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| Analysis of the inhibitory effect of gypenoside on Na+, K+-ATPase in rats’ heart and brain and its kinetics |
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| KeyWord:gypenoside Na K -ATPase heart and brain microsome enzyme kinetic |
| Author Name | Affiliation | E-mail | | Dr. Xiao-yan Han | Research Center, The Third Affiliated Hospital, Sun Yat-sen University, Guangzhou, 510630, China | hxy3706@126.com | | Hong-bo Wei | Research Center, The Third Affiliated Hospital, Sun Yat-sen University, Guangzhou, 510630, China | | | Fu-cheng Zhang | Research Center, The Third Affiliated Hospital, Sun Yat-sen University, Guangzhou, 510630, China | |
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| Abstract: |
| Objective To study the effects of gypenoside (Gyp) on the activity of microsomal Na+, K+-ATPase in rat’s heart and brain in vitro. Methods 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. Results 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+. Conclusion Gyp displays its cardiotonic and central inhibitory effects by way of inhibiting heart and brain’s microsomal Na+, K+-ATPase activities in rats. Supported by Guangdong Provincial Natural Science Foundation (No.010742) |
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