黄芩素衍生物的合成及舒张支气管活性

A novel synthesis of baicalein derivatives and their bronchodilation activity

摘要: 以黄芩苷为起始原料，利用其糖基做保护基，选择性地合成了10个具有舒张支气管平滑肌活性的黄芩素衍生物，其结构通过IR，MS和¹H NMR数据确证。初步活性结果显示，黄芩素衍生物可以抑制由KCl，乙酰胆碱和组胺所致的豚鼠平滑肌收缩，这提示黄芩素衍生物可能在治疗慢性阻塞性肺病方面有较好的应用前景。

Abstract: Ten baicalein derivatives with bronchodilation activity were selectively synthesized using baicalin as a starting material and applying its glycosyl group as a protecting group.Their structures were confirmed by IR，MS and ¹H NMR dataThe preliminary biological assay results showed that the Baicalein derivatives could inhibit contraction of tracheal smooth muscle induced by acetylcholine(Ach)，KCl and histamine(His) in guinea pigThis finding indicates a potential application of Baicalein derivatives in chronic obstructive pulmonary diseases(COPD).