Citation:

Aggregation versus Biological Activity in Gold(I) Complexes. An Unexplored Concept, Pinto, Andrea, Roma-Rodrigues Catarina, Ward {Jas S. }, Puttreddy Rakesh, Rissanen Kari, Baptista {Pedro V. }, Fernandes {Alexandra R. }, Lima {João Carlos}, and Rodríguez Laura , Inorganic Chemistry, dec, Volume 60, Number 24, p.18753–18763, (2021)

Abstract:

The aggregation process of a series of mono- and dinuclear gold(I) complexes containing a 4-ethynylaniline ligand and a phosphane at the second coordination position (PR3-Au-CCC6H4-NH2, complexes 1-5, and (diphos)(Au-CCC6H4-NH2)2, complexes 6-8), whose biological activity was previously studied by us, has been carefully analyzed through absorption, emission, and NMR spectroscopy, together with dynamic light scattering and small-angle X-ray scattering. These experiments allow us to retrieve information about how the compounds enter the cells. It was observed that all compounds present aggregation in fresh solutions, before biological treatment, and thus they must be entering the cells as aggregates. Inductively coupled plasma atomic emission spectrometry measurements showed that mononuclear complexes are mainly found in the cytosolic fraction; the dinuclear complexes are mainly found in a subsequent fraction composed of nuclei and cytoskeleton. Additionally, dinuclear complex 8 affects the actin aggregation to a larger extent, suggesting a cooperative effect of dinuclear compounds.

Notes:

Funding Information: info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F50006%2F2020/PT# info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDP%2F50006%2F2020/PT# info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDP%2F04378%2F2020/PT# info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F04378%2F2020/PT# The authors are grateful to the Spanish Ministerio de Ciencia, Innovación y Universidades (Project PID2019-104121GB-I00).LA/P/0140/2020 of the Associate Laboratory Institute for Health and Bioeconomy, i4HB. SAXS experiments were performed at the NCD-BL11 beamline of the ALBA Synchrotron Light Facility in collaboration with the ALBA staff. The authors also acknowledge COST Actions CA1740─Nano4clinics and CA18202─NECTAR. The Finnish Cultural Foundation (Grant 00201148 to J.S.W.) is also acknowledged for their support. Publisher Copyright: © 2021 American Chemical Society.