THE EFFECT OF STRUCTURE ON NUCLEOSIDE KINASE ACTIVITY

1967 ◽  
Vol 45 (10) ◽  
pp. 1619-1632 ◽  
Author(s):  
K. J. Pierre ◽  
A. P. Kimball ◽  
G. A. LePage
Keyword(s):  
Divalent Cation ◽  
Kinase Activity ◽  
Ehrlich Ascites Carcinoma ◽  
Guanosine Monophosphate ◽  
Inosine Monophosphate ◽  
Ehrlich Ascites ◽  
Derivatives Of ◽  
Effect Of Structure

A study was made of the in vitro phosphorylation of some nucleosides in cell-free extracts from a thioguanine-resistant subline of Ehrlich ascites carcinoma which lacked inosine monophosphate – guanosine monophosphate pyrophosphorylase. The results indicated that there were kinases which catalyzed the phosphorylation of a variety of nucleosides. Ribofuranosyl-6-thiopurme was phosphorylated whereas the xylofuranosyl-, arabinofuranosyl-, and lyxofuranosyl-6-thiopurine were not substrates. The xylose and ribose derivatives of 6-methylthiopurine were phosphorylated but the arabinose derivative was not. Guanosine and some of its analogs were also phosphorylated but no correlation could be found between structure and phosphorylation of the guanosine analogs tested.The reaction showed dependence on the addition of divalent cation and an ATP-regenerating system.

INHIBITION OF RIBONUCLEOSIDE METABOLISM IN EHRLICH ASCITES TUMOR CELLS BY PURINE ANALOGUE RIBONUCLEOSIDES

1965 ◽  
Vol 43 (10) ◽  
pp. 1701-1710 ◽  
Author(s):  
A. R. P. Paterson ◽  
A. I. Simpson
Keyword(s):  
Tumor Cells ◽  
Ehrlich Ascites Carcinoma ◽  
Carcinoma Cells ◽  
Ehrlich Ascites Tumor Cells ◽  
Purine Analogues ◽  
Intact Cells ◽  
Ehrlich Ascites ◽  
Derivatives Of ◽  
Related Compounds

Several aspects of the metabolism of inosine and uridine by Ehrlich ascites carcinoma cells in vitro have been found to be inhibited by ribonucleoside derivatives of four purine analogues. The synthesis of both inosine and uridine by intact tumor cells was profoundly inhibited in the presence of 6-methylmercaptopurine ribonucleoside. Also inhibited were inosine and uridine cleavage, and the exchange of isotope between these ribonucleosides and the corresponding C14 labelled bases. These reactions, however, were not inhibited when they took place in broken-cell preparations. Similarly, inosine metabolism in intact cells (but not in broken cells) was profoundly inhibited by three related compounds: the ribonucleosides of the 6-chloro, 6-methylmercapto, and 6-propylmercapto derivatives of 2-aminopurine.

METABOLISM OF 6-MERCAPTOPURINE RIBONUCLEOSIDE BY EHRLICH ASCITES CARCINOMA CELLS

1964 ◽  
Vol 42 (10) ◽  
pp. 1415-1423 ◽  
Author(s):  
A. R. P. Paterson ◽  
Aiko Sutherland
Keyword(s):  
Ehrlich Ascites Carcinoma ◽  
Carcinoma Cells ◽  
Glycosidic Linkage ◽  
Ascites Tumor ◽  
Resistant Line ◽  
Cell Compartment ◽  
Ehrlich Ascites ◽  
A Cell ◽  
Derivatives Of

Ribonucleoside derivatives of 6-mercaptopurine (6-MP) and other purine bases were rapidly catabolized when incubated with Ehrlich ascites carcinoma cells in vitro. The catabolism of purine ribonucleosides proceeded by way of phosphorolytic cleavage of the glycosidic linkage and resulted in accumulation of the liberated base in the incubation medium. The ribosyl portions of ribonucleoside substrates were utilized with the formation of lactate, which also appeared extracellularly.Cells of a 6-MP-resistant subline of the Ehrlich ascites tumor degraded 6-MP ribonucleoside (6-MPR) at rates comparable to those of the parent line. This finding, when considered with other characteristics of the resistant line of cells, implied that cleavage of 6-MPR took place in a cell compartment from which inosinate pyrophosphorylase was absent.

scholarly journals Biological screening and assessment of certain substituted monoazo heterocycles containing sulphur and / or nitrogen and their seleno like moieties

2017 ◽  
Vol 19 (4) ◽  
pp. 28-35
Author(s):  
Mohamed E. Khalifa ◽  
Adel A. Gobouri
Keyword(s):  
Carcinoma Cell ◽  
Ehrlich Ascites Carcinoma ◽  
Azo Compounds ◽  
Gram Negative Bacteria ◽  
Pathogenic Microorganisms ◽  
Gram Positive Bacteria ◽  
Ehrlich Ascites ◽  
Structural Activity Relationship ◽  
Derivatives Of

Abstract The monoazo substituted five membered heterocycles, along with their seleno like moieties are still of interest in organic chemistry due to their medicinal and valuable applications. In continuation of our interest in the study of heterocyclic azo compounds containing sulphur and / or nitrogen heteroatoms, the synthesis of 5-aryl mono azo-thiazol-2-ylcarbamoyl-thiophene along with their seleno like derivatives of pyridine, pyridazine and quinolone, were accomplished. All the synthesized compounds were in vitro screening of their antioxidant activity, antitumor activity against Ehrlich ascites carcinoma cell EACC cell line and antimicrobial activity against various pathogenic microorganisms, such as Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) and Gram-negative bacteria (Escherichia coli and Salmonella typhimurium) and fungi strains of Aspergillus flavus and Candida albicans. The structural–activity relationship was studied based on the obtained data.

Tumor cell metabolism in vitro: a study of incubation media

1970 ◽  
Vol 48 (4) ◽  
pp. 517-519 ◽  
Author(s):  
I. C. Caldwell ◽  
Marianne F. Chan
Keyword(s):  
Nucleic Acid ◽  
Structural Integrity ◽  
Cell Metabolism ◽  
Ehrlich Ascites Carcinoma ◽  
Leukemic Cells ◽  
Prolonged Incubation ◽  
Ehrlich Ascites ◽  
Eac Cells ◽  
Rna And Dna

A number of incubation media which have been used in studies of the metabolism of Ehrlich ascites carcinoma (EAC) cells in vitro have been examined with respect to their abilities to support the incorporation of radioactive precursors into nucleotides and nucleic acids, and to maintain the structural integrity and tumor-inducing abilities of EAC cells. Cells incubated in the chemically-defined "Fischer's medium for leukemic cells of mice" were able to produce lethal tumors in mice after more than 16 h of incubation, maintained their structural integrity on prolonged incubation, and catalyzed high rates of incorporation of exogenously added substrates into nucleotides, RNA, and DNA. However, cells incubated in balanced salts solutions supplemented with glucose had these characteristics: (a) were unable to produce lethal tumors after 4 h of incubation, (b) released large amounts of nucleotide, nucleic acid, and protein material into the medium after less than 2 h of incubation, and (c) catalyzed the incorporation of radioactive precursors into nucleotides and RNA at much lower rates than did cells incubated in Fischer's medium, and were virtually unable to catalyze the incorporation of adenine-14C into DNA.

STUDIES ON THE BIOSYNTHESIS OF NUCLEOTIDES IN EHRLICH ASCITES CARCINOMA CELLS IN VITRO

1965 ◽  
Vol 43 (2) ◽  
pp. 209-224 ◽  
Author(s):  
B. I. Uppin ◽  
P. G. Scholefield
Keyword(s):  
Exchange Reaction ◽  
Ehrlich Ascites Carcinoma ◽  
Carcinoma Cells ◽  
The Other ◽  
Metabolic Inhibitors ◽  
Ehrlich Ascites ◽  
Oxidative Pathway ◽  
Time Courses ◽  
Oxidation Of Glucose

Studies have been made of the effects of metabolic inhibitors on the oxidation and incorporation of radioactivity into nucleotides of glucose labelled in the 1, 2, and 6 positions. The results indicate that in Ehrlich ascites carcinoma cells the predominant oxidative pathway is the hexosemonophosphate shunt. Investigation of the time courses of oxidation of the labelled glucose molecules confirms this conclusion. The pattern of incorporation of radioactivity initially suggests that nucleotide ribose is not formed via this pathway. However, it is shown that the coupling of an active transketolase system with the other enzymes of the hexosemonophosphate shunt provides a sufficient explanation of all the experimental observations. The conclusion is reached that pentose is formed by oxidation of glucose through the shunt but that the labelling pattern is largely established as the result of the exchange reaction catalyzed by transketolase.

In vitro anticancer activity of Astaxanthin

2021 ◽  
Vol 5 (3) ◽  
pp. 033-037
Author(s):  
Uma Nath U ◽  
Ravi. R ◽  
Sundara Ganapathy ◽  
Lal Prasanth
Keyword(s):  
Anticancer Activity ◽  
Tumor Volume ◽  
Hematological Parameters ◽  
Ehrlich Ascites Carcinoma ◽  
High Dose ◽  
Ehrlich Ascites ◽  
Shrimp Shell ◽  
Shrimp Shell Waste ◽  
Wbc Count

This study was designed to determine the in vitro anticancer potential of the Astaxanthin isolated from shrimp shell waste (ETC) against Ehrlich Ascites Carcinoma (EAC) induced cancer in swiss albino mice. The anticancer activity was assessed using in vitro cytotoxicAity, mean survival time, tumor volume and hematological studies. The reliable criteria for evaluating the potential of any anticancer agent is the prolongation of lifespan of the animal and decrease in WBC count of blood. The high dose of ETC (200 mg/kg, orally) significantly reduced the tumor growth which was demonstrated by increased lifespan of the mice and restoration of hematological parameters. ETC was also found to be cytotoxic in the in vitro parameter which shows that ETC possesses significant anticancer potential.

scholarly journals Synthesis and Comparative Evaluation of Polymethoxy Substituted 1,4-Naphthoquinones and their Acetyl-O-glucosides as Cytotoxic Agents

2017 ◽  
Vol 12 (7) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Yuri E. Sabutski ◽  
Marina N. Semenova ◽  
Ekaterina A. Yurchenko ◽  
Nikita S. Polonik ◽  
Vladimir A. Denisenko ◽  
...  
Keyword(s):  
Comparative Evaluation ◽  
Ehrlich Ascites Carcinoma ◽  
Carcinoma Cells ◽  
Cytotoxic Agents ◽  
Cytotoxic Effects ◽  
Micromolar Concentration ◽  
Sea Urchin Embryo ◽  
Ehrlich Ascites ◽  
Methoxy Groups ◽  
Derivatives Of

Twenty five hydroxy-, chloro- and methoxy derivatives of natural and synthetic naphthazarins and their acetylated O-glycosides were synthesized. Targeted compounds were screened as cytotoxic agents on mouse Ehrlich ascites carcinoma cells using MTT test. Chloro- and methoxy-substituted naphthoquinones as well as naphthoquinone O-acetylglucosides were the most potent with IC50 in low micromolar concentration range. Glucosidation of hydroxynaphthoquinones was shown to enhance cytotoxicity, whereas methoxylation yielded both more active and less active derivatives depending on the number and position of methoxy groups. Evaluation using a phenotypic sea urchin embryo assay suggested that naphthazarins exerted their cytotoxic effects through tubulin-unrelated mechanism.

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