Bioprospection of Cytotoxic Compounds in Fungal Strains Recovered from Sediments of the Brazilian Coast

The cytotoxic activities of extracts (50 μg/ml) from 48 fungal strains, recovered from sediments of Pecém's offshore port terminal (Northeast coast of Brazil), against HCT‐116 colon cancer cell lines were investigated. The most promising extract was obtained from strain BRF082, identified as Di...

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Published in:Chemistry & biodiversity 2015-03, Vol.12 (3), p.432-442
Main Authors: Rodrigues, Bárbara S. F., Sahm, Bianca D. B., Jimenez, Paula C., Pinto, Francisco C. L., Mafezoli, Jair, Mattos, Marcos C., Rodrigues-Filho, Edson, Pfenning, Ludwig H., Abreu, Lucas M., Costa-Lotufo, Letícia V., Oliveira, Maria C. F.
Format: Article
Language:English
Subjects:
acetyl
Antineoplastic Agents - chemistry
Antineoplastic Agents - isolation & purification
Antineoplastic Agents - pharmacology
Biological Products - chemistry
Biological Products - isolation & purification
Biological Products - pharmacology
Brazil
Colonic Neoplasms - drug therapy
Cytotoxic activity
Dichotomomyces cejpii
Fiscalin B
Fungi
Fungi - chemistry
Fungi - genetics
Geologic Sediments - microbiology
Gliotoxin
Gliotoxin - analogs & derivatives
Gliotoxin - chemistry
Gliotoxin - isolation & purification
Gliotoxin - pharmacology
Gliotoxin G
Gliotoxin G, acetyl
HCT116 Cells
Humans
Indoles - chemistry
Indoles - isolation & purification
Indoles - pharmacology
Phylogeny
Quinazolines - chemistry
Quinazolines - isolation & purification
Quinazolines - pharmacology
Solanum tuberosum
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Summary:The cytotoxic activities of extracts (50 μg/ml) from 48 fungal strains, recovered from sediments of Pecém's offshore port terminal (Northeast coast of Brazil), against HCT‐116 colon cancer cell lines were investigated. The most promising extract was obtained from strain BRF082, identified as Dichotomomyces cejpii by phylogenetic analyses of partial RPB2 gene sequence. Thus, it was selected for bioassay‐guided isolation of the cytotoxic compounds. Large‐scale fermentation of BRF082 in potato dextrose broth, followed by chromatographic purification of the bioactive fractions from the liquid medium, yielded gliotoxin (4) and its derivatives acetylgliotoxin G (3), bis(dethio)bis(methylsulfanyl)gliotoxin (1), acetylgliotoxin (5), 6‐acetylbis(dethio)bis(methylsulfanyl)gliotoxin (2), besides the quinazolinone alkaloid fiscalin B. All isolated compounds were tested for their cytotoxicities against the tumor cell lines HCT‐116, revealing 4 and 3 as the most cytotoxic ones (IC50 0.41 and 1.06 μg/ml, resp.).
ISSN:1612-1872
1612-1880
DOI:10.1002/cbdv.201400193