Low Direct Cytotoxicity of Loxoprofen on Gastric Mucosal Cells
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- Yamakawa Naoki
- Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University
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- Suemasu Shintaro
- Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University
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- Kimoto Ayumi
- Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University
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- Arai Yasuhiro
- Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University
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- Ishihara Tomoaki
- Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University
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- Yokomizo Kazumi
- Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University
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- Okamoto Yoshinari
- Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University
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- Otsuka Masami
- Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University
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- Tanaka Ken-ichiro
- Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University
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- Mizushima Tohru
- Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University
書誌事項
- 公開日
- 2010
- 資源種別
- journal article
- DOI
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- 10.1248/bpb.33.398
- 公開者
- 公益社団法人 日本薬学会
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説明
Pro-drugs of non-steroidal anti-inflammatory drugs (NSAIDs), such as loxoprofen are widely used for clinical purposes because they are not so harmful to the gastrointestinal mucosa. We recently showed that NSAIDs such as indomethacin and celecoxib have direct cytotoxicity (ability to induce necrosis and apoptosis in gastric mucosal cells) due to their membrane permeabilizing activities, which is involved in NSAID-induced gastric lesions. We show here that under conditions where indomethacin and celecoxib clearly induce necrosis and apoptosis, loxoprofen and its active metabolite loxoprofen-OH, do not have such effects in primary culture of guinea pig gastric mucosal cells. Loxoprofen and loxoprofen-OH induced apoptosis more effectively in cultured human gastric cancer cells than in the primary culture. Loxoprofen and loxoprofen-OH exhibited much lower membrane permeabilizing activities than did indomethacin and celecoxib. We thus consider that the low direct cytotoxicity of loxoprofen observed in vitro is involved in its relative safety on production of gastric lesions in clinical situation.
収録刊行物
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- Ｂｉｏｌｏｇｉｃａｌ ＆ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｂｕｌｌｅｔｉｎ
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Ｂｉｏｌｏｇｉｃａｌ ＆ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｂｕｌｌｅｔｉｎ 33 (3), 398-403, 2010
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679602615552
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- NII論文ID
- 130000248088
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- NII書誌ID
- AA10885497
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- ISSN
- 13475215
- 09186158
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- NDL書誌ID
- 10582392
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- PubMed
- 20190399
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- 本文言語コード
- en
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- 資料種別
- journal article
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