Effects of Flavone Derivatives on Antigen-Stimulated Degranulation in RBL-2H3 Cells

被引：13

作者：

Hwang, Doseok ^{[1
]}

Park, Hye-Jin ^{[1
]}

Seo, Eun-Kyung ^{[1
]}

Oh, Joo Y. ^{[1
]}

Ji, Sang Y. ^{[2
]}

Park, Dong K. ^{[1
,3
]}

Lim, Yoongho ^{[1
]}

机构：

[1] Konkuk Univ, BMIC, Div Biosci & Biotechnol, Seoul 143701, South Korea

[2] Natl Inst Anim Sci, Rural Dev Adm, Suwon 441706, South Korea

[3] Cell Activat Res Inst, Gyeonggi Do 464870, South Korea

来源：

CHEMICAL BIOLOGY & DRUG DESIGN | 2013年 / 81卷 / 02期

关键词：

CoMFA; degranulation; flavone; in silico docking; QSAR; RBL-2H3; cells; ss-hexosaminidase; BASOPHILIC LEUKEMIA RBL-2H3; BETA-HEXOSAMINIDASE-A; MAST-CELLS; INHIBITION; INFLAMMATION; ACTIVATION; EXPRESSION; HOMOLOGY; PROTEIN; ALPHA;

D O I：

10.1111/cbdd.12067

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Mast cells are primarily responsible for IgE-mediated allergic responses. The activation level of mast cells is reflected in their degree of degranulation. This can in turn be determined by measuring the amount of beta-hexosaminidase release, a key parameter in degranulation. In this study, 40 flavone derivatives, including flavone, 14 methoxyflavones, 13 hydroxyflavones, and 12 hydroxymethoxyflavones, were evaluated for their inhibition of degranulation in rat basophilic leukemia RBL-2H3 cells. 3',7-Dihydroxyflavone inhibited degranulation (IC50 = 13.56 mu m), which was comparable to PP2 (3-(4-chlorophenyl)-1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine) used as a control. In addition, we report quantitative relationships between the structural properties of flavones and their inhibitory effects on degranulation.

引用

页码：228 / 237

页数：10

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