When Chirality Makes the Difference: The Case of Novel Enantiopure <i>N</i>-Heterocyclic Carbene–Gold and –Silver Complexes

<i>N</i>-heterocyclic carbene (NHC)–gold and –silver complexes have attracted the interest of the scientific community because of their multiple applications and their versatility in being chemically modified in order to improve their biological properties. However, most of these complex...

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Main Authors: Maria Marra, Annaluisa Mariconda, Domenico Iacopetta, Jessica Ceramella, Assunta D’Amato, Camillo Rosano, Kateryna Tkachenko, Michele Pellegrino, Stefano Aquaro, Maria Stefania Sinicropi, Pasquale Longo
Format: Article
Language:English
Published: MDPI AG 2024-11-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/29/22/5262
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author Maria Marra
Annaluisa Mariconda
Domenico Iacopetta
Jessica Ceramella
Assunta D’Amato
Camillo Rosano
Kateryna Tkachenko
Michele Pellegrino
Stefano Aquaro
Maria Stefania Sinicropi
Pasquale Longo
author_facet Maria Marra
Annaluisa Mariconda
Domenico Iacopetta
Jessica Ceramella
Assunta D’Amato
Camillo Rosano
Kateryna Tkachenko
Michele Pellegrino
Stefano Aquaro
Maria Stefania Sinicropi
Pasquale Longo
author_sort Maria Marra
collection DOAJ
description <i>N</i>-heterocyclic carbene (NHC)–gold and –silver complexes have attracted the interest of the scientific community because of their multiple applications and their versatility in being chemically modified in order to improve their biological properties. However, most of these complexes contain one or more chiral centers, and have been obtained and studied as racemic mixture. In particular, concerning the interesting biological and medicinal properties, many questions about how the chirality may influence these properties still remain unanswered. Aiming at a better understanding, herein a series of enantiopure NHC–gold and –silver complexes was synthesized, characterized and biologically evaluated in different in vitro systems. The individuated complexes exerted different properties based on the complexed metal and the specific configuration, with the (<i>R</i>)-gold–NHC complexes being the most active, particularly as anti-inflammatory molecules. Docking simulations indicated a different binding mode for each enantiomer. Moreover, anticancer and antibacterial activities were also evaluated for the considered enantiomers. Overall, the reported data may contribute to a better understanding of the different biological properties exerted by the enantiopure gold and silver complexes.
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institution Kabale University
issn 1420-3049
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publishDate 2024-11-01
publisher MDPI AG
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series Molecules
spelling doaj-art-67b99db78f124b0a9098662b5214a0962024-11-26T18:15:20ZengMDPI AGMolecules1420-30492024-11-012922526210.3390/molecules29225262When Chirality Makes the Difference: The Case of Novel Enantiopure <i>N</i>-Heterocyclic Carbene–Gold and –Silver ComplexesMaria Marra0Annaluisa Mariconda1Domenico Iacopetta2Jessica Ceramella3Assunta D’Amato4Camillo Rosano5Kateryna Tkachenko6Michele Pellegrino7Stefano Aquaro8Maria Stefania Sinicropi9Pasquale Longo10Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, ItalyDepartment of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, ItalyDepartment of Chemistry and Biology, University of Salerno, Via Giovanni Paolo II, 132, 84084 Fisciano, ItalyU.O. Proteomica e Spettrometria di Massa, IRCCS Ospedale Policlinico San Martino, L.go Rosanna Benzi 10, 16132 Genova, ItalyU.O. Proteomica e Spettrometria di Massa, IRCCS Ospedale Policlinico San Martino, L.go Rosanna Benzi 10, 16132 Genova, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, ItalyDepartment of Life, Health and Environmental Sciences, University of L’Aquila, Piazzale Salvatore Tommasi 1, Blocco 11, Coppito, 67010 L’Aquila, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Arcavacata di Rende, ItalyDepartment of Chemistry and Biology, University of Salerno, Via Giovanni Paolo II, 132, 84084 Fisciano, Italy<i>N</i>-heterocyclic carbene (NHC)–gold and –silver complexes have attracted the interest of the scientific community because of their multiple applications and their versatility in being chemically modified in order to improve their biological properties. However, most of these complexes contain one or more chiral centers, and have been obtained and studied as racemic mixture. In particular, concerning the interesting biological and medicinal properties, many questions about how the chirality may influence these properties still remain unanswered. Aiming at a better understanding, herein a series of enantiopure NHC–gold and –silver complexes was synthesized, characterized and biologically evaluated in different in vitro systems. The individuated complexes exerted different properties based on the complexed metal and the specific configuration, with the (<i>R</i>)-gold–NHC complexes being the most active, particularly as anti-inflammatory molecules. Docking simulations indicated a different binding mode for each enantiomer. Moreover, anticancer and antibacterial activities were also evaluated for the considered enantiomers. Overall, the reported data may contribute to a better understanding of the different biological properties exerted by the enantiopure gold and silver complexes.https://www.mdpi.com/1420-3049/29/22/5262<i>N</i>-heterocyclic carbenes (NHC)enantiopure complexesiNOS inhibitionanticancerantibacterial
spellingShingle Maria Marra
Annaluisa Mariconda
Domenico Iacopetta
Jessica Ceramella
Assunta D’Amato
Camillo Rosano
Kateryna Tkachenko
Michele Pellegrino
Stefano Aquaro
Maria Stefania Sinicropi
Pasquale Longo
When Chirality Makes the Difference: The Case of Novel Enantiopure <i>N</i>-Heterocyclic Carbene–Gold and –Silver Complexes
Molecules
<i>N</i>-heterocyclic carbenes (NHC)
enantiopure complexes
iNOS inhibition
anticancer
antibacterial
title When Chirality Makes the Difference: The Case of Novel Enantiopure <i>N</i>-Heterocyclic Carbene–Gold and –Silver Complexes
title_full When Chirality Makes the Difference: The Case of Novel Enantiopure <i>N</i>-Heterocyclic Carbene–Gold and –Silver Complexes
title_fullStr When Chirality Makes the Difference: The Case of Novel Enantiopure <i>N</i>-Heterocyclic Carbene–Gold and –Silver Complexes
title_full_unstemmed When Chirality Makes the Difference: The Case of Novel Enantiopure <i>N</i>-Heterocyclic Carbene–Gold and –Silver Complexes
title_short When Chirality Makes the Difference: The Case of Novel Enantiopure <i>N</i>-Heterocyclic Carbene–Gold and –Silver Complexes
title_sort when chirality makes the difference the case of novel enantiopure i n i heterocyclic carbene gold and silver complexes
topic <i>N</i>-heterocyclic carbenes (NHC)
enantiopure complexes
iNOS inhibition
anticancer
antibacterial
url https://www.mdpi.com/1420-3049/29/22/5262
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