Cytotoxicity and Phytotoxicity of Trichothecene Macrolides from Myrothecium gramminum

Abstract

¹H-NMR guided fractionation of the EtOAc extract from the culture of Myrothecium gramminum (strain no. 3.1968) led to the isolation of eight cytotoxic trichothecene macrolides (1 – 8), all being substantially inhibitory against HepG2 (human hepatocellular carcinoma) and KB (human nasopharynyeal epidermoid tumor) cell lines with IC₅₀ values ranging from 2.2 to 12.2 μg/mL. Their inactivity to or weaker action on Vero cells (IC₅₀ values > 20 μg/mL, originated from the African green monkey kidney) highlighted preliminarily the nature of the selective cytotoxicity of the fungal metabolites against the test cancer cell lines. In addition, verrucarin A (1) and roridin A (5) were found to be potent inhibitors of the radial growth of Echinochloa crusgalli with corresponding IC₅₀ values of (7.96 ± 0.31) × 10^– 6 and (9.18 ± 0.44) × 10^– 6 M, respectively, which were more potent than that of the positive control (2,4-dichlorophenoxyacetic acid) [(9.40 ± 0.04) × 10^– 5 M].

Key words

Myrothecium gramminum - Tuberculariaceae - trichothecene macrolides - cytotoxicity - phytotoxicity

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