Qi Yan-Yan, Su Jia, Zhang Zhi-Jun, Li Lai-Wei, Fan Min, Zhu Yu, Wu Xing-De, Zhao Qin-Shi
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201, P. R. China.
University of the Chinese Academy of Sciences, Beijing, 100049, P. R. China.
Chem Biodivers. 2018 Apr;15(4):e1800043. doi: 10.1002/cbdv.201800043. Epub 2018 Apr 16.
Activity-guided fractionation strategy was used to investigate chemical constituents from the roots of Podocarpus macrophyllus. Successfully, two new norditerpenes, 2β-hydroxymakilactone A (1) and 3β-hydroxymakilactone A (2), along with ten known analogues (3 - 12) were isolated. The structures of 1 and 2 were elucidated by spectroscopic analysis including 1D-, 2D-NMR, and HR-ESI-MS data. The previously reported structure of 2,3-dihydro-2α-hydroxypodolide was revised as 2,3-dihydro-2β-hydroxypodolide (3) by spectroscopic analysis, and was further confirmed by X-ray crystallographic analysis. Cytotoxic activities of all isolated compounds against five human solid tumour cell lines (AGS, HeLa, MDA-MB-231, HepG-2, and PANC-1) were evaluated. All of them exhibited anti-proliferative activities (IC = 0.3 - 27 μm), except for 10. Compounds 1, 4, 5, 6, and 8 exhibited potent inhibitory activities with IC < 1 μm against HeLa and AGS cells.
采用活性导向分离策略研究了罗汉松根中的化学成分。成功分离出两种新的降二萜，2β-羟基马基内酯A（1）和3β-羟基马基内酯A（2），以及十种已知类似物（3 - 12）。通过包括一维、二维核磁共振和高分辨电喷雾电离质谱数据在内的光谱分析阐明了1和2的结构。通过光谱分析将先前报道的2,3-二氢-2α-羟基坡豆醇内酯的结构修订为2,3-二氢-2β-羟基坡豆醇内酯（3），并通过X射线晶体学分析进一步证实。评估了所有分离化合物对五种人类实体瘤细胞系（AGS、HeLa、MDA-MB-231、HepG-2和PANC-1）的细胞毒性活性。除10外，所有化合物均表现出抗增殖活性（IC = 0.3 - 27μm）。化合物1、4、5、6和8对HeLa和AGS细胞表现出强效抑制活性，IC < 1μm。
