来自罗汉松的天然细胞毒 [3'→8″]-双黄酮。
Naturally Occurring Cytotoxic [3'→8″]-Biflavonoids from Podocarpus nakaii.
机构信息
Institute of Pharmacology, National Yang-Ming University, Taipei 112, Taiwan.
Institute of Pharmacology, National Yang-Ming University, Taipei 112, Taiwan ; National Research Institute of Chinese Medicine, Taipei 112, Taiwan.
出版信息
J Tradit Complement Med. 2012 Jul;2(3):220-6. doi: 10.1016/s2225-4110(16)30103-1.
Bioassay-guided fractionation of the EtOH extract of the dried twigs of Podocarpus nakaii Hayata (Podocarpaceae), endemic plant in Taiwan has resulted in isolation of four [3'→8″]-biflavonoid derivatives, amenotoflavone (AF), podocarpusflavone-A (PF), II-4″,I-7-dimethoxyamentoflavone (DAF), and heveaflavone (HF). Their structures were determined by physical and extensive spectroscopic analyses such as (1)H, (13)C, (1)H-(1)H COSY, HMQC, and HMBC, as well as comparison with literature values. Compounds PF and DAF showed significant inhibitions against DLD, KB, MCF-7, HEp-2 tumor cell lines (ED50 ca. 4.56-16.24 μg/mL) and induced cell apoptosis in MCF-7 via mainly sub-G1/S phase arrest. Furthermore, these compounds exhibited moderate Topoisomerase I inhibitory activity.
生物测定指导下对台湾特有植物罗汉松（罗汉松科）干枝的乙醇提取物进行分段，分离得到四种[3'→8″]-双黄酮衍生物，amenotoflavone（AF）、podocarpusflavone-A（PF）、II-4″，I-7-二甲氧基amentoflavone（DAF）和heveaflavone（HF）。通过物理和广泛的光谱分析，如（1）H、（13）C、（1）H-（1）H COSY、HMQC 和 HMBC，以及与文献值的比较，确定了它们的结构。PF 和 DAF 对 DLD、KB、MCF-7、HEp-2 肿瘤细胞系显示出显著的抑制作用（ED50 约为 4.56-16.24 μg/mL），并通过主要的 sub-G1/S 期阻滞诱导 MCF-7 细胞凋亡。此外，这些化合物表现出适度的拓扑异构酶 I 抑制活性。
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