Inhibitory effect of conjugated eicosapentaenoic acid on human DNA topoisomerases I and II

2005 ◽  
Vol 435 (1) ◽  
pp. 197-206 ◽  
Author(s):  
Yuko Yonezawa ◽  
Tsuyoshi Tsuzuki ◽  
Takahiro Eitsuka ◽  
Teruo Miyazawa ◽  
Takahiko Hada ◽  
...  
Keyword(s):  
Eicosapentaenoic Acid ◽  
Inhibitory Effect ◽  
Dna Topoisomerases ◽  
Human Dna

Antitumor Effect of Pomolic Acid in Acute Myeloid Leukemia Cells Involves Cell Death, Decreased Cell Growth and Topoisomerases Inhibition

2019 ◽  
Vol 18 (10) ◽  
pp. 1457-1468
Author(s):  
Michelle X.G. Pereira ◽  
Amanda S.O. Hammes ◽  
Flavia C. Vasconcelos ◽  
Aline R. Pozzo ◽  
Thaís H. Pereira ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Death ◽  
Acute Myeloid Leukemia ◽  
Cell Lines ◽  
Myeloid Leukemia ◽  
Natural Compound ◽  
Dna Topoisomerases ◽  
Human Dna ◽  
Pomolic Acid ◽  
Acute Myeloid

Background: Acute myeloid leukemia (AML) represents the largest number of annual deaths from hematologic malignancy. In the United States, it was estimated that 21.380 individuals would be diagnosed with AML and 49.5% of patients would die in 2017. Therefore, the search for novel compounds capable of increasing the overall survival rate to the treatment of AML cells is urgent. Objectives: To investigate the cytotoxicity effect of the natural compound pomolic acid (PA) and to explore the mechanism of action of PA in AML cell lines with different phenotypes. Methods: Three different AML cell lines, HL60, U937 and Kasumi-1 cells with different mechanisms of resistance were used to analyze the effect of PA on the cell cycle progression, on DNA intercalation and on human DNA topoisomerases (hTopo I and IIα) in vitro studies. Theoretical experiments of the inhibition of hTopo I and IIα were done to explore the binding modes of PA. Results: PA reduced cell viability, induced cell death, increased sub-G0/G1 accumulation and activated caspases pathway in all cell lines, altered the cell cycle distribution and inhibited the catalytic activity of both human DNA topoisomerases. Conclusion: Finally, this study showed that PA has powerful antitumor activity against AML cells, suggesting that this natural compound might be a potent antineoplastic agent to improve the treatment scheme of this neoplasm.

Specific inhibitory effect of dietary eicosapentaenoic acid on N-nitroso-N-methylurea-induced mammary carcinogenesis in female Sprague—Dawley rats

1990 ◽  
Vol 11 (11) ◽  
pp. 2015-2019 ◽  
Author(s):  
Toshiyuki Takata ◽  
Toshiyuki Minoura ◽  
Hideho Takada ◽  
Michitomo Sakaguchi ◽  
Manabu Yamamura ◽  
...  
Keyword(s):  
Eicosapentaenoic Acid ◽  
Mammary Carcinogenesis ◽  
Inhibitory Effect ◽  
Sprague Dawley ◽  
Sprague Dawley Rats

Inhibitory Effect of New Semisynthetic Usnic Acid Derivatives on Human Tyrosyl-DNA Phosphodiesterase 1

Planta Medica ◽  
2018 ◽  
Vol 85 (02) ◽  
pp. 103-111 ◽  
Author(s):  
Nadezhda Dyrkheeva ◽  
Olga Luzina ◽  
Aleksandr Filimonov ◽  
Olga Zakharova ◽  
Ekaterina Ilina ◽  
...  
Keyword(s):  
Biological Activity ◽  
Usnic Acid ◽  
Inhibitory Effect ◽  
Repair Enzyme ◽  
Topoisomerase 1 ◽  
Anticancer Properties ◽  
Human Dna ◽  
Whole Number ◽  
Ic50 Values ◽  
Low Cytotoxicity

AbstractUsnic acid, a lichen secondary metabolite produced by a whole number of lichens, has attracted the interest of researchers owing to its broad range of biological activity, including antiviral, antibiotic, anticancer properties, and it possessing a certain toxicity. The synthesis of new usnic acid derivatives and the investigation of their biological activity may lead to the discovery of compounds with better pharmacological and toxicity profiles. In this context, a series of new usnic acid derivatives comprising a terpenoid moiety were synthesized, and their ability to inhibit the catalytic activity of the human DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 was investigated. The most potent compounds (15a, 15b, 15g, and 16a, 16b, 16g) had IC50 values in the range of 0.33 – 2.7 µM. The inhibitory properties were mainly dependent on the flexibility and length of the terpenoid moiety, but not strongly dependent on the configuration of the asymmetric centers. The synthesized derivatives showed low cytotoxicity against human cell lines in an MTT assay. They could be used as a basis for the development of more effective anticancer therapies when combined with topoisomerase 1 inhibitors.

Anthocyanidins Modulate the Activity of Human DNA Topoisomerases I and II and Affect Cellular DNA Integrity

2005 ◽  
Vol 18 (9) ◽  
pp. 1395-1404 ◽  
Author(s):  
Michael Habermeyer ◽  
Jessica Fritz ◽  
Hans U. Barthelmes ◽  
Morten O. Christensen ◽  
Morten K. Larsen ◽  
...  
Keyword(s):  
Dna Integrity ◽  
Dna Topoisomerases ◽  
Human Dna ◽  
Cellular Dna

The Mechanism of Inhibitory Effect of Eicosapentaenoic Acid on Phagocytic Activity and Chemotaxis of Human Neutrophil Granulocytes

1996 ◽  
Vol 79 (3) ◽  
pp. 224-228 ◽  
Author(s):  
Sándor Sipka ◽  
Indranil Dey ◽  
Csaba Buda ◽  
József Csongor ◽  
Gyula Szegedi ◽  
...  
Keyword(s):  
Eicosapentaenoic Acid ◽  
Human Neutrophil ◽  
Phagocytic Activity ◽  
Inhibitory Effect ◽  
Neutrophil Granulocytes

The Topopyrones Poison Human DNA Topoisomerases I and II

2008 ◽  
Vol 130 (39) ◽  
pp. 12888-12889 ◽  
Author(s):  
Qasim A. Khan ◽  
Mark A. Elban ◽  
Sidney M. Hecht
Keyword(s):  
Dna Topoisomerases ◽  
Human Dna

scholarly journals Artemisinin Derivatives with Antimelanoma Activity Show Inhibitory Effect against Human DNA Topoisomerase 1

2020 ◽  
Vol 11 (5) ◽  
pp. 1035-1040
Author(s):  
Lorenzo Botta ◽  
Silvia Filippi ◽  
Claudio Zippilli ◽  
Silvia Cesarini ◽  
Bruno Mattia Bizzarri ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Dna Topoisomerase ◽  
Artemisinin Derivatives ◽  
Topoisomerase 1 ◽  
Human Dna

Human DNA topoisomerases IIα and IIβ can functionally substitute for yeast TOP2 in chromosome segregation and recombination

1996 ◽  
Vol 252 (1-2) ◽  
pp. 79-86 ◽  
Author(s):  
Sanne Jensen ◽  
Charles S. Redwood ◽  
John R. Jenkins ◽  
Anni H. Andersen ◽  
Ian D. Hickson
Keyword(s):  
Chromosome Segregation ◽  
Dna Topoisomerases ◽  
Human Dna
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