Anidulafungin|166663-25-8|安捷凯

Background

Anidulafungin （LY-303366）is a synthetic derivative of echinocandin B, used as a drug of antifungal [1].

Anidulafungin has been reported to inhibit systemic isolates of Candida species with the MIC90 values of 0.08μg/ml, 0.32μg/ml, 0.32μg/ml and 5.12μg/ml for C.albicans (n=99), C.glabrata(n=18), C.tropicalis(n=10), and C.parapsilosis (n=10), respectively. In addition, Anidulafungin has been found to be active against Aspergillus species(n=20) with the MIC90 values of ~0.02μg/ml. Apart from these, Anidulafungin has been revealed to inactively restrain with the MIC90 values of >10.24μg/ml and 16μg/ml, for C.neoformans and B.dermatitidis, respectively [1].

参考文献:
[1] Zhanel GG1, Karlowsky JA, Harding GA, Balko TV, Zelenitsky SA, Friesen M, Kabani A, Turik M, Hoban DJ. In vitro activity of a new semisynthetic echinocandin, LY-303366, against systemic isolates of Candida species, Cryptococcus neoformans, Blastomyces dermatitidis, and Aspergillus species. Antimicrob Agents Chemother. 1997 Apr;41(4):863-5.
[2]. Locke JB, et al. Characterization of In Vitro Resistance Development to the Novel Echinocandin CD101 in Candida Species. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6100-7.
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Protocol

Antifungal assay [1]:

Fungi

Aspergillus species

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

48 hrs

Applications

Anidulafungin potently inhibited Aspergillus species, with a MEC90 value of 0.02 mg/mL. The ranges of MIC and MEC of Anidulafungin against A. fumigatus, A. flavus, A. niger, A. glaucus group and A. versicolor were 0.00125 ~ 0.005 μ g/mL and 0.005 ~ 10.24 μ g/mL, respectively.

Animal experiment [2]:

Animal models

Mice infected with strains FMR 9965, FMR 8756, FMR 9960, FMR 10084 or FMR 9966 of Aspergillus flavus

Dosage form

1, 5 or 10 mg/kg; i.p.; q.d., for 7 days

Applications

In Mice infected with strains FMR 9965, FMR 8756, FMR 9960, FMR 10084 or FMR 9966 of Aspergillus flavus, Anidulafungin at the doses of 5 and 10 mg/kg significantly prolonged survival. There were no substantial difference between the doses of 5 and 10 mg/kg. Moreover, in spleens and kidneys, Anidulafungin significantly reduced the fungal load in a dose-dependent manner. According to the bioassay results, at day 5 of treatment, the Anidulafungin serum levels were beyond the corresponding minimum effective concentrations of all strains.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

参考文献:

[1]. Zhanel GG1, Karlowsky JA, Harding GA, Balko TV, Zelenitsky SA, Friesen M, Kabani A, Turik M, Hoban DJ. In vitro activity of a new semisynthetic echinocandin, LY-303366, against systemic isolates of Candida species, Cryptococcus neoformans, Blastomyces dermatitidis, and Aspergillus species. Antimicrob Agents Chemother. 1997 Apr;41(4):863-5.

[2]. Calvo E, Pastor FJ, Mayayo E, Salas V, Guarro J. In vitro activity and in vivo efficacy of anidulafungin in murine infections by Aspergillus flavus. Antimicrob Agents Chemother. 2011 Mar;55(3):1290-2.

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Anidulafungin

Anidulafungin详情

Background

Protocol

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