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

15 引文 斯高帕斯(Scopus)

摘要

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.
原文英語
頁(從 - 到)399-407
頁數9
期刊Toxicology and Applied Pharmacology
266
發行號3
DOIs
出版狀態已發佈 - 二月 1 2013
對外發佈Yes

Keywords

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

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology

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