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

被引：1

作者：

Tat'yanenko, L. V. ^{[1
]}

Khakina, E. A. ^{[1
]}

Zhilenkov, A. V. ^{[1
]}

Troshin, P. A. ^{[1
]}

Dobrokhotova, O. V. ^{[1
]}

Pikhteleva, I. Yu. ^{[1
]}

Kotel'nikov, A. I. ^{[1
]}

机构：

[1] Russian Acad Sci, Inst Problems Chem Phys, Chernogolovka, Moscow Region, Russia

来源：

BULLETIN OF EXPERIMENTAL BIOLOGY AND MEDICINE | 2017年 / 163卷 / 03期

关键词：

Ca2+-Mg2+-ATPase of the sarcoplasmic reticulum; cGMP phosphodiesterase; inhibition; fullerene derivatives; CHLOROFULLERENE C60CL6; COMPLEXES;

D O I：

10.1007/s10517-017-3794-y

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

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 5x10(-5) M completely inhibited hydrolytic and transport functions of Ca2+-ATPase. These compounds in a concentration of 5x10(-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 (K-i=2.3x10(-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 (K-i=7x10(-6) M). These results allow us to expect antimetastatic, antiaggregatory, antihypertensive and vasodilative activity of the studied compounds.

引用

页码：321 / 325

页数：5

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