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Issue 16, 2011
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Fullerenolates: metallated polyhydroxylated fullerenes with potent anti-amyloid activity

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Abstract

It has been revealed for the first time that sodium fullerenolate Na4[C60(OH)∼30] (NaFL), a water soluble polyhydroxylated [60]fullerene derivative, destroys amyloid fibrils of the Aβ(1–42) peptide in the brain and prevents their formation in in vitro experiments. The cytotoxicity of NaFL was found to be negligibly low with respect to nine different culture cell lines. At the same time, NaFL showed a very low acute toxicity in vivo. The maximal tolerable dose (MTD) and LD50 for NaFL correspond to 1000 mg kg−1 and 1800 mg kg−1, respectively, as revealed by in vivo tests in mice using intraperitoneal drug injection. The observed pronounced anti-amyloid activity and low toxicity of NaFL make it a very promising lead drug for the development of potent fullerene-based therapeutic approaches for the treatment of amyloidoses, such as Alzheimer's disease and others.

Graphical abstract: Fullerenolates: metallated polyhydroxylated fullerenes with potent anti-amyloid activity

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Publication details

The article was received on 12 Jan 2011, accepted on 26 Apr 2011 and first published on 27 Apr 2011


Article type: Paper
DOI: 10.1039/C1OB05067B
Citation: Org. Biomol. Chem., 2011,9, 5714-5719
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    Fullerenolates: metallated polyhydroxylated fullerenes with potent anti-amyloid activity

    A. G. Bobylev, A. B. Kornev, L. G. Bobyleva, M. D. Shpagina, I. S. Fadeeva, R. S. Fadeev, D. G. Deryabin, J. Balzarini, P. A. Troshin and Z. A. Podlubnaya, Org. Biomol. Chem., 2011, 9, 5714
    DOI: 10.1039/C1OB05067B

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