-DNA. Tumor growth inhibition, survival time increase, apoptosis, cell cycle arrest and oxidative stress were assessed in Ehrlich ascites carcinoma-bearing mice.. Extraction yielded 64mg/g (36% piperine and 4.2% piperyline). Treatments caused DNA damage and reduced cell viability (EC50=27.1±2.0 and 80.5±6.6µg/ml in MCF-7 and HT-29 cells, respectively), inhibiting cell proliferation by 57% and increased ROS generation in MCF-7 cells (65%). Ehrlich carcinoma was inhibited by the extract, which caused reduction of tumor growth (60%), elevated survival time (76%), cell cycle arrest and induced apoptosis. The treatment with extract increased Bax and p53 and inhibited Bcl-xL and cyclin A expression. It also induced an oxidative stress in vivo verified as enhanced lipid peroxidation and carbonyl proteins content and increased activities of glutathione reductase, superoxide dismutase and catalase. GSH concentration was decreased in tumor tissue from mice.. The ethanolic extract has cytotoxic and antiproliferative effect on MCF-7 cells and antitumor effect in vivo probably due to ROS overproduction that induced oxidative stress affecting key proteins involved in cell cycle arrest at G1/S and triggering apoptosis. Finally, the overall data from this study are well in line with the traditional claims for the antitumor effect of Piper nigrum fruits. Topics: Animals; Antineoplastic Agents, Phytogenic; Apoptosis; Apoptosis Regulatory Proteins; Biomarkers, Tumor; Breast Neoplasms; Carcinoma, Ehrlich Tumor; Cell Cycle Checkpoints; Cell Cycle Proteins; DNA Damage; Dose-Response Relationship, Drug; Ethanol; Female; HT29 Cells; Humans; Lipid Peroxidation; Male; MCF-7 Cells; Mice, Inbred BALB C; Oxidants; Oxidative Stress; Phytotherapy; Piper nigrum; Piperidines; Plant Extracts; Plants, Medicinal; Protein Carbonylation; Reactive Oxygen Species; Solvents; Time Factors; Tumor Burden; Up-Regulation | 2016 |
Induction of apoptosis in Ehrlich ascites tumour cells via p53 activation by a novel small-molecule MDM2 inhibitor - LQFM030.
The activation of the p53 pathway through the inhibition of MDM2 has been proposed as a novel therapeutic strategy against tumours. A series of cis-imidazoline analogues, termed nutlins, were reported to displace the recombinant p53 protein from its complex with MDM2 by binding to MDM2 in the p53 pocket, and exhibited an antitumour activity both in vitro and in vivo. Thus, the purpose of this study was to evaluate the antitumour properties of LQFM030 (2), a nutlin analogue created by employing the strategy of molecular simplification.. LQFM030 (2) cytotoxicity was evaluated in Ehrlich ascites tumour (EAT) cells, p53 wild type, by the trypan blue exclusion test, and the mechanisms involved in EAT cell death were investigated by light and fluorescence microscopy, flow cytometry, real-time PCR and Western blotting.. Our results demonstrate that LQFM030 has dose-dependent antiproliferative activity and cytotoxic activity on EAT cells, induces the accumulation of p53 protein and promotes cell cycle arrest and apoptosis. p53 gene transcription was unaffected by LQFM030 (2); however, MDM2 mRNA increased and MDM2 protein decreased.. These results suggest that the small-molecule p53 activator LQFM030 (2) has the potential for further development as a novel cancer therapeutic agent. Topics: Animals; Antineoplastic Agents; Apoptosis; Carcinoma, Ehrlich Tumor; Cell Cycle Checkpoints; Cell Proliferation; Imidazoles; Mice; Piperidines; Proto-Oncogene Proteins c-mdm2; Pyrazoles; RNA, Messenger; Tumor Suppressor Protein p53 | 2016 |
Possible anticancer activity of rosuvastatine, doxazosin, repaglinide and oxcarbazepin.
Rosuvastatine, doxazosin, repaglinide and oxcarbazepin are therapeutic drugs available in the market for the treatment of different diseases. Potential to display antitumor activities has also been suggested. The aim of the current study was to evaluate their in vitro effects on some human transformed cell lines.. Cytotoxicity of the four drugs was tested in MCF-7, HeLa and HepG2 cells by the neutral red assay method and also the effect of rosuvastatine and doxazosin against Ehrlich Ascities Carcinoma Cells (EACC) by trypan blue assay.. Rosuvastatine exerted the greatest cytotoxic effect against HepG2 cells with an IC50 value of 58.7±69.3; in contrast doxazosin showed least activity with IC50=104.4 ±115.7. Repaglinide inhibited the growth of both HepG2 and HeLa cells with IC50 values of 87.6±117.5 and 89.3±119.5, respectively. Oxcarbazepine showed a potent cytotoxicity against both HeLa (IC50=19.4±43.9) and MCF7 cancer cells ((IC50=22±35.7).On the other hand the growth of EACC was completely inhibited by doxazosine (100% inhibition) while rosuvastatine had weak inhibitory activity (11.6%) .. The four tested drugs may have cytotoxic effects against hepatic, breast and cervical carcinoma cells; also doxazosine may inhibit the growth of endometrial cancer cells. Further investigations in animals are needed to confirm these results. Topics: Animals; Anticonvulsants; Antihypertensive Agents; Antineoplastic Agents; Carbamates; Carbamazepine; Carcinoma, Ehrlich Tumor; Cell Proliferation; Cell Survival; Doxazosin; Fluorobenzenes; HeLa Cells; Hep G2 Cells; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; Hypoglycemic Agents; Inhibitory Concentration 50; MCF-7 Cells; Oxcarbazepine; Piperidines; Pyrimidines; Rosuvastatin Calcium; Sulfonamides | 2014 |
Immunomodulatory and antitumor activity of Piper longum Linn. and piperine.
Alcoholic extract of the fruits of the plant Piper longum and its component piperine was studied for their immunomodulatory and antitumor activity. Alcoholic extract of the fruits was 100% toxic at a concentration of 500 microg/ml to Dalton's lymphoma ascites (DLA) cells and 250 microg/ml to Ehrlich ascites carcinoma (EAC) cells. Piperine was found to be cytotoxic towards DLA and EAC cells at a concentration of 250 microg/ml. Alcoholic extract and piperine was also found to produce cytotoxicity towards L929 cells in culture at a concentration of 100 and 50 microg/ml, respectively. Administration of alcoholic extract of Piper longum (10 mg/dose/animal) as well as piperine (1.14 mg/dose/animal) could inhibit the solid tumor development in mice induced with DLA cells and increase the life span of mice bearing Ehrlich ascites carcinoma tumor to 37.3 and 58.8%, respectively. Administration of Piper longum extract and piperine increased the total WBC count to 142.8 and 138.9%, respectively, in Balb/c mice. The number of plaque forming cells also enhanced significantly by the administration of the extract (100.3%) and piperine (71.4%) on 5th day after immunization. Bone marrow cellularity and alpha-esterase positive cells were also increased by the administration of Piper longum extract and piperine. Topics: Adjuvants, Immunologic; Alkaloids; Animals; Antineoplastic Agents, Phytogenic; Benzodioxoles; Carcinoma, Ehrlich Tumor; Mice; Mice, Inbred BALB C; Piper; Piperidines; Plant Extracts; Polyunsaturated Alkamides; Sheep; Xenograft Model Antitumor Assays | 2004 |
Effects of 1-tetradecylperhydroazepine and 1-pentadecylpiperidine N-oxides on Ehrlich ascites mitochondria.
Non-aromatic amine oxides are widely known and used compounds. A great number of amine oxides occurring in nature, or prepared synthetically, are biologically active compounds (antimetabolites and chemotherapics, cancerostatic compounds, etc.). From seven series of newly synthesized amine oxides (63 compounds), 1-alkylperhydroazepine N-oxides (PHNO) and 1-alkylpiperadine N-oxides (PINO) have been chosen for further investigation. The effects of 8 derivatives of PHNO and 8 derivatives of PINO on state 3 and 4 respiration of Ehrlich ascites mitochondria (EAM) have been studied. Derivatives with longer side-chain significantly affected respiration of EAM according to the substrates used. To elucidate the mode of action, the most potent amine oxides from each series, 1-tetradecylperhydroazepine N-oxide (tPHNO) and 1-pentadecylpiperidine N-oxide (pPINO) have been chosen for further study. Both amine oxides stimulated state 4 respiration with glutamate-malate and succinate as substrates. The effect on state 3 respiration depended on the substrates used. Both tPHNO and pPINO were able to release respiration of EAM previously inhibited by oligomycin, both decreased the level of ATP in EAM. ATPase activity was significantly stimulated by both drugs only in higher concentrations. A possible mode of action of amine oxides on oxidative phosphorylation and the relationship between chemical structure are discussed. Topics: Adenosine Triphosphatases; Animals; Antineoplastic Agents; Azepines; Carcinoma, Ehrlich Tumor; Cyclic N-Oxides; Enzyme Activation; Mice; Mitochondria; Molecular Structure; Oxidative Phosphorylation; Piperidines; Structure-Activity Relationship | 1995 |
In vitro cytotoxic activity of 1-alkylpiperidine N-oxides and quantitative structure-activity relationships.
The main objective of the present investigation was to screen a series of 1-alkylpiperidine N-oxides for in vitro cytotoxicity, and to find out whether there is a quantitative structure-activity correlation (QSAR) between cytotoxic effect represented here by inhibition of incorporation of [14C]adenine into nucleic acid or [14C]valine into proteins in Ehrlich ascites carcinoma (EAC) cells and structure (as a structural parameter the number of carbon atoms m in the alkyl chain was used). On the basis of primary screening, one of the most active compounds, i.e. 1-decylpiperidine N-oxide, was chosen for further biochemical study. The drug inhibited the incorporation rate of 14C-labeled precursors (adenine, thymidine, uridine, valine) into appropriate macromolecules of Ehrlich cells, the extent of inhibition being dependent on both time and concentration of the compound in the incubation medium. The lengthening of the alkyl chain in 1-alkylpiperidine N-oxides positively affected their cytotoxic activity in Ehrlich cells. For these compounds the optimal m value is 12-15. Topics: Adenine; Animals; Antineoplastic Agents; Carbon Radioisotopes; Carcinoma, Ehrlich Tumor; Cyclic N-Oxides; DNA, Neoplasm; Drug Screening Assays, Antitumor; Macromolecular Substances; Piperidines; RNA, Neoplasm; Structure-Activity Relationship; Valine | 1993 |
Effect of membrane active 1-alkylpiperidine N-oxides on glycolysis, respiration and ATP level in tumor cells.
The aim of this study was to study the effect of the homologous series of 1-alkylpyrrolidine N-oxides on ATP-producing processes in Ehrlich ascites and L1210 murine leukemia cells. 1-Decylpiperidine N-oxide (deP-NO), one of the active compounds, significantly stimulated the course of aerobic glycolysis of Ehrlich cells. Derivatives with longer side-chains markedly inhibited endogenous respiration of both tumor cells. dePNO, immediately after addition to the suspension of Ehrlich cells in an ice bath, markedly decreased the level of ATP in Ehrlich ascites cells. The decrease in ATP level might be explained through impairment of cell membrane integrity. Topics: Adenosine Triphosphate; Animals; Carcinoma, Ehrlich Tumor; Cell Membrane; Cyclic N-Oxides; Glycolysis; Neoplasm Proteins; Oxygen Consumption; Piperidines; Sulfhydryl Compounds | 1993 |
Cytostatic activity of inorganic heterocycles in an in vitro screening system.
Six representatives of inorganic cyclic systems (NPAz2)2 NSOX(Az = aziridino, X = F, Az, Ph) and (NPAz2)2 NPAzR [R = Az, Morph (morpholino), Pyr (pyrrolidino)] show cytostatic activity in an in vitro screening system. The technique of the in vitro screening system used is described. L5178Y and Ehrlich ascites cells are grown as suspension cultures in concave-bottomed wells in microtiter test plates using serial dilutions of the drugs in the medium. The diameter of the cell sedimentation spots, which can be compared visually is taken to determine the lowest active dose. The results of this test correspond with the cytostatic activities observed in former in vivo experiments. Topics: Animals; Aziridines; Azirines; Carcinoma, Ehrlich Tumor; Cell Division; Cell Line; Cell Survival; Drug Evaluation, Preclinical; Leukemia L5178; Morpholines; Piperidines; Pyrrolidines | 1983 |
[Relationship between chemical reactions and antitumor activities of bis(haloalkyl)piperidine derivatives (author's transl)].
Topics: Animals; Carcinoma, Ehrlich Tumor; Chemical Phenomena; Chemistry; Female; Hydrolysis; Liver Neoplasms, Experimental; Mice; Piperidines; Pyridines; Rats | 1980 |
[Antitumor activity of 2,6-bis(halomethyl)piperidines on Ehrlich ascites carcinoma (author's transl)].
Topics: Animals; Carcinoma, Ehrlich Tumor; Female; Halogens; In Vitro Techniques; Mice; Piperidines; Structure-Activity Relationship | 1977 |
Modified transport substrates as probes for intramembrane gradients.
Topics: Adenosine Triphosphate; Amino Acids; Aminoisobutyric Acids; Animals; Biological Transport, Active; Carbon Radioisotopes; Carboxylic Acids; Carcinoma, Ehrlich Tumor; Cell Membrane; Choline; Dinitrophenols; Gramicidin; Kinetics; Lysine; Membrane Potentials; Methods; Mice; Models, Biological; Piperidines; Sodium; Time Factors | 1974 |
Amino acid stimulation of alkali-metal-independent ATP cleavage by an Ehrlich cell membrane preparation.
Topics: Adenosine Triphosphatases; Amino Acids; Animals; Antimetabolites; Arginine; Carcinoma, Ehrlich Tumor; Cell Membrane; Glycine; Gramicidin; Kinetics; Leucine; Oligomycins; Ornithine; Ouabain; Piperidines; Potassium; Sodium; Valinomycin | 1973 |
Antitumor activity of DL-1-beta-chloroethyl-2-chloromethylpiperidine hydrobromide (CAP-1) on some rodent tumors.
Topics: Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Carcinoma, Hepatocellular; Drug Evaluation, Preclinical; Female; In Vitro Techniques; Leukemia L1210; Liver Neoplasms; Mice; Neoplasms, Experimental; Piperidines; Rats; Sarcoma 180; Sarcoma, Yoshida | 1973 |
Chemotherapeutic effects of compound 593A (NSC-135758) on mouse leukemias and some transplanted animal tumors.
Topics: Alkylating Agents; Animals; Antibiotics, Antineoplastic; Ascites; Carcinoma 256, Walker; Carcinoma, Ehrlich Tumor; Drug Resistance; Leukemia L1210; Leukemia, Experimental; Mercaptopurine; Methotrexate; Mice; Neoplasm Transplantation; Neoplasms, Experimental; Piperazines; Piperidines; Transplantation, Homologous | 1973 |
[Cytostatically active N-acyloxymethyl compounds].
Topics: Acetates; Animals; Antineoplastic Agents; Benzoates; Carbon Isotopes; Carcinoma, Ehrlich Tumor; Cinnamates; Depression, Chemical; DNA, Neoplasm; Esters; Imidazoles; Imides; In Vitro Techniques; Leucine; Mice; Morpholines; Neoplasm Proteins; Oxazoles; Piperidines; Pyrrolidinones; RNA, Neoplasm; Thymidine; Uridine | 1969 |
FURTHER STUDIES CONCERNING CARCINOLYSIS.
Topics: Animals; Antineoplastic Agents; Blood; Carcinoma, Ehrlich Tumor; DNA; DNA, Neoplasm; Mice; Neoplasms; Neoplasms, Experimental; Piperidines; Prochlorperazine; Rabbits; Research; Reserpine; RNA; RNA, Neoplasm; Sarcoma 180 | 1963 |
[CYTOSTATIC EFFECTS OF N-AND S-HYDROXYMETHYL AND N-C-N COMPOUNDS].
Topics: Alkylating Agents; Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Cytostatic Agents; Neoplasms, Experimental; Nitrogen Mustard Compounds; Peroxides; Piperidines; Pyrrolidinones; Research | 1963 |
[ADDITIONAL CLASSES OF COMPOUNDS INHIBITING TUMORS. I. CYTOSTATIC EFFECTS OF N- AND S-HYDROXYMETHYL COMPOUNDS].
Topics: Amides; Animals; Antineoplastic Agents; Benzimidazoles; Carbohydrate Metabolism; Carcinoma, Ehrlich Tumor; Cytostatic Agents; Formaldehyde; Hydantoins; Imidazoles; Isonicotinic Acids; Mice; Morpholines; Neoplasms, Experimental; Niacin; Niacinamide; Piperazines; Piperidines; Pyrroles; Research; Urea | 1963 |