Effects of Covalent Conjugates of Fullerene Derivatives with Xanthene Dyes on Activity of Ca2+-ATPase of the Sarcoplasmic Reticulum

Tatyanenko, L.V.; Pokidova, O.V.; Goryachev, N.S.; Kraevaya, O.A.; Khakina, E.A.; Belik, A.Y.; Rybkin, A.Y.; Dobrokhotova, O.V.; Pikhteleva, I.Y.; Troshin, P.A.; Kotelnikov, A.I.

Авторы: Tatyanenko L.V., Pokidova O.V., Goryachev N.S., Kraevaya O.A., Khakina E.A., Belik A.Yu, Rybkin A.Yu, Dobrokhotova O.V., Pikhteleva I.Yu, Troshin P.A., Kotelnikov A.I.
Журнал: Bulletin of Experimental Biology and Medicine
Том: 169
Номер: 1
Год издания: 2020
Издательство: Springer Nature
Местоположение издательства: Switzerland
Первая страница: 89
Последняя страница: 94
DOI: 10.1007/s10517-020-04831-8
Аннотация: The effects of the newly synthesized covalent conjugates of water-soluble fullerene derivatives(WSFD) with xanthene dyes: polyanionic WSFD—fluorescein (1), polycationicWSFD—fluorescein (2), polyanionic WSFD—eosin (3), and polyanionic WSFD (4),polycationic WSFD (5), fluorescein (6) and eosin (7), on activity of the membrane-boundCa2 +-ATPase of the sarcoplasmic reticulum (SR Ca2 +-ATPase) were studied. Compounds 1,3, 4, 6, and 7 inhibit the hydrolytic function of the enzyme, the inhibition constants for thesecompounds are Ki=1.3×10—5 M (1), Ki=4.7×10—6 M (3), Ki=2.5×10—6 M (4), Ki=6.1×10—5 M(6), and Ki=5.8×10—6 M (7). The effects of compounds 3, 6, and 7 on the hydrolytic functionof the enzyme is competitive; compounds 1 and 4 are noncompetitive. Polycationic WSFDfluorescein (2) and polycationic WSFD (5) do not affect ATP hydrolysis, but inhibit activeCa2+ transport in a concentration of 0.01 mM by 100±10 and 40±4%, respectively. Conjugates1 and 3 completely inhibit the hydrolytic and transport functions of the enzyme in aconcentration of 0.01 mM, and in a concentration of 0.001 mM inhibit active Ca2+ transportby 60±6 and 55±6% uncoupling the hydrolytic and transport functions of SR Ca2+-ATPases.The obtained results demonstrate a significant effect of the studied compounds on the activetransmembrane transfer of Ca2 + and make it possible to predict the presence of antimetastatic and antiaggregatory activities of the studied compounds.
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Effects of Covalent Conjugates of Fullerene Derivatives with Xanthene Dyes on Activity of Ca2+-ATPase of the Sarcoplasmic Reticulumстатья

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