Liu Zhi-Ming, Huang Xiao-Yun, Cui Mao-Rong, Zhang Xiao-De, Chen Zhao, Yang Ben-Shou, Zhao Xiao-Kun
Second Xiangya Hospital, Central South University, No. 139 Middle Renmin Road, Changsha, Hunan 410011, China; The First People Hospital of Qujing, Qujing 655000, Yunnan Province, China.
Qujing Medical College, Qujing 655000, Yunnan Province, China.
Fitoterapia. 2015 Mar;101:188-93. doi: 10.1016/j.fitote.2015.01.003. Epub 2015 Jan 14.
Four new Amaryllidaceae alkaloids, (+)-1-hydroxy-ungeremine (1), (+)-6β-acetyl-8-hydroxy-9-methoxy-crinamine (2), (+)-2-hydroxy-8-demethyl-homolycorine-α-N-oxide (3), (+)-N-methoxylcarbonyl-2-demethyl-isocorydione (4), together with two known compounds, (+)-6β-acetyl-crinamine (5) and 8-demethyl-homolycorine-α-N-oxide (6) were isolated from the ethanol extract of the bulbs of Lycoris radiata. Structural elucidation of all the compounds were performed by spectral methods such as 1D and 2D ((1)H-(1)H COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. All the isolated alkaloids were in vitro evaluated for their cytotoxic activities against eight tumor cell lines (BEN-MEN-1, CCF-STTG1, CHG-5, SHG-44, U251, BGC-823, HepG2 and SK-OV-3) and anti-inflammatory activities against Cox-1 and Cox-2. As a result, alkaloids 1 and 4 exhibited significant cytotoxic activities against all tested tumor cell lines except against BEN-MEN-1. Additionally, alkaloids 1 and 4 possessed selective inhibition of Cox-2 comparable with the standard drug NS-398 (>90%).
从石蒜的鳞茎乙醇提取物中分离出四种新的石蒜科生物碱，即(+)-1-羟基安格来明（1）、(+)-6β-乙酰基-8-羟基-9-甲氧基环胺（2）、(+)-2-羟基-8-去甲基高石蒜碱-α-N-氧化物（3）、(+)-N-甲氧基羰基-2-去甲基异紫堇酮（4），以及两种已知化合物，(+)-6β-乙酰基环胺（5）和8-去甲基高石蒜碱-α-N-氧化物（6）。除了高分辨率质谱外，还通过一维和二维核磁共振光谱（(1)H-(1)H COSY、HMQC和HMBC）等光谱方法对所有化合物进行了结构解析。对所有分离得到的生物碱进行了体外实验，评估它们对八种肿瘤细胞系（BEN-MEN-1、CCF-STTG1、CHG-5、SHG-44、U251、BGC-823、HepG2和SK-OV-3）的细胞毒性活性以及对Cox-1和Cox-2的抗炎活性。结果表明，生物碱1和4对除BEN-MEN-1外的所有测试肿瘤细胞系均表现出显著的细胞毒性活性。此外，生物碱1和4对Cox-2具有选择性抑制作用，与标准药物NS-398相当（>90%）。
