Twenty Years of Promises: Fullerene in Medicinal Chemistry

Abstract

Many biological activities have been envisioned for fullerenes and some of them seem to be very promising. The lack of solubility in biologically friendly environments is the major obstacle in the development of this field. The possibility of multiple fuctionalization can be exploited to get more soluble compounds but, up to now, only a few polyadducts, presenting perfectly defined geometry, can be selectively prepared avoiding long purification processes.The toxicity of this third allotropic form of carbon is an aspect related to application in medicine and biology, while the concern about the environmental impact is due to the industrial production of fullerenes. Many studies are dedicated to both aspects and, so far, it is not possible to have a definitive answer although the current findings allow some optimistic vision.In this chapter the main biological applications of fullerene and fullerene derivatives will be reviewed, with special attention to the most recent advances in this field. Antiviral and antibacterial activity, enzymatic inhibition, and DNA photocleavage are some aspects considered herein, together with the use of these nanostructures as possible vectors for drug and gene delivery. The most promising applications include the use of endohedral fullerenes, filled by gadolinium, in magnetic resonance imaging (MRI) and the antioxidant capacity exploitation of some tris-adducts and fullerols.

Designing a C84 fullerene as a specific voltage-gated sodium channel blocker

“…Further development is needed regarding the toxicity of these materials in both biological and environmental environments, in the short and long terms, for these applications to be brought into widespread use. We refer the reader to recent reviews on the use of carbon nanotubes and fullerenes in biology and medicine [5,6,51]. Typically, non-functionalized carbon-based nanomaterials are considered to be toxic, but significant work has been done to make these structures soluble and biocompatible.…”

“…Increasing attention is being given to fullerenes for biological applications including antiviral and antibacterial agents, antioxidants, vectors for drug/gene delivery, photodynamic therapy, enzyme inhibitors, and diagnostics (e.g., magnetic resonance imaging) [5,6]. For example, fullerene derivatives have been shown to bind to and inhibit the activity of HIV protease [7].…”

“…One method which increases their solubility is chemical functionalization with moieties such as amino acids and carboxylic acid [5]. Fullerene chemistry has been intensely developed, and the main efforts are now devoted to broaden their application [6]. …”

Drought Impact Is Alleviated in Sugar Beets (Beta vulgaris L.) by Foliar Application of Fullerenol Nanoparticles

“…To overcome this, water-soluble fullerene derivatives have been designed and synthesised, which retain many of the unique properties of native fullerene, while enabling application for the desired biological activity. Because of their high solubility in water, these fullerene derivates represent attractive nanoparticles for various biological applications [10–14]. In particular, fullerene and its derivates exhibit strong antioxidative, antimicrobial, cytoprotective, neuroprotective and radioprotective effects in animal organisms [10,15–20].…”

Effect of C60 filling on structure and properties of composite films based on polystyrene

“…Biological activity of fullerenes is due to, firstly, lipophilic properties, so that they can penetrate into the cell membrane, secondly, electron deficit, promoting to react with free radicals, and, thirdly, capacity of excited C 60 to generate active oxygen species (Da Ros, 2008). There are researches regarding the effects of fullerenes and fullerene derivatives on bacteria (Mashino et al, 1999;Lyon et al, 2008).…”