1. Academic Validation
  2. The novel synthetic compound 6-acetyl-9-(3,4,5-trimetho-xybenzyl)-9H-pyrido[2,3-b]indole induces mitotic arrest and apoptosis in human COLO 205 cells

The novel synthetic compound 6-acetyl-9-(3,4,5-trimetho-xybenzyl)-9H-pyrido[2,3-b]indole induces mitotic arrest and apoptosis in human COLO 205 cells

  • Int J Oncol. 2013 Nov;43(5):1596-606. doi: 10.3892/ijo.2013.2069.
Yi-Chien Lin 1 Jui-Ying Tsai Jai-Sing Yang Yueh-Hsuan Lee Ernest Hamel Kuo-Hsiung Lee Sheng-Chu Kuo Li-Jiau Huang
Affiliations

Affiliation

  • 1 Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung 40402, Taiwan, R.O.C.
Abstract

A novel synthetic compound 6-acetyl-9-(3,4,5-trimetho-xybenzyl)-9H-pyrido[2,3-b]indole (HAC-Y6) demonstrated selective Anticancer activity. In the present study, COLO 205 cells were treated with HAC-Y6 to investigate the molecular mechanisms underlying its effects. HAC-Y6 induced growth inhibition, G2/M arrest and Apoptosis in COLO 205 cells with an IC50 of 0.52±0.035 µM. Annexin V/PI double staining demonstrated the presence of apoptotic cells. JC-1 staining analysis showed that HAC-Y6 decreased mitochondrial membrane potential in support of Apoptosis. An immunostaining assay revealed that HAC-Y6 depolymerized microtubules. Treatment of COLO 205 cells with HAC-Y6 resulted in increased expression of BubR1 and cyclin B1 and decreased expression of Aurora A, phospho-aurora A, Aurora B, phospho-aurora B and phospho-H3. HAC-Y6 treatment increased protein levels of active Caspase-3, caspase-9, Endo G, AIF, Apaf-1, cytochrome c and Bax, but treatment with the compound caused reduced levels of procaspase-3, procaspase-9, Bcl-xL and Bcl-2. Overall, our results suggest that HAC-Y6 exerts Anticancer effects by disrupting microtubule assembly and inducing G2/M arrest, polyploidy and Apoptosis via mitochondrial pathways in COLO 205 cells.

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