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PMID: 7486919 Published · ppublish English Comparative Study Journal Article

Aerosol and parenteral pneumocandins are effective in a rat model of pulmonary aspergillosis.

Antimicrobial agents and chemotherapy ·Vol. 39 ·No. 8 ·1995-08-00 ·Pages 1784-9

Kurtz MB, Bernard EM, Edwards FF, Marrinan JA, Dropinski J, Douglas CM, Armstrong D

Abstract

The pneumocandins are semisynthetic analogs of echinocandin-like compounds that have shown efficacy in animal models of systemic candidiasis, disseminated aspergillosis, and pneumocystis pneumonia. However, the most common form of Aspergillus infection in susceptible patients is pulmonary aspergillosis, which was not directly tested in the mouse models used in the past. We have evaluated three pneumocandins, L-693,989, L-731,373, and L-733,560, in a rat model of pulmonary aspergillosis. Male Sprague-Dawley rats were treated for 2 weeks with cortisone and tetracycline and fed a low-protein diet before being inoculated via the trachea with 10(6) conidia of Aspergillus fumigatus H11-20. In the absence of drug treatment, the animals developed a progressive, rapidly fatal bronchopneumonia. All three pneumocandins at doses of 5 mg/kg (intraperitoneally [i.p.] every 12 h [q12h]) were effective in delaying mortality in this model. Survival at day 7 postinfection was 20% among controls (n = 10 for all groups), while it was 60, 80, and 90% in groups that were treated with L-693,989, L-731,373, and L-733,560, respectively. In another trial, survival at day 7 postinfection was 25% among controls (n = 8 for all groups); it was 87.5% in a group treated with amphotericin B (0.5 mg/kg i.p. q12h) and was 100% in a group treated with L-733,560 (0.625 mg/kg i.p. q12h). In a separate trial, aerosol L-693,989 administered 2 h before infection (5 mg/kg) delayed mortality. Eight of the 10 animals treated with aerosol L-693,989 survived for 7 days, whereas only 2 of 10 control animals survived. We conclude that the pneumocandins we tested were highly effective in an animal model of pulmonary aspergillosis.

MeSH Terms
Aerosols Animals Anti-Bacterial Agents/administration & dosage,pharmacology,therapeutic use Antifungal Agents/administration & dosage,pharmacology,therapeutic use Aspergillosis/drug therapy,microbiology,pathology Aspergillus fumigatus/drug effects Infusions, Parenteral Lung/pathology Lung Diseases, Fungal/drug therapy,microbiology,pathology Male Microbial Sensitivity Tests Peptides Peptides, Cyclic/administration & dosage,pharmacology,therapeutic use Rats Rats, Sprague-Dawley
Chemicals
Aerosols Anti-Bacterial Agents Antifungal Agents L 731373 L 733560 Peptides Peptides, Cyclic L 693989
Authors & Affiliations
7 authors, click to expand affiliations / ORCID
Kurtz M B
Merck Research Laboratories, Rahway, New Jersey 07065, USA.
Bernard E M
Edwards F F
Marrinan J A
Dropinski J
Douglas C M
Armstrong D
References (29)
29 references, click to expand
  1. Lysis of growing yeast-form cells of Candida albicans by echinocandin: a cytological study.
    Sabouraudia. 1981 Jun;19(2):97-110 PMID: 7020114
  2. In vitro activity of the new semi-synthetic polypeptide cilofungin (LY121019) against Aspergillus and Candida species.
    Eur J Clin Microbiol Infect Dis. 1990 Sep;9(9):697-9 PMID: 2226501
  3. In vitro and in vivo anti-Candida activity and toxicology of LY121019.
    J Antibiot (Tokyo). 1984 Sep;37(9):1054-65 PMID: 6389460
  4. L-687,781, a new member of the papulacandin family of beta-1,3-D-glucan synthesis inhibitors. I. Fermentation, isolation, and biological activity.
    J Antibiot (Tokyo). 1991 Jan;44(1):45-51 PMID: 2001985
  5. Activity of cilofungin (LY 121019), a new lipopeptide antibiotic, on the cell wall and cytoplasmic membrane of Candida albicans. Structural modifications in scanning and transmission electron microscopy.
    J Med Vet Mycol. 1990;28(6):425-36 PMID: 2093115
  6. Efficacy of cilofungin alone and in combination with amphotericin B in a murine model of disseminated aspergillosis.
    Antimicrob Agents Chemother. 1991 Jul;35(7):1329-33 PMID: 1929289
  7. Synergy between cilofungin and amphotericin B in a murine model of candidiasis.
    Antimicrob Agents Chemother. 1991 Jul;35(7):1334-7 PMID: 1929290
  8. Synthesis, stability, and biological evaluation of water-soluble prodrugs of a new echinocandin lipopeptide. Discovery of a potential clinical agent for the treatment of systemic candidiasis and Pneumocystis carinii pneumonia (PCP).
    J Med Chem. 1992 Jan;35(1):194-8 PMID: 1732529
  9. Comparison of azoles against aspergilli in vitro and in an experimental model of pulmonary aspergillosis.
    Chemotherapy. 1992;38(2):118-26 PMID: 1317280
  10. US experience with itraconazole in Aspergillus, Cryptococcus and Histoplasma infections in the immunocompromised host.
    Chemotherapy. 1992;38 Suppl 1:12-22 PMID: 1319310
  11. Pneumocandins from Zalerion arboricola. I. Discovery and isolation.
    J Antibiot (Tokyo). 1992 Dec;45(12):1853-66 PMID: 1490876
  12. Synthesis and antifungal activity of novel cationic pneumocandin B(o) derivatives.
    J Med Chem. 1994 Jan 21;37(2):222-5 PMID: 8295208
  13. Low incidence of invasive fungal infections after bone marrow transplantation in patients receiving amphotericin B inhalations during neutropenia.
    Ann Hematol. 1994 Jan;68(1):21-6 PMID: 8110874
  14. A Saccharomyces cerevisiae mutant with echinocandin-resistant 1,3-beta-D-glucan synthase.
    J Bacteriol. 1994 Sep;176(18):5686-96 PMID: 8083161
  15. Morphological effects of lipopeptides against Aspergillus fumigatus correlate with activities against (1,3)-beta-D-glucan synthase.
    Antimicrob Agents Chemother. 1994 Jul;38(7):1480-9 PMID: 7979276
  16. Increased antifungal activity of L-733,560, a water-soluble, semisynthetic pneumocandin, is due to enhanced inhibition of cell wall synthesis.
    Antimicrob Agents Chemother. 1994 Dec;38(12):2750-7 PMID: 7695257
  17. In vitro evaluation of the pneumocandin antifungal agent L-733560, a new water-soluble hybrid of L-705589 and L-731373.
    Antimicrob Agents Chemother. 1995 May;39(5):1070-6 PMID: 7625791
  18. Evaluation of water-soluble pneumocandin analogs L-733560, L-705589, and L-731373 with mouse models of disseminated aspergillosis, candidiasis, and cryptococcosis.
    Antimicrob Agents Chemother. 1995 May;39(5):1077-81 PMID: 7625792
  19. New semisynthetic pneumocandins with improved efficacies against Pneumocystis carinii in the rat.
    Antimicrob Agents Chemother. 1995 Jun;39(6):1320-3 PMID: 7574523
  20. Papulacandin B: an inhibitor of glucan synthesis in yeast spheroplasts.
    Eur J Biochem. 1979 Jul;97(2):345-51 PMID: 380990
  21. Effect of aculeacin A, a wall-active antibiotic, on synthesis of the yeast cell wall.
    Microbiol Immunol. 1985;29(7):609-23 PMID: 2935715
  22. Effect of papulacandin B on glucan synthesis in Paracoccidioides brasiliensis.
    J Med Vet Mycol. 1986 Jun;24(3):193-202 PMID: 3735029
  23. LY121019 inhibits Neurospora crassa growth and (1-3)-beta-D-glucan synthase.
    J Antibiot (Tokyo). 1988 May;41(5):697-701 PMID: 2968332
  24. Anti-Candida activity and toxicology of LY121019, a novel semisynthetic polypeptide antifungal antibiotic.
    Ann N Y Acad Sci. 1988;544:294-309 PMID: 3063174
  25. Cilofungin (LY121019) inhibits Candida albicans (1-3)-beta-D-glucan synthase activity.
    Antimicrob Agents Chemother. 1988 Dec;32(12):1901-3 PMID: 2977537
  26. Aerosol amphotericin B is effective for prophylaxis and therapy in a rat model of pulmonary aspergillosis.
    Antimicrob Agents Chemother. 1988 Nov;32(11):1676-9 PMID: 3252750
  27. Effects of cilofungin (LY121019) on carbohydrate and sterol composition of Candida albicans.
    Eur J Clin Microbiol Infect Dis. 1989 Dec;8(12):1067-70 PMID: 2695329
  28. Treatment of Pneumocystis carinii pneumonia with 1,3-beta-glucan synthesis inhibitors.
    Proc Natl Acad Sci U S A. 1990 Aug;87(15):5950-4 PMID: 2198575
  29. The effect of aculeacin A and papulacandin B on morphology and cell wall ultrastructure in Candida albicans.
    Can J Microbiol. 1984 Jun;30(6):857-63 PMID: 6386132
Article Info
Journal
Antimicrobial agents and chemotherapy
Abbr.
Antimicrob Agents Chemother
ISSN
0066-4804
Published
1995-08-00
Pages
1784-9
Language
English
Region
United States
NLM ID
0315061
PMCID
PMC162826
Subset
IM
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