Green Engineering of Silver Nanoparticles Using Leucas aspera Extract: Cytotoxic Efficacy in HeLa Cell Line

Aims: The present study was conducted to examine the inhibitory effects of synthesized sulfonylhydrazones on the expression of CD73 (ecto-5′-NT). Background: CD73 (ecto-5′-NT) represents the most significant class of ecto-nucleotidases which are mainly responsible for dephosphorylation of adenosine monophosphate to adenosine. Inhibition of CD73 played an important role in the treatment of cancer, autoimmune disorders, precancerous syndromes, and some other diseases associated with CD73 activity. Objective: Keeping in view the significance of CD73 inhibitor in the treatment of cervical cancer, a series of sulfonylhydrazones (3a-3i) derivatives synthesized from 3-formylchromones were evaluated. Methods: All sulfonylhydrazones (3a-3i) were evaluated for their inhibitory activity towards CD73 (ecto-5′-NT) by the malachite green assay and their cytotoxic effect was investigated on HeLa cell line using MTT assay. Secondly, most potent compound was selected for cell apoptosis, immunofluorescence staining and cell cycle analysis. After that, CD73 mRNA and protein expression were analyzed by real-time PCR and Western blot. Results: Among all compounds, 3h, 3e, 3b, and 3c were found the most active against rat-ecto-5′-NT (CD73) enzyme with IC50 (µM) values of 0.70 ± 0.06 µM, 0.87 ± 0.05 µM, 0.39 ± 0.02 µM and 0.33 ± 0.03 µM, respectively. These derivatives were further evaluated for their cytotoxic potential against cancer cell line (HeLa). Compound 3h and 3c showed the cytotoxicity at IC50 value of 30.20 ± 3.11 µM and 86.02 ± 7.11 µM, respectively. Furthermore, compound 3h was selected for cell apoptosis, immunofluorescence staining and cell cycle analysis which showed promising apoptotic effect in HeLa cells. Additionally, compound 3h was further investigated for its effect on expression of CD73 using qRT-PCR and western blot. Conclusion: Among all synthesized compounds (3a-3i), Compound 3h (E)-N'-((6-ethyl-4-oxo-4H-chromen-3-yl) methylene)-4-methylbenzenesulfonohydrazide was identified as most potent compound. Additional expression studies conducted on HeLa cell line proved that this compound successfully decreased the expression level of CD73 and thus inhibiting the growth and proliferation of cancer cells.

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Molecular events after antisense inhibition of hMSH2 in a HeLa cell line

Mutation Research/Genetic Toxicology and Environmental Mutagenesis ◽

10.1016/s1383-5718(98)00108-9 ◽

1998 ◽

Vol 418 (2-3) ◽

pp. 61-71 ◽

Cited By ~ 6

Author(s):

Ying Qian ◽

Yingnian Yu ◽

Xingruo Cheng ◽

Jianhong Luo ◽

Haiyang Xie ◽

...

Keyword(s):

Hela Cell ◽

Cell Line ◽

Antisense Inhibition ◽

Hela Cell Line ◽

Molecular Events

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Synthesis, structural analysis, solution equilibria and biological activity of rhodium(iii) complexes with a quinquedentate polyaminopolycarboxylate

RSC Advances ◽

10.1039/c6ra26199j ◽

2017 ◽

Vol 7 (9) ◽

pp. 5282-5296 ◽

Cited By ~ 5

Author(s):

Marija S. Jeremić ◽

Hubert Wadepohl ◽

Vesna V. Kojić ◽

Dimitar S. Jakimov ◽

Ratomir Jelić ◽

...

Keyword(s):

Biological Activity ◽

Structural Analysis ◽

Antitumor Activity ◽

Hela Cell ◽

Cell Line ◽

Hela Cell Line ◽

Solution Equilibria ◽

Line P

Two new Rh(iii)–ed3a complexes [Rh(ed3a)(OH2)]·H2O and Na[Rh(ed3a)Cl]·H2O have shown good antitumor activity, especially against HeLa cell line.

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Exploring the potential of imines as antiprotozoan agents with focus on t. Brucei and p. Falciparum

10.21504/10962/62235 ◽

2018 ◽

Author(s):

◽

Kola Augustus Oluwafemi

Keyword(s):

Hela Cell ◽

Cell Line ◽

Special Focus ◽

Hela Cell Line ◽

Free Energies ◽

Imino Group ◽

Design Synthesis ◽

Lead Compounds ◽

Pyridine Moiety ◽

Nmr Study

This work focuses on the design, synthesis and evaluation of imine-containing heterocyclic and acyclic compounds with special focus on their bioactivity against parasitic protozoans (P. falciparum and T. brucei) - given the context of drug resistance in the treatment of malaria and Human African sleeping sickness and the fact that several bioactive organic compounds have been reported to possess the imino group. Starting from 2-aminopyridine, novel #-alkylated-5-bromo-7-azabenzimidazoles and substituted 5-bromo-1-(carbamoylmethy)-7-azabenzimidazole derivatives were prepared, and their bioactivity against parasitic protozoans was assessed. NMR spectra of the substituted 5- bromo-1-(carbamoylmethy)-7-azabenzimidazole derivatives exhibited rotational isomerism, and a dynamic NMR study was used in the estimation of the rate constants and the free- energies of activation for rotation. The free-energy differences between the two rotamers were determined and the more stable conformations were predicted. Novel 2-phenyl-7-azabenzimidazoles were also synthesised from 2-aminopyridine. A convenient method for the regioselective formylation of 2,3-diaminopyridines into 2-amino- 7-(benzylimino)pyridine analogues of 2-phenyl-7-azabenzimidazole was developed, and some of the resulting imino derivatives were hydrogenated to verify the importance of the imino moiety for bioactivity. The 2-phenyl-7-azabenzimidazoles and the 2-amino-7- (benzylimino)pyridine analogues were screened for their anti-protozoal activity and their cytotoxicity level was determined against the HeLa cell line. In order to validate the importance of the pyridine moiety, novel #-(phenyl)-2- hydroxybenzylimines, #-(benzyl)-2-hydroxybenzylimines and (±)-trans-1,2-bis[2- hydroxybenzylimino]cyclohexanes were also synthesized and screened for activity against the parasitic protozoans and for cytotoxicity against the HeLa cell line. The biological assay results indicated that these compounds are not significantly cytotoxic and a good number of them show potential as lead compounds for the development of new malaria and trypanosomiasis drugs.

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