The Discovery of Actinospene, a New Polyene Macrolide with Broad Activity against Plant Fungal Pathogens and Pathogenic Yeasts
Phytopathogenic fungi infect crops, presenting a worldwide threat to agriculture. Polyene macrolides are one of the most effective antifungal agents applied in human therapy and crop protection. In this study, we found a cryptic polyene biosynthetic gene cluster in <i>Actinokineospora sphecios...
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oai:doaj.org-article:87b71c72d34243659f90b09f1bb49d012021-11-25T18:29:15ZThe Discovery of Actinospene, a New Polyene Macrolide with Broad Activity against Plant Fungal Pathogens and Pathogenic Yeasts10.3390/molecules262270201420-3049https://doaj.org/article/87b71c72d34243659f90b09f1bb49d012021-11-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/22/7020https://doaj.org/toc/1420-3049Phytopathogenic fungi infect crops, presenting a worldwide threat to agriculture. Polyene macrolides are one of the most effective antifungal agents applied in human therapy and crop protection. In this study, we found a cryptic polyene biosynthetic gene cluster in <i>Actinokineospora spheciospongiae</i> by genome mining. Then, this gene cluster was activated via varying fermentation conditions, leading to the discovery of new polyene actinospene (<b>1</b>), which was subsequently isolated and its structure determined through spectroscopic techniques including UV, HR-MS, and NMR. The absolute configuration was confirmed by comparing the calculated and experimental electronic circular dichroism (ECD) spectra. Unlike known polyene macrolides, actinospene (<b>1</b>) demonstrated more versatile post-assembling decorations including two epoxide groups and an unusual isobutenyl side chain. In bioassays, actinospene (<b>1</b>) showed a broad spectrum of antifungal activity against several plant fungal pathogens as well as pathogenic yeasts with minimum inhibitory concentrations ranging between 2 and 10 μg/mL.Ying TangCuiyang ZhangTianqi CuiPing LeiZhaohui GuoHailong WangQingshu LiuMDPI AGarticlepolyene macrolideactinospenegenome mining<i>Actinokineospora spheciospongiae</i>antifungal activitycryptic gene clusterOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 7020, p 7020 (2021) |
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polyene macrolide actinospene genome mining <i>Actinokineospora spheciospongiae</i> antifungal activity cryptic gene cluster Organic chemistry QD241-441 |
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polyene macrolide actinospene genome mining <i>Actinokineospora spheciospongiae</i> antifungal activity cryptic gene cluster Organic chemistry QD241-441 Ying Tang Cuiyang Zhang Tianqi Cui Ping Lei Zhaohui Guo Hailong Wang Qingshu Liu The Discovery of Actinospene, a New Polyene Macrolide with Broad Activity against Plant Fungal Pathogens and Pathogenic Yeasts |
description |
Phytopathogenic fungi infect crops, presenting a worldwide threat to agriculture. Polyene macrolides are one of the most effective antifungal agents applied in human therapy and crop protection. In this study, we found a cryptic polyene biosynthetic gene cluster in <i>Actinokineospora spheciospongiae</i> by genome mining. Then, this gene cluster was activated via varying fermentation conditions, leading to the discovery of new polyene actinospene (<b>1</b>), which was subsequently isolated and its structure determined through spectroscopic techniques including UV, HR-MS, and NMR. The absolute configuration was confirmed by comparing the calculated and experimental electronic circular dichroism (ECD) spectra. Unlike known polyene macrolides, actinospene (<b>1</b>) demonstrated more versatile post-assembling decorations including two epoxide groups and an unusual isobutenyl side chain. In bioassays, actinospene (<b>1</b>) showed a broad spectrum of antifungal activity against several plant fungal pathogens as well as pathogenic yeasts with minimum inhibitory concentrations ranging between 2 and 10 μg/mL. |
format |
article |
author |
Ying Tang Cuiyang Zhang Tianqi Cui Ping Lei Zhaohui Guo Hailong Wang Qingshu Liu |
author_facet |
Ying Tang Cuiyang Zhang Tianqi Cui Ping Lei Zhaohui Guo Hailong Wang Qingshu Liu |
author_sort |
Ying Tang |
title |
The Discovery of Actinospene, a New Polyene Macrolide with Broad Activity against Plant Fungal Pathogens and Pathogenic Yeasts |
title_short |
The Discovery of Actinospene, a New Polyene Macrolide with Broad Activity against Plant Fungal Pathogens and Pathogenic Yeasts |
title_full |
The Discovery of Actinospene, a New Polyene Macrolide with Broad Activity against Plant Fungal Pathogens and Pathogenic Yeasts |
title_fullStr |
The Discovery of Actinospene, a New Polyene Macrolide with Broad Activity against Plant Fungal Pathogens and Pathogenic Yeasts |
title_full_unstemmed |
The Discovery of Actinospene, a New Polyene Macrolide with Broad Activity against Plant Fungal Pathogens and Pathogenic Yeasts |
title_sort |
discovery of actinospene, a new polyene macrolide with broad activity against plant fungal pathogens and pathogenic yeasts |
publisher |
MDPI AG |
publishDate |
2021 |
url |
https://doaj.org/article/87b71c72d34243659f90b09f1bb49d01 |
work_keys_str_mv |
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