Goondicones I–K and Cratermycins A–D: Cultivation Profiling Enabled the Search for New Anthelmintics from an Australian Pasture Soil-Derived <i>Actinomadura</i> sp.
A detailed chemical investigation of the Australian pasture soil-derived <i>Actinomadura</i> sp. S4S-00069B10, utilizing optimized cultivation on four different solid-phase media (M1, IMA, D400, and YEME), yielded the new isoindolinone goondicones I-K (<b>1</b>-<b>3</b>) and anthra-γ-pyrone cratermycins A-D (<b>4</b>-<b>7</b>). Structures were assigned to <b>1</b>-<b>7</b> on the basis of detailed spectroscopic, ECD, and X-ray analyses as well as chemical transformations and biosynthetic considerations. The goondicones <b>1</b>-<b>3</b> are especially noteworthy in that they feature an unprecedented carbo-heterocyclic framework, with <b>1</b> and <b>2</b> undergoing a facile keto-enol-mediated equilibration to a 1:3 mixture (of C-13 epimers) that exhibits promising anthelmintic properties against the dog heartworm <i>Dirofilaria immitis</i> microfilariae (EC<sub>50</sub> 1.1 μM) and L4 larvae (EC<sub>50</sub> 1.3 μM). Notably, this activity is accompanied by measurable mammalian cytotoxicity, indicating a narrow therapeutic window. Together, these findings highlight the chemical novelty of <i>Actinomadura</i>-derived metabolites, and their value as structurally unique anthelmintics leads to further optimization.
Authors
- Taizong Wu (ORCID: https://orcid.org/0000-0002-1817-6018)
- Dana Roberts (ORCID: https://orcid.org/0000-0003-3985-7215)
- David F. Bruhn
- Robert J. Capon (ORCID: https://orcid.org/0000-0002-8341-7754)
- Erica Burkman
- Paul V. Bernhardt (ORCID: https://orcid.org/0000-0001-6839-1763)
- Jianying Han (ORCID: https://orcid.org/0000-0003-4402-6598)
- Angela A. Salim
- Yovany Moreno
Institutions
- The University of Queensland (AU)
- Ministry of Natural Resources (CN)
- Research Institute for Bioscience and Biotechnology (NP)
- Boehringer Ingelheim (United States) (US)
- Fujian Institute of Oceanography (CN)
Publication Details
- Journal
- Journal of Agricultural and Food Chemistry
- Published
- 2026-03-12
- DOI
- https://doi.org/10.1021/acs.jafc.5c17192
- Primary Topic
- Beetle Biology and Toxicology Studies
- Type
- article
- Field-Weighted Citation Impact
- 0.00