Vol. 25, No. 4, 2003 (December)
	Content

SYNTHESIS AND ANTIPROLIFERATIVE PROPERTIES OF SUCCINYLATED AND ACONITYLATED DERIVATIVES OF a-2b-RECOMBINANT INTERFERON

А.V. Мartynov^1,*, V.P. Chernykh²

¹I.I. Mechnikov Institute of Microbiology and Virology AMS of Ukraine, Kharkiv, Ukraine
²National Pharmaceutical University of Ukraine, Kharkiv, Ukraine

Abstract. Aim: to study antiproliferative activity of aconitylated (AIFN) and succinylated (SIFN) derivatives of recombimnant a-2b-interferon (IFN). Methods: acylation of IFN was carried out using succinic and aconitic anhydrides; antiproliferative properties of AIFN and SIFN were studied in vitro using highly sensitive to IFN CaOV cell line and SW-480 cell line with low sensitivity to IFN. Results: acylation of 1 lysine of IFN molecule with cis-aconitic or succinic anhydride results in 3–3.5-fold increase of its antiproliferative activity against СаОv cells. The highest antiproliferative activity against SW-480 cells was registered for both AIFNs and SIFNs with 3 modified lysine residues. Conclusion: aconitylated and succinylated IFNs may be considered as perspective antiproliferative agents.

Key Words: recombinant a-2b-interferon, aconitylated interferon, succinylated interferon, antiproliferative activity in vitro.

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