Graduate Institute of Biotechnology, National Chung-Hsing University, Taichung 402, Taiwan.
School of Pharmacy, College of Medicine, National Cheng Kung University, Tainan 701, Taiwan.
Molecules. 2017 Dec 31;23(1):86. doi: 10.3390/molecules23010086.
Hayata, usually called Taiwan five-leaf pine (5LP), is an endemic species in Taiwan and is traditionally used to relieve hypertension symptoms and improve cardiovascular function. In this study, the needle extract of 5LP was fractionated and analyzed by LC/MS/MS to search for possible antihypertensive candidates. In addition, bioassay-guided purification of the bioactive components was performed by Ca fluorescent signal (Fluo 4-AM) assays. Two dihydrobenzofuran lignans, pinumorrisonide A () and icariside E4 (), and one acylated flavonoid glycoside, kaempferol 3--α-(6‴--coumaroylglucosyl-β-1,4-rhamnoside) () were characterized from the active fractions. The structure of a new compound was established on the basis of 2D NMR spectroscopic and mass spectrometric analyses, and the known compounds and were identified by comparison of their physical and spectroscopic data with those reported in the literature. The purified compounds - exhibited significant inhibition of Ca fluorescence with IC values of 0.71, 0.36, and 0.20 mM, respectively. A mechanism study showed that these compounds showed vasorelaxant effects by blocking the voltage-operated Ca channel (VOCC) and inhibiting Ca influx to the cytoplasmic. These results suggested that 5LP and the three characterized components could be promising antihypertensive candidates for the use as VOCC blockers.
油杉（Hayata），通常被称为台湾五叶松（5LP），是台湾特有的物种，传统上用于缓解高血压症状和改善心血管功能。在这项研究中，5LP 的针叶提取物通过 LC/MS/MS 进行了分离和分析，以寻找可能的降压候选物。此外，通过 Ca 荧光信号（Fluo 4-AM）测定进行了生物活性成分的生物测定指导的纯化。从活性部分鉴定出两种二氢苯并呋喃木脂素，pinomorrisonide A（）和 icariside E4（），以及一种酰化类黄酮糖苷，山柰酚 3--α-（6‴-咖啡酰基葡萄糖基-β-1,4-鼠李糖苷）（）。新化合物的结构是基于 2D NMR 光谱和质谱分析确定的，并且通过将已知化合物和的物理和光谱数据与文献中报道的数据进行比较来鉴定。纯化的化合物 - 对 Ca 荧光具有显著的抑制作用，IC 值分别为 0.71、0.36 和 0.20 mM。机制研究表明，这些化合物通过阻断电压门控 Ca 通道（VOCC）和抑制 Ca 内流到细胞质来表现出血管舒张作用。这些结果表明，5LP 和三种表征的成分可能是作为 VOCC 阻滞剂的有前途的抗高血压候选物。
