Antiparasitic Meroterpenoids Isolated from CF-080171.

Pharmaceutics

Fundación MEDINA, Centro de Excelencia en Investigación de Medicamentos Innovadores de Andalucía, Parque Tecnológico de Ciencias de la Salud, Avda. del Conocimiento 34, 18016 Granada, Spain.

Published: February 2023

is a fungal genus from which a wide range of diverse biologically active compounds have been isolated. A CF-080171 extract was identified to exhibit potent activity against 3D7 and Tulahuen whole parasites in a high-throughput screening (HTS) campaign of microbial extracts from the Fundación MEDINA's collection. Bioassay-guided isolation of the active metabolites from this extract afforded eight new meroterpenoids of varying potencies, namely, memnobotrins C-E (-), a glycosylated isobenzofuranone (), a tricyclic isobenzofuranone (), a tetracyclic benzopyrane (), a tetracyclic isobenzofuranone (), and a pentacyclic isobenzofuranone (). The structures of the isolated compounds were established by (+)-ESI-TOF high-resolution mass spectrometry and nuclear magnetic resonance spectroscopy. Compounds , and exhibited potent antiparasitic activity against 3D7 (EC 0.04-0.243 μM) and Tulahuen (EC 0.266-1.37 μM) parasites, as well as cytotoxic activity against HepG2 tumoral liver cells (EC 1.20-4.84 μM). The remaining compounds (, -) showed moderate or no activity against the above-mentioned parasites and cells.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9962372PMC
http://dx.doi.org/10.3390/pharmaceutics15020492DOI Listing

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