Abstract
Two undescribed cytochalasins, emeriglobosins A (1) and B (2), together with nine previously reported analogues (3–11) and two known tetramic acid derivatives (12, 13) were isolated from the solid culture of Emericellopsis sp. SCSIO41202. Their structures, including the absolute configurations of their stereogenic carbons, were fully elucidated based on spectroscopic analysis and the calculated ECD. Some of the isolated compounds were evaluated for their cytotoxicity and enzyme inhibitory activity against acetylcholinesterase (AChE) in vitro. Among them, 8 showed potent AChE inhibitory activity, with an IC50 value of 1.31 μM, and 5 showed significant cytotoxicity against PC-3 cells, with an IC50 value of 2.32 μM.
Highlights
Due to the high salinity, strong acidity, and high organic content of ecological conditions of mangroves, there is a very high diversity of microorganisms associated with mangrove sediments [1]
The most effective treatment of Alzheimer’s disease (AD) relies on three cholinesterase inhibitors and memantine, which can affect the glutamatergic system but cannot cure AD, as they only lead to a temporary slowdown in the loss of cognitive function by decreasing cholinesterase activity [8]
The results indicate that 8 showed potent AChE inhibitory activity, with an IC50 value of 1.31 μM, whereas 4–6 and 9 exhibited moderate effects, with IC50 values of 4.15, 31.68, 8.71, and 23.66 μM, respectively, when compared with the positive control tacrine (IC50 = 0.02 μM)
Summary
Due to the high salinity, strong acidity, and high organic content of ecological conditions of mangroves, there is a very high diversity of microorganisms associated with mangrove sediments [1]. Multiple different fungal species from mangrove sediment isolates have been cultured separately, including more classical fungal genera such as Aspergillus [2], Penicillium [3], Lasiodiplodia [4], and Trichoderma [5]. Emericellopsis, a new and rare fugal genus, was isolated from mangrove sediments for the first time. The genus Emericellopsis (Phycreales, Ascomycota) has more than 20 species, which are famous for their production of peptaibols with antibacterial and antifungal activities [6]. The most effective treatment of AD relies on three cholinesterase inhibitors (rivastigmine, donepezil, and galantamine) and memantine, which can affect the glutamatergic system but cannot cure AD, as they only lead to a temporary slowdown in the loss of cognitive function by decreasing cholinesterase activity [8].
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