5) showed anti-proliferative activity against HUVECs with IC50 values in the range 0.6-.2?μM, and the selective index was 7-00-fold in comparison with those for several cancer cell lines, while the desacyl mixture of senegasaponins (6) and tenuifolin (7) lost anti-proliferative activity, indicating that the 28-O-glycoside moiety and methoxycinnamoyl group were essential for the HUVEC-selective growth inhibition of senegasaponins. Senegin III (2) inhibited the vascular endothelial growth factor (VEGF)-induced in vitro tubular formation of HUVECs and basic fibroblast growth factor (bFGF)-induced in vivo neovascularization in the mouse Matrigel plug assay. Moreover, senegin III (2) suppressed tumor growth in the ddY mice s.c.-inoculated murine sarcoma S180 cells. The analysis of the action mechanism of senegin III (2) suggested that the induction of pigment epithelium-derived factor (PEDF) would contribute to the anti-angiogenic effects of senegasaponins." />
Anti-angiogenic effect of triterpenoidal saponins from Polygala senega
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  • 作者:Masayoshi Arai (1)
    Asami Hayashi (1)
    Mari Sobou (1)
    Shunsuke Ishida (1)
    Takashi Kawachi (1)
    Naoyuki Kotoku (1)
    Motomasa Kobayashi (1)
  • 关键词:Senegasaponins ; Polygala senega ; Angiogenesis ; Cancer ; HUVECs ; Tubular formation
  • 刊名:Journal of Natural Medicines
  • 出版年:2011
  • 出版时间:January 2011
  • 年:2011
  • 卷:65
  • 期:1
  • 页码:149-156
  • 全文大小:520KB
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    12. Desbène S, Hanquet B, Shoyama Y, Wagner H, Lacaille-Dubois MA (1999) Biologically active triterpene saponins from callus tissue of / Polygala amarella. J Nat Prod 62:923-26 CrossRef
    13. Lin KT, Lien JC, Chung CH, Kuo SC, Huang TF (2010) A novel compound, NP-184, inhibits the vascular endothelial growth factor induced angiogenesis. Eur J Pharmacol 630:53-0 CrossRef
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  • 作者单位:Masayoshi Arai (1)
    Asami Hayashi (1)
    Mari Sobou (1)
    Shunsuke Ishida (1)
    Takashi Kawachi (1)
    Naoyuki Kotoku (1)
    Motomasa Kobayashi (1)

    1. Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka, 565-0871, Japan
  • ISSN:1861-0293
文摘
Senegasaponins [senegin II (1), senegin III (2), senegin IV (3), senegasaponin a (4), and senegasaponin b (5)] from Polygala senega were re-discovered as selective anti-proliferative substances against human umbilical vein endothelial cells (HUVECs). Senegasaponins (1-strong class="a-plus-plus">5) showed anti-proliferative activity against HUVECs with IC50 values in the range 0.6-.2?μM, and the selective index was 7-00-fold in comparison with those for several cancer cell lines, while the desacyl mixture of senegasaponins (6) and tenuifolin (7) lost anti-proliferative activity, indicating that the 28-O-glycoside moiety and methoxycinnamoyl group were essential for the HUVEC-selective growth inhibition of senegasaponins. Senegin III (2) inhibited the vascular endothelial growth factor (VEGF)-induced in vitro tubular formation of HUVECs and basic fibroblast growth factor (bFGF)-induced in vivo neovascularization in the mouse Matrigel plug assay. Moreover, senegin III (2) suppressed tumor growth in the ddY mice s.c.-inoculated murine sarcoma S180 cells. The analysis of the action mechanism of senegin III (2) suggested that the induction of pigment epithelium-derived factor (PEDF) would contribute to the anti-angiogenic effects of senegasaponins.

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