TY - JOUR
T1 - In situ potentiometric method to evaluate bacterial outer membrane-permeabilizing ability of drugs
T2 - Example using antiprotozoal diamidines
AU - Ando, Makoto
AU - Kamei, Rie
AU - Komagoe, Keiko
AU - Inoue, Tsuyoshi
AU - Yamada, Keiichi
AU - Katsu, Takashi
N1 - Funding Information:
This work was supported by a Grant-in-Aid for the Scientific Research ( KAKENHI 22590036 ) from the Japan Society for the Promotion of Science .
Publisher Copyright:
© 2012 Elsevier B.V.
PY - 2012/12/1
Y1 - 2012/12/1
N2 - We introduced a new assay system, combining tyrocidine A and a K+-selective electrode, to evaluate the bacterial outer membrane-permeabilizing ability of drugs. Tyrocidine A, in the presence of an outer membrane permeabilizer, increased the permeability to K+ of the cytoplasmic membrane of Escherichia coli, because this antibiotic could markedly increase the permeability of phospholipid layers constituting the cytoplasmic membrane, while it acted weakly on the outer membrane. Hence, the novel function of agents increasing the permeability of the outer membrane could be examined directly by monitoring the tyrocidine A-induced leakage of K+ from the bacterial cytoplasm using a K+-selective electrode. We found that antiprotozoal diamidines, such as diminazene, pentamidine, and 4',6-diamidino-2-phenylindole (DAPI), can increase the permeability of the bacterial outer membrane and appropriate lipophilicity is important for diamidines to permeabilize the outer membrane.
AB - We introduced a new assay system, combining tyrocidine A and a K+-selective electrode, to evaluate the bacterial outer membrane-permeabilizing ability of drugs. Tyrocidine A, in the presence of an outer membrane permeabilizer, increased the permeability to K+ of the cytoplasmic membrane of Escherichia coli, because this antibiotic could markedly increase the permeability of phospholipid layers constituting the cytoplasmic membrane, while it acted weakly on the outer membrane. Hence, the novel function of agents increasing the permeability of the outer membrane could be examined directly by monitoring the tyrocidine A-induced leakage of K+ from the bacterial cytoplasm using a K+-selective electrode. We found that antiprotozoal diamidines, such as diminazene, pentamidine, and 4',6-diamidino-2-phenylindole (DAPI), can increase the permeability of the bacterial outer membrane and appropriate lipophilicity is important for diamidines to permeabilize the outer membrane.
KW - Bacterial outer membrane permeabilizer
KW - DAPI
KW - Diminazene
KW - K-selective electrode
KW - Pentamidine
KW - Tyrocidine A
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U2 - 10.1016/j.mimet.2012.09.033
DO - 10.1016/j.mimet.2012.09.033
M3 - Article
C2 - 23046554
AN - SCOPUS:84868250751
VL - 91
SP - 497
EP - 500
JO - Journal of Microbiological Methods
JF - Journal of Microbiological Methods
SN - 0167-7012
IS - 3
ER -