ABSTRACT
Objective:To investigate the effects of daurinsoline (DS) on L-type calcium channel Cav1.2 expressed in HEK293 cells.Methods:Cav1.2 was transferred into HEK293 cells using Lipofectamine 2000, and the effects of DS on Cav1.2 currents (ICav1.2) were analyzed by whole-cell patch clamp techniques. Results:DS at 1,3 and 10 μmol·L-1could inhibit the ICav1.2in HEK293 cells in a dose-dependent manner. The inhibitory rate was(14.68 ± 4.02) %,(32.37 ± 6.63) % and(59.63 ± 5.23) %,respectively. The inhibitory rate of DS at 3 μmol·L-1was 40 % of that of 3 μmol·L-1isradipine(a L-type calcium channel blocker). Conclusion:DS can inhibit the ICav1.2in HEK293 cells in a dose-dependent manner and the inhibition of DS is weaker than that of isradipine.
ABSTRACT
This paper reported the estimation of free calcium concentration in rabbit resting lymphocytes, and the effect of (-) Daurisoline (8701) on the cyto-plasmic free calcium concentration by using fluorescent indicator Fura -2/Am estimating technique. Results were compared with the effect of the Ca2-ionophore A23187.The results indicated that the free calcium concentration of resting lymphocytes was 109. 6nmol ? L-1, after 10-5 mol? L-1,10-4.5 mol ? L-1,and 10-4 mol ? L-1-)Daurisoline administration, the cyto-plasmic free calcium concentration increased to 178. 8%, 204. 4%and 817. 5% respectively, while same concentration A23187 only led the increase of 164. 6% , 198.4% and 327% respectively.Results suggested that ( - )Daurisoline may be a Ca2- agonist and may induce the cytotoxicity effect on lymphocytes at high concentr ation.