Department of Chemistry and the Virginia Tech Center for Drug Discovery, M/C 0212, Virginia Tech, Blacksburg, VA 24061, USA.
Bioorg Med Chem. 2013 Dec 15;21(24):7591-4. doi: 10.1016/j.bmc.2013.10.038. Epub 2013 Nov 1.
Bioassay-directed fractionation of the leaf and root extracts of the antiproliferative Madagascar plant Stuhlmannia moavi afforded 6-acetyl-5,8-dihydroxy-2-methoxy-7-methyl-1,4-naphthoquinone (stuhlmoavin, 1) as the most active compound, with an IC50 value of 8.1 μM against the A2780 human ovarian cancer cell line, as well as the known homoisoflavonoid bonducellin (2) and the stilbenoids 3,4,5'-trihydroxy-3'-methoxy-trans-stilbene (3), piceatannol (4), resveratrol (5), rhapontigenin (6), and isorhapontigenin (7). The structure elucidation of all compounds was based on NMR and mass spectroscopic data, and the structure of 1 was confirmed by a single crystal X-ray analysis. Compounds 2-5 showed weak A2780 activities, with IC50 values of 10.6, 54.0, 41.0, and 74.0 μM, respectively. Compounds 1-3 also showed weak antimalarial activity against Plasmodium falciparum with IC50 values of 23, 26, and 27 μM, respectively.
采用生物活性导向方法，对具有抗增殖活性的马达加斯加植物 Stuhlmannia moavi 的叶和根提取物进行分离，得到了 6-乙酰基-5,8-二羟基-2-甲氧基-7-甲基-1,4-萘醌（stuhlmoavin，1），它对 A2780 人卵巢癌细胞系的抑制活性最强，IC50 值为 8.1 μM，同时还分离得到了已知的同型异黄酮 bonducellin（2）和芪类化合物 3,4,5'-三羟基-3'-甲氧基-反式-二苯乙烯（3）、piceatannol（4）、白藜芦醇（5）、rapontigenin（6）和异白藜芦醇（7）。所有化合物的结构鉴定均基于 NMR 和质谱数据，并且通过单晶 X 射线分析确定了 1 的结构。化合物 2-5 对 A2780 的活性较弱，IC50 值分别为 10.6、54.0、41.0 和 74.0 μM。化合物 1-3 对疟原虫 Plasmodium falciparum 也表现出较弱的抗疟活性，IC50 值分别为 23、26 和 27 μM。
