Por favor, use este identificador para citar o enlazar este ítem: http://hdl.handle.net/10637/14176

Flavonoids from "Piper" species as promising antiprotozoal agents against "Giardia intestinalis" structure-activity relationship and drug-likeness studies

Título : Flavonoids from "Piper" species as promising antiprotozoal agents against "Giardia intestinalis" structure-activity relationship and drug-likeness studies
Autor : Ticona H., Juan Carlos
Bilbao Ramos, Pablo
Amesty Arrieta, Ángel Ernesto
Flores, Ninoska
Dea Ayuela, María Auxiliadora
Bazzocchi, Isabel L.
Jiménez Díaz, Ignacio Antonio
Materias: Flavonoides - Uso terapéutico.Lambliasis - Tratamiento.Diarrea - Tratamiento.Flavonoids - Therapeutic use.Diarrhea - Treatment.Giardiasis - Treatment.
Editorial : MDPI
Citación : Ticona, J. C., Bilbao-Ramos, P., Amesty, Á., Flores, N., Dea-Ayuela, M. A., Bazzocchi, I. L. & Jiménez, I. A. (2022). Flavonoids from "Piper" species as promising antiprotozoal agents against "Giardia intestinalis": structure-activity relationship and drug-likeness studies. Pharmaceuticals, vol. 15, i. 11 (10 nov.), art. 1386. DOI: https://doi.org/10.3390/ph15111386
Resumen : Diarrhea diseases caused by the intestinal protozoan parasite Giardia intestinalis are a major global health burden. Moreover, there is an ongoing need for novel anti-Giardia drugs due to drawbacks with currently available treatments. This paper reports on the isolation and structural elucidation of six new flavonoids (1–6), along with twenty-three known ones (7–29) from the Piper species. Their structures were established by spectroscopic and spectrometric techniques. Flavonoids were tested for in vitro antiprotozoal activity against Giardia intestinalis trophozoites. In addition, structure-activity relationship (SAR) and in silico ADME studies were performed to understand the pharmacophore and pharmacokinetic properties of these natural compounds. Eight flavonoids from this series exhibited remarkable activity in the micromolar range. Moreover, compound 4 was identified as having a 40-fold greater antiparasitic effect (IC50 61.0 nM) than the clinical reference drug, metronidazole (IC50 2.5 M). This antiprotozoal potency was coupled with an excellent selectivity index (SI 233) on murine macrophages and in silico drug-likeness. SAR studies revealed that the substitution patterns, type of functional group, and flavonoid skeleton played an essential role in the activity. These findings highlight flavonoid 4 as a promising candidate to develop new drugs for the treatment of Giardia infections.
Descripción : Este artículo se encuentra disponible en la siguiente URL: https://www.mdpi.com/1424-8247/15/11/1386
Este artículo pertenece a la sección "Natural Products".
URI : http://hdl.handle.net/10637/14176
Derechos: http://creativecommons.org/licenses/by/4.0/deed.es
ISSN : 1424-8247 (Electrónico)
Idioma: es
Fecha de publicación : 10-nov-2022
Centro : Universidad Cardenal Herrera-CEU
Aparece en las colecciones: Dpto. Farmacia





Los ítems de DSpace están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.