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Cytotoxic and pro-apoptotic activities of medicarpin from Canavalia maritima
(Aubl.) via the suppression of NF-κB activation in HeLa cells

Min-Juan Xu, Xin-Ping Huang, Min Li*, Wan Sun, Jing-Rong Cui, Wen-Han Lin   

  1. State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China
  • Received:2009-06-27 Revised:2009-10-15 Online:2009-11-30 Published:2009-11-30
  • Contact: Min Li*

Abstract:

Three known pterocarpin derivatives, (-)-medicarpin (PD1), (-)-2-hydroxy­4,9-dimethoxypterocarpan (PD2), and 4-hydroxy-3-methoxy-8,9-methylene-dioxypterocarpan (PD3) were isolated from Canavalia maritima, for the first time. The cytotoxic and pro-apoptotic activities of (-)-medicarpin in cutured human tumor HeLa cells and its effect on NF-κB activation were investigated. We found that PD1 inhibited NF-κB activation by high content screening analysis, and PD1 exhibited cytotoxicity by SRB assay. In addition, we found that PD1 induced nuclear condensation and increased membrane permeability and mitochondrial transmembrane potential in HeLa cells in a dose and time dependent manner. In conclusion, our data suggested that (-)-medicarpin was capable of inhibiting tumor cell growth in vitro and inducing apoptosis, which might be via the suppression of NF-κB activation.

Key words: Medicarpin, Medicarpin, Canavalia maritime, Canavalia maritime, Anticancer, Anticancer, Apoptosis, Apoptosis, NF-κB, NF-κB, High content screening, High content screening

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