TY - JOUR AU - Zhang Guo-lin AU - Dai De-zai AU - Xi Tao AU - Cong Xiao-dong AU - Zhang Yun AU - Dai Yin PY - 2016 TI - Isoproterenol-induced FKBP12.6/12 downregulation is modulated by ET A and ET B receptors and reversed by argirhein, a derivative of rhein JF - Acta Pharmacologica Sinica; Vol 32, No 2 (February 2011): Acta Pharmacologica Sinica Y2 - 2016 KW - N2 - Aim: To investigate which endothelin receptors mediated isoproterenol (ISO)-induced downregulation of FKBP12.6/12 in cardiomyocytes and study whether argirhein, a novel compound containing rhein and L-arginine that has anti-inflammatory activity, could reverse the downregulation of FKBP12.6/12 induced by ISO. Methods: Neonatal rat cardiomyocytes were incubated with ISO to downregulate FKBP12.6/12. Then the cells were treated with a selective ET A blocker (PD156707) and a ET B blocker (IRL1038), a dual ET A /ET B antagonist (CPU0213), and argirhein, respectively. FKBP12.6/12 expression was assayed by RT-PCR, Western blot, and immunocytochemistry. Results: The expression of FKBP12.6 mRNA was reduced by 37.7% ( P P in vitro . FKBP12.6/12 protein expression was reduced by 47.2% ( P P Conclusion: In cardiomyocytes, the ISO induced downregulation of FKBP12.6/12 is modulated by both ET A and ET B . A new compound, argirein, reversed the down-regulation of FKBP12.6/12 expression in myocardial cells stimulated with ISO. UR - http://www.chinaphar.com/article/view/5816