Sterol composition of itraconazole-resistant and
itraconazole-susceptible isolates of Aspergillus
fumigatus
Eric Dannaoui, Florence Persat, Elisabeth Borel, Marie-Antoinette Piens, and
Stéphane Picot
Abstract: Sterol composition of four clinical isolates of Aspergillus fumigatus resistant to itraconazole was determined
by gas chromatography – mass spectrometry and compared with that of four susceptible strains. For all strains, the ma-
jor sterol was ergosterol. Sterol compositions were qualitatively and quantitatively similar for the resistant and suscepti-
ble strains. These results suggest that itraconazole resistance is not related, for the strains studied, to alterations in the
ergosterol synthesis pathway.
Key words: Aspergillus fumigatus, itraconazole resistance, sterol composition.
Résumé : La composition en stérols de quatre souches d’Aspergillus fumigatus, d’origine clinique, résistantes à
l’itraconazole a été déterminée par chromatographie gazeuse couplée à la spectrométrie de masse et comparée avec
celle de quatre souches sensibles. Chez toutes les souches, le principal stérol était l’ergostérol. Les compositions en
stérols étaient qualitativement et quantitativement similaires chez les souches sensibles et chez les souches résistantes.
Ces résultats suggèrent que la résistance à l’itraconazole n’est pas liée, pour les souches étudiées, à des modifications
de la voie de synthèse de l’ergostérol.
Mots clés : Aspergillus fumigatus, résistance à l’itraconazole, composition en stérol.
710
Dannaoui et al. Introduction
The incidence of invasive infections caused by Aspergillus
spp. has risen dramatically in recent years (Denning 1998).
This partly reflects the increasing number of patients with
neutropenia resulting from cancer treatment and transplant
procedures. Invasive aspergillosis remains a life-threatening
infection, and amphotericin B and itraconazole are currently
the only two antifungal drugs available for treatment
(Georgopapadakou and Walsh 1994). Nevertheless, the over-
all success rate with either amphotericin B or itraconazole
therapy is 34% (Denning 1998). Although azole drug resis-
tance in yeasts has markedly increased in the last years
(Johnson and Warnock 1995), it is only recently that resis-
tance of Aspergillus fumigatus to itraconazole in vitro has
been reported (Chryssanthou 1997; Dannaoui et al. 1999b;
Denning et al. 1997). The in vitro detected resistance has
been confirmed in vivo in animal models for some strains
(Dannaoui et al. 1999a, 2001; Denning et al. 1997).
Itraconazole is an azole antifungal agent that prevents the
synthesis of ergosterol, the main sterol in fungi. This effect
originates from selective inhibition of the 14- α-demethylase
system (Vanden Bossche 1987). The consequences of 14- α-
demethylase inhibition are depletion of ergosterol and accu-
mulation of 14- α-methyl sterols, which cause alterations in
membrane fluidity and growth arrest. Azole resistance in
fungi can be related to different mechanisms (Vanden
Bossche et al. 1998). One of these is inactivation of sterol
C5-6 desaturase, which leads to the accumulation of inter-
mediate sterols (White et al. 1998). To determine if itra-
conazole resistance in A. fumigatus is mediated by an
alteration of the sterol C5-6 desaturase, we compared the
sterol composition of several clinical isolates of A. fumigatus
that were susceptible and resistant to itraconazole.
Materials and methods
Organisms
All strains were isolated in our laboratory. Four isolates (AF
1112, AF 1119, AF 1237, and AF 1290) were recovered from the
same patient in whom an aspergilloma with subsequent evolution
to chronic necrotizing aspergillosis was diagnosed. AF 1112 and
AF 1119 were isolated from sputum before any antifungal treat-
ment, and AF 1237 and AF 1290 were cultured after 4–5 months
of itraconazole therapy. Molecular typing has shown the common
identity of these four isolates (Dannaoui et al. 2001). AF 1412, AF
1422, and AF 1979 were cultured from three different patients with
Can. J. Microbiol. 47: 706–710 (2001) © 2001 NRC Canada
706
DOI: 10.1139/cjm-47-8-706
Received November 20, 2000. Revision received May 14,
2001. Accepted May 16, 2001. Published on the NRC
Research Press Web site at http://cjm.nrc.ca on August 2,
2001.
E. Dannaoui,
1,2
F. Persat, E. Borel, M.-A. Piens, and S.
Picot. Laboratoire de parasitologie, Mycologie médicale et
pathologie exotique, Université Claude-Bernard Lyon I, 8,
avenue Rockefeller, 69373 Lyon CEDEX, France.
1
Corresponding author (e-mail: e.dannaoui@mmb.azn.nl).
2
Present address: The Department of Medical Microbiology,
Division of Mycology, University Medical Center St.
Radboud, P.O. Box 9101, 6500 HB Nijmegen, The
Netherlands.