Biological Activity of NHC-Gold-Alkynyl Complexes Derived from 3-Hydroxyflavones
| Autor: | Inés Mármol, Javier Quero, Paula Azcárate, Elena Atrián-Blasco, Carla Ramos, Joana Santos, María Concepción Gimeno, María Jesús Rodríguez-Yoldi, Elena Cerrada |
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| Jazyk: | angličtina |
| Rok vydání: | 2022 |
| Předmět: | |
| Zdroj: | Pharmaceutics, Vol 14, Iss 10, p 2064 (2022) |
| Druh dokumentu: | article |
| ISSN: | 14102064 1999-4923 |
| DOI: | 10.3390/pharmaceutics14102064 |
| Popis: | 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. |
| Databáze: | Directory of Open Access Journals |
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