School of Pharmaceutical Sciences, Dalian Medical University, Dalian 116044, PR China.
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1615-8. doi: 10.1016/j.bmcl.2011.12.122. Epub 2012 Jan 4.
A series of analogues of deoxyandrographolide (1) transformed by Cunninghamella blakesleana AS 3.2004 were isolated and identified by spectral methods including 2D NMR. Among them, 3-oxo-17,19-dihydroxy-7,13-ent-labdadien-15,16-olide (9), 3-oxo-19-hydroxy-1,13-ent-labdadien-15,16-olide (16), 3-oxo-1β-hydroxy-14-deoxy-andrographolide (17) and 3-oxo-2β-hydroxy-14-deoxyandrographolide (18) are new compounds. And their structure-activity relationships (SAR) of inhibitory activity on LPS-induced NO production in RAW 264.7 macrophage cells were also discussed.
通过运用包括 2D NMR 在内的各种光谱方法，从被 Cunninghamella blakesleana AS 3.2004 转化的一系列去氧穿心莲内酯（1）类似物中分离并鉴定出了一系列化合物。其中，9）3-氧代-17,19-二羟基-7,13-表-二萜-15,16-内酯、16）3-氧代-19-羟基-1,13-表-二萜-15,16-内酯、17）3-氧代-1β-羟基-14-去氧穿心莲内酯和 18）3-氧代-2β-羟基-14-去氧穿心莲内酯均为新化合物。同时还探讨了它们对 LPS 诱导的 RAW 264.7 巨噬细胞细胞中 NO 生成的抑制活性的构效关系（SAR）。
