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Effects of Fullerene Derivatives on Activity of Ca2+-ATPase of the Sarcoplasmic Reticulum and cGMP Phosphodiesterase

  • BIOPHYSICS AND BIOCHEMISTRY
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Bulletin of Experimental Biology and Medicine Aims and scope

We studied the effects of new water-soluble polysubstituted fullerene C60 (PFD) derivatives on activity of Ca2+-Mg2+ ATPase of the sarcoplasmic reticulum and cGMP phosphodiesterase. All examined fullerene derivatives inhibited activity of both enzymes. For instance, PFD-I, PFD-II, PFD-III, PFD-V, PFD-IX, PFD-X, and PFD-XI in a concentration of 5×10—5 M completely inhibited hydrolytic and transport functions of Ca2+-ATPase. These compounds in a concentration of 5×10—6 suppressed active transport of calcium ions by 51±5, 77±8, 52±5, 52±5, 100±10, 80±8, and 100±10%, respectively, and inhibited ATP hydrolysis by 31±3, 78±8, 18±2, 29±3, 78±8, 63±7, and 73±9%, respectively, uncoupling the hydrolytic and transport functions of the enzyme. PFD-I noncompetitive and reversibly reduced activity of Ca2+-ATPase (Ki=2.3×10—6 M). All the studied fullerene derivatives (except for PFD-VII) inhibited cGMP phosphodiesterase by more than 80% in concentration of 10—4 M and higher and by more than 50% in concentration of 10—5 M. PFD-I is a non-competitive reversible inhibitor of cGMP phosphodiesterase (Ki=7×10—6 M). These results allow us to expect antimetastatic, antiaggregatory, antihypertensive and vasodilative activity of the studied compounds.

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Authors and Affiliations

  1. Institute of Problems of Chemical Physics, Russian Academy of Sciences, Chernogolovka, Moscow region, Russia

    L. V. Tat’yanenko, E. A. Khakina, A. V. Zhilenkov, P. A. Troshin, O. V. Dobrokhotova, I. Yu. Pikhteleva & A. I. Kotel’nikov

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  1. L. V. Tat’yanenko
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  2. E. A. Khakina
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  3. A. V. Zhilenkov
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  4. P. A. Troshin
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  5. O. V. Dobrokhotova
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  6. I. Yu. Pikhteleva
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  7. A. I. Kotel’nikov
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Correspondence to L. V. Tat’yanenko.

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Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 163, No. 3, pp. 298-303, March, 2017

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Tat’yanenko, L.V., Khakina, E.A., Zhilenkov, A.V. et al. Effects of Fullerene Derivatives on Activity of Ca2+-ATPase of the Sarcoplasmic Reticulum and cGMP Phosphodiesterase. Bull Exp Biol Med 163, 321–325 (2017). https://doi.org/10.1007/s10517-017-3794-y

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  • DOI: https://doi.org/10.1007/s10517-017-3794-y

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