Journal
FITOTERAPIA
Volume 110, Issue -, Pages 103-109Publisher
ELSEVIER
DOI: 10.1016/j.fitote.2016.03.004
Keywords
Scolopendra subspinipes mutilans; Isoquinoline alkaloid; Cytotoxicity; Apoptosis; Cell cycle
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Funding
- Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD)
- State Key Laboratory of Natural Medicines, China Pharmaceutical University [3010040038]
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Two new isoquinoline alkaloids 1-2 and seven known compounds 3-9 were isolated from the ethanol extract of centipede Scolopendra subspinipes mutilans L. Koch. The structures were elucidated by a combination of spectroscopic analyses including 1D and 2D NMR, and HRESIMS. Compounds 1-2 exhibited good cytotoxicity with IC50 values ranging from 1.19 to 31.28 mu M against six human cancer cell lines and low cytotoxicity against human normal liver L-02 cell lines, suggesting that compounds 1-2 had high specific cytotoxicity on human cancer cell lines. Further analyses showed that compounds 1-2 inhibited U87 cells proliferation by arresting cell cycle progress at G0/G1 phase and inducing apoptosis through loss of mitochondrial membrane potential (MMP), activation of caspase 9/3 and down-regulation of the Bcl-2/Bax protein ratio. The results suggest that compounds 1-2 induce apoptosis in U87 cells through the mitochondria apoptosis pathway, and they deserve further research as potential anti-glioma cancer agents. (C) 2016 Elsevier B.V. All rights reserved.
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