Kim Ki Hyun, Moon Eunjung, Ha Sang Keun, Suh Won Se, Kim Ho Kyung, Kim Sun Yeou, Choi Sang Un, Lee Kang Ro
Natural Products Laboratory, School of Pharmacy, Sungkyunkwan University.
Chem Pharm Bull (Tokyo). 2014;62(11):1136-40. doi: 10.1248/cpb.c14-00381.
A bioassay-guided fractionation and chemical investigation of the MeOH extract from the twigs of Lindera glauca (SIEB. et ZUCC.) BLUME resulted in the isolation and identification of six lignans (1-6) including three new lignan derivatives, named linderuca A (1), B (2), and C (3). The structures of the new compounds (1-3) were determined on the basis of spectroscopic analyses, including two dimensional NMR and circular dichroism (CD) spectroscopy studies. The cytotoxic activities of the isolates (1-6) were evaluated by determining their inhibitory effects on human tumor cell lines. Compounds 1-5 showed antiproliferative activities against A549, SK-OV-3, SK-MEL-2, and HCT-15 cell lines with IC50 values of 7.79-29.42 µM. Based on the understanding that inflammation is a crucial cause of tumor progression, we also investigated the anti-inflammatory activities of the isolates (1-6) in the lipopolysaccharide-stimulated murine microglia BV-2 cell line by measuring nitric oxide (NO) levels. The new lignans (1-3) significantly inhibited NO production with IC50 values of 12.10, 9.48, and 9.87 µM, respectively, without cytotoxicity.
对山胡椒(Lindera glauca (SIEB. et ZUCC.) BLUME)嫩枝甲醇提取物进行生物活性导向的分离和化学研究,从中分离并鉴定出6种木脂素(1 - 6),包括3种新的木脂素衍生物,分别命名为山胡椒素A(1)、B(2)和C(3)。通过二维核磁共振和圆二色(CD)光谱等光谱分析确定了新化合物(1 - 3)的结构。通过测定对人肿瘤细胞系的抑制作用来评估分离物(1 - 6)的细胞毒性活性。化合物1 - 5对A549、SK - OV - 3、SK - MEL - 2和HCT - 15细胞系显示出抗增殖活性,IC50值为7.79 - 29.42 μM。基于炎症是肿瘤进展的关键原因这一认识,我们还通过测量一氧化氮(NO)水平,研究了分离物(1 - 6)在脂多糖刺激的小鼠小胶质细胞BV - 2细胞系中的抗炎活性。新木脂素(1 - 3)分别以12.10、9.48和9.87 μM的IC50值显著抑制NO生成,且无细胞毒性。