Abstract
Three novel antitrypanosomal alkaloids, named spoxazomicins A-C, were isolated by silica gel column chromatography and HPLC from the culture broth of a new endophytic actinomycete species, Streptosporangium oxazolinicum K07-0460(T). The structures of the spoxazomicins were elucidated by NMR and X-ray crystal analyses and shown to be new types of pyochelin family antibiotic. Spoxazomicin A showed potent and selective antitrypanosomal activity with an IC₅₀ value of 0.11 μg ml⁻¹ in vitro without cytotoxicity against MRC-5 cells (IC₅₀=27.8 μg ml⁻¹).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Actinobacteria / metabolism*
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Alkaloids / chemistry
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Alkaloids / isolation & purification
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Alkaloids / pharmacology*
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Cell Line
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Chromatography / methods
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Chromatography, High Pressure Liquid / methods
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Humans
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Inhibitory Concentration 50
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Oxazoles / chemistry
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Oxazoles / isolation & purification
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Oxazoles / pharmacology*
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Phenols / chemistry
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Phenols / isolation & purification
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Phenols / pharmacology*
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Silica Gel
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Thiazoles / chemistry
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Thiazoles / isolation & purification
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Thiazoles / pharmacology*
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Trypanocidal Agents / chemistry
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Trypanocidal Agents / isolation & purification
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Trypanocidal Agents / pharmacology*
Substances
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Alkaloids
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Oxazoles
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Phenols
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Thiazoles
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Trypanocidal Agents
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spoxazomicin A
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spoxazomicin B
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spoxazomicin C
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Silica Gel
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pyochelin