文章基本信息

标题：Induction of p16INK4a Transcription and of Cellular Senescence by Aclacinomycin-Derivatives and Cardiac Glycosides
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作者：Kiyoshi Egawa ; Yosuke Kurihara ; Tatsuya Ito 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2002
卷号：25
期号：4
页码：461-465
DOI：10.1248/bpb.25.461
出版社：The Pharmaceutical Society of Japan
摘要：Stable transformants of Saos-2 cells that contain the luciferase reporter gene under the control of the human p16^INK4a transcriptional regulatory region were established, and were used to identify growth-inhibiting substances from culture broths of actinomycetes and extracts of plants. Among the active substances so far identified were an aclacinomycin-derivative, cenerubin B, and a cardiac glycoside, periplocin. These substances inhibited growth of normal human fibroblasts, and induced senescent phenotypes including a flattened morphology and increased acidic β-galactosidase activity, although the activities of their derivatives to induce p16^CDKN2 and β-galactosidase did not coincided with each other. These results suggest that the reporter system using the p16^CDKN2 transcriptional regulatory region is a useful means for screening growth inhibiting substances that are potential anti-tumor agents.
关键词：p16;luciferase;senescence;cinerubin B;periplocin