Secondary Metabolites from the Coral-Derived Fungus Aspergillus austwickii SCSIO41227 with Pancreatic Lipase and Neuraminidase Inhibitory Activities

Author:

Chen Ying12,He Yanchun12,Pang Xiaoyan1,Zhou Xuefeng12ORCID,Liu Yonghong12ORCID,Yang Bin12ORCID

Affiliation:

1. CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China

2. University of Chinese Academy of Sciences, 19 Yuquan Road, Beijing 100049, China

Abstract

The coral-derived fungus Aspergillus austwickii SCSIO41227 from Beibu Gulf yielded four previously uncharacterized compounds, namely asperpentenones B–E (1–4), along with twelve known compounds (5–16). Their structures were elucidated using HRESIMS and NMR (1H and 13C NMR, HSQC, HMBC), among which the stereo-structure of compounds 1–3 was determined by calculated ECD. Furthermore, compounds 1–16 were evaluated in terms of their enzyme (acetylcholinesterase (AChE), pancreatic lipase (PL), and neuraminidase (NA)) inhibitory activities. These bioassay results revealed that compounds 2 and 14 exerted noticeable NA inhibitory effects, with IC50 values of 31.28 and 73.64 μM, respectively. In addition, compound 3 exhibited a weak inhibitory effect against PL. Furthermore, these compounds showed the potential of inhibiting enzymes in silico docking analysis to demonstrate the interactions between compounds and proteins.

Funder

National Natural Science Foundation of China

Marine Economy Development Project of Guangdong Province

Guangdong Basic and Applied Basic Research Foundation

Publisher

MDPI AG

Subject

Drug Discovery,Pharmacology, Toxicology and Pharmaceutics (miscellaneous),Pharmaceutical Science

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