New inhibitors for expression of IgE receptor on human mast cell

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2299-302. doi: 10.1016/j.bmcl.2010.01.160. Epub 2010 Feb 4.

Abstract

Exploration for inhibitors against expression of IgE receptor (Fc epsilonRI) on human mast cell, a significant trigger to acute and chronic allergic symptoms, disclosed epigallocatechin gallate (EGCG), epicatechin gallate, and gallocatechin gallate as active principles. Additionally, the anthocyanidin, delphinidin, and the flavone, tricetinidin, possessing a pyrogallol function were also revealed to suppress expression of Fc epsilonRI. Structure-activity relationship analysis among catechins, anthocyanidins, and flavones revealed the pyrogallol moiety to be crucial for biological potency. Furthermore, EGCG was clarified to reduce generation of gamma-chain subunit to suppress expression of Fc epsilonRI on human mast cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anthocyanins / chemistry
  • Anthocyanins / pharmacology*
  • Anti-Allergic Agents / chemistry
  • Anti-Allergic Agents / pharmacology*
  • Catechin / analogs & derivatives
  • Catechin / chemistry
  • Catechin / pharmacology*
  • Cell Line
  • Flavones
  • Flavonoids / chemistry
  • Flavonoids / pharmacology*
  • Gene Expression / drug effects*
  • Humans
  • Hypersensitivity / drug therapy
  • Mast Cells / drug effects*
  • Mast Cells / metabolism
  • Receptors, IgE / genetics*
  • Receptors, IgE / metabolism

Substances

  • Anthocyanins
  • Anti-Allergic Agents
  • Flavones
  • Flavonoids
  • Receptors, IgE
  • Catechin
  • epigallocatechin gallate
  • delphinidin
  • flavone