Effects of Two Fullerene Derivatives on Monocytes and Macrophages

Abstract

Two fullerene derivatives (fullerenes 1 and 2), bearing a hydrophilic chain on the pyrrolidinic nitrogen, were developed with the aim to deliver anticancer agents to solid tumors. These two compounds showed a significantly different behaviour on human neoplastic cell lines in vitro in respect to healthy leukocytes. In particular, the pyrrolidinium ring on the fullerene carbon cage brings to a more active compound. In the present work, we describe the effects of these fullerenes on primary cultures of human monocytes and macrophages, two kinds of immune cells representing the first line of defence in the immune response to foreign materials. These compounds are not recognized by circulating monocytes while they get into macrophages. The evaluation of the pronecrotic or proapoptotic effects, analysed by means of analysis of the purinergic receptor P2X7 activation and of ROS scavenging activity, has allowed us to show that fullerene 2, but not its analogue fullerene 1, displays toxicity, even though at concentrations higher than those shown to be active on neoplastic cells.

Nanoquantitative Structure-Property Relationship Modeling on C42Fullerene Isomers

“…Since their discovery in 1985 [1], fullerenes attracted interest in different fields of science, including medical field (e.g., for potential use as antibiotics [2][3][4], as inhibitors of erythroid cells-fullerenol [5], as drug delivery system [6], or as inhibitors of inflammatory mediators [7]). Fullerene molecules are constructed from carbon atoms and take the shape of sphere (also known as buckyballs), ellipsoid, or tube [8].…”

Mixed Fluorinated/Hydrogenated Self‐Assembled Monolayer‐Protected Gold Nanoparticles: In Silico and In Vitro Behavior

“…MTT Metabolic Cytotoxicity Assay : The colorimetric MTT assay was performed, as previously described . Briefly, 10 5 cells per well were treated with 0.01–1 mg mL −1 of a tested NP.…”

“…Flow Cytometric Assays—Apoptosis Assay : JC‐1 cyanine iodide (5,5′,6,6′‐tetrachloro‐1,1′,3,3′‐tetraethyl‐benzimidazolcarbocyanine iodide; Molecular Probes Europe BV, Leiden, The Netherlands), a mitochondrial inner membrane potential probe, was used as previously described . Briefly, the probe (2.5 µg mL −1 ) was added for 15 min to NP‐treated or ‐untreated control cells, and then samples were washed twice, resuspended in PBS and immediately analyzed by flow cytometry, acquiring both LogFL2 and LogFL1 signals on viable cells (those excluding PI, run in parallel).…”

Fullerenes in biology and medicine

“…129 Compounds 52 and 53 were more active on neoplastic proliferating cells than on circulating monocytes. Compound 53 is more toxic than compound 52 against the tested cells.…”

“…129 studied the interaction between fullerene derivatives 52 and 53 (Fig. 12) and cells of the immune system and their results stress the important role of fullerene derivatives in the control of inflammatory and cancer diseases.…”