Membrane permeabilization by non-steroidal anti-inflammatory drugs

Wataru Tomisato, Ken Ichiro Tanaka, Takashi Katsu, Hiroki Kakuta, Kenji Sasaki, Shinji Tsutsumi, Tatsuya Hoshino, Mayuko Aburaya, Daiwei Li, Tomofusa Tsuchiya, Keitarou Suzuki, Kazumi Yokomizo, Tohru Mizushima

研究成果: Article査読

84 被引用数 (Scopus)


The cytotoxicity of non-steroidal anti-inflammatory drugs (NSAIDs) is involved in the formation of NSAID-induced gastric lesions. The mechanism(s) behind these cytotoxic effects, however, is not well understood. We found here that several NSAIDs tested caused hemolysis when employed at concentrations similar to those that result in cytotoxicity. Moreover, these same NSAIDs were found to directly permeabilize the membranes of calcein-loaded liposomes. Given the similarity in NSAID concentrations for cytotoxic and membrane permeabilization effects, the cytotoxic action of these NSAIDs may be mediated through the permeabilization of biological membranes. Increase in the intracellular Ca 2+ level can lead to cell death. We here found that all of NSAIDs tested increased the intracellular Ca 2+ level at concentrations similar to those that result in cytotoxicity. Based on these results, we consider a possibility that membrane permeabilization by NSAIDs induces cell death through increase in the intracellular Ca 2+ level.

ジャーナルBiochemical and Biophysical Research Communications
出版ステータスPublished - 2004 10月 22

ASJC Scopus subject areas

  • 生物理学
  • 生化学
  • 分子生物学
  • 細胞生物学


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