Tropical Journal of Pharmaceutical Research

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Original Research Article

Evaluation of Apoptotic and Growth Inhibitory Activity of Phloretin in BGC823 Gastric Cancer Cell

Mingqian Lu^1,2,3, Qingzhi Kong^1,4*, Xinhua Xu^2,3, Hongda Lu⁴, Zhongxin Lu⁴, Wei Yu^2,3, Bin Zuo^2,3, Jin Su^2,3 and Rong Guo^2,3

¹Hubei University of Chinese Medicine, Wuhan 430061, ²Institute of Oncology, China Three Gorges University, ³Oncology Department, Yichang Central Hospital,Yichang 443000, ⁴Wuhan Central Hospital & Wuhan Institute of Oncology, Wuhan 430061, China

*For correspondence: Email: lumqyc@sina.cn; Tel: +86-0717-6486745; Fax: +86-0717-6486745

Received: 19 June 2014 Revised accepted: 8 December 2014

Tropical Journal of Pharmaceutical Research, January 2015; 14(1): 27-31

http://dx.doi.org/10.4314/tjpr.v14i1.5

Abstract

Purpose: To evaluate the in vitro anti-proliferative activity and probable mechanism of phloretin in human gastric cancer BGC823 cell lines.

Methods: Phloretin was isolated from apple tree leaves and identified by ¹H-Nuclear Magnetic Resonance (NMR), ¹³C-NMR and electrospray ionization tandem mass spectrometry (ESI-MS). The inhibitory activity of the compound in BGC823 gastric cancer cells was determined by Methylthiazolyldiphenyl-tetrazolium bromide (MTT) assay and soft agar colony formation assay while its apoptotic activity was detected by fluorescene staining and Western blotting analysis.

Results: The results show that the inhibitory activity of phloretin in BGC823 gastric cancer cells was mediated by induction of apoptosis and down-regulation of Bcl2 (B-cell lymphoma 2) expression. The anti-proliferative effects of phloretin was dose-dependent and inhibited the growth of BGC823 gastric cancer cells by 73 % at 30 μM; this effectively induced cleavage of anti-poly (ADP-ribose) polymerase (PARP) as well as downregulation of Bcl2 protein expression in BGC823 cells after 24 h treatment.

Conclusion: Phloretin is a promising preventive and therapeutic agent for gastric cancer.

Keywords: Phloretin, Gastric cancer, Apoptosis, β-Cell lymphoma 2, Anti-poly (ADP-ribose) polymerase