Tang Jun, Li Ning, Dai Haofu, Wang Kaijin
Anhui Province Key Laboratory of Research and Development of Traditional Chinese Medicine, School of Life Sciences, Anhui University, Hefei 230039, China.
Zhongguo Zhong Yao Za Zhi. 2010 Jul;35(13):1710-4. doi: 10.4268/cjcmm20101313.
To study the chemical constituents from the seeds of A. katsumadai, and their inhibition on NF-kappaB activation and antitumor effect.
Tweleve compounds were isolated from the seeds of Aplinia katsumadai on repeated column chromatography on silica gel, and Sephadex LH-20, and their structures were determined mainly by means of MS and NMR techniques; and their inhibition on NF-kappaB activation and antitumor effect were also tested by High-Content Screening (image-based) with immunofluorescent probe and MTT method, respectively.
From the EtOAC fraction of the seeds of A. katsumadai 12 compounds were isolated and identified as follows: (3S,5S)-trans-3,5-dihydroxy-1 ,7-diphenyl-hept-1-ene (1), (3R,5S)-trans-3,5-dihydroxy-1,7-diphenyl-hept-1-ene (2), 5-hydroxy-1,7-diphenyl-hepta-6-en-3-one (3), cardamonin (4), alpinetin(5), pinocembrin(6), pinostrobin(7), naringenin (8), (+)-catechin(9), chrysin(10), rutin(11) and 2,4- dihydroxy-6-phenethl-benzinic acid methyl ester (12). Compound 14 showed inhibitory effect on NF-kappaB activation with the IC50 values as 14.8, 16.5, 23.2 and 7. 5 micromol x L(-1), respectively. Compound 4 displayed cytotoxicity against leukemia K562 cells and human hepatoma cell line SMMC-7721 with IC50 values as 3.2 and 3.5 mg x L(-1), and compound 6 showed moderate cytotoxicity against SMMC-7721 with the IC50 value as 18.3 mg x L(-1).
Compounds 7-12 were isolated from A. katsumadai for the first time and Compound 12 were isolated from the genus Aplinia for the first time; compound 4 has the activity of anti-tumor and NF-kappaB activation inhibition, compounds 1-3 have the activity NF-KB activation inhibition.
研究草豆蔻种子的化学成分及其对核因子-κB（NF-κB）激活的抑制作用和抗肿瘤作用。
采用硅胶柱色谱、葡聚糖凝胶LH-20柱色谱等反复柱色谱法从草豆蔻种子中分离得到12个化合物，主要通过质谱（MS）和核磁共振（NMR）技术确定其结构；分别采用基于免疫荧光探针的高内涵筛选（基于图像）和MTT法检测它们对NF-κB激活的抑制作用和抗肿瘤作用。
从草豆蔻种子的乙酸乙酯部位分离得到12个化合物，分别鉴定为：(3S,5S)-反式-3,5-二羟基-1,7-二苯基-1-庚烯（1）、(3R,5S)-反式-3,5-二羟基-1,7-二苯基-1-庚烯（2）、5-羟基-1,7-二苯基-6-庚烯-3-酮（3）、小豆蔻明（4）、山姜素（5）、松属素（6）、豆甾醇（7）、柚皮素（8）、(+)-儿茶素（(9)、白杨素（10）、芦丁（11）和2,4-二羟基-6-苯乙基苯甲酸甲酯（12）。化合物14对NF-κB激活具有抑制作用，IC50值分别为14.8、16.5、23.2和7.5 μmol·L-1。化合物4对白血病K562细胞和人肝癌细胞系SMMC-7721具有细胞毒性，IC50值分别为3.2和3.5 mg·L-1，化合物6对SMMC-7721显示出中等细胞毒性，IC50值为18.3 mg·L-1。
化合物7-12为首次从草豆蔻中分离得到，化合物12为首次从山姜属植物中分离得到；化合物4具有抗肿瘤和抑制NF-κB激活的活性，化合物1-3具有抑制NF-κB激活的活性。
