Antilymphoma Effect of Incomptine A: In Vivo, In Silico, and Toxicological Studies

Incomptine A (<b>IA</b>) is a sesquiterpene lactone isolated from <i>Decachaeta incompta</i> that induces apoptosis, reactive oxygen species production, and a differential protein expression on the U-937 (diffuse histiocytic lymphoma) cell line. In this work, the antitumor po...

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Autores principales:	Fernando Calzada, Elihú Bautista, Sergio Hidalgo-Figueroa, Normand García-Hernández, Elizabeth Barbosa, Claudia Velázquez, Rosa María Ordoñez-Razo, Angel Giovanni Arietta-García
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	incomptine A antilymphoma activity molecular docking acute toxicity brine shrimp lethality cancer Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/acafc31b43ab4a8ea3c0a4e160d42256
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spelling	oai:doaj.org-article:acafc31b43ab4a8ea3c0a4e160d422562021-11-11T18:36:55ZAntilymphoma Effect of Incomptine A: In Vivo, In Silico, and Toxicological Studies10.3390/molecules262166461420-3049https://doaj.org/article/acafc31b43ab4a8ea3c0a4e160d422562021-11-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6646https://doaj.org/toc/1420-3049Incomptine A (<b>IA</b>) is a sesquiterpene lactone isolated from <i>Decachaeta incompta</i> that induces apoptosis, reactive oxygen species production, and a differential protein expression on the U-937 (diffuse histiocytic lymphoma) cell line. In this work, the antitumor potential of <b>IA</b> was investigated on Balb/c mice inoculated with U-937 cells and through the brine shrimp lethality (BSL) test. Furthermore, <b>IA</b> was subjected to molecular docking study using as targets proteins associated with processes of cancer as apoptosis, oxidative stress, and glycolytic metabolism. In addition to determining the potential toxicity of <b>IA</b> in human, its acute toxicity was performed in mice. Results reveals that <b>IA</b> showed high antilymphoma activity and BSL with an EC<sub>50</sub> of 2.4 mg/kg and LC<sub>50</sub> 16.7 µg/mL, respectively. The molecular docking study revealed that <b>IA</b> has strong interaction on all targets used. In the acute oral toxicity, <b>IA</b> had a LD<sub>50</sub> of 149 mg/kg. The results showed that the activities of <b>IA</b> including antilymphoma activity, BSL, acute toxicity, and in silico interactions were close to the methotrexate, an anticancer drug used as positive control. These findings suggest that <b>IA</b> may serve as a candidate for the development of a new drug to combat lymphoma.Fernando CalzadaElihú BautistaSergio Hidalgo-FigueroaNormand García-HernándezElizabeth BarbosaClaudia VelázquezRosa María Ordoñez-RazoAngel Giovanni Arietta-GarcíaMDPI AGarticleincomptine Aantilymphoma activitymolecular dockingacute toxicitybrine shrimp lethalitycancerOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6646, p 6646 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	incomptine A antilymphoma activity molecular docking acute toxicity brine shrimp lethality cancer Organic chemistry QD241-441
spellingShingle	incomptine A antilymphoma activity molecular docking acute toxicity brine shrimp lethality cancer Organic chemistry QD241-441 Fernando Calzada Elihú Bautista Sergio Hidalgo-Figueroa Normand García-Hernández Elizabeth Barbosa Claudia Velázquez Rosa María Ordoñez-Razo Angel Giovanni Arietta-García Antilymphoma Effect of Incomptine A: In Vivo, In Silico, and Toxicological Studies
description	Incomptine A (<b>IA</b>) is a sesquiterpene lactone isolated from <i>Decachaeta incompta</i> that induces apoptosis, reactive oxygen species production, and a differential protein expression on the U-937 (diffuse histiocytic lymphoma) cell line. In this work, the antitumor potential of <b>IA</b> was investigated on Balb/c mice inoculated with U-937 cells and through the brine shrimp lethality (BSL) test. Furthermore, <b>IA</b> was subjected to molecular docking study using as targets proteins associated with processes of cancer as apoptosis, oxidative stress, and glycolytic metabolism. In addition to determining the potential toxicity of <b>IA</b> in human, its acute toxicity was performed in mice. Results reveals that <b>IA</b> showed high antilymphoma activity and BSL with an EC<sub>50</sub> of 2.4 mg/kg and LC<sub>50</sub> 16.7 µg/mL, respectively. The molecular docking study revealed that <b>IA</b> has strong interaction on all targets used. In the acute oral toxicity, <b>IA</b> had a LD<sub>50</sub> of 149 mg/kg. The results showed that the activities of <b>IA</b> including antilymphoma activity, BSL, acute toxicity, and in silico interactions were close to the methotrexate, an anticancer drug used as positive control. These findings suggest that <b>IA</b> may serve as a candidate for the development of a new drug to combat lymphoma.
format	article
author	Fernando Calzada Elihú Bautista Sergio Hidalgo-Figueroa Normand García-Hernández Elizabeth Barbosa Claudia Velázquez Rosa María Ordoñez-Razo Angel Giovanni Arietta-García
author_facet	Fernando Calzada Elihú Bautista Sergio Hidalgo-Figueroa Normand García-Hernández Elizabeth Barbosa Claudia Velázquez Rosa María Ordoñez-Razo Angel Giovanni Arietta-García
author_sort	Fernando Calzada
title	Antilymphoma Effect of Incomptine A: In Vivo, In Silico, and Toxicological Studies
title_short	Antilymphoma Effect of Incomptine A: In Vivo, In Silico, and Toxicological Studies
title_full	Antilymphoma Effect of Incomptine A: In Vivo, In Silico, and Toxicological Studies
title_fullStr	Antilymphoma Effect of Incomptine A: In Vivo, In Silico, and Toxicological Studies
title_full_unstemmed	Antilymphoma Effect of Incomptine A: In Vivo, In Silico, and Toxicological Studies
title_sort	antilymphoma effect of incomptine a: in vivo, in silico, and toxicological studies
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/acafc31b43ab4a8ea3c0a4e160d42256
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Antilymphoma Effect of Incomptine A: In Vivo, In Silico, and Toxicological Studies

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