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

RSC Advances ◽  
2017 ◽  
Vol 7 (9) ◽  
pp. 5282-5296 ◽  
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.

Glyco-gold nanoparticle shapes enhance carbohydrate–protein interactions in mammalian cells

Nanoscale ◽  
2016 ◽  
Vol 8 (25) ◽  
pp. 12729-12735 ◽  
Author(s):  
Sivakoti Sangabathuni ◽  
Raghavendra Vasudeva Murthy ◽  
Preeti Madhukar Chaudhary ◽  
Manalee Surve ◽  
Anirban Banerjee ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Hela Cell ◽  
Cell Line ◽  
Gold Nanoparticle ◽  
Protein Interactions ◽  
Mammalian Cells ◽  
Hela Cell Line ◽  
Line P ◽  
Nanoparticle Shapes

Shape dependent uptake of glyco-gold nanoparticles (G-AuNPs) in a HeLa cell line.

scholarly journals Methylation of 2-Aryl-2-(3-indolyl)acetohydroxamic Acids and Evaluation of Cytotoxic Activity of the Products

Molbank ◽  
10.3390/m1307 ◽  
2021 ◽  
Vol 2022 (1) ◽  
pp. M1307
Author(s):  
Dmitrii A. Aksenov ◽  
Alexander V. Aksenov ◽  
Lidiya A. Prityko ◽  
Nicolai A. Aksenov ◽  
Liliya V. Frolova ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Hela Cell ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Hydroxamic Acid ◽  
Methyl Esters ◽  
Hydroxamic Acids ◽  
Hela Cell Line ◽  
Lead Compounds

2-Aryl-2-(3-indolyl)acetohydroxamic acids demonstrate promising antitumor activity, but quickly metabolize in vivo via glucuronidation of hydroxamic acid residue. In an attempt to improve their pharmacokinetics, methyl esters were synthesized via a newly developed protocol for chemoselective mono-methylation of hydroxamic acids. The cytotoxicity of these derivatives against the HeLa cell line was evaluated and found to be inferior compared to the parent lead compounds.

scholarly journals Synthesis and Biological Activity Studies of Methyl-5-(Hydroxymethyl)-2-Furan Carboxylate and Derivatives

2019 ◽  
Vol 35 (3) ◽  
pp. 080-1085 ◽  
Author(s):  
Weerachai Phutdhawong ◽  
Siwaporn Inpang ◽  
Thongchai Taechowisan ◽  
Waya S. Phutdhawong
Keyword(s):  
Biological Activity ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Furfuryl Alcohol ◽  
Methyl Acetate ◽  
Biological Activities ◽  
Hela Cell Line ◽  
Amine Derivative

Methyl-5-(hydroxymethyl)-2-furan carboxylate and derivatives were prepared from furfuryl alcohol and their biological activities were studied for cytotoxicity against cancer cell lines HeLa, HepG2 and Vero, and Gram (+) and Gram (-) bacteria. The amine derivative, (5-(((2-(1H-indol-3-yl)ethyl)amino)methyl) furan-2-yl)methyl acetate, was found to have the most potent biological activity with IC50 62.37 µg/mL against the HeLa cell line and MIC 250 µg/mL against the photogenic bacteria.

Effect of secondary metabolites of Berberis vulgaris and Petasites hybridus on apoptosis and cell cycle of HeLa cell line.

2021 ◽  
Vol 39 (15_suppl) ◽  
pp. e15063-e15063
Author(s):  
Yaroslav S. Enin ◽  
Oleg N. Burov ◽  
Ludmila A. Ryadinskaya ◽  
Natalia A. Abramova ◽  
Aza A. Agieva ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Antitumor Activity ◽  
Hela Cell ◽  
Cell Line ◽  
Fold Increase ◽  
Hela Cell Line ◽  
Plant Metabolites ◽  
Secondary Plant Metabolites ◽  
Berberis Vulgaris

e15063 Background: The study of the possible antitumor activity of secondary plant metabolites either in the form of individual agents or in combination with clinically used drugs is considered as a promising direction in the therapy of malignant tumors. The aim of this study was an estimation of antitumor activity of secondary plant metabolites in the in vitro experiment on the HeLa cell line. Methods: Secondary metabolites were extracted from plant raw materials and were isolated by preparative chromatography. Determination of their composition was carried out using HPLC; obtained compound structures were identified by NMR. We selected 4 secondary metabolites from Petasites hybridus for testing: (2,4-dihydroxy-2,5-dimethylfuran-3 (2H), 5-(hydroxymethyl) furan-2-carbaldehyde, 2,2,8-trimethyldecahydroazulene-5,6-dicarbaldehyde, Corynan), and 1 secondary metabolite from Berberis vulgaris : a berberine chloride (BBR, C20H18NO4+Cl- is a derivative of 5,6-dihydrobenzo[a,g] isoquinolinium). HeLa CCL2 cultivation was carried out under standard conditions in the MEM medium. When reaching the 75-80% confluence level we replaced nutrient medium with the introduction of secondary metabolites (concentration 4 and 12 μg/ml) and cultured for 24 and 72 hours. Cell survival was determined on a NanoEnTek JuliFl counter (Korea) in the presence of 0.4% trypan blue. Apoptosis was assessed on a flow cytometer BD FACSCanto II using FITC Annexin V Apoptosis Detection Kit I. Post-exposure copy number and expression were assessed by Real-time PCR with a panel of genes CASP9, CASP8, CASP3, TP53, MDM2, BAX, BCL2, CDK1, BRCA1, BRCA 2, RB1. Results: All obtained data were normalized by negative control. When we used 4 μg/ml berberine solution with 72-hour exposition, the proapoptogenic effect was maximal, causing the death of 67.2% of HeLa cells (29.3% early apoptosis, 37.2% late apoptosis, 0.7% necrosis). Within 24 hours, berberine at the same concentration caused a 2-fold increase in TP53 expression relative to MDM2. An increase in its concentration to 12 μg/ml and exposure for up to 72 hours led to a 31-fold increase in TP53/MDM2. The terpenoid 2,2,8-trimethyldecahydroazulene-5,6-dicarbaldehyde at a concentration of 12 μg/ml after 72 hours of cultivation caused a 6.5-fold increase in the TP53/MDM2 ratio. The corynan alkaloid (12 μg/ml) at an exposure of 72 hours increased the BAX/BCL ratio by 2.4 times. There were no statistically significant differences in the expression and copy number of the remaining genes studied. Conclusions: Berberine, corynan, 2,2,8-trimethyldecahydroazulene-5,6-dicarbaldehyde showed high promise in the HeLa cell line in vitro, since they surpassed the antitumor activity of other metabolites of Berberis vulgaris and Petasites hybridus.

Identification and Expression Analysis of CD73 Inhibitors in Cervical Cancer

2020 ◽  
Vol 16 ◽  
Author(s):  
Jamshed Iqbal ◽  
Ayesha Basharat ◽  
Sehrish Bano ◽  
Syed Mobasher Ali Abid ◽  
Julie Pelletier ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cervical Cancer ◽  
Western Blot ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Apoptosis ◽  
Immunofluorescence Staining ◽  
Cell Cycle Analysis ◽  
Hela Cell Line ◽  
Cell Line Hela

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.

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

1998 ◽  
Vol 418 (2-3) ◽  
pp. 61-71 ◽  
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

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

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.

331P Synergistic effects of ferula gummosa and radiotherapy to induce cytotoxicity and apoptosis in the hela cell line

2016 ◽  
Vol 27 (suppl_9) ◽  
Author(s):  
A. Fani-Pakdel ◽  
S.H. Forouzmand ◽  
S.H. Mousavi ◽  
V. Vazifedan ◽  
M. Nourbakhsh ◽  
...  
Keyword(s):  
Hela Cell ◽  
Cell Line ◽  
Synergistic Effects ◽  
Hela Cell Line
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