-Review-

Water-soluble Fullerene Derivatives for Drug Discovery

Shigeo Nakamura¹ and Tadahiko Mashino²

¹Department of Chemistry, Nippon Medical School
²Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University

Fullerenes (represented by buckminsterfullerene, C₆₀) are a new kind of organic compound with a cage-like structure. A great deal of attention has been focused on their unique properties. From the viewpoint of drug discovery, fullerenes could be novel lead compounds for drug discovery. However, fullerenes are poorly soluble in aqueous media. Incorporation of water-soluble groups into the fullerene core enables investigation of its biological activities. Certain fullerene derivatives show inhibitory activity against human immunodeficiency virus reverse transcriptase. Hepatitis C virus RNA polymerase is also inhibited by fullerene derivatives. Therefore, fullerene derivatives are candidate antiviral agents. In addition, fullerene derivatives exhibit antiproliferative activity by inducing apoptosis related to the generation of reactive oxygen species. Fullerene derivatives also have the potential to be anticancer drugs.

J Nippon Med Sch 2012; 79: 248-254

Keywords
fullerenes, human immunodeficiency virus reverse transcriptase, antitumor agents, apoptosis, reactive oxygen species

Correspondence to
Shigeo Nakamura, PhD, Department of Chemistry, Nippon Medical School, 2-297-2 Kosugi-cho, Nakahara-ku, Kawasaki, Kanagawa 211-0063, Japan
shigeo-nakamura@nms.ac.jp

Received, February 6, 2012
Accepted, February 24, 2012