Publication: Design, synthesis and gene modulation insights into pigments derived from tryptophan-betaxanthin, which act against tumor development in Caenorhabditis elegans
Authors
Henarejos Escudero, Paula ; Méndez-García, Fernando F. ; Hernández García, Samanta ; Martínez Rodríguez, Pedro ; Gandía Herrero, Fernando
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Publisher
MDPI
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DOI
htpps://doi.org/10.3390/IJMS25010063
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info:eu-repo/semantics/article
Description
© 2023, MDPI. This manuscript version is made available under the CC-BY 4.0 license http://creativecommons.org/licenses/by/4.0/. This document is the Published version of a Published Work that appeared in final form in International Journal of Molecular Sciences. To access the final edited and published work see https://doi.org/10.3390/ijms25010063
Abstract
The use of betalains, which are nitrogenous plant pigments, by the food industry is widespread and reflects their safety after intake. The recent research showed outstanding results for L-tryptophan-betaxanthin, a phytochemical present in traditional Chinese medicine, as an antitumoral
agent when the activity was evaluated in the animal model Caenorhabditis elegans. Thus, L-tryptophanbetaxanthin is now presented as a lead compound, from which eleven novel structurally related betaxanthins have been designed, biotechnologically produced, purified, and characterized. The antitumoral effect of the derived compounds was evaluated on the JK1466 tumoral strain of C. elegans. All the tested molecules significantly reduced the tumoral gonad sizes in a range between 31.4%
and 43.0%. Among the novel compounds synthesized, tryptophan methyl ester-betaxanthin and tryptophan benzyl ester-betaxanthin, which are the first betalains to contain an ester group in their structures, caused tumor size reductions of 43.0% and 42.6%, respectively, after administration to
the model animal. Since these were the two most effective molecules, their mechanism of action was investigated by microarray analysis. Differential gene expression analysis showed that tryptophan methyl ester-betaxanthin and tryptophan benzyl ester-betaxanthin were able to down-regulate the
key genes of the mTOR pathway, such as daf-15 and rict-1.
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Citation
Int. J. Mol. Sci. 2024, 25, 63
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