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Toxicological Screening of Four Bioactive Citroflavonoids: In Vitro, In Vivo, and In Silico Approaches
ROLFFY RUBEN ORTIZ ANDRADE
JESUS ALFREDO ARAUJO LEON
AMANDA SANCHEZ RECILLAS
JUAN GABRIEL NAVARRETE VAZQUEZ
AVEL ADOLFO GONZALEZ SANCHEZ
SERGIO NEMORIO HIDALGO FIGUEROA
ANGEL JOSABAD ALONSO CASTRO
Irma Aranda Gonzalez
EMANUEL HERNANDEZ NUÑEZ
TANIA ISOLINA CORAL MARTINEZ
JUAN CARLOS SANCHEZ SALGADO
VICTOR YAÑEZ PEREZ
MONICA ARELY LUCIO GARCIA
Acceso Abierto
Atribución-NoComercial-SinDerivadas
https://doi.org/10.3390/molecules25245959
Citroflavonoids
Low-risk substances
Acute oral toxicity
MTT-based assay
Toxicity prediction
"Many studies describe different pharmacological effects of flavonoids on experimental animals and humans. Nevertheless, few ones are confirming the safety of these compounds for therapeutic purposes. This study aimed to investigate the preclinical safety of naringenin, naringin, hesperidin, and quercetin by in vivo, in vitro, and in silico approaches. For this, an MTT-based cytotoxicity assay in VERO and MDCK cell lines was performed. In addition, acute toxicity was evaluated on Wistar rats by OECD Guidelines for the Testing of Chemicals (Test No. 423: Acute Oral Toxicity-Class Method). Furthermore, we used the ACD/Tox Suite to predict toxicological parameters such as hERG channel blockade, CYP450 inhibition, and acute toxicity in animals. The results showed that quercetin was slightly more cytotoxic on cell lines (IC50 of 219.44 ± 7.22 mM and 465.41 ± 7.44 mM, respectively) than the other citroflavonoids. All flavonoids exhibited an LD50 value > 2000 mg/kg, which classifies them as low-risk substances as OECD guidelines established. Similarly, predicted LD50 was LD50 > 300 to 2000 mg/kg for all flavonoids as acute toxicity assay estimated. Data suggests that all these flavonoids did not show significant toxicological effects, and they were classified as low-risk, useful substances for drug development."
MDPI
2020
Artículo
Ortiz-Andrade, R.; Araujo-León, J.A.; Sánchez-Recillas, A.; Navarrete-Vazquez, G.; González-Sánchez, A.A.; Hidalgo-Figueroa, S.; Alonso-Castro, Á.J.; Aranda-González, I.; Hernández-Núñez, E.; Coral-Martínez, T.I.; Sánchez-Salgado, J.C.; Yáñez-Pérez, V.; Lucio-Garcia, M.A. Toxicological Screening of Four Bioactive Citroflavonoids: In Vitro, In Vivo, and In Silico Approaches. Molecules 2020, 25, 5959. https://doi.org/10.3390/molecules25245959
BIOQUÍMICA
Versión publicada
publishedVersion - Versión publicada
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