Glucosylated Polypropylenimine Dendrimer as a Novel Gene Carrier

2007 ◽  
Vol 342-343 ◽  
pp. 457-460 ◽  
Author(s):  
You Kyoung Kim ◽  
In Kyu Park ◽  
Hu Lin Jiang ◽  
Rohidas B. Arote ◽  
Hwan Jeong Jeong ◽  
...  
Keyword(s):  
Sulfuric Acid ◽  
Dna Binding ◽  
Gene Delivery ◽  
Hela Cell ◽  
Cell Line ◽  
Plasmid Dna ◽  
Transfection Efficiency ◽  
Hela Cell Line ◽  
Binding Ability ◽  
Low Cytotoxicity

Polypropylenimine (PPI) dendrimers have been used by many researchers as gene delivery carriers due to their high functionality. Glucose as a kind of carbohydrate is biocompatible and hydrophilic. In this study, we synthesized glucosylated PPI (G-PPI) dendrimers to reduce cytotoxicity. Glucose substitution of G-PPI dendrimers was determined by the sulfuric acid micromethod. The G-PPI dendrimer was complexed with plasmid DNA in various N/P ratios, and the complex was characterized. G-PPI dendrimers showed good DNA binding ability and high protection of DNA from nuclease attack. The G-PPI dendrimer had low cytotoxicity compared to PPI dendrimer by cytotoxicity assay. Also, transfection efficiency was influenced by glucosylation degree and the transfection efficiency for the G-PPI-5 was slightly higher than that of PPI dendrimer in HeLa cell line.

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

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.

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.

scholarly journals Synthesis, DNA-binding and antiproliferative activity of N-(Nitrogen heterocyclic) norcantharidin acylamide acid

2009 ◽  
Vol 7 (3) ◽  
pp. 569-575 ◽  
Author(s):  
Wen-Zhong Zhu ◽  
Rui-Ding Hu ◽  
Qiu-Yue Lin ◽  
Xiao-Xia Wang ◽  
Xiao-Liang Zheng
Keyword(s):  
Dna Binding ◽  
Cell Line ◽  
Elemental Analysis ◽  
Antiproliferative Activity ◽  
Plasmid Dna ◽  
H Nmr ◽  
Smmc7721 Cell ◽  
Calf Thymus ◽  
Binding Experiment ◽  
Pbr322 Plasmid

AbstractTwo novel norcantharidin acylamide acids (HL1=N-pyrimidine norcantharidin acylamide acid, C12H13N3O4; HL2=N-pyridine norcantharidin acylamide acid, C13H14N2O4) were synthesized by a reaction of norcantharidin(NCTD) with 2-aminopyrimidine and 2-aminopyridine, respectively. Their structures were characterized by elemental analysis, IR, UV and 1 H NMR. Fluorescence titration and viscosity measurements indicated that HL1, HL2 and HL3 (HL3=N-phenyl norcantharidin acylamide acid, C14H15NO4) can bind calf thymus DNA via partial intercalation. The liner Stern-Volmer quenching constant Ksv values for HL1, HL2 and HL3 were 2.05 × 104 L mol−1, 1.15 × 104 L mol−1 and 8.30×103 L mol−1, respectively. Two compounds containing heterocycle of HL1 and HL2 have been found to cleave pBR322 plasmid DNA at physiological pH and temperature. The test of antiproliferation activity showed that the compounds had moderate to strong antiproliferative ability against the tested cell lines except of HL3 against the SMMC7721 cell line. The results indicated that the heterocycle attached to the norcantharidin was favorable to antiproliferative activity. This result was consistent with the DNA binding experiment.

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

scholarly journals Synthesis, and Characterization, and Evaluation of Cellular Effects of the FOL-PEG-g-PEI-GAL Nanoparticles as a Potential Non-Viral Vector for Gene Delivery

2010 ◽  
Vol 2010 ◽  
pp. 1-10 ◽  
Author(s):  
S. Ghiamkazemi ◽  
A. Amanzadeh ◽  
R. Dinarvand ◽  
M. Rafiee-Tehrani ◽  
M. Amini
Keyword(s):  
Gene Delivery ◽  
Zeta Potential ◽  
Surface Charge ◽  
Cell Line ◽  
Graft Copolymer ◽  
Viral Vector ◽  
Transfection Efficiency ◽  
High Surface ◽  
Liver Cells ◽  
Dna Complexes

In this manuscript, we synthesized the potential non viral vector for gene delivery with proper transfection efficiency and low cytotoxicity. Polyethylenimine (PEI) is a well-known cationic polymer which has high positive surface charge for condensing plasmid DNA. However; it is highly cytotoxic in many cell lines because of the high surface charge, non-biodegradability and non-biocompatibility. To enhance PEI biodegradability, the graft copolymer “PEG-g-PEI” was synthesized. To target cancer liver cells, two targeting ligands folic acid and galactose (lactobionic acid) which are over expressed on human hepatocyte carcinoma were attached to graft copolymer and “FOL-PEG-g-PEI-GAL” copolymer was synthesized. Composition of this grafted copolymer was characterized using1H-NMR and FTIR spectra. The molecular weight and zeta potential of this copolymer was compared to PEI. The particle size and zeta potential of FOL-PEG-g-PEI-GAL/DNA complexes at various N/P ratio were measured using dynamic light scattering (DLS). Cytotoxicity of the copolymer was also studied in cultured HepG2 human hepatoblastoma cell line. The FOL-PEG-g-PEI-GAL/DNA complexes at various N/P ratios exhibited no cytotoxicity in HepG2 cell line compared to PEI 25K as a control. The novel copolymer showed enhanced biodegradability in physiological conditions in compared with PEI and targeted cultured HepG2 cells. More importantly, significant transfection efficiency was exhibited in cancer liver cells. Together, our results showed that “FOL-PEG-g-PEI-GAL” nanoparticals could be considered as a useful non-viral vector for targeted gene delivery.

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