In vitro Anti-atherogenic Properties of N-Heterocyclic Carbene Aurate(I) Compounds

Eleni Sioriki; Ronan Lordan; Fady Nahra; Kristof Van Hecke; Ioannis Zabetakis; Steven P. Nolan

doi:10.1002/cmdc.201800601

In vitro Anti-atherogenic Properties of N-Heterocyclic Carbene Aurate(I) Compounds

Eleni Sioriki, Ronan Lordan, Fady Nahra, Kristof Van Hecke, Ioannis Zabetakis, Steven P. Nolan

Research output: Contribution to journal › Article › peer-review

18 Scopus citations

Abstract

The anti-atherogenic (anti-inflammatory) properties of various aurate(I) salts, of the general formula [NHC⋅H][AuCl2] (NHC=N-heterocyclic carbene) were investigated. The aurates were easily synthesized and obtained in analytically pure form. In addition, the biological activity of these compounds against atheromatosis via in vitro inhibition of platelet-activating factor (PAF)-induced platelet aggregation was probed. All complexes were found to possess anti-aggregatory properties in vitro with [IPr*⋅H][AuCl2] (6) being the most potent inhibitor of PAF at micromolar concentration. Based on our findings, we conclude that these simply assembled aurates are a very promising class of PAF inhibitors and anti-inflammatory drugs.

Original language	English (US)
Pages (from-to)	2484-2487
Number of pages	4
Journal	ChemMedChem
Volume	13
Issue number	23
DOIs	https://doi.org/10.1002/cmdc.201800601
State	Published - Nov 1 2018
Externally published	Yes

ASJC Scopus subject areas

Organic Chemistry
Molecular Medicine
Pharmacology, Toxicology and Pharmaceutics(all)

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10.1002/cmdc.201800601

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title = "In vitro Anti-atherogenic Properties of N-Heterocyclic Carbene Aurate(I) Compounds",

abstract = "The anti-atherogenic (anti-inflammatory) properties of various aurate(I) salts, of the general formula [NHC⋅H][AuCl2] (NHC=N-heterocyclic carbene) were investigated. The aurates were easily synthesized and obtained in analytically pure form. In addition, the biological activity of these compounds against atheromatosis via in vitro inhibition of platelet-activating factor (PAF)-induced platelet aggregation was probed. All complexes were found to possess anti-aggregatory properties in vitro with [IPr*⋅H][AuCl2] (6) being the most potent inhibitor of PAF at micromolar concentration. Based on our findings, we conclude that these simply assembled aurates are a very promising class of PAF inhibitors and anti-inflammatory drugs.",

author = "Eleni Sioriki and Ronan Lordan and Fady Nahra and {Van Hecke}, Kristof and Ioannis Zabetakis and Nolan, {Steven P.}",

note = "KAUST Repository Item: Exported on 2022-06-09 Acknowledged KAUST grant number(s): OSR-2015-CCF-1974-03 Acknowledgements: This work was supported in part by the Department of Biological Sciences, University of Limerick, Limerick, Ireland. We thank King Saud University (Distinguished Scientist Fellowship Program) and King Abdullah University of Science and Technology (Award No. OSR-2015-CCF-1974-03) for their support. This publication acknowledges KAUST support, but has no KAUST affiliated authors.",

year = "2018",

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doi = "10.1002/cmdc.201800601",

language = "English (US)",

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AU - Sioriki, Eleni

AU - Lordan, Ronan

AU - Nahra, Fady

AU - Van Hecke, Kristof

AU - Zabetakis, Ioannis

AU - Nolan, Steven P.

N1 - KAUST Repository Item: Exported on 2022-06-09 Acknowledged KAUST grant number(s): OSR-2015-CCF-1974-03 Acknowledgements: This work was supported in part by the Department of Biological Sciences, University of Limerick, Limerick, Ireland. We thank King Saud University (Distinguished Scientist Fellowship Program) and King Abdullah University of Science and Technology (Award No. OSR-2015-CCF-1974-03) for their support. This publication acknowledges KAUST support, but has no KAUST affiliated authors.

PY - 2018/11/1

Y1 - 2018/11/1

N2 - The anti-atherogenic (anti-inflammatory) properties of various aurate(I) salts, of the general formula [NHC⋅H][AuCl2] (NHC=N-heterocyclic carbene) were investigated. The aurates were easily synthesized and obtained in analytically pure form. In addition, the biological activity of these compounds against atheromatosis via in vitro inhibition of platelet-activating factor (PAF)-induced platelet aggregation was probed. All complexes were found to possess anti-aggregatory properties in vitro with [IPr*⋅H][AuCl2] (6) being the most potent inhibitor of PAF at micromolar concentration. Based on our findings, we conclude that these simply assembled aurates are a very promising class of PAF inhibitors and anti-inflammatory drugs.

AB - The anti-atherogenic (anti-inflammatory) properties of various aurate(I) salts, of the general formula [NHC⋅H][AuCl2] (NHC=N-heterocyclic carbene) were investigated. The aurates were easily synthesized and obtained in analytically pure form. In addition, the biological activity of these compounds against atheromatosis via in vitro inhibition of platelet-activating factor (PAF)-induced platelet aggregation was probed. All complexes were found to possess anti-aggregatory properties in vitro with [IPr*⋅H][AuCl2] (6) being the most potent inhibitor of PAF at micromolar concentration. Based on our findings, we conclude that these simply assembled aurates are a very promising class of PAF inhibitors and anti-inflammatory drugs.

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DO - 10.1002/cmdc.201800601

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JO - ChemMedChem

JF - ChemMedChem

IS - 23

ER -

In vitro Anti-atherogenic Properties of N-Heterocyclic Carbene Aurate(I) Compounds

Abstract

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