National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, University of Mississippi, University, MS 38677, USA.
Department of BioMolecular Sciences, Division of Pharmacognosy, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.
Molecules. 2019 Feb 21;24(4):777. doi: 10.3390/molecules24040777.
Bioassay-guided fractionation of an EtOAc extract of the broth of the endophytic fungus sp. UM10M (Xylariaceae) isolated from a diseased leaf afforded three known cytochalasins, 19,20-epoxycytochalasins C () and D (), and 18-deoxy-19,20-epoxy-cytochalasin C (). All three compounds showed potent in vitro antiplasmodial activity and phytotoxicity with no cytotoxicity to Vero cells. These compounds exhibited moderate to weak cytotoxicity to some of the cell lines of a panel of solid tumor (SK-MEL, KB, BT-549, and SK-OV-3) and kidney epithelial cells (LLC-PK). Evaluation of in vivo antimalarial activity of 19,20-epoxycytochalasin C () in a mouse model at 100 mg/kg dose showed that this compound had weak suppressive antiplasmodial activity and was toxic to animals.
生物测定指导下，从内生真菌 sp.UM10M（木层孔菌科）的发酵液乙酸乙酯提取物中分离得到三种已知的细胞松弛素，19,20-环氧细胞松弛素 C () 和 D ()，以及 18-脱氧-19,20-环氧细胞松弛素 C ()。这三种化合物均表现出很强的体外抗疟原虫活性和植物毒性，对 Vero 细胞无细胞毒性。这些化合物对一组实体瘤（SK-MEL、KB、BT-549 和 SK-OV-3）和肾上皮细胞（LLC-PK）的细胞系表现出中等至弱的细胞毒性。在 100mg/kg 剂量的小鼠模型中评价 19,20-环氧细胞松弛素 C () 的体内抗疟原虫活性，表明该化合物具有较弱的抑制抗疟原虫活性，对动物有毒。
