Jiangsu Key Laboratory for Functional Substances of Chinese Medicine, Nanjing University of Chinese Medicine, Nanjing 210023, People's Republic of China; Research Department of Pharmacognosy, China Pharmaceutical University, Nanjing 211198, People's Republic of China.
Jiangsu Key Laboratory for Functional Substances of Chinese Medicine, Nanjing University of Chinese Medicine, Nanjing 210023, People's Republic of China.
Bioorg Chem. 2020 Jul;100:103809. doi: 10.1016/j.bioorg.2020.103809. Epub 2020 Apr 2.
Six pairs of octahydroindolizine-type alkaloid enantiomers (1-6) including three new compounds [(-)-1/(+)-1, 2] were isolated from the stems of Dendrobium crepidatum. Their structures including the absolute configurations were elucidated by extensive spectroscopic analyses and comparison between the experimental and calculated electronic circular dichroism (ECD). All compounds were examined for their inhibitory effects on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW264.7 cells. It was found that compounds (+)-1, 2 and (+)-6 exhibited pronounced inhibition on NO production with IC values in the range of 3.62-16.11 µM, being more active than the positive control, dexamethasone (IC = 47.04 µM). In vivo, compound 6 (100, 50 and 10 mg/kg) showed protective effects against LPS-induced acute lung injury (ALI) in mice.
从石斛属植物茎中分离得到了六对八氢吲哚嗪型生物碱对映异构体(1-6),包括三个新化合物[(-)-1/(+)-1, 2]。通过广泛的光谱分析和实验与计算电子圆二色性(ECD)的比较,阐明了它们的结构和绝对构型。所有化合物均进行了抑制脂多糖(LPS)诱导 RAW264.7 细胞中一氧化氮(NO)产生的抑制活性测试。结果发现,化合物(+)-1、2 和(+)-6 对 NO 产生具有显著的抑制作用,IC 值范围为 3.62-16.11 μM,比阳性对照地塞米松(IC = 47.04 μM)更具活性。在体内,化合物 6(100、50 和 10 mg/kg)对 LPS 诱导的小鼠急性肺损伤(ALI)具有保护作用。