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Cancer Chemistry

Abstract #2658: Trisindoline and indirubin-3\#8217;-monoxime exert anticancer activity through different mechanism.

Han Sun-Young, Miyoun Yoo, Gyu Hwan Yon, Eungbin Kim, Chong-Ock Lee and Sang-Un Choi
Han Sun-Young
Korea Research Institute of Chemical Technology, Daejeon, Korea, Republic of; Yonsei University, Seoul, Korea, Republic of
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Miyoun Yoo
Korea Research Institute of Chemical Technology, Daejeon, Korea, Republic of; Yonsei University, Seoul, Korea, Republic of
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Gyu Hwan Yon
Korea Research Institute of Chemical Technology, Daejeon, Korea, Republic of; Yonsei University, Seoul, Korea, Republic of
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Eungbin Kim
Korea Research Institute of Chemical Technology, Daejeon, Korea, Republic of; Yonsei University, Seoul, Korea, Republic of
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Chong-Ock Lee
Korea Research Institute of Chemical Technology, Daejeon, Korea, Republic of; Yonsei University, Seoul, Korea, Republic of
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Sang-Un Choi
Korea Research Institute of Chemical Technology, Daejeon, Korea, Republic of; Yonsei University, Seoul, Korea, Republic of
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DOI:  Published May 2009
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AACR Annual Meeting-- Apr 18-22, 2009; Denver, CO

Abstract

Recently, novel indigoid metabolites produced from Rhodococcus-derived oxygenase with anti-cancer activity were reported and active compound trisindoline was isolated (Biochem Biophys Res Commun, 376: 96). Trisindoline showed cytotoxicity against colorectal carcinoma HCT15 cells and uterine sarcoma MES-SA cells. Here, in an effort to find the mechanism of trisinoline\#8217;s cytotoxic activity, we compared trisindoline with indirubin-3\#8217;-monoxime, a bis-indole indigoid compound. Indirubin-3-\#8217;monoxime is mainly recognized as an inhibitor of cyclin-dependent kinase and glycogen synthase kinase-3, and has been considered for anticancer agent. In this report, we compared the cytotoxic activity of trisindoline and indirubin-3\#8217;-monoxime and studied the mechanism of action. Whereas trisindoline and indirubin-3\#8217;-monoxime showed similar activity against cancer cells, they exhibited different mode of action. Indirubin-3\#8217;-monoxime inhibited kinases like Flt-3, VEGFR2, and Met, which are major oncology target in drug discovery. IC50 of Indirubin-3\#8217;-monoxime was 0.142 \#956;M for Flt-3, 1.48 \#956;M for VEGFR2, and 5.5 \#956;M for Met. However, trisindoline do not affect the activities of these kinases. Although trisindoline and indirubin-3\#8217;-monoxime both belong to indigoid compound and exhibit similar cytotoxic activity, they have different mode of action for their anti-cancer activity.

Citation Information: In: Proc Am Assoc Cancer Res; 2009 Apr 18-22; Denver, CO. Philadelphia (PA): AACR; 2009. Abstract nr 2658.

Footnotes

  • 100th AACR Annual Meeting-- Apr 18-22, 2009; Denver, CO

  • American Association for Cancer Research
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Cancer Research: 69 (9 Supplement)
May 2009
Volume 69, Issue 9 Supplement
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Abstract #2658: Trisindoline and indirubin-3\#8217;-monoxime exert anticancer activity through different mechanism.
Han Sun-Young, Miyoun Yoo, Gyu Hwan Yon, Eungbin Kim, Chong-Ock Lee and Sang-Un Choi
Cancer Res May 1 2009 (69) (9 Supplement) 2658;

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Abstract #2658: Trisindoline and indirubin-3\#8217;-monoxime exert anticancer activity through different mechanism.
Han Sun-Young, Miyoun Yoo, Gyu Hwan Yon, Eungbin Kim, Chong-Ock Lee and Sang-Un Choi
Cancer Res May 1 2009 (69) (9 Supplement) 2658;
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Cancer Research Online ISSN: 1538-7445
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