4.1 Article

Interceptor effect of C60 fullerene on the in vitro action of aromatic drug molecules

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SPRINGER
DOI: 10.1007/s00249-014-0960-2

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DNA-binding drugs; C-60 fullerene; Caffeine; Human buccal epithelial cells; Hetero-association

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C-60 fullerenes are spherical molecules composed purely of carbon atoms. They inspire a particularly strong scientific interest because of their specific physico-chemical properties and potential medical and nanotechnological applications. In this work we are focusing on studying the influence of the pristine C-60 fullerene on biological activity of some aromatic drug molecules in human buccal epithelial cells. Assessment of the heterochromatin structure in the cell nucleus as well as the barrier function of the cell membrane was performed. The methods of cell microelectrophoresis and atomic force microscopy were also applied. A concentration-dependent restoration of the functional activity of the cellular nucleus after exposure to DNA-binding drugs (doxorubicin, proflavine and ethidium bromide) has been observed in human buccal epithelial cells upon addition of C-60 fullerene at a concentration of similar to 10(-5) M. The results were shown to follow the framework of interceptor/protector action theory, assuming that non-covalent complexation between C-60 fullerene and the drugs (i.e., hetero-association) is the major process responsible for the observed biological effects. An independent confirmation of this hypothesis was obtained via investigation of the cellular response of buccal epithelium to the coadministration of the aromatic drugs and caffeine, and it is based on the well-established role of hetero-association in drug-caffeine systems. The results indicate that C-60 fullerene may reverse the effects caused by the aromatic drugs, thereby pointing out the potential possibility of the use of aromatic drugs in combination with C-60 fullerene for regulation of their medico-biological action.

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