梓叶醌类化合物及其对一氧化氮生成的抑制作用。
Naphthoquinones from Catalpa ovata and their inhibitory effects on the production of nitric oxide.
机构信息
College of Pharmacy, Chungbuk National University, Cheongju, 361-763, Korea.
出版信息
Arch Pharm Res. 2010 Mar;33(3):381-5. doi: 10.1007/s12272-010-0306-2. Epub 2010 Mar 30.
Bioassay-guided fractionation of a CH2Cl2-soluble fraction of the stems of Catalpa ovata led to isolation of a new naphthoquinone, 4-hydroxy-2-(2-methoxy-3-hydroxy-3-methyl-but-1-enyl)-4-hydro-1H-naphthalen-1-one (10), together with nine known compounds, catalponol (1), catalponone (2), catalpalactone (3), alpha-lapachone (4), 9-hydroxy-alpha-lapachone (5), 4,9-dihydroxy-alpha-lapachone (6), 9-methoxy-alpha-lapachone (7), 4-oxo-alpha-lapachone (8), and 9-methoxy-4-oxo-alpha-lapachone (9). The structures were elucidated on the basis of spectroscopic analyses. The inhibitory effects of these isolates on lipopolysaccharide-induced NO synthesis in RAW 264.7 cells were evaluated. Among them, catapalactone (3), 9-hydroxy-alpha-lapachone (5) and 4,9-dihydroxy-alpha-lapachone (6) exhibited potent inhibitory effects, with IC(50) values of 9.80, 4.64 and 2.73 microM, respectively.
采用生物活性跟踪方法，从梓木的氯仿可溶部分分离得到一个新的萘醌化合物，4-羟基-2-(2-甲氧基-3-羟基-3-甲基-1-丁烯基)-4-氢-1H-萘-1-酮（10），同时还分离得到了 9 个已知化合物，梓酚（1）、梓酮（2）、梓醇内酯（3）、α-拉帕酮（4）、9-羟基-α-拉帕酮（5）、4,9-二羟基-α-拉帕酮（6）、9-甲氧基-α-拉帕酮（7）、4-氧代-α-拉帕酮（8）和 9-甲氧基-4-氧代-α-拉帕酮（9）。根据波谱分析鉴定了它们的结构。评价了这些分离物对 RAW 264.7 细胞中脂多糖诱导的 NO 合成的抑制作用。其中，梓醇内酯（3）、9-羟基-α-拉帕酮（5）和 4,9-二羟基-α-拉帕酮（6）表现出较强的抑制活性，IC50 值分别为 9.80、4.64 和 2.73 μM。
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