Biological activity of myricetin and its derivatives against human leukemic cell lines in vitro

2000 ◽  
Vol 42 (5) ◽  
pp. 475-478 ◽  
Author(s):  
Kostas Dimas ◽  
Costas Demetzos ◽  
Dimitra Angelopoulou ◽  
Antonios Kolokouris ◽  
Thomas Mavromoustakos
Keyword(s):  
Biological Activity ◽  
Cell Lines ◽  
Leukemic Cell ◽  
Human Leukemic Cell ◽  
Leukemic Cell Lines

A test system for leukotriene synthesis inhibitors based on the in-vitro differentiation of the human leukemic cell lines HL-60 and Mono Mac 6

1997 ◽  
Vol 356 (4) ◽  
pp. 441-445 ◽  
Author(s):  
Oliver Werz ◽  
Nicole Schneider ◽  
Martina Brungs ◽  
Eckart-Roderich Sailer ◽  
Hasan Safayhi ◽  
...  
Keyword(s):  
Cell Lines ◽  
Leukemic Cell ◽  
Test System ◽  
In Vitro Differentiation ◽  
Human Leukemic Cell ◽  
Leukemic Cell Lines

Repositioning of Difluorinated Propanediones as Inhibitors of Histone Methyltransferases and their Biological Evaluation in Human Leukemic Cell Lines

2019 ◽  
Vol 18 (13) ◽  
pp. 1892-1899 ◽  
Author(s):  
Tanushree Pal ◽  
Asmita Sharda ◽  
Bharat Khade ◽  
C. Sinha Ramaa ◽  
Sanjay Gupta
Keyword(s):  
Cell Lines ◽  
Physiological Role ◽  
Leukemic Cell ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Leukemic Cell Lines ◽  
Histone Lysine ◽  
Histone Lysine Methyltransferase ◽  
Subsequent Decrease

Background: At present, ‘pharmaco-epigenomics’ constitutes the hope in cancer treatment owing to epigenetic deregulation- a reversible process and playing a role in malignancy. Objective: Chemotherapy has many limitations like host-tissue toxicity, drug resistance. Hence, it is imperative to unearth targets to better treat cancer. Here, we intend to repurpose a set of our previously synthesized difluorinated Propanediones (PR) as Histone lysine Methyltransferase inhibitors (HMTi). Methods: The cell lines of leukemic origin viz. histiocytic lymphoma (U937) and acute T-cell leukemia (JURKAT) were treated with PR-1 to 7 after docking studies with active pocket of HMT. The cell cycle analysis, in vitro methylation and cell proliferation assays were carried out to delineate their physiological role. Results: A small molecule PR-4, at 1 and 10µM, has shown to alter the methylation of histone H3 and H4 in both cell lines. Also, treatment shows an increase in G2/M population and a subsequent decrease in the G0/G1 population in U937. In JURKAT, an increase in both G2/M and S phase population was observed. The sub-G1 population showed a steady rise with increase in dose and prolonged time intervals in U937 and JURKAT cell lines. In SRB assay, the PR showed a cell growth of 42.6 and 53.4% comparable to adriamycin; 44.5 and 53.2% in U937 and JURKAT, respectively. The study suggests that PR-4 could emerge as a potential HMT inhibitor. Conclusion: The molecule PR-4 could be a lead in developing more histone lysine methyltransferases inhibitors with potential to be pro-apoptotic agents.

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