In vitro cytotoxicity assessment of imidazolium ionic liquids: Biological effects in fish Channel Catfish Ovary (CCO) cell line

2013 ◽  
Vol 92 ◽  
pp. 112-118 ◽  
Author(s):  
Kristina Radošević ◽  
Marina Cvjetko ◽  
Nevenka Kopjar ◽  
Rudjer Novak ◽  
Jerka Dumić ◽  
...  
2004 ◽  
Vol 23 (11) ◽  
pp. 513-517 ◽  
Author(s):  
P Stepnowski ◽  
A C Skladanowski ◽  
A Ludwiczak ◽  
E Laczyńska

This paper presents cytotoxicity data of selected imidazolium ionic liquids evaluated in vitro on the human tumor cell line HeLa. It was found that for 1-n-butyl-3-methylimidazolium entities the toxicity depends strongly on the associated anion; EC50 values are lowest for tetrafluoroborate. No direct dependence of the reduced effect concentration was found on elongating the short, methyl chain to ethyl or n-hexyl. Only for the ionic liquid with an n-decyl chain, the longest one studied, did higher hydrophobicity result in a EC50 one order of magnitude lower than that obtained with the n-butyl entity. The effect concentrations of imidazolium ionic liquids in the HeLa system used are lower than the values obtained for conventional organic solvents such as dichloromethane, toluene or xylene.


2020 ◽  
Vol 17 (1) ◽  
pp. 1-12
Author(s):  
Rita Caparica ◽  
André Rolim Baby ◽  
Tânia Almeida ◽  
João Guilherme Costa

Bioactive compounds from natural sources have been extensively studied as potential therapeutic agents, due to their chemical, structural, and biological properties. Among them, hydroxycinnamic acids emerge with a very interesting pharmacological potential to prevent and treat several diseases, including cancer. However, while some studies support their anticancer activity, other reports indicate otherwise. Since the impact of these compounds on renal cancer is not well established, further studies are needed to better understand their biological effects and their potential therapeutic uses in this cancer. In this work, the cytotoxicity of three hydroxycinnamic acids: ferulic, caffeic and p-coumaric acids, was evaluated on 786-O human renal cancer cells by MTT and CV assays. At concentrations up to 250 µM, none of the studied natural compounds showed cytotoxic effects to 786-O cell line. At higher concentrations (500 and 1000 µM), while ferulic acid also did not significantly influence the cell viability of 786-O cells, p-coumaric and caffeic acids decreased the renal cancer cells viability. Nevertheless, further studies on the biological activity of these compounds, using other methodologies, as well as using other cancer cell models, should be performed.


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 ◽  
...  

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.


2020 ◽  
Vol 20 (6) ◽  
pp. 700-708
Author(s):  
Mitra Korani ◽  
Sara Nikoofal-Sahlabadi ◽  
Amin R. Nikpoor ◽  
Solmaz Ghaffari ◽  
Hossein Attar ◽  
...  

Aims: Here, three liposomal formulations of DPPC/DPPG/Chol/DSPE-mPEG2000 (F1), DPPC/DPPG/Chol (F2) and HSPC/DPPG/Chol/DSPE-mPEG2000 (F3) encapsulating BTZ were prepared and characterized in terms of their size, surface charge, drug loading, and release profile. Mannitol was used as a trapping agent to entrap the BTZ inside the liposomal core. The cytotoxicity and anti-tumor activity of formulations were investigated in vitro and in vivo in mice bearing tumor. Background: Bortezomib (BTZ) is an FDA approved proteasome inhibitor for the treatment of mantle cell lymphoma and multiple myeloma. The low solubility of BTZ has been responsible for the several side effects and low therapeutic efficacy of the drug. Encapsulating BTZ in a nano drug delivery system; helps overcome such issues. Among NDDSs, liposomes are promising diagnostic and therapeutic delivery vehicles in cancer treatment. Objective: Evaluating anti-tumor activity of bortezomib liposomal formulations. Methods: Data prompted us to design and develop three different liposomal formulations of BTZ based on Tm parameter, which determines liposomal stiffness. DPPC (Tm 41°C) and HSPC (Tm 55°C) lipids were chosen as variables associated with liposome rigidity. In vitro cytotoxicity assay was then carried out for the three designed liposomal formulations on C26 and B16F0, which are the colon and melanoma cancer mouse-cell lines, respectively. NIH 3T3 mouse embryonic fibroblast cell line was also used as a normal cell line. The therapeutic efficacy of these formulations was further assessed in mice tumor models. Result: MBTZ were successfully encapsulated into all the three liposomal formulations with a high entrapment efficacy of 60, 64, and 84% for F1, F2, and F3, respectively. The findings showed that liposomes mean particle diameter ranged from 103.4 to 146.8nm. In vitro cytotoxicity studies showed that liposomal-BTZ formulations had higher IC50 value in comparison to free BTZ. F2-liposomes with DPPC, having lower Tm of 41°C, showed much higher anti-tumor efficacy in mice models of C26 and B16F0 tumors compared to F3-HSPC liposomes with a Tm of 55°C. F2 formulation also enhanced mice survival compared with untreated groups, either in BALB/c or in C57BL/6 mice. Conclusion: Our findings indicated that F2-DPPC-liposomal formulations prepared with Tm close to body temperature seem to be effective in reducing the side effects and increasing the therapeutic efficacy of BTZ and merits further investigation.


2016 ◽  
Vol 54 (2) ◽  
Author(s):  
Ana Ljevar ◽  
◽  
Natka Ćurko ◽  
Marina Tomašević ◽  
Kristina Radošević ◽  
...  

Carbon ◽  
2008 ◽  
Vol 46 (11) ◽  
pp. 2-3
Author(s):  
Hong-mei Han ◽  
Gary J. Phillips ◽  
Sergey V. Mikhalovsky ◽  
Andrew W. Lloyd

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3179 ◽  
Author(s):  
Peng Zhang ◽  
Xin Li ◽  
Xiao-Long Yuan ◽  
Yong-Mei Du ◽  
Bin-Gui Wang ◽  
...  

An endophytic fungus Arthrinium arundinis TE-3 was isolated and purified from the fresh leaves of cultivated tobacco (Nicotiana tabacum L.). Chemical investigation on this fungal strain afforded three new prenylated diphenyl ethers (1−3) as well as three known analogues (4−6). Structure elucidation of the isolated compounds was carried out by analysis of 1D and 2D nuclear magnetic resonance (NMR) and high-resolution electrospray ionization mass spectroscopy (HRESIMS) spectra, as well as by comparison of those data with literature data. The absolute configuration of the stereogenic center at C-8 in 1 was assigned by comparison of the experimental and calculated ECD spectra. Compounds 1 and 2 showed selective antifungal activity against Mucor hiemalis with minimum inhibitory concentration (MIC) values of 8 and 4 μg/mL, respectively. Compounds 5 and 6 exhibited inhibitory activity against Alteraria alternata with an MIC value of 8 μg/mL. In the cytotoxic assay, 2, 5, and 6 displayed moderate in vitro cytotoxicity against the human monocytic cell line (THP-1 cell line), with IC50 values of 40.2, 28.3, and 25.9 μM, respectively. This study indicated that endophytic fungi possess great potential for exploring new bioactive secondary metabolites.


2019 ◽  
Vol 6 (1) ◽  
pp. 30-32
Author(s):  
Poonkodi K ◽  
Mini R ◽  
Vimaladevi K ◽  
Prabhu V ◽  
Anusuya M ◽  
...  

The present investigation is carried out to study the invitro cytotoxicity of ethanol extract of Syzygium samarangense leaves on HeLa cell line by using MTT assay. Ethanol extract of S. samarangense showed concentration dependent activity on HeLa cell line with IC50 value of 40.5 μg/ml which shows that ethanol extract of S. samarangense posses significant cytoxicity.Moreover the preliminary phytochemical screening showed the presence of fatty acids, alkaloids, flavonoids, terphenoids, saponins, tannins and steroids which are responsible for its cytotoxicity. There are only a few reports are available for cytotoxicity of ethanol extract of S. samarangense.


2021 ◽  
Vol 33 ◽  
pp. 03001
Author(s):  
Annise Proboningrat ◽  
Amaq Fadholly ◽  
Sri Agus Sudjarwo ◽  
Fedik Abdul Rantam ◽  
Agung Budianto Achmad

Several efforts have been made to discover new anticancer agents based on natural ingredients. Meanwhile, previous studies have shown that different Pine genus species exhibit cytotoxic activity against various types of cancer cells. This plant is rich in phenolic compounds, especially procyanidins, flavonoids, and phenolic acids. Therefore, this study aims to investigate the in vitro cytotoxicity of Pinus merkusii needles extract on HeLa cancer cell lines. The cytotoxicity assessment was measured using MTT assay and expressed as IC50 value. The results showed that the ethanolic extract poses a dose and time-dependent cytotoxic activity with an IC50 value of 542.5 µg/ml at 48 hours of incubation. Based on this result, Pinus merkusii needles’ ethanolic extract has the potential of a novel candidate for an anticancer agent.


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