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Biological Activity of Water-Soluble Fullerenes. Structural Dependence of DNA Cleavage, Cytotoxicity, and Enzyme Inhibitory Activities Including HIV-Protease Inhibition
Abstract
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.
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Citations
Cited by
Fulleropyrrolidines: A Family of Full-Fledged Fullerene Derivatives
Prato, M., & Maggini, M. (1998) · Accounts of Chemical Research · doi:10.1021/ar970210p · Cited by 830
Photocleavage of Nucleic Acids
Armitage, B. (1998) · Chemical Reviews · doi:10.1021/cr960428+ · Cited by 688
•OH and O2•- Generation in Aqueous C60 and C70 Solutions by Photoirradiation: An EPR Study
Yamakoshi, Y., Sueyoshi, S., Fukuhara, K., Miyata, N., Masumizu, T., & Kohno, M. (1998) · Journal of the American Chemical Society · doi:10.1021/ja9823969 · Cited by 157
DNA Cleavage by UVA Irradiation of NADH with Dioxygen via Radical Chain Processes
Tanaka, M., Ohkubo, K., & Fukuzumi, S. (2006) · The Journal of Physical Chemistry A · doi:10.1021/jp064130r · Cited by 45
Metadata
- Authors
- Nakamura, E., Tokuyama, H., Yamago, S., Shiraki, T., & Sugiura, Y.
- Venue
- Bulletin of the Chemical Society of Japan
- Publisher
- Oxford University Press (OUP)
- Published
- 1996-08-01
- Volume
- 69
- Issue
- 8
- Pages
- 2143-2151
- ISSN
- 0009-2673 (ISSN-L)
- 1348-0634
- OpenAlex
- W2005382895
- Cited by
- 190
- References
- 0
- FWCI
- 8.08
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Biological Activity of Water-Soluble Fullerenes. Structural Dependence of DNA Cleavage, Cytotoxicity, and Enzyme Inhibitory Activities Including HIV-Protease Inhibition. https://app.cochat.ai/papers/10.1246/bcsj.69.2143
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- Nakamura, E., Tokuyama, H., Yamago, S., Shiraki, T., & Sugiura, Y. (1996). Biological Activity of Water-Soluble Fullerenes. Structural Dependence of DNA Cleavage, Cytotoxicity, and Enzyme Inhibitory Activities Including HIV-Protease Inhibition. Bulletin of the Chemical Society of Japan. https://doi.org/10.1246/bcsj.69.2143
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