Amphotericin B-induced ion flux is markedly attenuated in phosphatidylglycerol membrane as evidenced by a newly devised fluorometric method

Tetsuro Takano; Keiichi Konoki; Nobuaki Matsumori; Michio Murata

doi:10.1016/j.bmc.2009.07.036

Amphotericin B-induced ion flux is markedly attenuated in phosphatidylglycerol membrane as evidenced by a newly devised fluorometric method

Tetsuro Takano, Keiichi Konoki, Nobuaki Matsumori, Michio Murata

Research output: Contribution to journal › Article › peer-review

9 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	6301-6304
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry
Volume	17
Issue number	17
DOIs	https://doi.org/10.1016/j.bmc.2009.07.036
Publication status	Published - 2009 Sept 1
Externally published	Yes

Keywords

Amphotericin B
Phospholipid

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmc.2009.07.036

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title = "Amphotericin B-induced ion flux is markedly attenuated in phosphatidylglycerol membrane as evidenced by a newly devised fluorometric method",

abstract = "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.",

keywords = "Amphotericin B, Phospholipid",

author = "Tetsuro Takano and Keiichi Konoki and Nobuaki Matsumori and Michio Murata",

note = "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, {\textquoteleft}Global Education and Research Center for Bio-Environmental Chemistry,{\textquoteright} is also acknowledged. ",

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doi = "10.1016/j.bmc.2009.07.036",

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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.

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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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KW - Phospholipid

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Amphotericin B-induced ion flux is markedly attenuated in phosphatidylglycerol membrane as evidenced by a newly devised fluorometric method

Abstract

Keywords

ASJC Scopus subject areas

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