In situ screening of 3-arylcoumarin derivatives reveals new inhibitors of mast cell degranulation
In situ screening of 3-arylcoumarin derivatives reveals new inhibitors of mast cell degranulation
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3-芳基香豆素衍生物的原位筛选揭示了肥大细胞脱粒的新抑制剂
DOI：
10.1007/s12272-013-0084-8
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发表时间：
2013
影响因子：
6.7
通讯作者：
Rose Mary Zumstein Georgetto Naal
中科院分区：
文献类型：
--
作者：
Marcela de Souza Santos;Maria Perpétua Freire de Morais Del Lama;L. Deliberto;Flávio Silva Emery;Mônica Tallarico Pupo;Rose Mary Zumstein Georgetto Naal
由于过敏性疾病的严重性和高患病率，人们对开发这种疾病的抑制剂越来越感兴趣。3-芳基香豆素衍生物作为治疗过敏性疾病的有希望的化合物出现，特别是由于它们与黄酮类化合物的结构相似，黄酮类化合物的抗过敏活性已被广泛报道。这项工作的目的是进行筛选的一组3-芳基香豆素作为潜在的抑制剂肥大细胞脱粒，过敏反应的发展的关键事件。为此目的，利用了基于肥大细胞的生物传感器模型，其体外测定允许以高通量方式进行这种筛选，并且还允许引起注意对其生物活性重要的一些香豆素结构特征。肥大细胞为基础的生物传感器被证明区分，具有高灵敏度和再现性，香豆素之间不影响或引起不同程度的抑制脱粒。在活性香豆素类化合物中，除了邻苯二酚、氨基和噻吩外，还存在一些取代基，如3-苯基香豆素的6位和2′位的羟基化。综上所述，3-芳基香豆素类化合物可作为开发新型抗过敏药物的潜在候选物。
Due to the severity and high prevalence of allergic diseases, there is growing interest in the development of inhibitors of such conditions. 3-Arylcoumarin derivatives emerge as promising compounds for the treatment of allergic disorders, in particular due to their close structural similarity to flavonoids, whose anti-allergic activity has been extensively reported. The aim of this work was to perform a screening of a set of 3-arylcoumarins as potential inhibitors of mast cell degranulation, a key event for the development of allergic reactions. For that purpose, it was utilized a biosensor model based on mast cells, whose in vitro assay allows for such screening, in a high throughput fashion, and also permits bringing to attention some coumarin structural features that are important for their biological activity. The mast cell-based biosensor was shown to discriminate, with high sensitivity and reproducibility, between coumarins that did not affect or caused different degrees of inhibition of degranulation. Among active coumarins, some substituents could be accounted for their inhibitory activity, such as the hydroxylation of positions 6 and 2′ of 3-phenylcoumarins, in addition to catechol, amino and thiophene moieties. In summary, 3-arylcoumarins could be suggested as potential candidates for the development of new anti-allergic drugs.
影响因子：
12.6
作者：
Curtis, Theresa;Naal, Rose Mary Z. G.;Holowka, David
通讯作者：
Holowka, David