Abstract
Viridicatin and its derivatives were found to be the potent strong inhibitors of the tumor necrosis factor-induced replication of many serious diseases. Their extremely low solubility in aqueous medium at a physiological pH compromises bioavailability and leads to poor pharmacokinetic performance and low exposure. Since the pharmacologic activation represents a valuable strategy for treatment of major diseases, we first obtained water-soluble form of viridicatin and viridicatol and realized this by encapsulation in the cyclodextrin cavity. We also investigated self-assembling behavior of resulting complexes and showed that the cyclodextrin complex is more than four times more active against diseased cells than to healthy ones. Measurement of cytotoxic activity performed with normal human embryonic lung cells and human lung carcinoma cell cultures demonstrated that the functional group in the chemical structure of viridicatin derivatives also influences its biologic properties.
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