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In this paper the method of determination of membranes affinity of hydroxycamptothecins is described. Under physiological conditions hydroxycamptothecins easily hydrolyze and convert into inactive carboxylate form. The process of deactivation is inhibited when the molecules of drug are bound to cell membranes so it is desirable that hydroxycamptothecins molecules bind easily to membranes. A quantitative measure of drugs affinity to membranes is the association constant. To determine this parameter the small unilamellar liposomes are used as model membranes. The affinities of 10-hydroxycamptothecin, SN-38 and DB-67 to membranes are determined. The association constants are calculated on the basis of changes of fluorescence spectra.
Słowa kluczowe
Czasopismo
Rocznik
Tom
Strony
209--215
Opis fizyczny
Bibliogr. 9 poz.,
Twórcy
autor
autor
autor
- Collegium Medicum of N. Copernicus University ul. Jagiellońska 13, 85-067 Bydgoszcz Poland
Bibliografia
- [1] WALL M.E., WANI M.C., COOK C.E., PALMER K.H., MCPHAIL A.T., SIM G.A., Plant antitumor agents. I. The isolation and structure of camptothecin, a novel alkaloidal leukemia and tumor inhibitor from Camptotheca acuminata, Journal of the American Chemical Society 88(16), 1966, pp. 3888–90.
- [2] KOHN K.W., POMMIER Y., Molecular and biological determinants of the cytotoxic actions of camptothecins. Perspective for the development of new topoisomerase I inhibitors, Annals of the New York Academy of Sciences 922, 2000, pp. 11–26.
- [3] LIU L.F., DESAI S.D., LI T.-K., MAO Y., SUN M., SIM S.-P., Mechanism of action of camptothecin, Annals of the New York Academy of Sciences 922, 2000, pp. 1–10.
- [4] MI Z., BURKE T.G., Differential interactions of camptothecin lactone and carboxylate forms with human blood components, Biochemistry 33(34), 1994, pp. 10325–36.
- [5] BURKE T.G., MISHRA A.K., WANI M.C., WALL M.E., Lipid bilayer partitioning and stability of camptothecin drugs, Biochemistry 32(20), 1993, pp. 5352–64.
- [6] BIAŁEK H., System for computer recording and analysis of fluorescence spectra using monochromator SPM-2, Diploma Thesis, Institute of Mathematics And Physics, University of Technology and Agriculture (AkademiaTechniczno-Rolnicza – the ATR), Bydgoszcz, Poland 2003 (in Polish).
- [7] JOLLIFFE I.T., Principal Component Analysis, Springer Verlag, New York, Berlin, Heidelberg, Tokyo 1986.
- [8] KRUSZEWSKI S., BURKE T.G., Camptothecins affinity to HSA and membranes determined by fluorescence anisotropy measurements, Optica Applicata 32(4), 2002, pp. 721–30.
- [9] BOM D., CURRAN D.P., CHAVAN A.J., KRUSZEWSKI S., ZIMMER S.G., FRALEY K.A., BURKE T.G., Novel A,B,E-ring-modified camptothecins displaying high lipophilicity and markedly improved human blood stabilities, Journal of Medicinal Chemistry 42(16), 1999, pp. 3018–22.
Typ dokumentu
Bibliografia
Identyfikator YADDA
bwmeta1.element.baztech-article-BPW7-0002-0064