2. Academic Validation
  3. Cytotoxic Nitrogenated Azaphilones from the Deep-Sea-Derived Fungus Chaetomium globosum MP4-S01-7

Cytotoxic Nitrogenated Azaphilones from the Deep-Sea-Derived Fungus Chaetomium globosum MP4-S01-7

  • J Nat Prod. 2020 Apr 24;83(4):1157-1166. doi: 10.1021/acs.jnatprod.9b01165.
Weiyi Wang 1,  Jing Yang 2,  Yan-Yan Liao 3,  Gang Cheng 2,  Jing Chen 2,  Xiang-Dong Cheng 4,  Jiang-Jiang Qin 2 4,  Zongze Shao 1
Affiliations

Affiliations

  • 1 Key Laboratory of Marine Biogenetic Resources, Third Institute of Oceanography, Ministry of Natural Resources, 184 Daxue Road, Xiamen 361005, People's Republic of China.
  • 2 College of Pharmaceutical Sciences, Zhejiang Chinese Medical University, 548 Binwen Road, Hangzhou 310053, People's Republic of China.
  • 3 Key Laboratory of Urban Environment and Health, Institute of Urban Environment, Chinese Academy of Sciences, 1799 Jimei Road, Xiamen 361021, People's Republic of China.
  • 4 Institute of Cancer and Basic Medicine, Chinese Academy of Sciences; Cancer Hospital of the University of Chinese Academy of Sciences, Zhejiang Cancer Hospital, Banshan Road #1, Hangzhou 310022, People's Republic of China.
PMID: 32193933 DOI: 10.1021/acs.jnatprod.9b01165
Abstract

Eight new nitrogenated azaphilones (1-8) and two known compounds (chaetoviridin A and chaetoviridin E, 9, 10) were isolated from the culture of the deep-sea-derived fungus Chaetomium globosum MP4-S01-7. The absolute configurations of new compounds were elucidated by HSQC-HECADE NMR data, J-based configuration analysis, and modified Mosher's method and finally verified by comparison of recorded and computed NMR chemical shifts from quantum chemical calculations coupled with a statistical procedure (DP4+). All of the compounds were evaluated for their in vitro cytotoxicities against the gastric Cancer cell lines MGC803 and AGS, and most of them showed significant inhibition on Cancer cell viability at 10 μM. Among them, compounds 1, 2, and 5 exerted the most potent cytotoxic activities, with IC50 values less than 1 μM. Further studies showed that compound 2 inhibited cell cycle progression, and both compounds 1 and 2 induced Apoptosis of gastric Cancer cells in a concentration-dependent manner.

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