Chen Li-Ping, Zhao Feng, Wang Yao, Zhao Lian-Lian, Li Qiu-Ping, Liu Hong-Wei
School of Pharmacy, Yantai University, Yantai, China.
J Asian Nat Prod Res. 2011 Aug;13(8):734-43. doi: 10.1080/10286020.2011.587412.
Two new resorcinol derivatives 2-methoxy-4-hydroxy-6-(8Z-pentadecenyl)-benzene-1-O-acetate (1) and 2-methoxy-4-hydroxy-6-pentadecyl-benzene-1-O-acetate (2), together with four known compounds 2-methoxy-4-hydroxy-6-tridecyl-benzene-1-O-acetate (ardisiphenol D, 3), 5-(8Z-pentadecenyl)resorcinol (4), 5-pentadecylresorcinol (5), 5-tridecylresorcinol (6), have been isolated from the roots of Ardisia brevicaulis in our previous work. In the present study, the inhibitory effect of 1-6 on the proliferation of human pancreatic PANC-1, human lung A549, human gastrointestinal carcinoma SGC 7901, human breast MCF-7, and human prostate PC-3 cancer cells was evaluated by the methyl thiazolyl tetrazolium method. Compounds 1-6 all showed inhibitory activities against the proliferation of PANC-1, A549, SGC7901, MCF-7, and PC-3 cancer cells. Compound 3, the most active agent and the main constituent with the highest yield, induced apoptosis of PANC-1 cells (the most sensitive cell line among the cell lines screened) via the activation of caspase-3 and caspase-9, up-regulation of the ratio of bax/bcl-2 protein expression.
在我们之前的工作中，已从短茎紫金牛的根部分离出两种新的间苯二酚衍生物2-甲氧基-4-羟基-6-(8Z-十五碳烯基)-苯-1-O-乙酸酯(1)和2-甲氧基-4-羟基-6-十五烷基-苯-1-O-乙酸酯(2)，以及四种已知化合物2-甲氧基-4-羟基-6-十三烷基-苯-1-O-乙酸酯(紫金牛酚D，3)、5-(8Z-十五碳烯基)间苯二酚(4)、5-十五烷基间苯二酚(5)、5-十三烷基间苯二酚(6)。在本研究中，采用甲基噻唑基四氮唑法评估了化合物1-6对人胰腺PANC-1、人肺A549、人胃肠道癌SGC 7901、人乳腺癌MCF-7和人前列腺癌PC-3癌细胞增殖的抑制作用。化合物1-6均对PANC-1、A549、SGC7901、MCF-7和PC-3癌细胞的增殖表现出抑制活性。化合物3是活性最强的药物且是产量最高的主要成分，通过激活caspase-3和caspase-9、上调bax/bcl-2蛋白表达比值，诱导PANC-1细胞(筛选的细胞系中最敏感的细胞系)凋亡。
