scholarly journals Synthesis, Spectroscopy, Light Stability, Single-Crystal Analysis, and In Vitro Cytotoxic Activity on HepG2 Liver Cancer of Two Novel Silver(I) Complexes of Miconazole

2020 ◽  
Vol 21 (10) ◽  
pp. 3629
Author(s):  
Karolina Stryjska ◽  
Lidia Radko ◽  
Lilianna Chęcińska ◽  
Joachim Kusz ◽  
Andrzej Posyniak ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Membrane Damage ◽  
Membrane Integrity ◽  
Free Ligand ◽  
Cellular Membrane ◽  
Biologically Active ◽  
Total Protein Content ◽  
Mitochondrial Activity ◽  
Cytotoxic Activities

Two novel silver(I) complexes of the biologically active ligand miconazole in the form of Ag(MCZ)2X (MCZ = 1-[2-(2,4-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]-1H-imidazole]; X = NO3− (1), ClO4− (2)) were synthesized and fully characterized. The complexes were obtained by reactions of Ag(I) salts with miconazole (MCZ). Silver(I) complexes were characterized by elemental analysis, 1H-NMR and infrared (IR) spectroscopy, electrospray ionization (ESI)-MS spectrometry, and X-ray-crystallography. This work also presents a cytotoxicity study of the silver(I) complexes of miconazole and appropriate silver(I) salts using Balb/c 3T3 and HepG2 cell lines. The cytotoxicity of the compounds was assessed based on four biochemical endpoints: lysosomal activity (neutral red uptake (NRU) assay), mitochondrial activity (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay), total protein content (TPC assay), and cellular membrane integrity (lactate dehydrogenase (LDH) assay). The cancer HepG2 cells were more sensitive to the complexes tested, and the most affected endpoint was cellular membrane damage compared to Balb/c 3T3 fibroblasts. Moreover, study complexes inhibited the growth of cancer cells at submicromolecular concentrations (0.26–0.47 μM) lower than that required for the anticancer agent, cisplatin, in MTT, NRU, and TPC assays. Both complexes were characterized by higher toxicity to human cancer cells (HepG2) than silver(I) salts and the free ligand. Combination of Ag(I) salts with miconazole is associated with the marked improvement of cytotoxic activities that can be considered as the significant point in the construction of a new generation of antineoplastic agents.

scholarly journals Silver(I) Complexes of the Pharmaceutical Agents Metronidazole and 4-Hydroxymethylpyridine: Comparison of Cytotoxic Profile for Potential Clinical Application

Molecules ◽  
2019 ◽  
Vol 24 (10) ◽  
pp. 1949 ◽  
Author(s):  
Lidia Radko ◽  
Sylwia Stypuła-Trębas ◽  
Andrzej Posyniak ◽  
Dominik Żyro ◽  
Justyn Ochocki
Keyword(s):  
Silver Nitrate ◽  
Clinical Application ◽  
Hepg2 Cells ◽  
Membrane Damage ◽  
Membrane Integrity ◽  
Cellular Membrane ◽  
Water Soluble ◽  
Total Protein Content ◽  
Silver Complexes ◽  
Potential Clinical Application

In previous papers, we have reported on the high antifungal and significant antibacterial activity against Gram-positive and Gram-negative bacteria of the water-soluble silver(I) complexes of metronidazole and derivatives of pyridine compared to silver nitrate. In the present study, the cytotoxic activity of the silver(I) complexes of metronidazole and 4-hydroxymethylpyridine was compared with that of silver nitrate. Metronidazole and 4-hydroxymethylpyridine were investigated using Balb/c 3T3 and HepG2 cell lines in order to evaluate the potential clinical application of silver(I) complexes. The cells were exposed for 72 h to compounds at eight concentrations. The cytotoxic concentrations (IC50) of the study compounds were assessed within four biochemical endpoints: mitochondrial activity, lysosomal activity, cellular membrane integrity, and total protein content. The investigated silver(I) complexes displayed comparable cytotoxicity to that of silver nitrate used in clinics. Mean cytotoxic concentrations calculated for investigated silver(I) complexes from concentration–response curves ranged from 2.13 to 26.5 µM. HepG2 cells were less sensitive to the tested complexes compared to fibroblasts (Balb/c 3T3). However, the most affected endpoint for HepG2 cells was cellular membrane damage. The cytotoxicity of both silver complexes was comparable for Balb/c 3T3 cells. The cytotoxic potential of the new silver(I) compounds compared to that of silver nitrate used in medicine indicates that they are safe and could be used in clinical practice. The presented results are yet more stimulating to further studies that evaluate the therapeutic use of silver complexes.

scholarly journals Influence of fluoroquinolones on viability of Balb/c 3T3 and HepG2 cells

2013 ◽  
Vol 57 (4) ◽  
pp. 599-606 ◽  
Author(s):  
Lidia Radko ◽  
Maria Minta ◽  
Sylwia Stypuła-Trębas
Keyword(s):  
Cell Lines ◽  
Membrane Integrity ◽  
Cellular Membrane ◽  
Neutral Red ◽  
Total Protein Content ◽  
Mitochondrial Activity ◽  
Response Curves ◽  
Lactate Dehydrogenase Release ◽  
Hepg2 Cell Lines ◽  
Hepatoma Hepg2

Abstract The cytotoxic potential of fluoroquinolones (enrofloxacin, ciprofloxacin, difloxacin, sarafloxacin, danofloxacin, norfloxacin and marbofloxacin) was investigated using mouse fibroblasts Balb/c 3T3 and human hepatoma HepG2 cell lines. The cells were exposed for 24, 48, and 72 h to drugs at eight concentrations ranged from 0.78 to 100 μg/mL. Four independent cytotoxicity assays were applied, in which various endpoints were assessed: mitochondrial activity - MTT reduction, lysosomal activity - neutral red uptake, total protein content, and cellular membrane integrity - lactate dehydrogenase release. Mean effective cytotoxic concentrations (EC50) calculated at different time points from concentration-response curves ranged from 10 to 100 μg/mL. The most affected endpoint in both cell lines was mitochondrial activity. The EC50-MTT-72 h <10 μg/mL was found for difloxacin, marbofloxacin (fibroblasts), sarafloxacin, and norfloxacin (HepG2). The data shows that cytotoxicity of the fluoroquinolones appears after longer exposure of both cell cultures to these compounds.

Rhodium(i) N-heterocyclic carbene complexes: synthesis and cytotoxic properties

2021 ◽  
Vol 45 (11) ◽  
pp. 5176-5183
Author(s):  
Ichraf Slimani ◽  
Serap Şahin-Bölükbaşı ◽  
Mustafa Ulu ◽  
Enes Evren ◽  
Nevin Gürbüz ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Mtt Assay ◽  
Incubation Time ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Carbene Complexes ◽  
Human Cancer Cells ◽  
Benzimidazolium Salts ◽  
Ht 29

A series of benzimidazolium salts and their [RhCl(NHC)(COD)] complexes were synthesized. All compounds were screened for in vitro cytotoxic activities against a panel of human cancer cells (HT-29 colon, Ishikawa endometrial, U-87 glioblastoma) using the MTT assay for 48 h incubation time.

scholarly journals Antioxidant and Cytotoxic Activities of Myrtaceae Essential Oils Rich in Terpenoids From Brazil

2021 ◽  
Vol 16 (2) ◽  
pp. 1934578X2199615
Author(s):  
Lucas Botelho Jerônimo ◽  
Jamile S. da Costa ◽  
Laine C. Pinto ◽  
Raquel C. Montenegro ◽  
William N. Setzer ◽  
...  
Keyword(s):  
Essential Oils ◽  
Cancer Cells ◽  
Antioxidant Activities ◽  
Human Cancer ◽  
Psidium Guajava ◽  
Cytotoxic Activities ◽  
Chemical Compositions ◽  
Main Compound ◽  
Human Cancer Cells ◽  
High Concentrations

This work analyzed the chemical compositions and evaluated the antioxidant and cytotoxic activities of essential oils (EO) of Eugenia patrisii (Epat), Eugenia stipitata (Esti), Myrcia splendens (Mspl), Myrcia sylvatica (Msyl), Psidium guajava (Pgua), and Psidium guineense (Pgui-1 and Pgui-2) from the Brazilian Amazon. Sesquiterpenoids were found in high concentrations in the oils of E. patrisii and M. splendens, which were rich in E-caryophyllene (32.0% and 45.8%); E. stipitata and M. sylvatica, which displayed germacrene D (11.8%) and germacrene B (24.5%); and P. guajava that showed epi-β-bisabolol (16.1%) as the main compound. However, P. guineense samples (Pgui-1 and Pgui-2) were rich in monoterpenoids such as limonene (Pgui-1: 30.2%; Pgui-2 30.4%) and α-pinene (Pgui-1: 22.5%; Pgui-2: 17.7%). The samples showed a weak and moderate antioxidant activities in the DPPH assay, displaying inhibition rates from 11.5% to 38.6% (at 10 mg/mL). All samples were cytotoxic against human cancer cells by the MTT method. Epat oil showed higher activity against melanoma (SKMEL-19, IC505.8 µg/mL), gastric (AGP01, IC503.2 µg/mL), and colon (HCT116, IC506.7 µg/mL). Meanwhile, the samples Pgua and Pgui were more active against breast cancer cells (MCF7, IC5012.4 µg/mL and 11.6 µg/mL, respectively).

Synthesis, antimicrobial and cytotoxic activities, and structure–activity relationships of gypsogenin derivatives against human cancer cells

2014 ◽  
Vol 82 ◽  
pp. 565-573 ◽  
Author(s):  
Safiye Emirdağ-Öztürk ◽  
Tamer Karayıldırım ◽  
Aysun Çapcı-Karagöz ◽  
Özgen Alankuş-Çalışkan ◽  
Ali Özmen ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Structure Activity Relationships ◽  
Human Cancer Cells ◽  
Structure Activity

ChemInform Abstract: Sesquiterpenes from Rhizomes of Cyperus rotundus with Cytotoxic Activities on Human Cancer Cells in vitro.

ChemInform ◽  
2016 ◽  
Vol 47 (8) ◽  
pp. no-no ◽  
Author(s):  
Byeol Ryu ◽  
Hye Mi Kim ◽  
Jae-Seung Lee ◽  
Yoon Jin Cho ◽  
Myung Sook Oh ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Cyperus Rotundus ◽  
Cytotoxic Activities ◽  
Human Cancer Cells

Enniatin Exerts p53-Dependent Cytostatic and p53-Independent Cytotoxic Activities against Human Cancer Cells

2007 ◽  
Vol 20 (3) ◽  
pp. 465-473 ◽  
Author(s):  
Rita Dornetshuber ◽  
Petra Heffeter ◽  
Majid-Reza Kamyar ◽  
Thomas Peterbauer ◽  
Walter Berger ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Human Cancer Cells

scholarly journals Half-Wave Potentials and In Vitro Cytotoxic Evaluation of 3-Acylated 2,5-Bis(phenylamino)-1,4-benzoquinones on Cancer Cells

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1780 ◽  
Author(s):  
Julio Benites ◽  
Jaime A. Valderrama ◽  
Maryan Ramos ◽  
Maudy Valenzuela ◽  
Angélica Guerrero-Castilla ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Colorimetric Method ◽  
Cytotoxic Activities ◽  
Cyclic Voltammograms ◽  
Electronic Effects ◽  
Human Embryonic Kidney Cells ◽  
Human Cancer Cells ◽  
Half Wave

A broad range of 3-acyl-2,5-bis(phenylamino)-1,4-benzoquinones were synthesized and their voltammetric values, as well as in vitro cancer cell cytotoxicities, were assessed. The members of this series were prepared from acylbenzoquinones and phenylamines, in moderate to good yields (47–74%), through a procedure involving a sequence of two in situ regioselective oxidative amination reactions. The cyclic voltammograms of the aminoquinones exhibit two one-electron reduction waves to the corresponding radical-anion and dianion, and two quasi-reversible oxidation peaks. The first and second half-wave potential values (E1/2) of the members of the series were sensitive to the push-pull electronic effects of the substituents around the benzoquinone nucleus. The in vitro cytotoxic activities of the 3-acyl-2,5-bis(phenylamino)-1,4-benzoquinones against human cancer cells (bladder and prostate) and non-tumor human embryonic kidney cells were measured using the MTT colorimetric method. The substitution of both aniline groups, by either methoxy (electron donating effect) or fluorine (electron withdrawal effect), decreased the cytotoxicity in the aminoquinones. Among the members of the unsubstituted phenylamino series, two of the 18 compounds showed interesting anti-cancer activities. A preliminary assay, looking for changes in the expression of selected genes, was performed. In this context, the two compounds increased TNF gene expression, suggesting an association with an inflammatory-like response.

scholarly journals Syntheses of l-Rhamnose-Linked Amino Glycerolipids and Their Cytotoxic Activities against Human Cancer Cells

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 566
Author(s):  
Makanjuola Ogunsina ◽  
Pranati Samadder ◽  
Temilolu Idowu ◽  
Mark Nachtigal ◽  
Frank Schweizer ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Cytotoxic Activities ◽  
Drug Resistant ◽  
Ether Lipids ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
Synthetic Procedure ◽  
Major Impediment

A major impediment to successful cancer treatment is the inability of clinically available drugs to kill drug-resistant cancer cells. We recently identified metabolically stable l-glucosamine-based glycosylated antitumor ether lipids (GAELs) that were cytotoxic to chemotherapy-resistant cancer cells. In the absence of commercially available l-glucosamine, many steps were needed to synthesize the compound and the overall yield was poor. To overcome this limitation, a facile synthetic procedure using commercially available l-sugars including l-rhamnose and l-glucose were developed and the l-GAELs tested for anticancer activity. The most potent analog synthesized, 3-amino-1-O-hexadecyloxy-2R-(O–α-l-rhamnopyranosyl)-sn- glycerol 3, demonstrated a potent antitumor effect against human cancer cell lines derived from breast, prostate, and pancreas. The activity observed was superior to that observed with clinical anticancer agents including cisplatin and chlorambucil. Moreover, like other GAELs, 3 induced cell death by a non-membranolytic caspase-independent pathway.

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