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Issue 71, 2018
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Synthesis and anti-glioblastoma effects of artemisinin-isothiocyanate derivatives

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Abstract

A series of novel artemisinin (ART) derivatives containing an isothiocyanate (ITC) group were synthesized. All the compounds showed more potent anti-tumor effects than those of parent dihydroartemisinin (DHA) towards glioblastoma multiforme U87 in vitro. Among them, 5b had the strongest cytotoxic activity which exerted its effects in a concentration-dependent but not time-dependent manner (IC50 7.41 μM for 24 h, 7.35 μM for 72 h). Pyknosis was observed in 5b-treated U87 cells. Multiple intrinsic apoptotic pathways were induced by 5b including the upregulation of caspase 9, the release of cytochrome c, an increase of the proapoptotic protein Bax, a decrease of the anti-apoptotic protein Bcl 2, and the activation of execution pathways by the upregulation of caspase 3. In addition to apoptosis, an autophagic mechanism was also involved in 5b-induced cytotoxicity to human GBM U87 cells by upregulating the expression of LC3-II and downregulating p62. Furthermore, 5b also significantly attenuated the migration of U87 cells. Therefore, our results suggest that 5b may be a promising molecule for the further development of a novel drug for the treatment of glioblastoma.

Graphical abstract: Synthesis and anti-glioblastoma effects of artemisinin-isothiocyanate derivatives

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Publication details

The article was received on 02 Oct 2018, accepted on 19 Nov 2018 and first published on 07 Dec 2018


Article type: Paper
DOI: 10.1039/C8RA08162J
RSC Adv., 2018,8, 40974-40983
  • Open access: Creative Commons BY-NC license
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    Synthesis and anti-glioblastoma effects of artemisinin-isothiocyanate derivatives

    C. M. Nyein, X. Zhong, J. Lu, H. Luo, J. Wang, S. Rapposelli, M. Li, Y. Ou-yang, R. Pi and X. He, RSC Adv., 2018, 8, 40974
    DOI: 10.1039/C8RA08162J

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