Ce(SO4)2-catalysed the highly diastereoselective synthesis of tetrahydroquinolines via an imino Diels Alder ABB′ type reaction and their in vivo toxicity and imaging in zebrafish embryos

RSC Advances ◽  
2016 ◽  
Vol 6 (44) ◽  
pp. 37478-37486 ◽  
Author(s):  
Carlos A. Martínez Bonilla ◽  
Carlos E. Puerto Galvis ◽  
Leonor Y. Vargas Méndez ◽  
Vladimir V. Kouznetsov
Keyword(s):  
Zebrafish Embryo ◽  
Diels Alder ◽  
Zebrafish Embryos ◽  
Diastereoselective Synthesis ◽  
In Vivo Toxicity ◽  
Type Reaction ◽  
Povarov Reaction

The synthesis of tetrahydroquinolines via the Povarov reaction has been developed using Ce(SO2)4 as a catalyst. This efficient protocol allowed the toxicity and phenotypic study of these products using a zebrafish embryo model.

Heteroleptic mononuclear compounds of ruthenium(ii): synthesis, structural analyses, in vitro antitumor activity and in vivo toxicity on zebrafish embryos

2016 ◽  
Vol 45 (47) ◽  
pp. 19127-19140 ◽  
Author(s):  
O. A. Lenis-Rojas ◽  
A. R. Fernandes ◽  
C. Roma-Rodrigues ◽  
P. V. Baptista ◽  
F. Marques ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Dna Interaction ◽  
Zebrafish Embryos ◽  
In Vivo Toxicity ◽  
Mononuclear Compounds

Cytotoxic properties, DNA-interaction and in vivo toxicity were evaluated in Ru(ii) compounds.

scholarly journals An Orthotopic Model of Uveal Melanoma in Zebrafish Embryo: A Novel Platform for Drug Evaluation

Biomedicines ◽  
2021 ◽  
Vol 9 (12) ◽  
pp. 1873
Author(s):  
Chiara Tobia ◽  
Daniela Coltrini ◽  
Roberto Ronca ◽  
Alessandra Loda ◽  
Jessica Guerra ◽  
...  
Keyword(s):  
Uveal Melanoma ◽  
Zebrafish Embryo ◽  
Drug Evaluation ◽  
Metastatic Tumor ◽  
Melanoma Cells ◽  
Response To Therapy ◽  
Neoplastic Disease ◽  
Zebrafish Embryos ◽  
Orthotopic Model

Uveal melanoma is a highly metastatic tumor, representing the most common primary intraocular malignancy in adults. Tumor cell xenografts in zebrafish embryos may provide the opportunity to study in vivo different aspects of the neoplastic disease and its response to therapy. Here, we established an orthotopic model of uveal melanoma in zebrafish by injecting highly metastatic murine B16-BL6 and B16-LS9 melanoma cells, human A375M melanoma cells, and human 92.1 uveal melanoma cells into the eye of zebrafish embryos in the proximity of the developing choroidal vasculature. Immunohistochemical and immunofluorescence analyses showed that melanoma cells proliferate during the first four days after injection and move towards the eye surface. Moreover, bioluminescence analysis of luciferase-expressing human 92.1 uveal melanoma cells allowed the quantitative assessment of the antitumor activity exerted by the canonical chemotherapeutic drugs paclitaxel, panobinostat, and everolimus after their injection into the grafted eye. Altogether, our data demonstrate that the zebrafish embryo eye is a permissive environment for the growth of invasive cutaneous and uveal melanoma cells. In addition, we have established a new luciferase-based in vivo orthotopic model that allows the quantification of human uveal melanoma cells engrafted in the zebrafish embryo eye, and which may represent a suitable tool for the screening of novel drug candidates for uveal melanoma therapy.

scholarly journals Organoruthenium(II) Complexes Bearing an Aromatase Inhibitor: Synthesis, Characterization, in Vitro Biological Activity and in Vivo Toxicity in Zebrafish Embryos

2019 ◽  
Vol 38 (3) ◽  
pp. 702-711 ◽  
Author(s):  
Golara Golbaghi ◽  
Mohammad Mehdi Haghdoost ◽  
Debbie Yancu ◽  
Yossef López de los Santos ◽  
Nicolas Doucet ◽  
...  
Keyword(s):  
Biological Activity ◽  
Aromatase Inhibitor ◽  
Zebrafish Embryos ◽  
In Vivo Toxicity

scholarly journals The zebrafish embryo as an in vivo model for screening nanoparticle-formulated lipophilic anti-tuberculosis compounds

2021 ◽  
Author(s):  
Nils-Jørgen Knudsen Dal ◽  
Martin Speth ◽  
Kerstin Johann ◽  
Matthias Barz ◽  
Claire Beauvineau ◽  
...  
Keyword(s):  
Zebrafish Embryo ◽  
Polymeric Micelles ◽  
Water Soluble ◽  
In Vivo Model ◽  
In Vivo Toxicity ◽  
Conventional Animal ◽  
In Vivo Testing ◽  
Poorly Water Soluble

With the increasing emergence of drug-resistant Mycobacterium tuberculosis strains, new and effective antibiotics against tuberculosis (TB) are urgently needed. However, the high frequency of poorly water-soluble compounds among hits in high-throughput drug screening (HTS) campaigns is a major obstacle in drug discovery. Moreover, in vivo testing using conventional animal TB models such as mice is time-consuming and costly, and represents a major bottleneck in lead compound discovery and development. Here, we report the use of the zebrafish embryo TB model, to evaluate the in vivo toxicity and efficacy of five poorly water-soluble nitronaphthofuran derivatives, which were recently identified to possess anti-tuberculosis activity in vitro. To aid solubilization compounds were formulated in biocompatible polymeric micelles (PM). Three of the five PM-formulated nitronaphthofuran derivatives showed low toxicity in vivo, significantly reduced bacterial burden and improved survival in infected zebrafish embryos. We propose the zebrafish embryo TB-model as a quick and sensitive tool for evaluating in vivo toxicity and efficacy of new anti-TB compounds during early stages of drug development. Thus, this model is well suited to pinpoint promising compounds for further development.

scholarly journals Quantifying endothelial cell proliferation in the zebrafish embryo

F1000Research ◽  
2021 ◽  
Vol 10 ◽  
pp. 1032
Author(s):  
George Bowley ◽  
Timothy JA Chico ◽  
Jovana Serbanovic-Canic ◽  
Paul C Evans
Keyword(s):  
Cell Proliferation ◽  
Endothelial Cell ◽  
Zebrafish Embryo ◽  
Time Lapse ◽  
Endothelial Cell Proliferation ◽  
Small Scale ◽  
Zebrafish Embryos ◽  
Time Lapse Imaging

Introduction: Endothelial cell (EC) proliferation is a fundamental determinant of vascular development and homeostasis, and contributes to cardiovascular disease by increasing vascular permeability to blood-borne lipoproteins. Rodents have been traditionally used to analyse EC proliferation mechanisms in vascular health and disease; however, alternative models such as the zebrafish embryo allow researchers to conduct small scale screening studies in a physiologically relevant vasculature whilst reducing the use of mammals in biomedical research. In vitro models of EC proliferation are valuable but do not fully recapitulate the complexity of the in vivo situation. Several groups have used zebrafish embryos for vascular biology research because they offer the advantages of an in vivo model in terms of complexity but are also genetically manipulable and optically transparent. Methods: Here we investigated whether zebrafish embryos can provide a suitable model for the study of EC proliferation. We explored the use of antibody, DNA labelling, and time-lapse imaging approaches. Results: Antibody and DNA labelling approaches were of limited use in zebrafish due to the low rate of EC proliferation combined with the relatively narrow window of time in which they can label proliferating nuclei. By contrast, time-lapse imaging of fluorescent proteins localised to endothelial nuclei was a sensitive method to quantify EC proliferation in zebrafish embryos. Discussion: We conclude that time-lapse imaging is suitable for analysis of endothelial cell proliferation in zebrafish, and that this method is capable of capturing more instances of EC proliferation than immunostaining or cell labelling alternatives. This approach is relevant to anyone studying endothelial cell proliferation for screening genes or small molecules involved in EC proliferation. It offers greater biological relevance than existing in vitro models such as HUVECs culture, whilst reducing the overall number of animals used for this type of research.

Discovery of Quinoline-Derived Trifluoromethyl Alcohols, Determination of Their in vivo Toxicity and Anticancer Activity in a Zebrafish Embryo Model

ChemMedChem ◽  
2015 ◽  
Vol 10 (11) ◽  
pp. 1802-1807 ◽  
Author(s):  
Vinoth Sittaramane ◽  
Jihan Padgett ◽  
Philip Salter ◽  
Ashley Williams ◽  
Shauntelle Luke ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Zebrafish Embryo ◽  
In Vivo Toxicity
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