Abstract
The aim of this research is to explore the biological and chemical diversity of bacteria associated with a marine flatworm Paraplanocera sp., and to discover the bioactive metabolites from culturable strains. A total of 141 strains of bacteria including 45 strains of actinomycetes and 96 strains of other bacteria were isolated, identified and fermented on a small scale. Bioactive screening (antibacterial and cytotoxic activities) and chemical screening (ultra-performance liquid chromatography–mass spectrometry (UPLC-MS)) yielded several target bacterial strains. Among these strains, the ethyl acetate (EA) crude extract of Streptomyces sp. XY-FW47 fermentation broth showed strong antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC43300 (MRSA ATCC43300) and potent cytotoxic effects on HeLa cells. The UPLC-MS spectral analysis of the crude extract indicated that the strain XY-FW47 could produce a series of geldanamycins (GMs). One new geldanamycin (GM) analog, 4,5-dihydro-17-O-demethylgeldanamycin (1), and three known GMs (2–4) were obtained. All of these compounds were tested for antibacterial, cytotoxic, and antifungal activities, yet only GM (3) showed potent cytotoxic (HeLa cells, EC50 = 1.12 μg/mL) and antifungal (Setosphaeria turcica MIC = 2.40 μg/mL) activities. Their structure–activity relationship (SAR) was also preliminarily discussed in this study.
Highlights
Flatworms are invertebrates that belong to Platyhelminthes
This study firstly explored biological and chemical diversity of bacteria associated with the marine flatworm Paraplanocera sp
There were three novel strains, suggesting that a rich biodiversity of bacteria may be associated with marine flatworms
Summary
Flatworms are invertebrates that belong to Platyhelminthes. About 4500 species of flatworms have been reported, of which over 1000 species are exclusively marine flatworms primarily belonging to Turbellaria polyclad [1]. Marine flatworms are 3–20 cm in length but some are quite small. Most marine flatworms are free-living organisms and they are found to hide under rocks or inside empty shells in the. Mar. Drugs 2017, 15, 281; doi:10.3390/md15090281 www.mdpi.com/journal/marinedrugs. Flatworms have attracted broad research interests worldwide. Several studies on the reproductive system of flatworms provided useful information for research on stem cells [2], ageing [3] and bioadhesion [4]. Recent reports showed that flatworms are suitable models for probing environmental changes, such as salinity stress [5] and oxygen concentrations variations [6]
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