New inhibitors for expression of IgE receptor on human mast cell.

Bioorganic & medicinal chemistry letters (2010-03-06)
Satoru Tamura, Kunichika Yoshihira, Katsuaki Fujiwara, Nobutoshi Murakami
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
(−)-Epigallocatechin gallate, ≥95%
Sigma-Aldrich
Apigenin, ≥95.0% (HPLC)
Sigma-Aldrich
(−)-Epicatechin, ≥90% (HPLC)
Sigma-Aldrich
Luteolin, ≥98% (TLC), powder
Sigma-Aldrich
Baicalein, 98%
Sigma-Aldrich
(−)-Epicatechin gallate, ≥98% (HPLC), from green tea
Sigma-Aldrich
(−)-Epigallocatechin gallate, ≥80% (HPLC), from green tea
Sigma-Aldrich
(−)-Epicatechin, ≥98% (HPLC), from green tea
Supelco
(−)-Epicatechin, analytical standard
Sigma-Aldrich
(−)-Gallocatechin gallate, from green tea, ≥98% (HPLC)