酞
化学
血管舒张
立体化学
对映体
药理学
有机化学
心脏病学
医学
作者
Fei Tang,Yong‐Ming Yan,Hong-Ling Yan,Lixia Wang,C. Hu,Hongliang Wang,Hui Ao,Cheng Peng,Yuzhu Tan
标识
DOI:10.1016/j.bioorg.2020.104523
摘要
Chuanxiongdiolides R4-R6 (1–3), three novel phthalide dimers featuring two classes of unreported monomeric units (ligustilide/senkyunolide A and ligustilide/neocnidilide) with an unprecedented linkage style (3a,7′/7a,7′a), were isolated from the aerial parts of Ligusticum chuanxiong, together with three pairs of enantiomeric phthalide dimers [(−)/(+)-4a/4b, 5a/5b, and 6a/6b]. The bioassays revealed that compounds 1, 3, 4, 5, and 6 showed significant vasodilation effects, and the mechanism may be attributed to Cav1.2 activation blockade. Based on the established compounds library, the structure activity relationship of the phthalides was proposed. Our findings afford possible leads for developing new vasodilator against cardiovascular and cerebrovascular diseases such as hypertension and ischemic stroke.
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