Pearce F L, Befus A D, Bienenstock J
J Allergy Clin Immunol. 1984 Jun;73(6):819-23. doi: 10.1016/0091-6749(84)90453-6.
Quercetin, a naturally occurring flavonol structurally related to the antiallergic drug disodium cromoglycate inhibits anaphylactic histamine release from MMC isolated from the small bowel LP of the rat previously infected with the nematode Nippostrongylus brasiliensis. This contrasts with our previous observation that cromoglycate is inactive in this system. The present effect is immediate and does not decrease on preincubation with the drug. The flavonoids acacetin , apigenin , chrysin , and phloretin also demonstrate significant activity but are less potent than quercetin. Catechin, flavone, morin, and taxifolin are inactive. These results resemble those previously reported for the human basophil. In contrast, all compounds with the possible exception of taxifolin demonstrate significant activity against rat PMC. Acacetin and chrysin are the most effective inhibitors and are more active than quercetin. Rutin (the glycane of quercetin) and phlorezin (the glycane of phloretin) are inactive in both systems. These results are discussed in terms of the functional heterogeneity of mast cells from different sources and identify a group of compounds other than doxantrazole (reported previously), which inhibit histamine secretion by MMC.
槲皮素是一种天然存在的黄酮醇,其结构与抗过敏药物色甘酸钠相关,它能抑制从先前感染巴西日圆线虫的大鼠小肠固有层分离出的肥大细胞释放过敏组胺。这与我们之前观察到的色甘酸钠在该系统中无活性形成对比。目前的作用是即时的,且与药物预孵育后不会减弱。黄酮类化合物刺槐素、芹菜素、白杨素和根皮素也表现出显著活性,但效力低于槲皮素。儿茶素、黄酮、桑色素和紫杉叶素无活性。这些结果与先前报道的人类嗜碱性粒细胞的结果相似。相比之下,除紫杉叶素可能例外,所有化合物对大鼠腹腔肥大细胞均表现出显著活性。刺槐素和白杨素是最有效的抑制剂,且比槲皮素更具活性。芦丁(槲皮素的糖苷)和根皮苷(根皮素的糖苷)在两个系统中均无活性。我们从不同来源肥大细胞的功能异质性方面讨论了这些结果,并确定了一组除多柔比星(先前报道)之外的化合物,它们能抑制肥大细胞分泌组胺。