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

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.

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 Effect of Cinnamomum verum leaf essential oil on virulence factors of Candida species and determination of the in-vivo toxicity with Galleria mellonella model

2020 ◽  
Vol 115 ◽  
Author(s):  
Gayan Kanchana Wijesinghe ◽  
Flávia Camila Maia ◽  
Thaís Rossini de Oliveira ◽  
Simone N Busato de Feiria ◽  
Felipe Joia ◽  
...  
Keyword(s):  
Essential Oil ◽  
Virulence Factors ◽  
Candida Species ◽  
Galleria Mellonella ◽  
In Vivo Toxicity ◽  
Leaf Essential Oil

Investigations on the in-vivo toxicity analysis of reduced graphene oxide/TiO2 nanocomposite in zebrafish embryo and larvae (Danio rerio)

2019 ◽  
Vol 481 ◽  
pp. 1360-1369 ◽  
Author(s):  
J. Prakash ◽  
Manigandan Venkatesan ◽  
Joy Sebastian Prakash J ◽  
G. Bharath ◽  
Shoaib Anwer ◽  
...  
Keyword(s):  
Graphene Oxide ◽  
Reduced Graphene Oxide ◽  
Danio Rerio ◽  
Zebrafish Embryo ◽  
In Vivo Toxicity ◽  
Reduced Graphene ◽  
Toxicity Analysis

In vivo toxicity assessment of angiogenesis and the live distribution of nano-graphene oxide and its PEGylated derivatives using the developing zebrafish embryo

Carbon ◽  
2015 ◽  
Vol 93 ◽  
pp. 431-440 ◽  
Author(s):  
Jinyoung Jeong ◽  
Hyun-Ju Cho ◽  
Mijin Choi ◽  
Wang Sik Lee ◽  
Bong Hyun Chung ◽  
...  
Keyword(s):  
Graphene Oxide ◽  
Zebrafish Embryo ◽  
Toxicity Assessment ◽  
In Vivo Toxicity ◽  
Nano Graphene

scholarly journals Determination of the anticancer properties of cis- and trans-diadamanthylcarboxylates of dirhenium(III)

2020 ◽  
pp. 8-12
Author(s):  
Natalia Shtemenko ◽  
Katerina Polokhina ◽  
Alexander Golichenko ◽  
Svetlana Babiy ◽  
Alexander Shtemenko
Keyword(s):  
Anticancer Activity ◽  
Intraperitoneal Administration ◽  
Anticancer Properties ◽  
Adamantanecarboxylic Acid ◽  
Carboxylic Groups ◽  
Guerin’S Carcinoma ◽  
Cross Links ◽  
Cis And Trans

The aim of the study. The aim of the work was to investigate in vivo anticancer activity of cis- and trans-diadamanthylcarboxylates of dirhenium(III) alone and together with cisplatin in form of nanobins.Materials and methods. Model of tumor growth, Guerin’s carcinoma; intraperitoneal administration of cisplatin, dirhenium(III) compounds in liposomes and of binary liposomes, containing both cytostatics; volumes and final weights of tumors were measured.Results. In vivo antitumor properties of two dirhenium(III) dicarboxylates with 1-adamantanecarboxylic acid moieties as ligands with cis- (I) and trans- (II) orientation of the carboxylic groups around a cluster fragment alone and together with cisplatin were presented; an attempt to understand differences in a possible mechanism of anticancer activity of the substances were undertaken. Antiradical and DNA-binding properties of I and II were the matter of consideration.Conclusions. Cis- and trans- compounds of dirhenium I and II had close antitumor activity in vivo with a little bit superiority of the cis- analog. Mechanisms of anticancer activity of I and II are different and may also include monofunctional adduct formation and subsequent interstrand cross-linking for the II substance, formation of protein-DNA cross-links, etc.

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