scholarly journals ACONITINE-CONTAINING AGENT ENHANCES ANTITUMOR ACTIVITY OF DICHLOROACETATE AGAINST EHRLICH CARCINOMA

2015 ◽  
Vol 37 (3) ◽  
pp. 192-196 ◽  
Author(s):  
O N Pyaskovskaya ◽  
I V Boychuk ◽  
A G Fedorchuk ◽  
D L Kolesnik ◽  
O I Dasyukevich ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Total Dose ◽  
Lactate Level ◽  
Phagocytic Activity ◽  
Tumor Tissue ◽  
Antitumor Action ◽  
Ehrlich Carcinoma ◽  
Ros Production ◽  
Antiangiogenic Agent ◽  
Ldh Activity

Significant variability of anticancer efficacy of dichloroacetate (DCA) stimulated an active search for the agents capable to enhance it antitumor action. Therefore, the aim of this work is the study of capability of aconitine-containing antiangiogenic agent BC1 to enhance anticancer activity of DCA against Ehrlich carcinoma. Materials and Methods: DCA (total dose was 1.3 g/kg of b.w.) and BC1 (total dose was 0.9 mg/kg of b.w.) were administered per os starting from the 2nd and 3rd days, respectively (8 admini strations for each agent). Antitumor efficacy of agents was estimated. Lactate level, LDH activity and the state of mitochondrial electron transport chain in tumor cells as well as phagocytic activity and reactive oxygen species (ROS) production of tumor-associated macrophages (TAM) were studied. Results: Combined administration of DCA and ВС1 resulted in 89.8% tumor growth inhibition (p < 0.001), what is by 22.5% (p < 0.05) higher that that of DCA alone. This combined treatment was accompanied with a decrease of lactate level in tumor tissue by 30% (p < 0.05) and significant elevation of LDH activity by 70% (p < 0.01). Increased level of NO-Fe-S clusters and 2-fold reduction of Fe-S cluster content were revealed in tumor tissue of mice after DCA and BC1 administration. It was shown that combined therapy did not effect TAM quantity and their phagocytic activity but stimulated ROS production by TAMs by 78% (p < 0.05) compared to this index in control animals. Conclusion: Antiangiogenic agent ВС1 in combination with DCA considerably enhances antitumor activity of DCA via significant decrease of Fe-S-containing protein level resulted from substantial elevation of nitrosylation of these proteins.

THE EFFECTS OF THE COMBINATION OF RAPAMYCIN WITH DOXORUBICIN AND PACLITAXEL ON THE MODELS OF TRANSPLANTABLE TUMORS IN MICE

2019 ◽  
Vol 65 (4) ◽  
pp. 614-622
Author(s):  
Mariya Yurova ◽  
Margarita Tyndyk ◽  
Yekaterina Gubareva ◽  
Yelena Fedoros ◽  
Viktor Anisimov
Keyword(s):  
Antitumor Activity ◽  
Protective Effect ◽  
Total Dose ◽  
Mtor Inhibitor ◽  
Combined Treatment ◽  
Mammary Adenocarcinoma ◽  
Ehrlich Carcinoma ◽  
Tumor Growth Inhibition ◽  
Chemotherapeutic Drugs ◽  
Transplantable Tumors

The study aimed to assess combined treatment with mTOR inhibitor rapamycin and cytotoxic drugs (doxorubicin and paclitaxel) on two models of transplantable tumors - mammary adenocarcinoma in male HER-2/neu transgenic FVB/N mice and solid Ehrlich carcinoma in male 129/Sv mice. Rapamycin (total dose of 3.6 mg kg), doxorubicin (total dose of 15 mg/ kg), paclitaxel (total dose of 6 mg/kg) or their combination were intraperitoneally injected to mice with developed tumor node. Rapamycin showed its own antitumor activity by tumor growth inhibition up to 42% in mammary adenocarcinoma model and up to 57% in Ehrlich carcinoma model. A tendency to an increase in the antitumor activity of chemotherapeutic drugs with the addition of rapamycin was revealed. The cyto-protective effect of the mTOR inhibitor was observed during therapy with doxorubicin and paclitaxel, expressed in a significant decrease in the level of apoptosis in normal epithelium of jejunum crypts. Thus, revealed protective effect of mTOR inhibitor on jejunum epithelium could be applied for reduction of chemotherapeutic drugs enterotoxic effect without any efficiency reduction. Thus, in perspective that could expand the possibilities of standard chemotherapeutic treatment and improve the quality of life of cancer patients.

ANTITUMOR EFFECT OF COLLOIDAL SILVER BISILICATE IN EXPERIMENTAL IN VITRO AND IN VIVO STUDIES

2019 ◽  
Vol 65 (5) ◽  
pp. 760-765
Author(s):  
Margarita Tyndyk ◽  
Irina Popovich ◽  
A. Malek ◽  
R. Samsonov ◽  
N. Germanov ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Tumor Growth ◽  
Tumor Cells ◽  
Human Tumor ◽  
Significant Inhibition ◽  
In Vivo Studies ◽  
Ehrlich Carcinoma ◽  
In Vivo Experiments

The paper presents the results of the research on the antitumor activity of a new drug - atomic clusters of silver (ACS), the colloidal solution of nanostructured silver bisilicate Ag6Si2O7 with particles size of 1-2 nm in deionized water. In vitro studies to evaluate the effect of various ACS concentrations in human tumor cells cultures (breast cancer, colon carcinoma and prostate cancer) were conducted. The highest antitumor activity of ACS was observed in dilutions from 2.7 mg/l to 5.1 mg/l, resulting in the death of tumor cells in all studied cell cultures. In vivo experiments on transplanted Ehrlich carcinoma model in mice consuming 0.75 mg/kg ACS with drinking water revealed significant inhibition of tumor growth since the 14th day of experiment (maximally by 52% on the 28th day, p < 0.05) in comparison with control. Subcutaneous injections of 2.5 mg/kg ACS inhibited Ehrlich's tumor growth on the 7th and 10th days of the experiment (p < 0.05) as compared to control.

Phase II Trial of Thalidomide and Carmustine for Patients With Recurrent High-Grade Gliomas

2003 ◽  
Vol 21 (12) ◽  
pp. 2299-2304 ◽  
Author(s):  
Howard A. Fine ◽  
Patrick Y. Wen ◽  
Elizabeth A. Maher ◽  
Elene Viscosi ◽  
Tracy Batchelor ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Malignant Gliomas ◽  
Cytotoxic Agents ◽  
Clinical Activity ◽  
Antiangiogenic Agents ◽  
High Grade ◽  
Antiangiogenic Agent ◽  
Histologic Diagnosis ◽  
Anaplastic Gliomas ◽  
High Grade Gliomas

Purpose: The use of thalidomide as an antiangiogenic agent has met with only limited success in the treatment of malignant gliomas. On the basis of preclinical data demonstrating synergistic antitumor activity when antiangiogenic agents are combined with cytotoxic agents, we explored the clinical activity of the combination of thalidomide and carmustine (BCNU) in patients with recurrent high-grade gliomas. Patients and Methods: Patients with a histologic diagnosis of high-grade glioma and radiographic evidence of tumor progression after standard surgery, radiation, and chemotherapy were eligible for the study. Patients received BCNU 200 mg/m2 on day 1 of every 6-week cycle, and 800 mg/d of thalidomide that was escalated to a maximal dose of 1,200 mg/d as tolerated. Results: A total of 40 patients (38 with glioblastomas, two with anaplastic gliomas) were accrued to the study. The combination of thalidomide and BCNU was well tolerated; mild myelosuppression and mild to moderate sedation were the most common side effects. The median progression-free survival (100 days) and the objective radiographic response rate (24%) for patients with glioblastoma compared favorably with data from historical controls. Conclusion: This is one of the first clinical trials to evaluate the strategy of combining a putative antiangiogenic agent with a cytotoxic agent in patients with primary brain tumors. Our data demonstrate that thalidomide in combination with BCNU is well tolerated and has antitumor activity in patients with recurrent high-grade gliomas. Although the combination seems to be more active than either agent alone, such conclusions await confirmatory trials.

scholarly journals Fruticuline A, a chemically-defined diterpene, exerts antineoplastic effects in vitro and in vivo by multiple mechanisms

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Claudia Rita Corso ◽  
Maria Carolina Stipp ◽  
Débora Rasec Radulski ◽  
Marihá Mariott ◽  
Luisa Mota da Silva ◽  
...  
Keyword(s):  
Cyclin D1 ◽  
Molecular Mechanisms ◽  
Tumor Tissue ◽  
Human Cancer ◽  
Biological Properties ◽  
Ehrlich Carcinoma ◽  
Antitumor Effects ◽  
Mcf 7

Abstract Natural products have been recognized as important bioactive compounds on the basis of their wide biological properties. Here we investigated the antitumor effect and molecular mechanisms of the diterpene Fruticuline A (fruti) from Salvia lachnostachys, in human cancer cell lineages and Solid Ehrlich Carcinoma in mice. Fruti reduced MCF-7 and HepG2 proliferation by the reduction of Cyclin D1 levels and decreased NF-κB gene levels in both cell types. Furthermore, fruti also induced apoptosis in HepG2 cells, reduced Bcl-2 gene expression and induced necroptosis by increasing Ripk in MCF-7 cells. In mice, fruti prevented tumor development and reduced Cyclin D1, Bcl-2 and Rela gene levels, and reduced the p-NF-κB/NF-κB ratio in tumor tissue. Furthermore, fruti induced necrosis and apoptosis, increased N-acetyl-β-D-glucosaminidase and TNF-α levels and reduced IL-10 and Vegf levels in tumor tissue. Collectively, fruti exerts antitumor effects through the inhibition of the NF-κB pathway, reducing Cyclin D1 and Bcl-2 levels. In vitro the apoptosis and necroptosis pathways are involved in the cellular death, whereas in vivo, cells undergo necrosis by increased tumor inflammation and reduction of angiogenesis. Thus, fruticuline A acts in tumor cells by multiple mechanisms and represents a promising molecule for drug development in cancer treatment.

scholarly journals Antitumor Activity of Liposomal Prednisolone Phosphate Depends on the Presence of Functional Tumor-Associated Macrophages in Tumor Tissue

Neoplasia ◽  
2008 ◽  
Vol 10 (2) ◽  
pp. 108-117 ◽  
Author(s):  
Manuela Banciu ◽  
Josbert M. Metselaar ◽  
Raymond M. Schiffelers ◽  
Gert Storm
Keyword(s):  
Antitumor Activity ◽  
Tumor Tissue ◽  
Tumor Associated Macrophages

scholarly journals Synthesis and investigation of modified gastrin fragments

2017 ◽  
Vol 16 (3) ◽  
pp. 63-68
Author(s):  
L. P. Sushinina ◽  
A. P. Smirnova ◽  
S. V. Ustinkina ◽  
L. I. Smirnova ◽  
T. A. Sidorova ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cytotoxic Activity ◽  
High Selectivity ◽  
Peptide Hormone ◽  
Antitumor Action ◽  
Transplanted Tumors ◽  
Peptide Chemistry ◽  
Cytotoxic Group ◽  
Inhibition Of Tumor Growth ◽  
New Compounds

Background. The purpose of this investigation is the search of new compounds with high selectivity of antitumor action on the tumor of the gastrointestinal tract (GIT) in the series of analogues of the peptide hormone gastrin. Objective: synthesis of 2 analogues of gastrin, 1 of which contains the cytotoxic group, the study of their cytotoxic and antitumor activity. Materials and methods. Synthesis of peptides was carried out by classical methods of peptide chemistry. Cytotoxic activity was studied on the cell culture НСТ116. Antitumor activity of analogues of gastrin were studied on transplanted tumors of the GIT of mice AKATOL and AKATON. Results. Two analogues of gastrin (octapeptide) were synthesized, 1 of which contains a cytotoxic group. Analogue containing cytotoxic group revealed the cytotoxic activity. Antitumor activity of two analogues of gastrin were studied on transplanted tumors of the GIT of mice AKATOL and AKATON. The cytotoxic and non-cytotoxic analogues of gastrin showed antitumor activity only on AKATON. Inhibition of tumor growth is 74 and 84 %, respectively. Conclusions. The therapeutic effect of two analogues of gastrin on adenocarcinome AKATON, probably, is associated with the expression of gastrin receptors ССК2 in this tumor.

scholarly journals Polystyrene nanoplastics and microplastics can act as Trojan horse carriers of benzo(a)pyrene to mussel hemocytes in vitro

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Alberto Katsumiti ◽  
María Paula Losada-Carrillo ◽  
Marta Barros ◽  
Miren P. Cajaraville
Keyword(s):  
Plasma Membrane ◽  
Cell Viability ◽  
Phagocytic Activity ◽  
Membrane Integrity ◽  
Aquatic Organisms ◽  
Particle Aggregation ◽  
Ros Production ◽  
Plasma Membrane Integrity ◽  
Intracellular Fate

AbstractIn this work we studied the ability of polystyrene (PS) nanoplastics (NPs) and microplastics (MPs) to transfer benzo(a)pyrene (BaP) to mussel hemocytes and to produce toxic effects in vitro. For this, intracellular fate and toxicity of PS NPs (0.05 μm) and MPs (0.5 and 4.5 μm) alone or with BaP and of BaP alone were assessed. Particles of 0.05 and 0.5 µm largely aggregated in the exposure medium whereas presence of BaP reduced particle aggregation. Cells internalized PS NPs and MPs alone or with BaP and these were found inside and outside lysosomes, depending on their size. PS particles alone or with BaP were cytotoxic to hemocytes only at the highest concentrations tested. The same was true for most sublethal endpoints except for increased phagocytic activity provoked by NPs and 0.5 μm MPs at lower concentrations. Plastic particles appeared to be the main drivers for reduced plasma membrane integrity and increased phagocytic and lysosomal activities whereas BaP appeared to contribute more to reduced cell viability and phagocytosis and increased ROS production and genotoxicity. Overall, PS NPs and MPs can act as carriers of BaP to mussel hemocytes, rising concerns about risks plastics associated to pollutants may pose to aquatic organisms.

scholarly journals Phytochemical profile, toxicological evaluation of Rhipsalis baccifera (Sol.) Stearn (Cactaceae) extract and their antitumor activity in Ehrlich carcinoma-bearing mice

2021 ◽  
Author(s):  
Jéssica Alves Cavalcantea ◽  
Luiz da Silva Maia Neto ◽  
Anna Lígia de Castro Figueiredo ◽  
Weslley Oliveira ◽  
José Roberto Pimentel Cabral de Seixas ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Therapeutic Potential ◽  
Lethal Dose ◽  
Artemia Salina ◽  
Subsequent Treatment ◽  
Ehrlich Carcinoma ◽  
Toxicological Evaluation ◽  
Phytochemical Profile

<i>Rhipsalis baccifera</i> (Sol.) Stearn is a typical cactus from tropical regions with wide geographic distribution, and its therapeutic potential is not yet fully understood, such as antitumoral property. Thus, this study evaluated the cytotoxic ethanolic extract of <i>R. baccifera</i> (EERB) and its antitumor activity against Erlich's tumor in mice. The EERB was obtained, and its phytochemical profile was filed by thin-layer chromatography. The toxicity was evaluated in vitro and in vivo using the microcrustacean<i> Artemia salina</i> Leach and mice. The lethal dose was determined after implantation of a tumor cell suspension, with subsequent treatment with EERB (200 mg/kg and 100 mg/kg) 48h after implantation. These values represent the tenth part of the DL<sub>50</sub> and CL<sub>50</sub>, respectively. The presence of phenols, tannins and triterpenes were demonstrated in the phytochemical results. Toxicity was dose-dependent, and the tumor inhibition was 84.1% and 75.8% at doses of 200 mg/kg and 100 mg/kg, respectively. We can highlight that the growth of Erlich's carcinoma suffered inhibitory effects against the EERB. EERB was found to have low acute toxicity and a high potential for use in antitumor therapy. Thus, new studies involving pre-clinical and clinical analyses of the extract are essential to determine the safe dose.

STUDIES ON THE IN VITRO ANTITUMOR ACTIVITY OF FATTY ACIDS: II. SATURATED DICARBOXYLIC ACIDS

1960 ◽  
Vol 38 (6) ◽  
pp. 597-603 ◽  
Author(s):  
Joseph F. Morgan ◽  
Susan Tolnai ◽  
Gordon F. Townsend
Keyword(s):  
Fatty Acids ◽  
Antitumor Activity ◽  
Royal Jelly ◽  
Dicarboxylic Acids ◽  
Ehrlich Carcinoma ◽  
Decenoic Acid ◽  
Fatty Acid Chain ◽  
Transplantable Leukemia ◽  
Akr Mice

Previous studies, which showed that 10-hydroxy-2-decenoic acid from royal jelly possessed in vitro antitumor activity, have been extended to saturated dicarboxylic fatty acids. Seven of eight compounds tested in a series of chain length from C3 to C10 completely prevented the development of the ascites forms of the 6C3HED lymphosarcoma, the Ehrlich carcinoma, and the TA3 mammary carcinoma, as well as the transplantable leukemia of AKR mice. This in vitro antitumor activity could be demonstrated only at pH values below 5.0 and required admixture of the tumor cells and test compounds prior to inoculation of the mice. In general, the antitumor activity of the saturated dicarboxylic acids was found to increase progressively with increasing length of the fatty acid chain.

Abnormal lactate dehydrogenase isoenzyme in serum and tumor tissue of a patient with neuroblastoma.

1985 ◽  
Vol 31 (2) ◽  
pp. 318-320 ◽  
Author(s):  
N Otsu ◽  
M Hirata ◽  
K Miyazawa ◽  
S Tuboi
Keyword(s):  
Lactate Dehydrogenase ◽  
Gel Electrophoresis ◽  
Tumor Tissue ◽  
Surgical Removal ◽  
Marker Enzyme ◽  
Agarose Gel Electrophoresis ◽  
Neurogenic Tumors ◽  
Ldh Activity ◽  
Ldh Isoenzyme ◽  
Normal Human

Abstract Serum and tumor tissue of a patient with neuroblastoma contained an abnormal isoenzyme of lactate dehydrogenase (LDH; EC 1.1.1.27), which, on agarose gel electrophoresis, migrated between LDH-2 and LDH-3 with a mobility the same as that of the extra LDH isoenzyme found in normal human erythrocytes. On surgical removal of the tumor, the high total LDH activity (775 U/L) in the serum of the patient rapidly decreased to normal (70-220 U/L), and the abnormal LDH isoenzyme was no longer detected. The total LDH activity of the abnormal LDH isoenzyme per gram of hemoglobin in the tumor tissue was 26 times that of erythrocytes, suggesting that the abnormal isoenzyme originated mainly from the tumor cells themselves rather than the erythrocytes contained in the tumor tissue. This first report on the appearance of the abnormal LDH isoenzyme in a patient with neuroblastoma suggests that this abnormal LDH isoenzyme may have some significance as a marker enzyme for neurogenic tumors.

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