Interactions of amphotericin B derivative of low toxicity with biological membrane components—the Langmuir monolayer approach

2005 ◽  
Vol 116 (1) ◽  
pp. 77-88 ◽  
Author(s):  
K. Hąc-Wydro ◽  
P. Dynarowicz-Łątka ◽  
J. Grzybowska ◽  
E. Borowski
Keyword(s):  
Amphotericin B ◽  
Biological Membrane ◽  
Langmuir Monolayer ◽  
Low Toxicity ◽  
Membrane Components

scholarly journals Pharmacokinetics of liposomal amphotericin B (Ambisome) in critically ill patients.

1997 ◽  
Vol 41 (6) ◽  
pp. 1275-1280 ◽  
Author(s):  
V Heinemann ◽  
D Bosse ◽  
U Jehn ◽  
B Kähny ◽  
K Wachholz ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Standard Dose ◽  
Drug Distribution ◽  
Parent Drug ◽  
Volume Of Distribution ◽  
Liposomal Formulation ◽  
Drug Concentrations ◽  
Amphotericin B Deoxycholate ◽  
Lower Volume ◽  
Low Toxicity

The liposomal formulation of amphotericin B (AmBisome) greatly reduces the acute and chronic side effects of the parent drug. The present study describes the pharmacokinetic characteristics of AmBisome applied to 10 patients at a dose of 2.8 to 3.0 mg/kg of body weight and compares them to the pharmacokinetics observed in 6 patients treated with amphotericin B deoxycholate at the standard dose of 1.0 mg/kg. Interpatient variabilities of amphotericin B peak concentrations (Cmax) and areas under concentration-time curves (AUC) were 8- to 10-fold greater for patients treated with AmBisome than for patients treated with amphotericin B deoxycholate. At the threefold greater dose of AmBisome, median Cmaxs were 8.4-fold higher (14.4 versus 1.7 microg/ml) and median AUCs exceeded those observed with amphotericin B deoxycholate by 9-fold. This was in part explained by a 5.7-fold lower volume of distribution (0.42 liters/kg) in AmBisome-treated patients. The elimination of amphotericin B from serum was biphasic for both formulations. However, the apparent half-life of elimination was twofold shorter for AmBisome (P = 0.03). Neither hemodialysis nor hemofiltration had a significant impact on AmBisome pharmacokinetics as analyzed in one patient. In conclusion, the liposomal formulation of amphotericin B significantly (P = 0.001) reduces the volume of drug distribution, thereby allowing for greater drug concentrations in serum. The low toxicity of AmBisome therefore cannot readily be explained by its serum pharmacokinetics.

scholarly journals N-Methyl-N-D-fructopyranosylamphotericin B Methyl Ester, New Amphotericin B Derivative of Low Toxicity.

1997 ◽  
Vol 50 (8) ◽  
pp. 709-711 ◽  
Author(s):  
JOLANTA GRZYBOWSKA ◽  
PAWEL SOWINSKI ◽  
JERZY GUMIENIAK ◽  
TERESA ZIENIAWA ◽  
EDWARD BOROWSKI
Keyword(s):  
Methyl Ester ◽  
Amphotericin B ◽  
Low Toxicity

Langmuir Monolayer Study toward Combined Antileishmanian Therapy Involving Amphotericin B and Edelfosine

2009 ◽  
Vol 113 (43) ◽  
pp. 14239-14246 ◽  
Author(s):  
Katarzyna Ha̧c-Wydro ◽  
Patrycja Dynarowicz-Ła̧tka ◽  
Radosław Żuk
Keyword(s):  
Amphotericin B ◽  
Langmuir Monolayer

Orientation and mobility of molecules in membranes studied by polarized light spectroscopy

1980 ◽  
Vol 13 (1) ◽  
pp. 63-118 ◽  
Author(s):  
Lennart B.-Å. Johansson ◽  
Göran Lindblom
Keyword(s):  
Molecular Orientation ◽  
Biological Membrane ◽  
Polarized Light ◽  
Spatial Arrangement ◽  
Chemical Processes ◽  
Orientation And Mobility ◽  
Mobility Of Molecules ◽  
Membrane Components ◽  
The Guardian ◽  
Functional Mechanisms

Biological membranes are composed of mainly lipids and proteins. The physical properties of the lipids, forming a bilayer structure, are of crucial importance for the living cell, since the plasma membrane is the guardian barrier towards the environment. Thus, the functioning cell needs a highly stable lipid bilayer, which depends on molecular packing and orientation properties of the various membrane components (Wieslander et al. 1980). The spatial arrangement of the membrane proteins incorporated in the lipid matrix plays an essential role for the different chemical processes occurring at or within the membrane. Information about molecular orientation and mobility is therefore necessary for unravelling the functional mechanisms of a biological membrane.

Lateral mobility of biological membrane components

1991 ◽  
Author(s):  
Dusan Chorvat ◽  
Peter Shvec ◽  
P. Kvasnichka ◽  
Tibor Shipocz ◽  
B. Jarkovska
Keyword(s):  
Biological Membrane ◽  
Lateral Mobility ◽  
Membrane Components

scholarly journals Comparative studies on cell stimulatory, permeabilizing and toxic effects induced in sensitive and multidrug resistant fungal strains by amphotericin B (AMB) and N-methyl-N-D-fructosyl amphotericin B methyl ester (MFAME).

2000 ◽  
Vol 47 (1) ◽  
pp. 133-140 ◽  
Author(s):  
J Szlinder-Richert ◽  
B Cybulska ◽  
J Grzybowska ◽  
E Borowski ◽  
R Prasad
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Methyl Ester ◽  
Amphotericin B ◽  
Mammalian Cells ◽  
Parent Compound ◽  
Multidrug Resistant ◽  
Solubility In Water ◽  
Good Solubility ◽  
Low Toxicity ◽  
Amphotericin B Methyl Ester

N-Methyl-N-D-fructosyl-amphotericin B methyl ester (MFAME) is a new derivative of amphotericin B, which is characterised by low toxicity to mammalian cells and good solubility in water of its salts. The antifungal activity and effects of MFAME towards Candida albicans and Saccharomyces cerevisiae multidrug resistant MDR(+) and sensitive MDR(-) strains was compared with those of parent compound. The results obtained indicate that MDR(+) S. cerevisiae was sensitive to MFAME as well as to AMB. MFAME exhibited the same effects on fungal cells studied as parent antibiotic. The two antibiotics, depending on the dose applied induced cell stimulation, K+ efflux, and/or had a toxic effect.

Interactions between amphotericin B 3-(N',N'-dimethylamino) propyl amide and cellular membrane components in Langmuir monolayers

2008 ◽  
Vol 516 (6) ◽  
pp. 1197-1203 ◽  
Author(s):  
Katarzyna Hąc-Wydro ◽  
Patrycja Dynarowicz-Łątka ◽  
Jolanta Grzybowska ◽  
Edward Borowski
Keyword(s):  
Amphotericin B ◽  
Langmuir Monolayers ◽  
Cellular Membrane ◽  
Membrane Components

scholarly journals A Highly Active Triterpene Derivative Capable of Biofilm Damage to Control Cryptococcus spp.

Biomolecules ◽  
2019 ◽  
Vol 9 (12) ◽  
pp. 831 ◽  
Author(s):  
Maria E. Krummenauer ◽  
William Lopes ◽  
Ane W. A. Garcia ◽  
Augusto Schrank ◽  
Simone C. B. Gnoatto ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Betulinic Acid ◽  
Biofilm Formation ◽  
Inhibitory Concentration ◽  
Potential Drug ◽  
Pentacyclic Triterpenoid ◽  
Highly Active ◽  
Low Toxicity ◽  
Cryptococcus Spp ◽  
Derivatives Of

Cryptococcus neoformans is an encapsulated yeast responsible for more than 180,000 deaths per year. The standard therapeutic approach against cryptococcosis is a combination of amphotericin B with flucytosine. In countries where cryptococcosis is most prevalent, 5-fluorocytosine is rarely available, and amphotericin B requires intravenous administration. C. neoformans biofilm formation is related to increased drug resistance, which is an important outcome for hospitalized patients. Here, we describe new molecules with anti-cryptococcal activity. A collection of 66 semisynthetic derivatives of ursolic acid and betulinic acid was tested against mature biofilms of C. neoformans at 25 µM. Out of these, eight derivatives including terpenes, benzazoles, flavonoids, and quinolines were able to cause damage and eradicate mature biofilms. Four terpene compounds demonstrated significative growth inhibition of C. neoformans. Our study identified a pentacyclic triterpenoid derived from betulinic acid (LAFIS13) as a potential drug for anti-cryptococcal treatment. This compound appears to be highly active with low toxicity at minimal inhibitory concentration and capable of biofilm eradication.

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