Polayene Target Ergosterol

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Polyene target ergosterol which is main sterol component of fungal membranes. Eight AmB molecules bind eight ergosterol molecules through their hydrophobic moieties, with their hydrophilic sides forming a central channel of 70–100nm in diameter. Because of such channel, polyene leads to leakage of intracellular components such as K+ ions, hence cell lysis occur. There is still controversy between magnetic nuclear resonance data and experimentally demonstrated data on chemical property of polyenes towards binding of ergosterol [M. Baginski, 1997] [J. Milhaud 2002]. Some research suggested that polyene drugs are able to induce an oxidative stress (particularly in C. albicans [M. A. Ghannoum, 1999] [R. A. Akins, 2005] as well as their activity seems to be reduced in hypoxic conditions [P. A. Warn et al. 2004].…show more content…
For this reason, only AmB is given systemically, while nystatin and natamycin are only used locally or orally. Because of its high hydrophobicity and poor absorption through the gastrointestinal tract, AmB is the most used polyene antifungal for systemic infections. However, AmB administration is accompanied with adverse effects, mostly at the level of kidneys and
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