Biological Activity of Water-Soluble Fullerenes--Structural Dependence of DNA Cleavage,Cytotoxicity,and Enzyme Inhibitory Activities Including HIV-Protease Inhibition

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  • Biological Activity of Water-Soluble Fu

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<jats:title>Abstract</jats:title> <jats:p>Two different classes of water-soluble fullerene derivatives, detergent-type and sphere-type, were synthesized. The derivatives were evaluated for their biological activities including cytotoxicity, DNA cleavage, and inhibition of HIV-protease and other enzymes. Both classes of compounds display generally similar behavior except for their cytotoxicity spectra against several cell lines. The fullerene derivatives bearing N-methylpyrrole were found to be photo-inactive with respect to DNA cleaving activity and cytotoxicity. A study on the kinetics for the inhibition of HIV-protease with detergent type derivative revealed that the compound is a potent fullerene-based HIV protease inhibitor, inhibiting the enzyme activity in a reversible and competitive manner with a Ki value of 0.32 μM.</jats:p>

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