Fullerene (C60), a carbon buckyball, was discovered by Harold Kroto, James R. Heath, Sean O’Brien, Robert Curl, and Richard Smalley in 1985 [18]. It has since been utilized in electronic and mechanical applications [19]. In physiological studies, the biological effects of water-soluble fullerene derivatives containing several hydrophilic groups are noteworthy because fullerene itself is water-insoluble. Water-soluble fullerene derivatives are known to possess various biological and pharmacological properties, including antioxidant activity and inhibitory effects against human immunodeficiency virus (HIV) proteases and DNA photocleavage [20]–[23]. Mashino et al. also demonstrated that pyrrolidinium fullerene derivative 6 (Fig. 1) has antiproliferative and antibacterial activity [24], malonic acid fullerene derivative 2 (Fig. 1) has excellent antioxidant activity [25], and proline-modified fullerene derivative 3 (Fig. 1) inhibits HIV-reverse transcriptase [22]. Thus, fullerene derivatives are expected to become a novel type of medication because of their unique skeleton.