Discovery of a new autophagy inducer for A549 lung cancer cells

  • Bioorg Med Chem. 2019 Jul 1;27(13):2845-2856. doi: 10.1016/j.bmc.2019.05.015.
Na Li  1 GuoJing Qu  1 JingNa Xue  1 Xiao Li  1 Xuan Zhao  1 YeHao Yan  2 DongFang Gao  3 Lu Zhang  3 Peng Wang  3 Ming Zhang  3 BaoXiang Zhao  2 JunYing Miao  1 ZhaoMin Lin  4
Affiliations
  • 1. Shandong Provincial Key Laboratory of Animal Cells and Developmental Biology, School of Life Science, Shandong University, Jinan 250100, PR China.
  • 2. Institute of Organic Chemistry, School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, PR China.
  • 3. Institute of Medical Science, The Second Hospital of Shandong University, Jinan 250033, PR China.
  • 4. Institute of Medical Science, The Second Hospital of Shandong University, Jinan 250033, PR China. Electronic address: [email protected].
Abstract

Biological activities of a series of fluorescent compounds against human lung Cancer cell line A549 were investigated. The results showed that (E)-1,3,3-trimethyl-2-(4-(piperidin-1-yl)styryl)-3H-indol-1-ium iodide (8) and (E)-2-(5,5-dimethyl-3-(4-(piperazin-1-yl)styryl)cyclohex-2-en-1-ylidene) malononitrile (11) could inhibit the growth of A549 Cancer cells in a dose and time-dependent manner. Furthermore, compound 8 could trigger Autophagy and Apoptosis, but not obviously induce necrosis under the stimulatory condition. Therefore, 8 can be used as Autophagy activator to investigate the regulatory mechanism of Autophagy and may offer a new candidate for the treatment of lung Cancer.

Keywords
A549 lung cancer cells; Apoptosis; Autophagy; Small molecules; mTOR.