Arugosins G and H: prenylated polyketides from the marine-derived fungus Emericellanidulans var. acristata.
The fungus Emericella nidulans var. acristata was isolated as an endophyte from a Mediterranean green alga. Cultivation of this fungus yielded two new compounds, arugosins G (1) and H (2), together with the known metabolites 3-9. Arugosins (1-4) are benzophenone derivatives, biosynthetically related to the xanthones 5, 6, and 9. The indole alkaloid 7 displayed antitumor activity in a panel of 36 human tumor cell lines, exhibiting a mean IC(50) value of 5.5 microg/mL in an in vitro survival and proliferation assay. Furthermore, compounds 3 and 4 showed moderate antitumor activity toward individual tumor cell lines. None of compounds 1-8 exhibited any immunostimulatory activity assessed as the capacity to induce cytokines in PBMCs from healthy donors.
Kralj
Ana
A
Institute for Pharmaceutical Biology, University of Bonn, Nussallee 6, D-53115 Bonn, Germany, and Oncotest GmbH, Institute of Experimental Oncology, Am Flughafen 12-14, D-79108 Freiburg, Germany.
Kehraus
Stefan
S
Krick
Anja
A
Eguereva
Ekaterina
E
Kelter
Gerhard
G
Maurer
Martina
M
Wortmann
Andreas
A
Fiebig
Heinz-Herbert
HH
König
Gabriele M
GM
D001410:Bacillus megaterium / Q000187:drug effects; D002708:Chlorella / Q000187:drug effects; D000460:Chlorophyta; D016207:Cytokines / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D004926:Escherichia coli / Q000187:drug effects; D005658:Fungi / Q000737:chemistry*; D006575:Heterocyclic Compounds, 3-Ring / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D008386:Marine Biology; D008522:Mediterranean Sea; D010636:Phenols / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D014407:Tumor Cells, Cultured; D044004:Xanthones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology
D016207:Cytokines; D006575:Heterocyclic Compounds, 3-Ring; D010636:Phenols; D044004:Xanthones; C513374:arugosin G; C513375:arugosin H