Fluorescence Spectroscopy in Camptothecins Studies
S. Kruszewskia and D.M. Kruszewskab
aMedical Physics Division, Biophysics Department, Collegium Medicum of Nicolaus Copernicus University, JagielloĊ„ska 13-15, 85-067 Bydgoszcz, Poland
bDepartment of Theoretical Foundations of Biomedical Sciences and Medical Informatics, Collegium Medicum of Nicolaus Copernicus University, JagielloĊ„ska 13-15, 85-067 Bydgoszcz, Poland
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The application of fluorescence spectroscopy methods to determining the properties of analogues of campto-thecin, promising anticancer agents, are described in this paper. The fluorescence anisotropy measurements provide useful information about the binding of campto-thecin and its analogues to cell membranes and human serum albumin (HSA) that is important for potential clinical applications of these agents, and permit the selection from many campto-thecin analogues those ones exhibiting desirable biomedical properties. Fluorescence anisotropy measurements prove that 3 new campto-thecin analogues: 7-tert butyl-dimethyl-silyl 10 hydroxy camptho-thecin, 7 tri-methyl sily-lethyl 10 hydroxy campto-thecin and 7 tri-methyl silyl ethyl 10 amino campto-thecin exhibit high affinity of their lactone forms to membranes and low affinity of their carboxylate forms to HSA. Such properties should ensure high stability of these agents in physiological fluids, including blood.
DOI: 10.12693/APhysPolA.118.99
PACS numbers: 87.64.kv, 87.15.kp