Tokyo University of Pharmacy and Life Sciences, School of Pharmacy, 1432-1, Horinouchi, Hachiouji, Tokyo 192-0392, Japan.
Phytochemistry. 2012 May;77:304-11. doi: 10.1016/j.phytochem.2012.02.007. Epub 2012 Mar 10.
A bioassay-guided fractionation of the heartwood of Santalum album led to the isolation of seven α-santalol derivatives including (9S,10E)-9-hydroxy-α-santalal, (10R,11S)-10,11-dihydroxy-α-santalol, (9E)-11,13-dihydroxy-α-santalol, and (10E)-12-hydroxy-α-santalic acid. Their structures were determined on the basis of results of spectroscopic analysis, including two-dimensional (2D) NMR spectroscopic data. The isolated compounds and derivatives were evaluated for cytotoxicity against HL-60 human promyelocytic leukemia cells and TIG-3 normal human diploid fibroblasts. Of these (9S,10E)-9-hydroxy-α-santalal, exhibited tumor-selective cytotoxicity. The apoptosis induction properties of sesquiterpenes with cytotoxic potency in HL-60 cells are also described.
基于光谱分析结果，包括二维（2D）NMR 光谱数据，确定了从檀香心材中分离得到的 7 种 α-檀香醇衍生物的结构，包括（9S，10E）-9-羟基-α-檀香醇、（10R，11S）-10，11-二羟基-α-檀香醇、（9E）-11，13-二羟基-α-檀香醇和（10E）-12-羟基-α-檀香酸。对这些化合物和衍生物进行了人早幼粒细胞白血病细胞 HL-60 和正常二倍体成纤维细胞 TIG-3 的细胞毒性评估。其中（9S，10E）-9-羟基-α-檀香醇表现出肿瘤选择性细胞毒性。本文还描述了具有 HL-60 细胞细胞毒性的倍半萜类化合物诱导细胞凋亡的特性。
