The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
L-671, 329, A NEW ANTIFUNGAL AGENT
III. IN VITRO ACTIVITY, TOXICITY AND EFFICACY IN COMPARISON TO ACULEACIN
ROBERT A. FROMTLINGGEORGE K. ABRUZZO
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JOURNAL FREE ACCESS

1989 Volume 42 Issue 2 Pages 174-178

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Abstract

L-671, 329 is a novel, echinocandin-like natural product that possesses potent anti-Candida activity, including activity against Candida parapsilosis. The in vitro MICs of L-671, 329 were comparable to aculeacin against 18 yeasts and three filamentous fungi in an agar dilution assay. L-671, 329 lysed mouse red blood cells (RBCs) at a concentration of 400 μg/ml, but not at 50 or 12.5 μg/ml. Aculeacin lysed RBCs at 400 and 50 μg/ml.
L-671, 329 significantly prolonged survival of mice infected with Candida albicans (ED50 3.38 mg/kg) following twice-daily intraperitoneal dosing for five consecutive days. The prolongation observed was greater than that seen with aculeacin therapy (ED50 6.44 mg/kg). No acute or chronic toxicities of L-671, 329 or aculeacin (as measured by mortality) were detected at a concentration of 100 mg/kg following intraperitoneal administration (TD50 > 100 mg/kg). Both L-671, 329 and aculeacin eradicated cells of C. albicans from the kidneys of infected mice. L-671, 329 eradicated the yeast at therapeutic concentrations of 12.5 to 100 mg/kg. Aculeacin eradicated yeast cells at therapy concentrations of 25 to 100 mg/kg. L-671, 329 has potential as an anti-Candida compound.

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© Japan Antibiotics Research Association
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