A Novel Isaindigotone Derivative Displays Better Anti-Proliferation Activities and Induces Apoptosis in Gastric Cancer Cells

Kangjia Du, Chengjie Yang, Zhongkun Zhou, Yunhao Ma, Yanan Tian, Rentao Zhang, Hao Zhang, Xinrong Jiang, Hongmei Zhu, Huanxiang Liu, Peng Chen, Yingqian Liu

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)

Abstract

Isaindigotone is an alkaloid containing a pyrrolo-[2,1-b]quinazoline moiety conjugated with a benzylidene group and isolated from the root of Isatis indigotca Fort. However, further anticancer activities of this alkaloid and its derivatives have not been fully explored. In this work, a novel isaindigotone derivative was synthesized and three different gastric cell lines and one human epithelial gastric cell line were used to study the anti-proliferation effects of the novel isaindigotone derivative BLG26. HGC27 cells and AGS cells were used to further explore the potential mechanisms. BLG26 exhibited better anti-proliferation activities in AGS cells with a half-maximal inhibitory concentration (IC50) of 1.45 μM. BLG26 caused mitochondrial membrane potential loss and induced apoptosis in both HGC27 cells and AGS cells by suppressing mitochondrial apoptotic pathway and PI3K/AKT/mTOR axis. Acute toxicity experiment showed that LD50 (median lethal dose) of BLG26 was above 1000.0 mg/kg. This research suggested that BLG26 can be a potential candidate for the treatment of gastric cancer.

Original languageEnglish
Article number8028
JournalInternational Journal of Molecular Sciences
Volume23
Issue number14
DOIs
Publication statusPublished - Jul 2022
Externally publishedYes

Keywords

  • anti-proliferation
  • gastric cancer
  • isaindigotone
  • mitochondrial potential

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