Taylor & Francis Group
Browse
gnpl_a_1973460_sm1754.pdf (1.65 MB)

Indole diketopiperazine alkaloids and aromatic polyketides from the Antarctic fungus Penicillium sp. SCSIO 05705

Download (1.65 MB)
journal contribution
posted on 2021-09-09, 13:06 authored by Yi-Wei Hu, Wei-Hao Chen, Meng-Meng Song, Xiao-Yan Pang, Xin-Peng Tian, Fa-Zuo Wang, Yong-Hong Liu, Jun-Feng Wang

A new indole diketopiperazine alkaloid, named penilline D (1), together with five known indole alkaloid analogues (25, 11), two meroterpenoids (6 and 12), and four butenolide derivatives (710), were isolated from the Antarctic fungus Penicillium sp. SCSIO 05705. Extensive spectroscopic analysis and electronic circular dichroism (ECD) calculation were used to elucidate the structure of penilline D (1), including its absolute configuration. All isolated compounds (112) were evaluated for their cytotoxic, antibacterial and enzyme inhibitory activities against acetylcholinesterase (AChE) and pancreatic lipase (PL). Among them, compound 5 exhibited moderate in vitro cytotoxic activity against the 143B cell line with IC50 value of 12.64 ± 0.78 μM. Compound 6 showed strong inhibitory activity against AChE with IC50 value of 0.36 nM (IC50 18.7 nM for Tacrine), while compounds 6 and 11 showed weak PL enzyme inhibitory activity. Furthermore, an in silico molecular docking study was also performed between 6 and AChE.

Funding

This work was financially supported by the Finance Science and Technology Project of Hainan Province (ZDKJ202018), the Guangdong MEPP Funds (No. GDNRC [2021]48, [2020]037), Guangdong Basic and Applied Basic Research Foundation (2021A1515011523), National Natural Science Foundation of China (Nos. 41776169, 42006084, and 21772210), Key Special Project for Introduced Talents Team of Southern Marine Science and Engineering Guangdong Laboratory (Guangzhou) (GML2019ZD0406), Project from Institution of South China Sea Ecology and Environmental Engineering, CAS (NO. ISEE2018PY04).

History