College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea; Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Caugiay, Hanoi, Viet Nam.
Bioorg Med Chem Lett. 2014 Apr 15;24(8):1895-900. doi: 10.1016/j.bmcl.2014.03.014. Epub 2014 Mar 15.
Two new compounds, euphorbinoside (1) and dehydropicrorhiza acid methyl diester (2), along with 24 known compounds (3-26) were isolated from Euphorbia humifusa Willd. The effects of these compounds on soluble epoxide hydrolase (sEH) inhibitory activity were evaluated. Flavonoid compounds (10-21) exhibited high sEH inhibitory activity. Among them, compounds 12, 13, and 19 greatly inhibited sEH enzymatic activity, with IC50 values as low as 18.05±1.17, 18.64±1.83, and 17.23±0.84 μM, respectively. In addition, the effects of these compounds on lipopolysaccharide (LPS)-induced nitric oxide (NO) and tumor necrosis factor alpha (TNF-α) production by RAW 264.7 cells were investigated. Compounds 3-6, 8, 18, 20-23, and 25-26 inhibited the production of both NO and TNF-α, with IC50 values ranging from 11.1±0.9 to 45.3±1.6 μM and 14.4±0.5 to 44.5±1.2 μM, respectively.
从地锦草中分离得到了两个新化合物，大戟宁（1）和脱水异佛尔可酸甲酯二酯（2），以及 24 个已知化合物（3-26）。评价了这些化合物对可溶性环氧化物水解酶（sEH）抑制活性的影响。黄酮类化合物（10-21）表现出很高的 sEH 抑制活性。其中，化合物 12、13 和 19 对 sEH 酶活性有很强的抑制作用，IC50 值分别低至 18.05±1.17、18.64±1.83 和 17.23±0.84 μM。此外，还研究了这些化合物对 RAW 264.7 细胞中脂多糖（LPS）诱导的一氧化氮（NO）和肿瘤坏死因子-α（TNF-α）产生的影响。化合物 3-6、8、18、20-23 和 25-26 抑制了 NO 和 TNF-α 的产生，IC50 值范围为 11.1±0.9 至 45.3±1.6 μM 和 14.4±0.5 至 44.5±1.2 μM。
