The effects of discodermin A, an antimicrobial peptide extracted from sea sponge Discodermia kiiensis, on cell membranes were investigated using vascular smooth muscle cells and erythrocytes. At lower concentrations (0.1 - 3 μM), discodermin A increased muscle tension with an increase in intracellular free Ca2+ concentration ([Ca2+](i)) indicated by the fluorescence of Ca2+ indicator, fura-PE3, in rat aortic smooth muscle. On the other hand, the higher concentration of discodermin A (10 - 30 μM) accelerated the leakage of loaded fura-PE3 from cells. In rabbit mesenteric artery treaded with discodermin A, addition of micromolar concentration of Ca2+ evoked contraction in the presence of ATP, suggesting that permeability of the membrane to Ca2+ and ATP is increased by discodermin A. Confocal fluorescence microscopy showed that discodermin A permeabilized the plasma membrane of A10 cells to fluorescent agents EthD-1 and the intracellular esterase coupled with another fluorescent agent calcein. Discodermin A also showed a hemolytic effect on rabbit erythrocytes, suggesting that discodermin A permitted transmembrane passage of hemoglobin. These results suggest that discodermin A form pores of different sizes on the cytoplasm membrane in concentration- and time-dependent manners. Discodermin A may be a saponin-like bioactive peptide.
CITATION STYLE
Sato, K., Horibe, K., Saito-Mitsui, M., Hori, M., Matsunaga, S., Fusetani, N., … Karaki, H. (1997). Effect of discodermin A, an antimicrobial peptide, on the cytoplasm membrane. Folia Pharmacologica Japonica, 110(SUPPL. 1). https://doi.org/10.1254/fpj.110.supplement_199
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