Background and Objective: Artimisinin (an anti-malaria drug) is extracted from Artemisia annua and its water soluble derivative is dihydroartimisinin. Previous in vivo and in vitro studies showed that it has an inhibitory effect on T cells. It is also useful for immunosuppression of immune system. Materials and Methods: The stable state kinetic for comparison of inhibitory effect of artimisinin, dihydroartimisinin and cyclosporine A on calcineurin activation was used in this study. First, the best inhibitory concentration of artimisinin, dihydroartimisinin and cyclosporine A was calculated. Afterwards, the km and Vmax of them in the presence of substrate, paranitrophenylphosphate (P-NPP) were measured. The KI was calculated in the presence of cyclosporine A, artemisinin and dihydroartemisinin. In this study, we used distilled water instead of sample in blank and cyclosporinA as a positive control group. Results: The Vmax in the control group was 81.97 M/min and in the presence of cyclosporine A and artemisinin or dihydroartemisinin were 81.97 M/min and 66.225 M/min, respectively. The Km in the absence of inhibitors was 1.886 M and in the presence of cyclosporine A and artemisinin or dihydroartemisinin was 2.819 M and 1.736, respectively. Also, KI in the presence of artimisinin and dihydroartimisinin was 4.219 ×10-5 M and in the presence of cyclosporine A was 2.021×10-5 M. Conclusion: This study indicates that the inhibitory power of artimisinin and dihydroartimisinin is almost equal and they inhibited calcineurin competitively, while inhibitory effect of cyclosporine A is non-competitive.
Naderi, G., Moukhah, R., & Yousefi, A. (2015). In Vitro Evaluation of Inhibitory Effect of Artemisinin and Dihydroartemisinin on Calcineurin Enzyme. Journal of Basic and Clinical Pathophysiology, 3(2), 37-42. doi: 10.22070/jbcp.2015.230
MLA
Gholamali Naderi; Rasul Moukhah; Ali Yousefi. "In Vitro Evaluation of Inhibitory Effect of Artemisinin and Dihydroartemisinin on Calcineurin Enzyme". Journal of Basic and Clinical Pathophysiology, 3, 2, 2015, 37-42. doi: 10.22070/jbcp.2015.230
HARVARD
Naderi, G., Moukhah, R., Yousefi, A. (2015). 'In Vitro Evaluation of Inhibitory Effect of Artemisinin and Dihydroartemisinin on Calcineurin Enzyme', Journal of Basic and Clinical Pathophysiology, 3(2), pp. 37-42. doi: 10.22070/jbcp.2015.230
VANCOUVER
Naderi, G., Moukhah, R., Yousefi, A. In Vitro Evaluation of Inhibitory Effect of Artemisinin and Dihydroartemisinin on Calcineurin Enzyme. Journal of Basic and Clinical Pathophysiology, 2015; 3(2): 37-42. doi: 10.22070/jbcp.2015.230
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