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Issue 16, 2010
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Constituents of Amoora cucullata with TRAIL resistance-overcoming activity

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Abstract

In search of bioactive natural products for overcoming TRAIL resistance from natural resources, we previously reported a number of active compounds. Bioassay-guided fractionation of mangrove, Amoora cucullata, collected from Sundarbans Mangrove Forest, Bangladesh, led to the isolation of four new compounds (1–4), along with seven known compounds (5–11). Of the isolates, compounds 1, 5, 8, and 9 showed TRAIL resistance-overcoming activity, among which 8 showed the most potent activity and enhanced TRAIL-induced apoptosis in TRAIL-resistant human gastric adenocarcinoma (AGS) cells through the activation of caspase-3/7, enhancing the expression of DR4 and DR5 mRNA in AGS cells. Cell death caused by the combined treatment of 8 and TRAIL was inhibited by human recombinant DR5/Fc and DR4/Fc chimera proteins, indicating that 8 sensitizes TRAIL-resistant AGS cells to TRAIL through the induction of DR4 and DR5.

Graphical abstract: Constituents of Amoora cucullata with TRAIL resistance-overcoming activity

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Publication details

The article was received on 06 Apr 2010, accepted on 03 Jun 2010 and first published on 23 Jun 2010


Article type: Paper
DOI: 10.1039/C004927A
Citation: Org. Biomol. Chem., 2010,8, 3696-3703
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    Constituents of Amoora cucullata with TRAIL resistance-overcoming activity

    F. Ahmed, K. Toume, S. K. Sadhu, T. Ohtsuki, M. A. Arai and M. Ishibashi, Org. Biomol. Chem., 2010, 8, 3696
    DOI: 10.1039/C004927A

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