scholarly journals Exploring the Anticancer Potential of Diiron Bis-cyclopentadienyl Complexes with Bridging Hydrocarbyl Ligands: Behavior in Aqueous Media and In Vitro Cytotoxicity

2020 ◽  
Vol 39 (5) ◽  
pp. 645-657 ◽  
Author(s):  
Gabriele Agonigi ◽  
Lorenzo Biancalana ◽  
Maria Giovanna Lupo ◽  
Monica Montopoli ◽  
Nicola Ferri ◽  
...  
Keyword(s):  
Aqueous Media ◽  
In Vitro Cytotoxicity ◽  
Cyclopentadienyl Complexes

scholarly journals Synthesis and Characterization of Macroinitiators Based on Polyorganophosphazenes for the Ring Opening Polymerization of N-Carboxyanhydrides

Polymers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1446
Author(s):  
Natalia Zashikhina ◽  
Marina Vasileva ◽  
Olga Perevedentseva ◽  
Irina Tarasenko ◽  
Tatiana Tennikova ◽  
...  
Keyword(s):  
Amino Acids ◽  
Degradation Rate ◽  
Aqueous Media ◽  
Delivery Systems ◽  
In Vitro Cytotoxicity ◽  
Side Chains ◽  
Amphiphilic Copolymers ◽  
Hybrid Copolymers

Among the various biocompatible amphiphilic copolymers, biodegradable ones are the most promising for the preparation of drug delivery systems since they are destroyed under physiological conditions, that, as a rule, reduce toxicity and provide controlled release of the drug. Hybrid graft-copolymers consisting of the main inorganic polyphosphazene chain and polypeptide side chains are of considerable interest for the development of delivery systems with a controlled degradation rate, since the main and side chains will have different degradation mechanisms (chemical and enzymatic hydrolysis, respectively). Variable particle degradation rate, controlled by the adjusting the composition of substituents, will allow selective delivery in vivo and controlled drug release. The present work proposes the preparation of biodegradable macroinitiators based on polyorganophosphazenes for the synthesis of hybrid copolymers. Synthesis of novel biodegradable macroinitiators based on polyorganophosphazenes was performed via macromolecular substitution of a polydichlorophosphazene chain with the sodium alcoholates, amines and amino acids. The composition of copolymers obtained was calculated using NMR. These polyorganophosphazenes bearing primary amino groups can be considered as convenient macroinitiators for the polymerization of NCA of α-amino acids in order to prepare hybrid copolymers polyphosphazene-graft-polypeptide. The developed macroinitiators were amphiphilic and self-assembled in the aqueous media into nanoparticles. Furthermore, the ability to encapsulate and release a model substance was demonstrated. In addition, the in vitro cytotoxicity of synthesized polymers was evaluated using two cell lines.

Effects of Antibiotics and Organic Solvents on the In Vitro Cytotoxicity of Other Chemicals

1984 ◽  
Vol 12 (4) ◽  
pp. 203-213
Author(s):  
Richard Clothier ◽  
Thompson Robinson ◽  
Sally Greengrass ◽  
Vivien Heyes ◽  
Julie Ratcliffe ◽  
...  
Keyword(s):  
Cell Line ◽  
Organic Solvents ◽  
Antibacterial Agents ◽  
Culture Media ◽  
Aqueous Media ◽  
In Vitro Cytotoxicity ◽  
Toxic Chemicals ◽  
V79 Cells ◽  
V79 Cell

Since the methods used to maintain cells in vitro can profoundly influence their survival, stability and growth, their effects on responses to potentially toxic chemicals must also be considered. In addition, many xenobiotics are insoluble in aqueous media, and the organic solvents used in presenting them to the cells used in in vitro cytotoxicity tests could themselves be toxic and/or could modify the toxicities of test chemicals. Experiments on an antifungal agent, fungizone, and two aminoglycoside antibacterial agents, gentamicin and kanamycin, showed that BCL-D1 cells (a finite-lived cell line) were more sensitive than V79 cells (a continuous cell line), but increase in total protein during a 3-day culture period was not seriously inhibited when the antibiotics were present at the concentrations recommended for routine use in culture media. Experiments on five organic solvents indicated that DMSO had a significant effect on cell growth, but provided that comparisons were made with the relevant solvent controls, the toxicities of two xenobiotics (dinitrophenol and cycloheximide) were not significantly altered when they were dissolved in organic solvents before being added to V79 cell cultures.

scholarly journals The Cytotoxic Activity of Diiron Bis-Cyclopentadienyl Complexes with Bridging C3-Ligands

2021 ◽  
Vol 11 (10) ◽  
pp. 4351
Author(s):  
Simona Braccini ◽  
Giacomo Provinciali ◽  
Lorenzo Biancalana ◽  
Guido Pampaloni ◽  
Federica Chiellini ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Ovarian Cancer Cell Line ◽  
Iron Oxidation ◽  
Aqueous Media ◽  
Cancer Cell Line ◽  
Resistant Cell ◽  
In Vitro Cytotoxicity ◽  
Resistant Cell Line

Diiron bis-cyclopentadienyl bis-carbonyl cationic complexes with a bridging vinyliminium ligand, [Fe2Cp2(CO)(μ-CO){μ-η1:η3-C3(R′)C2HC1NMe(R″)}]CF3SO3 (R = Xyl = 2,6-C6H3Me2, R′ = Ph, R″ = H, 2a; R = Xyl, R′ = R″ = Me, 2b; R = R′ = Me, R″ = H, 2c; R = Me, R′ = 2-naphthyl, R″ = H, 2d; R = Me, R′ = R″ = Ph, 2e), are easily available from commercial chemicals, robust in aqueous media and exert a variable in vitro cytotoxicity against cancer cell lines depending on the nature of the substituents on the vinyliminium ligand. The anticancer activity is, at least in part, associated to fragmentation reactions, leading to iron oxidation and active neutral and well-defined monoiron species. We report an innovative synthetic procedure for the preparation of 2a,c,d, and a facile method to access the monoiron derivative of 2a, i.e., [FeCp(CO){C1(NMeXyl)C2HC3(Ph)C(O)}] (3a). According to IC50 analyses at different times of incubation of the complexes, 3a is significantly faster in inhibiting cell viability compared to its diiron precursor 2a. The neutral complexes [Fe2Cp2(CO)(μ-CO){μ-k1N:k1C:k1C-C3(R′)C2(Se)C1(NMe2)C4(CO2Y)C5(CO2Y)}] (R′ = Y = Me, 4a; R′ = Pr, Y = tBu, 4b; R′ = Y = Et, 4c) are obtained via the two-step modification of the vinyliminium moiety and comprise a bridging selenophene-decorated alkylidene ligand. The antiproliferative activity exhibited by 4a-c is moderate but comparable on the ovarian cancer cell line A2780 and the corresponding cisplatin resistant cell line, A2780cisR. Complexes 4a-c in aqueous solutions undergo progressive release of the alkylidene ligand as a functionalized selenophene, this process being slower in cell culture medium. Since the released selenophenes SeC1{C(O)R′}C2(NMe2)C3(CO2Y)C4(CO2Y) (R′ = Y = Me, 5a; R′ = Pr, Y = tBu, 5b) are substantially not cytotoxic, it is presumable that the activity of 4a-c is largely ascribable to the {Fe2Cp2(CO)2} scaffold.

scholarly journals Amphiphilic QP(DMAEMA-co-LMA)-b-POEGMA Random-Block Terpolymers as Nanocarriers for Insulin

Biomedicines ◽  
2020 ◽  
Vol 8 (10) ◽  
pp. 392
Author(s):  
Martha Kafetzi ◽  
Stergios Pispas ◽  
Xiaoyan Bao ◽  
Ping Yao
Keyword(s):  
Surface Charge ◽  
Conformational Changes ◽  
Self Assembly ◽  
Electrostatic Interactions ◽  
Aqueous Media ◽  
Physicochemical Characteristics ◽  
In Vitro Cytotoxicity ◽  
Assembly Features

We report on the utilization of the amphiphilic poly[quaternized (2-(N,N-dimethylamino) ethyl methacrylate)]-co-(lauryl methacrylate))-b-poly[(oligo ethylene glycol) methyl ether methacrylate] QP(DMAEMA-co-LMA)-b-POEGMA cationic diblock terpolymer aggregates as nanocarriers for insulin delivery applications. QP(DMAEMA-co-LMA)-b-POEGMA random diblock terpolymer is derived from the chemical modification of the precursor amino diblock copolymer via quaternization, producing permanent positive charges on the macromolecular chain. The QP(DMAEMA-co-LMA)-b-POEGMA diblock terpolymer as well as its amino precursor investigated self-assemble in aqueous media, forming aggregates. In vitro cytotoxicity and in vivo biocompatibility studies on QP(DMAEMA-co-LMA)-b-POEGMA and its amino precursor aggregates, showed good cytocompatibility and biocompatibility. QP(DMAEMA-co-LMA)-b-POEGMA aggregates were chosen to be complexed with insulin due to their self-assembly features and the permanent positive charge in each amino group. QP(DMAEMA-co-LMA)-b-POEGMA aggregates were complexed with insulin through electrostatic interactions. Light scattering techniques were used in order to study the ability of the polymer aggregates to complex with insulin, to determine critical physicochemical parameters such as size, mass, and surface charge of the stable complexes and study the effect of salt addition on their properties. The results showed that in both cases, the complexation process was successful and as the insulin concentration increases, nanosized complexes of different physicochemical characteristics (mass, size, surface charge) and spherical morphology are formed. UV-Vis and fluorescence spectroscopy studies showed that no conformational changes of insulin occurred after the complexation.

In vitro Cytotoxicity and Genotoxicity Analysis of Ten Tannery Chemicals Using SOS/umu Tests and High-content In vitro Micronucleus Tests

2018 ◽  
Vol 21 (4) ◽  
pp. 262-270 ◽  
Author(s):  
Zehao Huang ◽  
Na Li ◽  
Kaifeng Rao ◽  
Cuiting Liu ◽  
Zijian Wang ◽  
...  
Keyword(s):  
Micronucleus Test ◽  
A549 Cells ◽  
Quantitative Structure Activity Relationship ◽  
In Vitro Cytotoxicity ◽  
Cytotoxic Effects ◽  
Qsar Analysis ◽  
Cell Assays ◽  
Micronucleus Tests ◽  
Damaging Effects

Background: More than 2,000 chemicals have been used in the tannery industry. Although some tannery chemicals have been reported to have harmful effects on both human health and the environment, only a few have been subjected to genotoxicity and cytotoxicity evaluations. Objective: This study focused on cytotoxicity and genotoxicity of ten tannery chemicals widely used in China. Materials and Methods: DNA-damaging effects were measured using the SOS/umu test with Salmonella typhimurium TA1535/pSK1002. Chromosome-damaging and cytotoxic effects were determined with the high-content in vitro Micronucleus test (MN test) using the human-derived cell lines MGC-803 and A549. Conclusion: The cytotoxicity of the ten tannery chemicals differed somewhat between the two cell assays, with A549 cells being more sensitive than MGC-803 cells. None of the chemicals induced DNA damage before metabolism, but one was found to have DNA-damaging effects on metabolism. Four of the chemicals, DY64, SB1, DB71 and RR120, were found to have chromosome-damaging effects. A Quantitative Structure-Activity Relationship (QSAR) analysis indicated that one structural feature favouring chemical genotoxicity, Hacceptor-path3-Hacceptor, may contribute to the chromosome-damaging effects of the four MN-test-positive chemicals.

Mixed Micelles as Nano Polymer Therapeutics of Docetaxel: Increased In vitro Cytotoxicity and Decreased In vivo Toxicity

2018 ◽  
Vol 15 (4) ◽  
pp. 564-575 ◽  
Author(s):  
Arehalli S. Manjappa ◽  
Popat S. Kumbhar ◽  
Prajakta S. Khopade ◽  
Ajit B. Patil ◽  
John I. Disouza
Keyword(s):  
Mixed Micelles ◽  
In Vitro Cytotoxicity ◽  
Polymer Therapeutics ◽  
In Vivo Toxicity

Mannose Conjugated Starch Nanoparticles for Preferential Targeting of Liver Cancer

2020 ◽  
Vol 17 ◽  
Author(s):  
Akhlesh Kumar Jain ◽  
Hitesh Sahu ◽  
Keerti Mishra ◽  
Suresh Thareja
Keyword(s):  
Side Effects ◽  
Liver Cancer ◽  
Entrapment Efficiency ◽  
Xrd Analysis ◽  
In Vitro Cytotoxicity ◽  
Physical Interaction ◽  
Scanning Calorimetry ◽  
Starch Nanoparticles

Aim: To design D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for site specific delivery. Background: Liver cancer is the third leading cause of death in world and fifth most often diagnosed cancer is the major global threat to public health. Treatment of liver cancer with conventional method bears several side effects, thus to undertake these side effects as a formulation challenge, it is necessary to develop novel target specific drug delivery system for the effective and better localization of drug into the proximity of target with restricting the movement of drug in normal tissues. Objective: To optimize and characterize the developed D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for effective treatment of liver cancer. Materials and methods: 5-FU loaded JFSSNPs were prepared and optimized formulation had higher encapsulation efficiency were conjugated with D-Mannose. These formulations were characterized for size, morphology, zeta potential, X-Ray Diffraction, and Differential Scanning Calorimetry. Potential of NPs were studied using in vitro cytotoxicity assay, in vivo kinetic studies and bio-distribution studies. Result and discussion: 5-Fluorouracil loaded NPs had particle size between 336 to 802nm with drug entrapment efficiency was between 64.2 to 82.3%. In XRD analysis, 5-FU peak was diminished in the diffractogram, which could be attributed to the successful incorporation of drug in amorphous form. DSC study suggests there was no physical interaction between 5- FU and Polymer. NPs showed sustained in vitro 5-FU release up to 2 hours. In vivo, mannose conjugated NPs prolonged the plasma level of 5-FU and assist selective accumulation of 5-FU in the liver (vs other organs spleen, kidney, lungs and heart) compared to unconjugated one and plain drug. Conclusion: In vivo, bio-distribution and plasma profile studies resulted in significantly higher concentration of 5- Fluorouracil liver suggesting that these carriers are efficient, viable, and targeted carrier of 5-FU treatment of liver cancer.

5-Nitro-Thiophene-Thiosemicarbazone Derivatives Present Antitumor Activity Mediated by Apoptosis and DNA Intercalation

2019 ◽  
Vol 19 (13) ◽  
pp. 1075-1091 ◽  
Author(s):  
Karla Mirella Roque Marques ◽  
Maria Rodrigues do Desterro ◽  
Sandrine Maria de Arruda ◽  
Luiz Nascimento de Araújo Neto ◽  
Maria do Carmo Alves de Lima ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Antitumor Activity ◽  
Cell Line ◽  
Mitochondrial Membrane ◽  
In Vitro Cytotoxicity ◽  
Dna Intercalation ◽  
Phase Cell ◽  
Fluorescence Studies ◽  
In Silico Studies

Background: Considering the need for the development of new antitumor drugs, associated with the great antitumor potential of thiophene and thiosemicarbazonic derivatives, in this work we promote molecular hybridization approach to synthesize new compounds with increased anticancer activity. Objective: Investigate the antitumor activity and their likely mechanisms of action of a series of N-substituted 2-(5-nitro-thiophene)-thiosemicarbazone derivatives. Methods: Methods were performed in vitro (cytotoxicity, cell cycle progression, morphological analysis, mitochondrial membrane potential evaluation and topoisomerase assay), spectroscopic (DNA interaction studies), and in silico studies (docking and molecular modelling). Results: Most of the compounds presented significant inhibitory activity; the NCIH-292 cell line was the most resistant, and the HL-60 cell line was the most sensitive. The most promising compound was LNN-05 with IC50 values ranging from 0.5 to 1.9 µg.mL-1. The in vitro studies revealed that LNN-05 was able to depolarize (dose-dependently) the mitochondrial membrane, induceG1 phase cell cycle arrest noticeably, promote morphological cell changes associated with apoptosis in chronic human myelocytic leukaemia (K-562) cells, and presented no topoisomerase II inhibition. Spectroscopic UV-vis and molecular fluorescence studies showed that LNN compounds interact with ctDNA forming supramolecular complexes. Intercalation between nitrogenous bases was revealed through KI quenching and competitive ethidium bromide assays. Docking and Molecular Dynamics suggested that 5-nitro-thiophene-thiosemicarbazone compounds interact against the larger DNA groove, and corroborating the spectroscopic results, may assume an intercalating interaction mode. Conclusion: Our findings highlight 5-nitro-thiophene-thiosemicarbazone derivatives, especially LNN-05, as a promising new class of compounds for further studies to provide new anticancer therapies.

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