Title |
Amycolatopsins A–C: antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494
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Published in |
The Journal of Antibiotics, October 2017
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DOI | 10.1038/ja.2017.119 |
Pubmed ID | |
Authors |
Zeinab G Khalil, Angela A Salim, Daniel Vuong, Andrew Crombie, Ernest Lacey, Antje Blumenthal, Robert J Capon |
Abstract |
A southern Australian soil isolate, Amycolatopsis sp. MST-108494, was subjected to a panel of fermentation and media optimization trials, supported by analytical chemical profiling, to detect and enhance production of a rare class of secondary metabolites. Chemical fractionation of two complementary fermentations yielded three new polyketides, identified by detailed spectroscopic analysis as the glycosylated macrolactones, amycolatopsins A (1), B (2) and C (3), closely related to the ammocidins and apoptolidins. Amycolatopsins 1 and 3 selectively inhibited growth of Mycobacterium bovis (BCG) and Mycobacterium tuberculosis (H37Rv) when compared with other Gram-positive or Gram-negative bacteria, with 3 exhibiting low levels of cytotoxicity toward mammalian cells. Thus, our data reveal promising structure activity relationship correlations where the antimycobacterial properties of amycolatopsins are enhanced by hydroxylation of the 6-Me (that is, 1 and 3), whereas mammalian cytotoxicity is decreased by hydrolysis of the disaccharide moiety (that is, 3).The Journal of Antibiotics advance online publication, 25 October 2017; doi:10.1038/ja.2017.119. |
X Demographics
Geographical breakdown
Country | Count | As % |
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United Kingdom | 1 | 33% |
Germany | 1 | 33% |
Unknown | 1 | 33% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 3 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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Unknown | 41 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
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Researcher | 8 | 20% |
Student > Bachelor | 5 | 12% |
Student > Master | 5 | 12% |
Student > Ph. D. Student | 4 | 10% |
Professor > Associate Professor | 2 | 5% |
Other | 2 | 5% |
Unknown | 15 | 37% |
Readers by discipline | Count | As % |
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Agricultural and Biological Sciences | 4 | 10% |
Chemistry | 3 | 7% |
Immunology and Microbiology | 3 | 7% |
Pharmacology, Toxicology and Pharmaceutical Science | 2 | 5% |
Other | 7 | 17% |
Unknown | 14 | 34% |