TY - JOUR
T1 - Amphotericin B-induced ion flux is markedly attenuated in phosphatidylglycerol membrane as evidenced by a newly devised fluorometric method
AU - Takano, Tetsuro
AU - Konoki, Keiichi
AU - Matsumori, Nobuaki
AU - Murata, Michio
N1 - Funding Information:
We are grateful to Dr. Tohru Oishi in our laboratory for discussions. This work was supported by Grants-in-Aid for Scientific Research (S) (No. 18101010), for Priority Area (A) (No. 16073211), and for Young Scientists (A) (No. 17681027) from MEXT, Japan. A research fellowship to T.T. from GCOE program, ‘Global Education and Research Center for Bio-Environmental Chemistry,’ is also acknowledged.
PY - 2009/9/1
Y1 - 2009/9/1
N2 - The effect of phospholipid head group on the membrane-permeabilizing activity of amphotericin B (AmB) was examined using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) liposomes and 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphatidylglycerol (POPG) liposomes. The activity of AmB was evaluated as K+ influx measured as pH change inside liposomes by fluorescent measurements of 2′,7′-bis(carboxyethyl)-4 or 5-carboxyfluorescein (BCECF). AmB showed prominent permeability in POPC liposomes, whereas hardly inducing ion flux in POPG membrane. POPC added to POPG liposomes as a minor constituent markedly enhanced membrane permeability, indicating the importance of a phosphonocholine group of PC for the drug's activity.
AB - The effect of phospholipid head group on the membrane-permeabilizing activity of amphotericin B (AmB) was examined using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) liposomes and 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphatidylglycerol (POPG) liposomes. The activity of AmB was evaluated as K+ influx measured as pH change inside liposomes by fluorescent measurements of 2′,7′-bis(carboxyethyl)-4 or 5-carboxyfluorescein (BCECF). AmB showed prominent permeability in POPC liposomes, whereas hardly inducing ion flux in POPG membrane. POPC added to POPG liposomes as a minor constituent markedly enhanced membrane permeability, indicating the importance of a phosphonocholine group of PC for the drug's activity.
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U2 - 10.1016/j.bmc.2009.07.036
DO - 10.1016/j.bmc.2009.07.036
M3 - Article
C2 - 19665387
AN - SCOPUS:68649121645
SN - 0968-0896
VL - 17
SP - 6301
EP - 6304
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 17
ER -