Wyniki wyszukiwania - BazTech

1

Affinity of new anticancer agent, 7-trimethylsilyl-ethyl-10-amino-camptothecin, to membranes and HSA determined by fluorescence spectroscopy methods

Kruszewski S., Kruszewska D. M.

Optica Applicata

|

2008

|

Vol. 38, nr 4

625-633

EN

The application of fluorescence anisotropy measurements in determining the properties of camptothecin analogue 7-trimethylsilylethyl-10-amino-camptothecin - a promising anticancer agent - is described in this paper. The fluorescence anisotropy measurements provide useful information about binding of camptothecins to membranes and proteins, including human serum albumin (HSA). Knowledge of these properties is important for potential clinical applications of these agents, and permits to select from camptothecin analogues only those which exhibit desirable properties. An active lactone form of camptothecin in fluids at pH 7.4 hydrolyses and converts into an inactive carboxylate form. The carboxylate form of camptothecin binds easily and irreversibly to HSA. Only free carboxylate form can transform back into lactone, then in the presence of HSA one direction transition occurs (from lactone to carboxylate); therefore in HSA solution, after about two hours, the lactone form almost totaly decays. On the other hand, the camptothecins bound to membranes do not hydrolyse. Fluorescence anisotropy measurements prove that 7-trimethylsilylethyl-10-amino-camptothecin exhibits desirable properties: high affinity of its lactone form to membranes and low affinity of its carboxylate form to HSA. Such properties should ensure high stability of this drug in physiological fluids, including blood.

2

Affinity of new anticancer agent, DB-174, to membranes and HSA determined by fluorescence spectroscopy methods

Kruszewski S., Bom D., Ziomkowska B., Cyrankiewicz M.

Optica Applicata

|

2006

|

Vol. 36, nr 2-3

199-207

EN

The application of fluorescence spectroscopy methods to determining the properties of camptothecins promising anticancer agents are described in this paper. The fluorescence anisotropy measurements provide useful information about the binding of camptothecin and its analogues to cell membranes and human serum albumin (HSA) that is important for potential clinical applications of these agents, and permits the selection from many camptothecin analogues those ones exhibiting desirable biomedical properties. Binding properties of 7-trimethylsilyl-ethyl-10 hydroxy-camptothecin are the subject of this paper.

3

Zastosowanie metod fluorometrycznych do określania właściwości kamptotecyny i jej pochodnych

Kruszewski S.

Acta Bio-Optica et Informatica Medica. Inżynieria Biomedyczna

|

2003

|

Vol. 9, nr 3-4

151-156

PL

Kamptotecyna (CPT) i jej pochodne stanowią ważną klasę S-fazowych przeciwnowotworowych związków. W warunkach fizjologicznych CPT szybko hydrolizuje i przechodzi w nieaktywną formę karboksylową. Zanik biologicznie aktywnej formy CPT jest szczególnie szybki w osoczu krwi. Analog kamptotecyny DB-67, w przeciwieństwie do CPT, wykazuje wyjątkowo dużą stabilność we krwi. Metody spektroskopii fluorescencyjnej zostały zastosowane do określania fizycznych i przewidywania biologicznych właściwości kamptotecyny i jej analogów.

EN

Camptothecin (CPT) and related congeners have became an important class of S-phase anticancer agent. Unfortunately CPT hydrolyses under physiological conditions, and converts into inactive carboxylate form. Decrease of active form of CPT occurs especially fast in plasma of human blood. The new camptothecin analogue DB-67, in contrary to CPT, exhibits impressive blood stability. Fluorescence spectroscopy methods were used to determine physical and to predict biological properties of camptothecins.