2-Aminoethoxydiphenyl borate reduces degranulation and release of cytokines in a rat mast cell line.
OBJECTIVE
2-aminoethoxydiphenyl borate (2-APB) has been reported to be a useful pharmacological tool in the study of calcium signaling. It is used either as a membrane-permeable inhibitor for inositol 1,4,5-trisphosphate (IP3) receptors or a store-operated calcium (Ca2+) entry (SOCE) inhibitor. The present study aimed to evaluate the effects of 2-APB on degranulation and cytokine production after antigen activation in a rat mast cell line, RBL-2H3 cells.


METHODS
Degranulation levels were analyzed by beta-hexosaminidase assay. Intracellular calcium concentrations were measured by Fluo-3 assay. The mRNA expression of interleukin-4 (IL-4) and tumor necrosis factor (TNF)-alfa were analyzed by Real-time PCR.


RESULTS
The intracellular Ca2+ levels were greatly suppressed in the absence or presence of 2 mmol/L Ca2+ in the extracellular medium when RBL-2H3 cells were pretreated with 100 micromol/L 2-APB for 15 min. The beta-hexosaminidase activity as well as the mRNA expression of IL-4 and TNF-alfa levels were significantly decreased after application of 2-APB.


CONCLUSIONS
This study indicates that the application of 2-APB may be a useful method to inhibit mast cell activation.
Clinical Department of School of Medicine, Shenzhen University, Shenzhen, China.
Ngai-Mui
NM
Ng
Shan-Ping
SP
Jiang
Wei
W
Zhang
D000818:Animals; D001896:Boron Compounds / Q000494:pharmacology*; D020013:Calcium Signaling / Q000187:drug effects*; D015550:Cell Degranulation / Q000187:drug effects*; D002478:Cells, Cultured; D016207:Cytokines / Q000096:biosynthesis*; D015847:Interleukin-4 / Q000235:genetics; D008407:Mast Cells / Q000187:drug effects* / Q000502:physiology; D012333:RNA, Messenger / Q000032:analysis; D051381:Rats; D014409:Tumor Necrosis Factor-alpha / Q000235:genetics
D001896:Boron Compounds; D016207:Cytokines; D012333:RNA, Messenger; D014409:Tumor Necrosis Factor-alpha; D015847:Interleukin-4; C109986:2-aminoethoxydiphenyl borate