Spreghini Elisabetta, Maida Carmelo Massimo, Tomassetti Serena, Orlando Fiorenza, Giannini Daniele, Milici Maria Eleonora, Scalise Giorgio, Barchiesi Francesco
Istituto di Malattie Infettive e Medicina Pubblica, Università Politecnica delle Marche, Ancona, Italy.
Antimicrob Agents Chemother. 2008 Jun;52(6):1929-33. doi: 10.1128/AAC.00130-08. Epub 2008 Apr 7.
We investigated the in vitro activities of posaconazole (POS), fluconazole (FLC), amphotericin B (AMB), and caspofungin (CAS) against four clinical isolates of Candida glabrata with various susceptibilities to FLC (FLC MICs ranging from 1.0 to >64 microg/ml). POS MICs ranged from < or =0.03 to 0.5 microg/ml; AMB MICs ranged from 0.25 to 2.0 microg/ml, while CAS MICs ranged from 0.03 to 0.25 microg/ml. When FLC MICs increased, so did POS MICs, although we did not observe any isolate with a POS MIC greater than 0.5 mug/ml. Time-kill experiments showed that POS, FLC, and CAS were fungistatic against all isolates, while AMB at eight times the MIC was fungicidal against three out of four isolates of C. glabrata tested. Then, we investigated the activity of POS in an experimental model of disseminated candidiasis using three different isolates of C. glabrata: one susceptible to FLC (S; FLC MICs ranging from 1.0 to 4.0 microg/ml; POS MIC of < or =0.03 microg/ml), one susceptible in a dose-dependent manner (SDD; FLC MICs ranging from 32 to 64 microg/ml; POS MICs ranging from 0.125 to 0.25 microg/ml), and another one resistant to FLC (R; FLC MIC of >64 microg/ml; POS MIC of 0.5 microg/ml). FLC significantly reduced the kidney burden of mice infected with the S strain (P = 0.0070) but not of those infected with the S-DD and R strains. POS was significantly effective against all three isolates at reducing the kidney fungal burden with respect to the controls (P ranging from 0.0003 to 0.029). In conclusion, our data suggest that POS may be a useful option in the management of systemic infections caused by C. glabrata. Additionally, the new triazole may be a therapeutic option in those cases where an FLC-resistant isolate is found to retain a relatively low POS MIC.
我们研究了泊沙康唑(POS)、氟康唑(FLC)、两性霉素B(AMB)和卡泊芬净(CAS)对4株对FLC敏感性各异(FLC MIC范围为1.0至>64μg/ml)的光滑念珠菌临床分离株的体外活性。POS的MIC范围为≤0.03至0.5μg/ml;AMB的MIC范围为0.25至2.0μg/ml,而CAS的MIC范围为0.03至0.25μg/ml。当FLC的MIC升高时,POS的MIC也升高,不过我们未观察到任何一株POS的MIC大于0.5μg/ml。时间杀菌实验表明,POS、FLC和CAS对所有分离株均为抑菌作用,而8倍MIC的AMB对4株受试光滑念珠菌中的3株具有杀菌作用。然后,我们在播散性念珠菌病的实验模型中,使用3株不同的光滑念珠菌研究了POS的活性:1株对FLC敏感(S;FLC MIC范围为1.0至4.0μg/ml;POS MIC≤0.03μg/ml),1株呈剂量依赖性敏感(SDD;FLC MIC范围为32至64μg/ml;POS MIC范围为0.125至0.25μg/ml),另一株对FLC耐药(R;FLC MIC>64μg/ml;POS MIC为0.5μg/ml)。FLC显著降低了感染S株小鼠的肾脏菌量(P = 0.0070),但对感染SDD株和R株的小鼠无效。与对照组相比,POS对所有3株分离株均能显著降低肾脏真菌负荷(P范围为0.0003至0.029)。总之,我们的数据表明,POS可能是治疗光滑念珠菌引起的全身感染的有用选择。此外,在发现对FLC耐药的分离株对POS的MIC相对较低的情况下,这种新型三唑类药物可能是一种治疗选择。