BFPP, a phloroglucinol derivative, induces cell apoptosis in human chondrosarcoma cells through endoplasmic reticulum stress

Ju Fang Liu, Wei Hung Yang, Yi Chin Fong, Sheng Chu Kuo, Chih Shiang Chang, Chih Hsin Tang

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

Chondrosarcoma is a malignant primary bone tumor that responds poorly to both chemotherapy and radiation therapy. This study is the first to investigate the anticancer effects of the new phloroglucinol derivative (2,4-bis(2-fluorophenylacetyl)phloroglucinol; BFPP) in human chondrosarcoma cells. BFPP induced cell apoptosis in two human chondrosarcoma cell lines, JJ012 and SW1353 but not in primary chondrocytes. BFPP triggered endoplasmic reticulum (ER) stress, as indicated by changes in cytosol calcium levels, and increased glucose-regulated protein 78 (GRP78) expression, but failed to show the same effects on GRP94 expression. BFPP also increased calpain expression and activity. Transfection of cells with GRP78 or calpain siRNA reduced BFPP-mediated cell apoptosis in JJ012 cells. Importantly, animal studies have revealed a dramatic 50% reduction in tumor volume after 21 days of treatment. This study demonstrates novel anticancer activity of BFPP against human chondrosarcoma cells and in murine tumor models.

Original languageEnglish
Pages (from-to)1410-1417
Number of pages8
JournalBiochemical Pharmacology
Volume79
Issue number10
DOIs
Publication statusPublished - May 15 2010

Keywords

  • BFPP
  • Calpain
  • Chondrosarcoma
  • ER
  • GRP78

ASJC Scopus subject areas

  • Biochemistry
  • Pharmacology

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