In vitro antiherpetic activity of water-soluble amphotericin B methyl ester

1975 ◽  
Vol 48 (4) ◽  
pp. 391-394 ◽  
Author(s):  
N. M. Stevens ◽  
C. G. Engle ◽  
P. B. Fisher ◽  
W. Mechlinski ◽  
C. P. Schaffner
Keyword(s):  
Methyl Ester ◽  
Amphotericin B ◽  
Water Soluble ◽  
Antiherpetic Activity ◽  
Amphotericin B Methyl Ester

scholarly journals N-Methyl-N-D-fructosyl amphotericin B methyl ester (MF-AME), a novel antifungal agent of low toxicity: monomer/micelle control over selective toxicity.

2000 ◽  
Vol 47 (1) ◽  
pp. 121-131 ◽  
Author(s):  
B Cybulska ◽  
I Gadomska ◽  
J Mazerski ◽  
J G E Borowski ◽  
M Cheron ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Amphotericin B ◽  
Mammalian Cells ◽  
Spectroscopic Properties ◽  
Water Soluble ◽  
Selective Toxicity ◽  
Human Red Blood Cells ◽  
Amphotericin B Methyl Ester

Rational chemical modification of amphotericin B (AMB) led to the synthesis of sterically hindered AMB derivatives. The selected optimal compound, N-methyl-N-D-fructosyl amphotericin B methyl ester (MF-AME) retains the broad spectrum of antifungal activity of the parent antibiotic, and exhibits a two orders of magnitude lower toxicity in vivo and in vitro against mammalian cells. Comparative studies of MF-AME and AMB comprising the determination of the spectroscopic properties of monomeric and self-associated forms of the antibiotics, the investigation of the influence of self-association on toxicity to human red blood cells, and of the antibiotic-sterol interaction were performed. On the basis of the results obtained it can be assumed that the improvement of the selective toxicity of MF-AME could in part be a consequence of the diminished concentration of water soluble oligomers in aqueous medium, and the better ability to differentiate between cholesterol and ergosterol.

Synergistic Antiviral Effect in vitro of Azidothymidine and Amphotericin B Methyl Ester in Combination on HIV infection

1992 ◽  
Vol 24 (1) ◽  
pp. 35-39 ◽  
Author(s):  
John-Erik Stig Hansen ◽  
Claus Nielsen ◽  
Annette Svenningsen ◽  
Niels Witzke ◽  
Lars R. Mathiesen
Keyword(s):  
Methyl Ester ◽  
Hiv Infection ◽  
Amphotericin B ◽  
Antiviral Effect ◽  
Amphotericin B Methyl Ester

scholarly journals Comparative in vitro studies on liposomal formulations of amphotericin B and its derivative, N-methyl-N-D-fructosyl amphotericin B methyl ester (MFAME).

2002 ◽  
Vol 49 (1) ◽  
pp. 67-75 ◽  
Author(s):  
Barbara Cybulska ◽  
Karolina Kupczyk ◽  
Joanna Szlinder-Richert ◽  
Edward Borowski
Keyword(s):  
Methyl Ester ◽  
Amphotericin B ◽  
Mammalian Cells ◽  
Biological Properties ◽  
Antagonistic Effect ◽  
Molar Ratio ◽  
Selective Toxicity ◽  
Liposomal Formulations ◽  
Amphotericin B Methyl Ester

N-Methyl-N-D-fructosyl amphotericin B methyl ester (MFAME) is a semisynthetic derivative of the antifungal antibiotic amphotericin B (AMB). In contrast to the parent antibiotic, the derivative is characterised by low toxicity to mammalian cells and good solubility in water of its salts. Comparative studies on biological properties of free MFAME, AMB and their liposomal formulations were performed. To obtain liposomal forms, the antibiotics were incorporated into small unilamellar vesicles composed of dimyristoyl phosphatidylcholine (DMPC) and DMPC:cholesterol or ergosterol, 8:2 molar ratio. The effectivity of the liposomal and free forms of AMB and MFAME were compared by determination of fungistatic and fungicidal activity against Candida albicans ATCC 10261, potassium release from erythrocytes, and haemolysis. The results obtained indicate that in contrast to AMB, incorporation of MFAME into liposomes did not further improve its selective toxicity. Studies on the antagonistic effect of ergosterol and cholesterol on the antifungal activity of the antibiotics indicated that sterol interference was definitely less pronounced in the case of MFAME than in the case of AMB.

scholarly journals Comparative in vitro and in vivo evaluation of N-D-ornithyl amphotericin B methyl ester, amphotericin B methyl ester, and amphotericin B.

1987 ◽  
Vol 31 (11) ◽  
pp. 1756-1760 ◽  
Author(s):  
R M Parmegiani ◽  
D Loebenberg ◽  
B Antonacci ◽  
T Yarosh-Tomaine ◽  
R Scupp ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Amphotericin B ◽  
In Vivo Evaluation ◽  
Amphotericin B Methyl Ester

scholarly journals In vitro anti-mycoplasmal activity of amphotericin B methyl ester.

1976 ◽  
Vol 29 (6) ◽  
pp. 656-661 ◽  
Author(s):  
NEIL I. GOLDSTEIN ◽  
ARTHUR H. MCINTOSH ◽  
PAUL B. FISHER ◽  
KARL MARAMOROSCH ◽  
CARL P. SCHAFFNER
Keyword(s):  
Methyl Ester ◽  
Amphotericin B ◽  
Amphotericin B Methyl Ester

Subchronic Toxicity Studies of N-D-Ornithyl Amphotericin B Methyl Ester in Dogs and Rats

1985 ◽  
Vol 5 (4) ◽  
pp. 737-753
Author(s):  
TOBIAS MASSA ◽  
DINESH P. SINHA ◽  
JERRY D. FRANTZ ◽  
MARY E. FILIPEK ◽  
RAYMOND C. WEGLEIN ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Amphotericin B ◽  
Subchronic Toxicity ◽  
Toxicity Studies ◽  
Amphotericin B Methyl Ester
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