Precursor-fed cultivation of endophytic Chaetomium globosum 1C51 afforded nine novel "unnatural" halogenated chaetoglobosins including those with more preferable immunosuppressive activity.
A new sesquiterpenoid, diaporol A (1), possessing a unique tricyclic lactone framework, eight new drimane sesquiterpenoids, diaporols B-I (2-9), and the known compounds 10 and 11 were isolated from a culture of the mangrove-derived endophyte Diaporthe sp. The absolute configurations of 1-5 were determined by low-temperature (100 K) single-crystal X-ray diffraction with Cu Kα radiation. The compounds were evaluated for cytotoxic activity; however, no compound showed significant cytotoxicity against the tested cell lines at a concentration of 20 μM.
Diaporine (1), an unprecedented symmetric polyketide, was characterized from the endophytic fungus. The structure was determined by extensive spectroscopic analyses. Diaporine can inhibit significantly the differentiation of macrophages and has potential to induce conversion from the M2 to the M1 phenotype, in addition to regulation of the TLR4-MAPK signal pathway and PPARγ activity.
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