Analysis of the inhibitory effect of gypenoside on Na+, K+-ATPase in rats’ heart and brain and its kinetics

Han  Xiao-yan; Wei Hong-bo; Zhang Fu-cheng

doi:10.1007/s11655-007-0128-3

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Analysis of the inhibitory effect of gypenoside on Na+, K+-ATPase in rats’ heart and brain and its kinetics

OriginalPaper | Updated：2021-08-27

- Analysis of the inhibitory effect of gypenoside on Na+, K+-ATPase in rats’ heart and brain and its kinetics
- Analysis of the inhibitory effect of gypenoside on Na+, K+-ATPase in rats’ heart and brain and its kinetics
- 中国结合医学杂志（英文版） 2007年13卷第2期页码：128-131
- Affiliations：
  
  Research Center, The Third Affiliated Hospital, Sun Yat-sen University,Guangzhou,China
- Author bio：
- Funds：
  
  Supported by Guangdong Provincial Natural Science Foundation (No.010742)
- DOI：10.1007/s11655-007-0128-3
  中图分类号：
- 纸质出版日期：2007，
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Han, Xy., Wei, Hb. & Zhang, Fc. Analysis of the inhibitory effect of gypenoside on Na+, K+-ATPase in rats’ heart and brain and its kinetics., Chin. J Integ. Med. 13, 128–131 (2007). https://doi.org/10.1007/s11655-007-0128-3

Han Xiao-yan, Wei Hong-bo, Zhang Fu-cheng. Analysis of the inhibitory effect of gypenoside on Na+, K+-ATPase in rats’ heart and brain and its kinetics[J]. Chinese Journal of Integrative Medicine, 2007,13(2):128-131.
Han, Xy., Wei, Hb. & Zhang, Fc. Analysis of the inhibitory effect of gypenoside on Na+, K+-ATPase in rats’ heart and brain and its kinetics., Chin. J Integ. Med. 13, 128–131 (2007). https://doi.org/10.1007/s11655-007-0128-3 DOI：

Han Xiao-yan, Wei Hong-bo, Zhang Fu-cheng. Analysis of the inhibitory effect of gypenoside on Na+, K+-ATPase in rats’ heart and brain and its kinetics[J]. Chinese Journal of Integrative Medicine, 2007,13(2):128-131. DOI： 10.1007/s11655-007-0128-3.

摘要

To study the effects of gypenoside (Gyp) on the activity of microsomal Na+

K+-ATPase in rat’s heart and brain in vitro. The microsomal Na+

K+-ATPase was prepared from rat’s heart and brain by differential centrifugation. The activity of microsomal Na+

K+-ATPase was assayed by colorimetric technique. Enzyme kinetic analysis method was used to analyze the effect of Gyp on the microsomal Na+

K+-ATPase of rats. Gyp reversibly inhibited the brain and heart’s microsomal Na+

K+-ATPase in a concentration-dependent manner

and showed a more potent effect on enzyme in the brain. The IC50 of Gyp for the heart and brain were 58.79±8.05 mg/L and 52.07±6.25 mg/L

respectively. The inhibition was enhanced by lowering the Na+

or K+ concentrations or increasing the ATP concentration. Enzyme kinetic studies indicated that the inhibitory effect of Gyp on the enzyme is like that of competitive antagonist of Na+

the counter-competitive inhibitor for the substrate ATP

and the mixed-type inhibitor for K+. Gyp displays its cardiotonic and central inhibitory effects by way of inhibiting heart and brain’s microsomal Na+

K+-ATPase activities in rats.

Abstract

To study the effects of gypenoside (Gyp) on the activity of microsomal Na+

K+-ATPase in rat’s heart and brain in vitro. The microsomal Na+

K+-ATPase was prepared from rat’s heart and brain by differential centrifugation. The activity of microsomal Na+

K+-ATPase was assayed by colorimetric technique. Enzyme kinetic analysis method was used to analyze the effect of Gyp on the microsomal Na+

K+-ATPase of rats. Gyp reversibly inhibited the brain and heart’s microsomal Na+

K+-ATPase in a concentration-dependent manner

and showed a more potent effect on enzyme in the brain. The IC50 of Gyp for the heart and brain were 58.79±8.05 mg/L and 52.07±6.25 mg/L

respectively. The inhibition was enhanced by lowering the Na+

or K+ concentrations or increasing the ATP concentration. Enzyme kinetic studies indicated that the inhibitory effect of Gyp on the enzyme is like that of competitive antagonist of Na+

the counter-competitive inhibitor for the substrate ATP

and the mixed-type inhibitor for K+. Gyp displays its cardiotonic and central inhibitory effects by way of inhibiting heart and brain’s microsomal Na+

K+-ATPase activities in rats.

关键词

gypenosideNa+K+-ATPaseheart and brain microsomeenzyme kinetic

Keywords

gypenosideNa+K+-ATPaseheart and brain microsomeenzyme kinetic

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