Anticancer and antitrypanosomal activities of trinuclear ruthenium compounds with orthometalated phenazine ligands

2020 ◽  
Vol 49 (45) ◽  
pp. 16440-16452 ◽  
Author(s):  
Camila Fontes Neves da Silva ◽  
Pedro Branco Hauch Chrispim ◽  
Bruna Possato ◽  
Gisele Bulhões Portapilla ◽  
Thomas N. Rohrabaugh ◽  
...  
Keyword(s):  
Dna Intercalation ◽  
Melanoma Cancer ◽  
Ruthenium Compounds

Four metalo-intercalators ([Ru3(μ3-O)(μ2-OAc)5(L)(py)2]PF6, L = phenazines) present high DNA intercalation constants and high HSA affinity. They are active against melanoma cancer and T. Cruzi parasite.

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.

Single-chain antibody-decorated Au nanocages@liposomal layer nanoprobes for targeted SERS imaging and remote-controlled photothermal therapy of melanoma cancer cells

2021 ◽  
Vol 124 ◽  
pp. 112086
Author(s):  
Ghazal Farahavar ◽  
Samira Sadat Abolmaali ◽  
Foroogh Nejatollahi ◽  
Amin Safaie ◽  
Sanaz Javanmardi ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Photothermal Therapy ◽  
Single Chain ◽  
Single Chain Antibody ◽  
Melanoma Cancer ◽  
Sers Imaging

scholarly journals Cross-Modality Imaging of Murine Tumor Vasculature—a Feasibility Study

2021 ◽  
Author(s):  
Lydia M. Zopf ◽  
Patrick Heimel ◽  
Stefan H. Geyer ◽  
Anoop Kavirayani ◽  
Susanne Reier ◽  
...  
Keyword(s):  
Cancer Biology ◽  
Tumor Vasculature ◽  
Vascular Imaging ◽  
Melanoma Cancer ◽  
Positron Emission ◽  
Vessel Network ◽  
Research Questions ◽  
Magnetic Resonance Imaging Mri ◽  
Single Tumor ◽  
Penetration Depths

AbstractTumor vasculature and angiogenesis play a crucial role in tumor progression. Their visualization is therefore of utmost importance to the community. In this proof-of-principle study, we have established a novel cross-modality imaging (CMI) pipeline to characterize exactly the same murine tumors across scales and penetration depths, using orthotopic models of melanoma cancer. This allowed the acquisition of a comprehensive set of vascular parameters for a single tumor. The workflow visualizes capillaries at different length scales, puts them into the context of the overall tumor vessel network and allows quantification and comparison of vessel densities and morphologies by different modalities. The workflow adds information about hypoxia and blood flow rates. The CMI approach includes well-established technologies such as magnetic resonance imaging (MRI), positron emission tomography (PET), computed tomography (CT), and ultrasound (US), and modalities that are recent entrants into preclinical discovery such as optical coherence tomography (OCT) and high-resolution episcopic microscopy (HREM). This novel CMI platform establishes the feasibility of combining these technologies using an extensive image processing pipeline. Despite the challenges pertaining to the integration of microscopic and macroscopic data across spatial resolutions, we also established an open-source pipeline for the semi-automated co-registration of the diverse multiscale datasets, which enables truly correlative vascular imaging. Although focused on tumor vasculature, our CMI platform can be used to tackle a multitude of research questions in cancer biology.

B16 Melanoma Cancer Cells with Higher Metastatic Potential are More Deformable at a Whole-Cell Level

2021 ◽  
Author(s):  
Yoshihiro Ujihara ◽  
Daichi Ono ◽  
Koki Nishitsuji ◽  
Megumi Ito ◽  
Shukei Sugita ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Metastatic Potential ◽  
B16 Melanoma ◽  
Cell Level ◽  
Whole Cell ◽  
Melanoma Cancer

scholarly journals CD36 promotes vasculogenic mimicry in melanoma by mediating adhesion to the extracellular matrix

BMC Cancer ◽  
2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Carmela Martini ◽  
Mark DeNichilo ◽  
Danielle P. King ◽  
Michaelia P. Cockshell ◽  
Brenton Ebert ◽  
...  
Keyword(s):  
Extracellular Matrix ◽  
Cancer Cells ◽  
Vasculogenic Mimicry ◽  
Tumor Vasculature ◽  
Melanoma Cells ◽  
Human Melanoma ◽  
Cell Surface Glycoprotein ◽  
Melanoma Cancer ◽  
In Vitro Angiogenesis

Abstract Background The formation of blood vessels within solid tumors directly contributes to cancer growth and metastasis. Until recently, tumor vasculature was thought to occur exclusively via endothelial cell (EC) lined structures (i.e. angiogenesis), but a second source of tumor vasculature arises from the cancer cells themselves, a process known as vasculogenic mimicry (VM). While it is generally understood that the function of VM vessels is the same as that of EC-lined vessels (i.e. to supply oxygen and nutrients to the proliferating cancer cells), the molecular mechanisms underpinning VM are yet to be fully elucidated. Methods Human VM-competent melanoma cell lines were examined for their VM potential using the in vitro angiogenesis assays (Matrigel), together with inhibition studies using small interfering RNA and blocking monoclonal antibodies. Invasion assays and adhesion assays were used to examine cancer cell function. Results Herein we demonstrate that CD36, a cell surface glycoprotein known to promote angiogenesis by ECs, also supports VM formation by human melanoma cancer cells. In silico analysis of CD36 expression within the melanoma cohort of The Cancer Genome Atlas suggests that melanoma patients with high expression of CD36 have a poorer clinical outcome. Using in vitro ‘angiogenesis’ assays and CD36-knockdown approaches, we reveal that CD36 supports VM formation by human melanoma cells as well as adhesion to, and invasion through, a cancer derived extracellular matrix substrate. Interestingly, thrombospondin-1 (TSP-1), a ligand for CD36 on ECs that inhibits angiogenesis, has no effect on VM formation. Further investigation revealed a role for laminin, but not collagen or fibronectin, as ligands for CD36 expressing melanoma cells. Conclusions Taken together, this study suggests that CD36 is a novel regulator of VM by melanoma cancer cells that is facilitated, at least in part, via integrin-α3 and laminin. Unlike angiogenesis, VM is not perturbed by the presence of TSP-1, thus providing new information on differences between these two processes of tumor vascularization which may be exploited to combat cancer progression.

scholarly journals Cytotoxicity of Labruscol, a New Resveratrol Dimer Produced by Grapevine Cell Suspensions, on Human Skin Melanoma Cancer Cell Line HT-144

Molecules ◽  
2017 ◽  
Vol 22 (11) ◽  
pp. 1940 ◽  
Author(s):  
Laetitia Nivelle ◽  
Jane Hubert ◽  
Eric Courot ◽  
Nicolas Borie ◽  
Jean-Hugues Renault ◽  
...  
Keyword(s):  
Cell Line ◽  
Human Skin ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Cell Suspensions ◽  
Skin Melanoma ◽  
Melanoma Cancer

scholarly journals Computational Modeling of PI3K/AKT and MAPK Signaling Pathways in Melanoma Cancer

PLoS ONE ◽  
2016 ◽  
Vol 11 (3) ◽  
pp. e0152104 ◽  
Author(s):  
Francesco Pappalardo ◽  
Giulia Russo ◽  
Saverio Candido ◽  
Marzio Pennisi ◽  
Salvatore Cavalieri ◽  
...  
Keyword(s):  
Computational Modeling ◽  
Signaling Pathways ◽  
Mapk Signaling ◽  
Melanoma Cancer ◽  
Mapk Signaling Pathways
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