Reactivation of neferine on mice brain cholinesterase inhibited by organophosphate / 中草药

ABSTRACT

Object To study the reactivation of neferine (Nef) and pralidoxime chloride (2-PAM?Cl) on mice brain cholinestrase (ChE) inhibited by organophosphate. Methods Micro-DTNB method was used to determine the ChE activity of mice brain inhibited by DDVP in vitro and in vivo, then the inhibitory effect of DDVP (0.001-0.03 mg/L) on mice brain ChE in vitro was observed. The reactivative effect of Nef and 2-PAM?Cl on brain ChE of poisoned mice with DDVP in vivo and in vitro was compared. Results In vitro, the inhibitory effect of DDVP at different concentrations on mice brain ChE showed a concentration-effect relationship. The IC_(50) was 0.003 mg/L. The reactivative effect of Nef (2.4, 4.8 mg/L) and 2-PAM?Cl (5, 12.5 mg/L) on brain ChE inhibited by DDVP (0.02 mg/L) enhanced with increasing their concentrations. In vivo, after 30 min of treated with DDVP (10 mg/L, sc), the mice were given (ip) with Nef (15, 30 mg/kg) or 2-PAM?Cl (25, 50 mg/kg), respectively. The ChE activity rate in these two treated groups were (41.6?10.9) %, (56.5?12.4) % and (24.1?14.3) %, (28.4?11.9) %, respectively. The difference between poisoned group (sc DDVP) and Nef treated group was significant (P0.05). Conclusion The results suggest that Nef have a more remarkable reactivative effect on inhibited brain ChE in vitro and in vivo than 2-PAM?Cl. This may be contributed to that Nef can penetrate the blood-brain barrier.