Laboratoire de Toxicologie and Laboratoire de Chimie Analytique, Toxicologie et Chimie Physique Appliquee, Institut de Pharmacie, Universite Libre de Bruxelles (ULB), Brussels, Belgium.
J Nat Prod. 2010 May 28;73(5):969-71. doi: 10.1021/np900731p.
Fourteen metabolites, isolated from phytopathogenic and toxigenic fungi, were evaluated for their in vitro antigrowth activity for six distinct cancer cell lines, using the MTT colorimetric assay. Bislongiquinolide (1) and dihydrotrichodimerol (5), which belong to the bisorbicillinoid structural class, displayed significant growth inhibitory activity against the six cancer cell lines studied, while the remaining compounds displayed weak or no activity. The data show that 1 and 5 have similar growth inhibitory activities with respect to those cancer cell lines that display certain levels of resistance to pro-apoptotic stimuli or those that are sensitive to apoptosis. Quantitative videomicroscopy analysis revealed that 1 and 5 exert their antiproliferative effect through cytostatic and not cytotoxic activity. The preliminary results from the current study have stimulated further structure-activity investigations with respect to the growth inhibitory activity of compounds belonging to the bisorbicillinoid group.
从植物病原真菌和产毒真菌中分离得到的 14 种代谢产物,采用 MTT 比色法,评估了它们对 6 种不同癌细胞系的体外生长抑制活性。双贝壳杉烯内酯(1)和二氢三齿二聚醇(5)属于双贝壳杉烷类结构,对所研究的 6 种癌细胞系表现出显著的生长抑制活性,而其余化合物则表现出较弱或无活性。数据表明,1 和 5 对某些对促凋亡刺激物有一定抗性或对凋亡敏感的癌细胞系的生长抑制活性相似。定量视频显微镜分析表明,1 和 5 通过细胞生长抑制而不是细胞毒性发挥其抗增殖作用。目前的研究初步结果刺激了对属于双贝壳杉烷类化合物的生长抑制活性的进一步结构活性研究。