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

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

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)

Abstract

The effects of the newly synthesized covalent conjugates of water-soluble fullerene derivatives (WSFD) with xanthene dyes: polyanionic WSFD—fluorescein (1), polycationic WSFD—fluorescein (2), polyanionic WSFD—eosin (3), and polyanionic WSFD (4), polycationic WSFD (5), fluorescein (6) and eosin (7), on activity of the membrane-bound Ca2+-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 these compounds 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 function of the enzyme is competitive; compounds 1 and 4 are noncompetitive. Polycationic WSFD fluorescein (2) and polycationic WSFD (5) do not affect ATP hydrolysis, but inhibit active Ca2+ transport in a concentration of 0.01 mM by 100±10 and 40±4%, respectively. Conjugates 1 and 3 completely inhibit the hydrolytic and transport functions of the enzyme in a concentration of 0.01 mM, and in a concentration of 0.001 mM inhibit active Ca2+ transport by 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 active transmembrane transfer of Ca2+ and make it possible to predict the presence of antimetastatic and antiaggregatory activities of the studied compounds.

Original languageEnglish
Pages (from-to)89-94
Number of pages6
JournalBulletin of Experimental Biology and Medicine
Volume169
Issue number1
DOIs
Publication statusPublished - 1 May 2020
Externally publishedYes

Keywords

  • Ca2+-ATPase of the sarcoplasmic reticulum
  • fullerene derivatives
  • inhibition
  • xanthene dyes

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