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Article

Daidzein and Equol: Ex Vivo and In Silico Approaches Targeting COX-2, iNOS, and the Canonical Inflammasome Signaling Pathway

by
Yazmín K. Márquez-Flores
1,*,
Elizdath Martínez-Galero
1,
José Correa-Basurto
2,
Yudibeth Sixto-López
2,3,
Isabel Villegas
4,
María Á. Rosillo
4,
Ana Cárdeno
4 and
Catalina Alarcón-de-la-Lastra
4
1
Departamento de Farmacia, Escuela Nacional de Ciencias Biológicas, Campus Zacatenco, Instituto Politécnico Nacional, Av. Wilfrido Massieu s/n Col. Zacatenco, Mexico City C.P. 07738, Mexico
2
Laboratorio de Diseño y Desarrollo de Nuevos Fármacos y Productos Biotecnológicos, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón s/n, Col. Santo Tomas, Mexico City C.P. 11340, Mexico
3
Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Campus de Cartuja, Universidad de Granada, 18071 Granada, Spain
4
Department of Pharmacology, Faculty of Pharmacy, University of Seville, Professor García González Street 2, 41012 Seville, Spain
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2024, 17(5), 647; https://doi.org/10.3390/ph17050647
Submission received: 22 February 2024 / Revised: 22 March 2024 / Accepted: 8 May 2024 / Published: 16 May 2024
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Background: The inflammasome is a cytosolic multiprotein complex associated with multiple autoimmune diseases. Phytochemical compounds in soy (Glycine max) foods, such as isoflavones, have been reported for their anti-inflammatory properties. Aim: the anti-inflammatory activity of DZ (daidzein) and EQ (equol) were investigated in an ex vivo model of LPS-stimulated murine peritoneal macrophages and by molecular docking correlation. Methods: Cells were pre-treated with DZ (25, 50, and 100 µM) or EQ (5, 10, and 25 µM), followed by LPS stimulation. The levels of PGE2, NO, TNF-α, IL-6, and IL-1β were analyzed by ELISA, whereas the expressions of COX-2, iNOS, NLRP3, ASC, caspase 1, and IL-18 were measured by Western blotting. Also, the potential for transcriptional modulation by targeting NF-κB, COX-2, iNOS, NLRP3, ASC, and caspase 1 was investigated by molecular docking. Results: The anti-inflammatory responses observed may be due to the modulation of NF-κB due to the binding of DZ or EQ, which is translated into decreased TNF-α, COX-2, iNOS, NLRP3, and ASC levels. Conclusion: This study establishes that DZ and EQ inhibit LPS-induced inflammatory responses in peritoneal murine macrophages via down-regulation of NO and PGE2 generation, as well as the inhibition of the canonical inflammasome pathway, regulating NLRP3, and consequently decreasing IL-1β and IL-18 activation.
Keywords: soy; daidzein; equol; docking; inflammasome; inflammation soy; daidzein; equol; docking; inflammasome; inflammation
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MDPI and ACS Style

Márquez-Flores, Y.K.; Martínez-Galero, E.; Correa-Basurto, J.; Sixto-López, Y.; Villegas, I.; Rosillo, M.Á.; Cárdeno, A.; Alarcón-de-la-Lastra, C. Daidzein and Equol: Ex Vivo and In Silico Approaches Targeting COX-2, iNOS, and the Canonical Inflammasome Signaling Pathway. Pharmaceuticals 2024, 17, 647. https://doi.org/10.3390/ph17050647

AMA Style

Márquez-Flores YK, Martínez-Galero E, Correa-Basurto J, Sixto-López Y, Villegas I, Rosillo MÁ, Cárdeno A, Alarcón-de-la-Lastra C. Daidzein and Equol: Ex Vivo and In Silico Approaches Targeting COX-2, iNOS, and the Canonical Inflammasome Signaling Pathway. Pharmaceuticals. 2024; 17(5):647. https://doi.org/10.3390/ph17050647

Chicago/Turabian Style

Márquez-Flores, Yazmín K., Elizdath Martínez-Galero, José Correa-Basurto, Yudibeth Sixto-López, Isabel Villegas, María Á. Rosillo, Ana Cárdeno, and Catalina Alarcón-de-la-Lastra. 2024. "Daidzein and Equol: Ex Vivo and In Silico Approaches Targeting COX-2, iNOS, and the Canonical Inflammasome Signaling Pathway" Pharmaceuticals 17, no. 5: 647. https://doi.org/10.3390/ph17050647

APA Style

Márquez-Flores, Y. K., Martínez-Galero, E., Correa-Basurto, J., Sixto-López, Y., Villegas, I., Rosillo, M. Á., Cárdeno, A., & Alarcón-de-la-Lastra, C. (2024). Daidzein and Equol: Ex Vivo and In Silico Approaches Targeting COX-2, iNOS, and the Canonical Inflammasome Signaling Pathway. Pharmaceuticals, 17(5), 647. https://doi.org/10.3390/ph17050647

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