The NeaNAT Group, Dipartimento di Chimica delle Sostanze Naturali, Università degli Studi di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy.
J Nat Prod. 2011 Oct 28;74(10):2299-303. doi: 10.1021/np2005055. Epub 2011 Oct 10.
One new (1) and three known (2-4) isonitrile diterpenes, isolated from the Caribbean sponge Pseudoaxinella flava, were assayed in human cancer cell lines in vitro using an MTT colorimetric assay and quantitative videomicroscopy. Compounds 1-4 displayed activity for human PC3 prostate apoptosis-sensitive cancer cell lines. Compounds 3 and 4 demonstrated similar growth inhibitory effects for three apoptosis-sensitive and three apoptosis-resistant cancer cell lines. Quantitative videomicroscopy analysis revealed that compounds 1 and 2 exerted their activity through cytotoxic effects, and compounds 3 and 4 through cytostatic effects. These results identify marine diterpene isonitriles as potential lead compounds for anticancer drug discovery.
从加勒比海海绵 Pseudoaxinella flava 中分离得到的一种新的(1)和三种已知的(2-4)异腈二萜,通过 MTT 比色法和定量视频显微镜在体外的人类癌细胞系中进行了检测。化合物 1-4 对人前列腺 PC3 凋亡敏感癌细胞系具有活性。化合物 3 和 4 对三种凋亡敏感和三种凋亡抗性癌细胞系显示出相似的生长抑制作用。定量视频显微镜分析表明,化合物 1 和 2 通过细胞毒性作用发挥其活性,化合物 3 和 4 通过细胞抑制作用发挥其活性。这些结果表明海洋二萜异腈类化合物可能是抗癌药物发现的潜在先导化合物。