Tubulin Inhibitors from an Endophytic Fungus Isolated from Cedrus deodara

From an endophytic fungus, a close relative of Talaromyces sp., found in association with Cedrus deodara, four compounds including two new ones (2 and 4) were isolated and characterized. The structures of two compounds (1 and 4) were confirmed by X-ray crystallography. The compounds displayed a range of cytotoxicities against human cancer cell lines (HCT-116, A-549, HEP-1, THP-1, and PC-3). All the compounds were found to induce apoptosis in HL-60 cells, as evidenced by fluorescence and scanning electron microscopy studies. Also, the compounds caused significant microtubule inhibition in HL-60 cells.研究人员从与雪松（Cedrus deodara）共生的、属于篮状菌属（Talaromyces sp.）近缘种的内生真菌中，分离并鉴定得到4个化合物，其中包含2个新化合物（编号2和4）。通过X射线晶体衍射法确认了化合物1和4的化学结构。该系列化合物对多株人癌细胞系（HCT-116、A-549、HEP-1、THP-1及PC-3）展现出不同程度的细胞毒性。荧光显微镜与扫描电子显微镜实验证实，所有化合物均可诱导HL-60细胞发生细胞凋亡。此外，上述化合物对HL-60细胞具有显著的微管抑制活性。