Abstract
Two new β-bergamotane sesquiterpenoids, E-β-trans-5,8,11-trihydroxybergamot-9-ene (1) and β-trans-2β,5,15-trihydroxybergamot-10-ene (2), were isolated from the marine-derived fungus Aspergillus fumigatus YK-7, along with three known terpenoids 3–5. Their structures were determined by spectroscopic methods (1D and 2D NMR, HR-ESI-MS). Antiproliferative effects on human leukemic monocyte lymphoma U937 and human prostate cancer PC-3 cell lines were measured in vitro. Compound 4 exhibited potent activity against the U937 cell line with an IC50 value of 4.2 μM.
Highlights
Microbial secondary metabolites are an important source of lead compounds for new drug development [1,2]
U937 cells were treated for 3 days, and PC-3 cells were treated for 4 days
Optical rotations were obtained on a Perkin-Elmer 241MC polarimeter (Perkin-Elmer, Waltham, MA, USA)
Summary
Microbial secondary metabolites are an important source of lead compounds for new drug development [1,2]. In our search for novel antitumor compounds from marine microorganisms, an extract of the fungus Aspergillus fumigatus YK-7, which was isolated from the sea mud of intertidal zone collected from Yingkou, China, exhibited significant activity against the U937 human leukemic monocyte lymphoma cell line (IC50 < 6.25 μg/mL) Previous investigation of this fungus had led to the isolation of fourteen 2,5-diketopiperazines [7].
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