Potent inhibition of human neutrophil activations by bractelactone, A novel chalcone from Fissistigma bracteolatum

Yang Chang Wu, Munisamy Sureshbabu, Yao Ching Fang, Yi Hsiu Wu, Yu Hsuan Lan, Fang Rong Chang, Ya Wen Chang, Tsong Long Hwang

研究成果: 雜誌貢獻文章同行評審

21 引文 斯高帕斯(Scopus)


Fissistigma bracteolatum is widely used in traditional medicine to treat inflammatory diseases. However, its active components and mechanisms of action remain unclear. In this study, (3Z)-6,7-dihydroxy-4-methoxy-3-(phenylmethylidene)-5-(3-phenylpropanoyl)-1-benzofuran-2(3H) (bractelactone), a novel chalcone from F. bracteolatum, showed potent inhibitory effects against superoxide anion (O2 -) production, elastase release, and CD11b expression in formyl-l-methionyl-l-leucyl-l-phenylalanine (FMLP)-induced human neutrophils. However, bractelactone showed only weak inhibition of phorbol myristate acetate-caused O2 - production. The peak cytosolic calcium concentration ([Ca2+]i) was unaltered by bractelactone in FMLP-induced neutrophils, but the decay time of [Ca2+]i was significantly shortened. In a calcium-free solution, changes in [Ca2+]i caused by the addition of extracellular Ca2+ were inhibited by bractelactone in FMLP-activated cells. In addition, bractelactone did not alter the phosphorylation of p38 MAPK, ERK, JNK, or AKT or the concentration of cAMP. These results suggest that bractelactone selectively inhibits store-operated calcium entry (SOCE). In agreement with this concept, bractelactone suppressed sustained [Ca2+]i changes in thapsigargin-activated neutrophils. Furthermore, bractelactone did not alter FMLP-induced formation of inositol 1,4,5-triphosphate. Taken together, our results demonstrate that the anti-inflammatory effects of bractelactone, an active ingredient of F. bracteolatum, in human neutrophils are through the selective inhibition of SOCE.
頁(從 - 到)399-407
期刊Toxicology and Applied Pharmacology
出版狀態已發佈 - 2月 1 2013


  • Bractelactone
  • Calcium
  • Elastase
  • Fissistigma bracteolatum
  • Neutrophils
  • Superoxide anion

ASJC Scopus subject areas

  • 藥理
  • 毒理學


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