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Volume 14
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Article

Biological Activity of NHC-Gold-Alkynyl Complexes Derived from 3-Hydroxyflavones

by
Inés Mármol
1,2,
Javier Quero
2,
Paula Azcárate
1,
Elena Atrián-Blasco
3,
Carla Ramos
4,
Joana Santos
4,
María Concepción Gimeno
1,
María Jesús Rodríguez-Yoldi
2,* and
Elena Cerrada
1,*
1
Departamento de Química Inorgánica, Instituto de Síntesis Química y Catálisis Homogénea-ISQCH, Universidad de Zaragoza-C.S.I.C., Pedro Cerbuna 12, 50009 Zaragoza, Spain
2
Departamento de Farmacología y Fisiología, Medicina Legal y Forense, Unidad de Fisiología, Universidad de Zaragoza, CIBERobn, IIS Aragón, IA2, 50013 Zaragoza, Spain
3
Instituto de Nanociencia y Materiales de Aragón (INMA), CSIC-Universidad de Zaragoza, 50009 Zaragoza, Spain
4
Escola Superior de Tecnologia e Gestão, Instituto Politécnico de Viana do Castelo, Avenida do Atlântico No. 644, 4900-348 Viana do Castelo, Portugal
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2022, 14(10), 2064; https://doi.org/10.3390/pharmaceutics14102064
Submission received: 1 September 2022 / Revised: 19 September 2022 / Accepted: 23 September 2022 / Published: 27 September 2022
(This article belongs to the Section Biologics and Biosimilars)
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Abstract

In this paper we describe the synthesis of new N-heterocyclic carbene (NHC) gold(I) derivatives with flavone-derived ligands with a propargyl ether group. The compounds were screened for their antimicrobial and anticancer activities, showing greater activity against bacteria than against colon cancer cells (Caco-2). Complexes [Au(L2b)(IMe)] (1b) and [Au(L2b)(IPr)] (2b) were found to be active against both Gram-positive and Gram-negative strains. The mechanism of action of 1b was evaluated by measurement of thioredoxin reductase (TrxR) and dihydrofolate reductase (DHFR) activity, besides scanning electron microscopy (SEM). Inhibition of the enzyme thioredoxin reductase is not observed in either Escherichia Coli or Caco-2 cells; however, DHFR activity is compromised after incubation of E. coli cells with complex 1b. Moreover, loss of structural integrity and change in bacterial shape is observed in the images obtained from scanning electron microscopy (SEM) after treatment E. coli cells with complex 1b.
Keywords: Alkynyl; N-heterocyclic carbene; gold complexes; hydroxyflavones; antibacterial; anticancer; dihydrofolate reductase; thioredoxin reductase Alkynyl; N-heterocyclic carbene; gold complexes; hydroxyflavones; antibacterial; anticancer; dihydrofolate reductase; thioredoxin reductase
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MDPI and ACS Style

Mármol, I.; Quero, J.; Azcárate, P.; Atrián-Blasco, E.; Ramos, C.; Santos, J.; Gimeno, M.C.; Rodríguez-Yoldi, M.J.; Cerrada, E. Biological Activity of NHC-Gold-Alkynyl Complexes Derived from 3-Hydroxyflavones. Pharmaceutics 2022, 14, 2064. https://doi.org/10.3390/pharmaceutics14102064

AMA Style

Mármol I, Quero J, Azcárate P, Atrián-Blasco E, Ramos C, Santos J, Gimeno MC, Rodríguez-Yoldi MJ, Cerrada E. Biological Activity of NHC-Gold-Alkynyl Complexes Derived from 3-Hydroxyflavones. Pharmaceutics. 2022; 14(10):2064. https://doi.org/10.3390/pharmaceutics14102064

Chicago/Turabian Style

Mármol, Inés, Javier Quero, Paula Azcárate, Elena Atrián-Blasco, Carla Ramos, Joana Santos, María Concepción Gimeno, María Jesús Rodríguez-Yoldi, and Elena Cerrada. 2022. "Biological Activity of NHC-Gold-Alkynyl Complexes Derived from 3-Hydroxyflavones" Pharmaceutics 14, no. 10: 2064. https://doi.org/10.3390/pharmaceutics14102064

APA Style

Mármol, I., Quero, J., Azcárate, P., Atrián-Blasco, E., Ramos, C., Santos, J., Gimeno, M. C., Rodríguez-Yoldi, M. J., & Cerrada, E. (2022). Biological Activity of NHC-Gold-Alkynyl Complexes Derived from 3-Hydroxyflavones. Pharmaceutics, 14(10), 2064. https://doi.org/10.3390/pharmaceutics14102064

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