Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California at San Diego, La Jolla, 92093-0204, USA.
Bioorg Med Chem. 2010 Dec 1;18(23):8324-33. doi: 10.1016/j.bmc.2010.09.067. Epub 2010 Oct 7.
The synthesis and in vivo anti-inflammatory activity of a series of pseudopterosin analogues are presented. Synthetic tricyclic catechol aglycons with different substitution patterns were monofucosylated or -xylosylated. Anti-inflammatory activity was conserved over a wide range of structural modifications. The most active synthetic compound 33 reduced phorbol myristate acetate (PMA)-induced inflammation in the mouse ear by 72% at 50 μg/ear. This corresponds to 80% of the activity of natural pseudopterosin A.
本文介绍了一系列假单胞菌类似物的合成及体内抗炎活性。具有不同取代模式的合成三环儿茶酚糖苷配基被单岩藻糖基化或单木糖基化。抗炎活性在广泛的结构修饰范围内得以保留。最活性的合成化合物 33 在 50μg/耳时，可使 PMA 诱导的小鼠耳炎症减少 72%。这相当于天然假单胞菌素 A 的 80%。
