Ph.D. program in Clinical Drug Development of Herbal Medicine, College of Pharmacy, Taipei Medical University, Taipei 11031, Taiwan.
Division of Chinese Materia Medica Development, National Research Institute of Chinese Medicine, Taipei 11221, Taiwan.
J Nat Prod. 2021 Feb 26;84(2):259-267. doi: 10.1021/acs.jnatprod.0c00919. Epub 2021 Jan 17.
Seven new polyhydroxylated oleanane-type triterpene saponins, arenarosides A-G (-), together with four known compounds, were isolated from an ethanol extract of the aerial parts of the Vietnamese plant . The chemical structures of the newly isolated oleanane saponins were elucidated on the basis of spectroscopic and spectrometric analysis, especially 2D NMR and HRMS. Biological evaluation revealed that , , , and showed moderate activities against four human cancer cell lines (A549, HTC116, PC3, and RT112) with IC values of 6.0-9.9 μM, and , , , and also displayed promising antiangiogenesis effects with IC values <5 μM in the test system used. Among the isolates, arenaroside D () exhibited the most potent inhibitory effects, not only in cancer cell proliferation but also in angiogenic activities. Preliminary SAR studies revealed that the presence of an acetyl group at C-22 in oleanane-type triterpene saponins increases these bioactivities.
从越南植物的地上部分的乙醇提取物中分离得到了七种新的多羟基齐墩果烷型三萜皂苷，分别为arenarosides A-G（-），以及四种已知化合物。根据光谱和光谱分析，特别是 2D NMR 和 HRMS，阐明了新分离的齐墩果烷皂苷的化学结构。生物评价结果表明，arenaroside D（）不仅在癌细胞增殖方面，而且在所用测试系统中的血管生成活性方面，都显示出对四种人癌细胞系（A549、HTC116、PC3 和 RT112）具有中等的活性，IC 值为 6.0-9.9 μM，arenaroside D（）还显示出有希望的抗血管生成作用，IC 值<5 μM。在分离得到的化合物中，arenaroside D（）不仅在癌细胞增殖方面，而且在血管生成活性方面，表现出最有效的抑制作用。初步的 SAR 研究表明，齐墩果烷型三萜皂苷在 C-22 位上存在乙酰基可以提高这些生物活性。
