Li Feng, Awale Suresh, Zhang Hongyan, Tezuka Yasuhiro, Esumi Hiroyasu, Kadota Shigetoshi
Institute of Natural Medicine, University of Toyama, 2630-Sugitani, Toyama 930-0194, Japan.
J Nat Prod. 2009 Jul;72(7):1283-7. doi: 10.1021/np9002433.
A methanolic extract of propolis obtained in Myanmar was found to inhibit PANC-1 human pancreatic cancer cells preferentially under nutrient-deprived conditions (NDM), with a PC(50) value of 9.3 microg/mL. Bioactivity-guided fractionation of the extract led to the isolation of two new cycloartane-type triterpenes, (22Z,24E)-3-oxocycloart-22,24-dien-26-oic acid (1) and (24E)-3-oxo-27,28-dihydroxycycloart-24-en-26-oic acid (2), together with 13 cycloartanes (3-13) and four known prenylated flavanones (14-17). Among these, compound 1 exhibited the most potent preferential cytotoxicity (PC(50) 4.3 microM) in a concentration- and time-dependent manner. Furthermore, 1 induced apoptosis-like morphological changes of PANC-1 cells within 24 h of treatment.
在缅甸获得的蜂胶甲醇提取物被发现,在营养缺乏条件(NDM)下能优先抑制PANC - 1人胰腺癌细胞,半数抑制浓度(PC50)值为9.3微克/毫升。对该提取物进行生物活性导向分离,得到了两种新的环阿尔廷型三萜,(22Z,24E)-3 - 氧代环阿尔廷-22,24 - 二烯-26 - 酸(1)和(24E)-3 - 氧代-27,28 - 二羟基环阿尔廷-24 - 烯-26 - 酸(2),以及13种环阿尔廷类化合物(3 - 13)和4种已知的异戊烯基化黄烷酮(14 - 17)。其中,化合物1在浓度和时间依赖性方面表现出最有效的优先细胞毒性(PC50为4.3微摩尔)。此外,在处理24小时内,1诱导PANC - 1细胞出现凋亡样形态变化。