化学
圆二色性
立体化学
丁烯内酯
IC50型
乙酰胆碱酯酶
脂肪酶
酶
吲哚试验
对接(动物)
吲哚生物碱
生物碱
体外
生物化学
医学
护理部
作者
Yiwei Hu,Wei-Hao Chen,Mengmeng Song,Xiaoyan Pang,Xinpeng Tian,Fa‐Zuo Wang,Yonghong Liu,Junfeng Wang
标识
DOI:10.1080/14786419.2021.1973460
摘要
A new indole diketopiperazine alkaloid, named penilline D (1), together with five known indole alkaloid analogues (2-5, 11), two meroterpenoids (6 and 12), and four butenolide derivatives (7-10), 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 (1-12) 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.
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