In Vitro Evaluation of Inhibitory Effect of Artemisinin and Dihydroartemisinin on Calcineurin Enzyme | ||
| Journal of Basic and Clinical Pathophysiology | ||
| مقاله 8، دوره 3، شماره 2، تیر 2015، صفحه 37-42 اصل مقاله (371.91 K) | ||
| نوع مقاله: Research Paper | ||
| شناسه دیجیتال (DOI): 10.22070/jbcp.2015.230 | ||
| نویسندگان | ||
| Gholamali Naderi* 1؛ Rasul Moukhah2؛ Ali Yousefi3 | ||
| 1Department of Biochemistry, School of Medicine, Shahed University, Tehran, Iran | ||
| 2Department of BCG, Pasteur Institute, Tehran, Iran | ||
| 3School of Medicine, Shahed University, Tehran, Iran | ||
| چکیده | ||
| 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. | ||
| کلیدواژهها | ||
| Cyclosporine A؛ Artimisinin؛ Dihydroartimisinin؛ Calcineurin؛ Calmudulin | ||
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