School of Pharmacy, College of Pharmacy, China Medical University , Taichung 40402, Taiwan.
Chinese Medicine Research and Development Center, China Medical University Hospital , Taichung 40447, Taiwan.
J Nat Prod. 2014 Aug 22;77(8):1770-83. doi: 10.1021/np500057b.
Eight new spirostanol saponins, macaosides A-H (1-8), and 10 new furostanol saponins, macaosides I-R (9-18), together with six known spirostanol compounds (19-24) were isolated from Solanum macaonense. The structures of the new compounds were determined from their spectroscopic data, and the compounds were tested for in vitro antineutrophilic inflammatory activity. It was found that both immediate inflammation responses including superoxide anion generation and elastase release were significantly inhibited by treatment with compounds 20, 21, and 24 (superoxide anion generation: IC50 7.0, 7.6, 4.0 μM; elastase release: IC50 3.7, 4.4, 1.0 μM, respectively). However, compounds 1 and 4 exhibited effects on the inhibition of elastase release only, with IC50 values of 3.2 and 4.2 μM, respectively, while 19 was active against superoxide anion generation only, with an IC50 value of 6.1 μM. Accordingly, spirostanols may be promising lead compounds for further neutrophilic inflammatory disease studies.
从茄参中分离得到了 8 个新的螺甾烷醇皂苷，即 macaosides A-H（1-8），和 10 个新的呋甾烷醇皂苷，即 macaosides I-R（9-18），以及 6 个已知的螺甾烷醇化合物（19-24）。新化合物的结构通过其光谱数据确定，并测试了它们对体外嗜中性粒细胞炎症的活性。结果发现，化合物 20、21 和 24 对即刻炎症反应（包括超氧阴离子生成和弹性蛋白酶释放）具有显著的抑制作用（超氧阴离子生成：IC50 为 7.0、7.6 和 4.0 μM；弹性蛋白酶释放：IC50 为 3.7、4.4 和 1.0 μM）。然而，化合物 1 和 4 仅对弹性蛋白酶释放的抑制有作用，IC50 值分别为 3.2 和 4.2 μM，而 19 仅对超氧阴离子生成有活性，IC50 值为 6.1 μM。因此，螺甾烷醇可能是进一步研究中性粒细胞炎症性疾病的有前途的先导化合物。
