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  • Title: Effect of E6, a novel calmodulin inhibitor, on activity of P-glycoprotein in purified primary cultured rat brain microvessel endothelial cells.
    Author: Zhu HJ, Liu GQ.
    Journal: Acta Pharmacol Sin; 2003 Nov; 24(11):1143-9. PubMed ID: 14627500.
    Abstract:
    AIM: To study the effect of E6, a novel calmodulin inhibitor, on the activity of P-glycorprotein (P-gp) in purified primary cultured rat brain microvessel endothelial cells (RBMEC). METHODS: Flow cytometry was used to purify RBMEC from other cell types. Fluorescence of P-gp substrate rhodamine123 (Rh123) in RBMEC was measured to evaluate the effect of E6 on the function of P-gp. RESULTS: Purified RBMEC was obtained after being sorted from other cell types by flow cytometry. Intracellular fluorescence of Rh123 in RBMEC increased after incubation with E6 3, 10 micromol/L or verapamil (VER) 50 micromol/L (P<0.01), respectively. After the treatment of E6 10 micromol/L, intracellular Rh123 accumulation was increased nearly to 3-fold. E6 and VER have no effect on accumulation of Rh123 in human umbilical vein endothelial cells (HUVEC), which do not express P-gp. CONCLUSION: E6 exhibited a strong inhibitory effect on the activity of P-gp in RBMEC.
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