A Zebrafish<i>In Vivo</i>Phenotypic Assay to Identify 3-Aminothiophene-2-Carboxylic Acid-Based Angiogenesis Inhibitors

Papakyriakou, Athanasios; Kefalos, Panagiotis; Sarantis, Panagiotis; Tsiamantas, Christos; Xanthopoulos, Kleanthis P.; Vourloumis, Dionisios; Beis, Dimitris

doi:10.1089/adt.2014.606

Cited by 18 publications

(13 citation statements)

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“…In vivo phenotypic screens using zebrafish embryos have been particularly valuable in identifying novel bioactive natural compounds or optimizing the activity of lead compounds [ 19 ]. Chemical library screens using zebrafish embryos for the identification of melanogenesis inhibitors [ 20 ] and or transgenic-based screens for angiogenesis [ 21 ] or neoglucogenesis [ 18 ] have been very productive.…”

Section: Introductionmentioning

confidence: 99%

Crocins from Crocus sativus L. in the Management of Hyperglycemia. In Vivo Evidence from Zebrafish

et al. 2020

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Diabetes mellitus is a disease characterized by persistent high blood glucose levels and accompanied by impaired metabolic pathways. In this study, we used zebrafish to investigate the effect of crocins isolated from Crocus sativus L., on the control of glucose levels and pancreatic β-cells. Embryos were exposed to an aqueous solution of crocins and whole embryo glucose levels were measured at 48 h post-treatment. We showed that the application of crocins reduces zebrafish embryo glucose levels and enhances insulin expression. We also examined whether crocins are implicated in the metabolic pathway of gluconeogenesis. We showed that following a single application of crocins and glucose level reduction, the expression of phosphoenolpyruvate carboxykinase1 (pck1), a key gene involved in glucose metabolism, is increased. We propose a putative role for the crocins in glucose metabolism and insulin management.

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Section: Introductionmentioning

confidence: 99%

Crocins from Crocus sativus L. in the Management of Hyperglycemia. In Vivo Evidence from Zebrafish

et al. 2020

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“…This core is, indeed, a well-known bioisostere of anilines used in drug design and can be found in agrochemicals such as in dimethenamid [2] and penthiopyrad, [3] showing herbicidal and fungicidal activity respectively, and also in pharmaceuticals like the local anesthetic articaine [4] or telenzepine [5,6] which is used for the treatment of peptic ulcer (Figure 1). Moreover, according to recent studies, this scaffold is present in potent inhibitors of hepatitis C virus [7,8] and tumor growth, [9,10] as well as in anti-inflammatory [11] and anti-microbial [12] compounds.…”

Section: Introductionmentioning

confidence: 99%

Straightforward Synthesis of 3‐Aminothiophenes Using Activated Amides

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Kolleth

Lumbroso

et al. 2019

Helvetica Chimica Acta

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Herein, we describe a facile approach towards the synthesis of diversely substituted 3‐aminothiophenes. A wide range of functional groups can be incorporated at the C(2), C(4), and C(5) positions of the thiophenes, and this route is also suitable for the synthesis of fused bicyclic heterocycles such as 3‐aminotetrahydrobenzothiophenes. This methodology relies on a 6π‐electrocyclization involving a vinyl sulfide linked to a keteniminium salt, the latter being formed in‐situ through activation of the corresponding amide with triflic anhydride.

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“…Zebrafish is a popular vertebrate model that has been extensively used on phenotypic screens for bioactive compounds ( Papakyriakou et al, 2014 ; MacRae and Peterson, 2015 ). By employing a fast and robust zebrafish screen, we identified that the dibenzofuran compounds isolated from C. pycnoloba exhibit strong inhibition of melanogenesis.…”

Section: Discussionmentioning

confidence: 99%

Identification of Novel Melanin Synthesis Inhibitors From Crataegus pycnoloba Using an in Vivo Zebrafish Phenotypic Assay

et al. 2018

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Zebrafish has emerged as a powerful model organism for high throughput drug screening. Several morphological criteria, transgenic lines and in situ expression screens have been developed to identify novel bioactive compounds and their mechanism of action. Here, we used the inhibition of melanogenesis during early zebrafish embryo development to identify natural compounds that block melanogenesis. We identified an extract from the Greek hawthorn Crataegus pycnoloba as a potent inhibitor of melanin synthesis and used activity based subfractionation to identify active subfractions and eventually three single compounds of the same family (dibenzofurans). These compounds show reversible inhibition of melanin synthesis and do not act via inhibition of tyrosinase. We also showed that they do not interfere with neural crest differentiation or migration. We identified via in silico modeling that the compounds can bind to the aryl hydrocarbon receptor (AHR) and verified activation of the Ahr signaling pathway showing the induction of the expression of target genes.

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A ZebrafishIn VivoPhenotypic Assay to Identify 3-Aminothiophene-2-Carboxylic Acid-Based Angiogenesis Inhibitors

Cited by 18 publications

References 30 publications

Crocins from Crocus sativus L. in the Management of Hyperglycemia. In Vivo Evidence from Zebrafish

Crocins from Crocus sativus L. in the Management of Hyperglycemia. In Vivo Evidence from Zebrafish

Straightforward Synthesis of 3‐Aminothiophenes Using Activated Amides

Identification of Novel Melanin Synthesis Inhibitors From Crataegus pycnoloba Using an in Vivo Zebrafish Phenotypic Assay

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