title: The inhibitory effect of piperine from Fructus piperis extract on the degranulation of RBL-2H3 cells.
abstract: Allergy is an abnormal immune response to an allergen. Type I hypersensitivity is an immunoglobulin (Ig) E-mediated allergic disorder. Fructus piperis is derived from the ripe fruit of the pepper, which is widely used as a spice in human diets and is also administered as a medicine in many countries. Piperine has been shown to have anti-oxidant, anti-depressant, anti-tumor, and anti-inflammatory activities. However, the effect of piperine on IgE-mediated allergic responses has not been reported. Here, the rat basophilic leukemia cells by membrane chromatography (RBL-2H3/CMC) coupled to high performance liquid chromatography/mass spectrometry (HPLC/MS) to discover and identify piperine can bind to RBL-2H3 cell membranes. Piperine inhibited the expression of cytokines, and the release of both β-hexosaminidase and histamine, which could be stimulated by antigen in RBL-2H3 mast cells. We found that the levels of intracellular Ca(2+) also decreased. Furthermore, RT-PCR showed that the mRNA expression levels of IL-4, IL-13, and TNF-α were significantly suppressed by piperine. The inhibitory effect of piperine on IgE-mediated degranulation and cytokine production by RBL-2H3 cells may be caused by the inhibition of IgE-mediated signaling pathways, including the phosphorylation of Lyn, p38, Erk, and Ras. In summary, piperine can inhibit antigen-induced allergic reactions that control degranulation.
authors.affiliation: School of Pharmacy, Heath Science Center Xi'an Jiaotong University, 76#, Yanta Westroad, Xi'an 710061, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Huang
authors.affiliation: School of Pharmacy, Heath Science Center Xi'an Jiaotong University, 76#, Yanta Westroad, Xi'an 710061, China.
authors.forename: Tao
authors.initials: T
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Heath Science Center Xi'an Jiaotong University, 76#, Yanta Westroad, Xi'an 710061, China.
authors.forename: Shengli
authors.initials: S
authors.lastname: Han
authors.affiliation: School of Pharmacy, Heath Science Center Xi'an Jiaotong University, 76#, Yanta Westroad, Xi'an 710061, China.
authors.forename: Jingjing
authors.initials: J
authors.lastname: Cao
authors.affiliation: Institute of Pharmaceutical Analysis and Drug Screening, Hubei University of Medicine, Hubei, Shiyan, 442008, China.
authors.forename: Qinhua
authors.initials: Q
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Heath Science Center Xi'an Jiaotong University, 76#, Yanta Westroad, Xi'an 710061, China. Electronic address: wangsicen@gmail.com.
authors.forename: Sicen
authors.initials: S
authors.lastname: Wang
mesh_terms: D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D052117:Benzodioxoles / Q000494:pharmacology*; D002118:Calcium / Q000378:metabolism; D015550:Cell Degranulation; D045744:Cell Line, Tumor; D016207:Cytokines / Q000378:metabolism; D006632:Histamine / Q000378:metabolism; D006967:Hypersensitivity / Q000188:drug therapy; D007073:Immunoglobulin E / Q000378:metabolism; D008407:Mast Cells / Q000187:drug effects*; D029222:Piper nigrum / Q000737:chemistry*; D010880:Piperidines / Q000494:pharmacology*; D010936:Plant Extracts / Q000494:pharmacology*; D053284:Polyunsaturated Alkamides / Q000494:pharmacology*; D051381:Rats; D015398:Signal Transduction / Q000187:drug effects; D001619:beta-N-Acetylhexosaminidases / Q000378:metabolism
chemical_list: D000470:Alkaloids; D052117:Benzodioxoles; D016207:Cytokines; D010880:Piperidines; D010936:Plant Extracts; D053284:Polyunsaturated Alkamides; D007073:Immunoglobulin E; D006632:Histamine; D001619:beta-N-Acetylhexosaminidases; D002118:Calcium; C008922:piperine
keywords: Degranulation; Histamine; Piperine; Rat basophilic leukemia cell; β-Hexosaminidase