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. 2022 Mar 11;27(6):1823.
doi: 10.3390/molecules27061823.

Diversified Chaetoglobosins from the Marine-Derived Fungus Emericellopsis sp. SCSIO41202

Affiliations

Diversified Chaetoglobosins from the Marine-Derived Fungus Emericellopsis sp. SCSIO41202

Surun Shao et al. Molecules. .

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.

Keywords: Emericellopsis sp.; chaetoglobosins; emeriglobosin; marine-derived fungus.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Chemical structures of compounds 113.
Figure 2
Figure 2
Selected HMBC and COSY correlations in 1 and 2.
Figure 3
Figure 3
Key NOESY correlations in 1 and 2.
Figure 4
Figure 4
The cell viability of two prostatic carcinoma cell lines, PC-3 and 22Rv1, treated with 413 at 10 µM. All experiments were performed in triplicate.
Figure 5
Figure 5
(a) IC50 values of docetaxel (positive control) against PC-3 cells. (b) IC50 values of 5 against PC-3 cells. All experiments were performed in triplicate.
Figure 6
Figure 6
Proposed binding interactions of 4 (a) and 8 (b), with the active site residues of AChE (PDB ID: 4EY7). Yellow line: hydrogen bond; tiffany blue line: π–π stacking interaction.

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