Abstract

The isolation and structural elucidation of a structurally new desertomycin, designated as desertomycin G (1), with strong antibiotic activity against several clinically relevant antibiotic resistant pathogens are described herein. This new natural product was obtained from cultures of the marine actinomycete Streptomyces althioticus MSM3, isolated from samples of the intertidal seaweed Ulva sp. collected in the Cantabrian Sea (Northeast Atlantic Ocean). Particularly interesting is its strong antibiotic activity against Mycobacterium tuberculosis clinical isolates, resistant to antibiotics in clinical use. To the best of our knowledge, this is the first report on a member of the desertomycin family displaying such activity. Additionally, desertomycin G shows strong antibiotic activities against other relevant Gram-positive clinical pathogens such as Corynebacterium urealyticum, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecium, Enterococcus faecalis, and Clostridium perfringens. Desertomycin G also displays moderate antibiotic activity against relevant Gram-negative clinical pathogens such as Bacteroides fragilis, Haemophilus influenzae and Neisseria meningitidis. In addition, the compound affects viability of tumor cell lines, such as human breast adenocarcinoma (MCF-7) and colon carcinoma (DLD-1), but not normal mammary fibroblasts.

Highlights

  • Desertomycins are a family of macrolide natural products of pharmacological interest due to their diverse biological activities

  • Previous research in the Cantabrian Sea (Biscay Bay, Northeast Atlantic) has revealed that bioactive Streptomyces species are sometimes associated with marine macro-algae [12,13,14]

  • Oceanic and atmospheric environments in this region [13,14,15] are emerging as novel sources for the discovery of new natural products with antibiotic properties and cytotoxic activities towards cancer cell lines [16,17,18,19,20]

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Summary

Introduction

Desertomycins are a family of macrolide natural products of pharmacological interest due to their diverse biological activities. After a report on the first member of the family, desertomycin A, with antibiotic activity against bacteria and fungi, [2], other structurally related compounds of the family such as the desertomycins B and D [3], E [4] and F [5] have been identified. They are mainly produced by Streptomyces species isolated from soils, such as Streptomyces macronensis and Streptomyces flavofungini [6], but have been found in cultures of Streptoverticillium baldaccii [7]. Oceanic and atmospheric environments in this region [13,14,15] are emerging as novel sources for the discovery of new natural products with antibiotic properties and cytotoxic activities towards cancer cell lines [16,17,18,19,20]

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