2. Academic Validation
  3. Arenarosides A-G, Polyhydroxylated Oleanane-Type Saponins from Polycarpaea arenaria and their Cytotoxic and Antiangiogenic Activities

Arenarosides A-G, Polyhydroxylated Oleanane-Type Saponins from Polycarpaea arenaria and their Cytotoxic and Antiangiogenic Activities

  • J Nat Prod. 2021 Feb 26;84(2):259-267. doi: 10.1021/acs.jnatprod.0c00919.
Nham-Linh Nguyen 1 2,  Thanh-Hoa Vo 1 2,  Yu-Chi Lin 2 3,  Chia-Ching Liaw 2 4,  Mei-Kuang Lu 2,  Jing-Jy Cheng 2,  Mei-Chuan Chen 1 5,  Yao-Haur Kuo 1 2 6
Affiliations

Affiliations

  • 1 Ph.D. program in Clinical Drug Development of Herbal Medicine, College of Pharmacy, Taipei Medical University, Taipei 11031, Taiwan.
  • 2 Division of Chinese Materia Medica Development, National Research Institute of Chinese Medicine, Taipei 11221, Taiwan.
  • 3 Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
  • 4 Department of Biochemical Science and Technology, National Chiayi University, Chiayi 60004, Taiwan.
  • 5 Traditional Herbal Medicine Research Center of Taipei Medical University Hospital, Taipei 11031, Taiwan.
  • 6 Graduate Institute of Integrated Medicine, College of Chinese Medicine, China Medical University, Taichung 40402, Taiwan.
PMID: 33459007 DOI: 10.1021/acs.jnatprod.0c00919
Abstract

Seven new polyhydroxylated oleanane-type triterpene saponins, arenarosides A-G (1-7), together with four known compounds, were isolated from an ethanol extract of the aerial parts of the Vietnamese plant Polycarpaea arenaria. 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 3, 4, 6, and 7 showed moderate activities against four human Cancer cell lines (A549, HTC116, PC3, and RT112) with IC50 values of 6.0-9.9 μM, and 3, 4, 5, and 7 also displayed promising antiangiogenesis effects with IC50 values <5 μM in the test system used. Among the isolates, arenaroside D (4) 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.

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