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Galactomannan-amphotericin B conjugate: Synthesis and biological activity
Year:
2011
Source of publication :
Polymers for Advanced Technologies
Authors :
Sionov, Edward
;
.
Volume :
22
Co-Authors:
Farber, S., Institute of Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 91120, Israel
Ickowicz, D., Institute of Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 91120, Israel
Sionov, E., Department of Clinical Microbiology and Infectious Diseases, Hadassah-Hebrew University Medical Center, Jerusalem 91120, Israel
Kagan, S., Department of Clinical Microbiology and Infectious Diseases, Hadassah-Hebrew University Medical Center, Jerusalem 91120, Israel
Polacheck, I., Department of Clinical Microbiology and Infectious Diseases, Hadassah-Hebrew University Medical Center, Jerusalem 91120, Israel
Domb, A.J., Institute of Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 91120, Israel
Facilitators :
From page:
119
To page:
125
(
Total pages:
7
)
Abstract:
Polysaccharide conjugated amphotericin B (AmB) was synthesized by conjugation of AmB to oxidized galactomannan (GM) by reductive amination and tested for antifungal activity. AmB conjugates were investigated for their ability to inhibit Candida albicans growth. Antifungal efficiency of the synthetic AmB-GM depends on both, AmB content and duration of exposure. The most potent compound was a conjugate which contains 40% AmB with minimal inhibition concentration of 0.25 mg/l. In vitro toxicity analysis revealed that conjugates with 20, 30, and 40% w/w AmB content have no hemolytic effect and no influence on the viability of the VERO kidney cells. Furthermore, maximal tolerant dose (MTD) of the conjugate was determined in vivo and found to be 60 mg/kg (equivalent to AmB), while commercial Fungizone® demonstrated increased toxicity of 3 mg/kg on mice model. © 2010 John Wiley & Sons, Ltd.
Note:
Related Files :
amphotericin B
antifungal activity
Biological activities
fungi
Kidney cells
Mice models
Potent compounds
Toxicity
Show More
Related Content
More details
DOI :
10.1002/pat.1874
Article number:
Affiliations:
Database:
Scopus
Publication Type:
article
;
.
Language:
English
Editors' remarks:
ID:
29747
Last updated date:
02/03/2022 17:27
Creation date:
17/04/2018 00:49
Scientific Publication
Galactomannan-amphotericin B conjugate: Synthesis and biological activity
22
Farber, S., Institute of Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 91120, Israel
Ickowicz, D., Institute of Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 91120, Israel
Sionov, E., Department of Clinical Microbiology and Infectious Diseases, Hadassah-Hebrew University Medical Center, Jerusalem 91120, Israel
Kagan, S., Department of Clinical Microbiology and Infectious Diseases, Hadassah-Hebrew University Medical Center, Jerusalem 91120, Israel
Polacheck, I., Department of Clinical Microbiology and Infectious Diseases, Hadassah-Hebrew University Medical Center, Jerusalem 91120, Israel
Domb, A.J., Institute of Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem 91120, Israel
Galactomannan-amphotericin B conjugate: Synthesis and biological activity
Polysaccharide conjugated amphotericin B (AmB) was synthesized by conjugation of AmB to oxidized galactomannan (GM) by reductive amination and tested for antifungal activity. AmB conjugates were investigated for their ability to inhibit Candida albicans growth. Antifungal efficiency of the synthetic AmB-GM depends on both, AmB content and duration of exposure. The most potent compound was a conjugate which contains 40% AmB with minimal inhibition concentration of 0.25 mg/l. In vitro toxicity analysis revealed that conjugates with 20, 30, and 40% w/w AmB content have no hemolytic effect and no influence on the viability of the VERO kidney cells. Furthermore, maximal tolerant dose (MTD) of the conjugate was determined in vivo and found to be 60 mg/kg (equivalent to AmB), while commercial Fungizone® demonstrated increased toxicity of 3 mg/kg on mice model. © 2010 John Wiley & Sons, Ltd.
Scientific Publication
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