Tumor Biology

, Volume 36, Issue 5, pp 3499–3509 | Cite as

The effect of benzyl isothiocyanate and its computer-aided design derivants targeting alkylglycerone phosphate synthase on the inhibition of human glioma U87MG cell line

  • Yu Zhu
  • Anmin Liu
  • Xuebin Zhang
  • Lisha Qi
  • Ling Zhang
  • Jing Xue
  • Yi Liu
  • Ping Yang
Research Article


Benzyl isothiocyanate (BITC) has been shown to have inhibitory potential for human glioma U87MG cells; however, the effect and mechanism were not fully clear. In the present study, we found that BITC could inhibit U87MG cell proliferation, adhesion, invasion, and vasculogenic mimicry (VM) formation potential and induce oxidative stress, apoptosis, and cell cycle arrest. We also found that the expression of proliferation, invasion, VM oxidative stress, apoptosis, and cell cycle-related gene and the activity of tumor-related signaling pathways, including protein kinase C (PKC) ζ and Akt/nuclear factor-kappa B (NF-κB) pathways, were suppressed by BITC treatment. We also explored the anti-tumor potential of BITC in vivo, and we found that BITC also could regulate the expression of tumor-related gene and angiogenesis in nude mice model. Finally, we optimized the BITC construction targeting alkylglycerone phosphate synthase (AGPS) by computer-aided design, and the derivants also showed anti-tumor potential in vitro.


Benzyl isothiocyanate Glioma Computer-aided design Alkylglycerone phosphate synthase 



This study was supported by the Fund of the Health Bureau of Tianjin (Grant No. 2013KY17), Tianjin Research Program of Application Foundation, and Advanced Technology (Grant No. 14JCQNJC12000).

Conflicts of interest



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Copyright information

© International Society of Oncology and BioMarkers (ISOBM) 2014

Authors and Affiliations

  1. 1.Department of Clinical LaboratoryTianjin Huan Hu Hospital, Tianjin Key Laboratory of Cerebral Vessels and Neural DegenerationTianjinPeople’s Republic of China
  2. 2.Department of Traditional Chinese MedicineGeneral Hospital of Tianjin Medical UniversityTianjinChina
  3. 3.Department of PathologyTianjin Huan Hu Hospital, Tianjin Key Laboratory of Cerebral Vessels and Neural DegenerationTianjinChina
  4. 4.Department of PathologyTianjin Medical University Cancer Institute and Hospital, The Key Laboratory of Tianjin Cancer Prevention and TreatmentTianjinChina
  5. 5.School of Public HealthTaishan Medical UniversityTai AnChina

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