Cytotoxic activity of rearranged drimane meroterpenoids against colon cancer cells via down-regulation of β-catenin expression.
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| Abstract |
Colorectal cancer has emerged as a major cause of death in Western countries. Down-regulation of β-catenin expression has been considered a promising approach for cytotoxic drug formulation. Eight 4,9-friedodrimane-type sesquiterpenoids (1-8) were acquired using the oxidative potential of Verongula rigida on bioactive metabolites from two Smenospongia sponges. Compounds 3 and 4 contain a 2,2-dimethylbenzo[d]oxazol-6(2H)-one moiety as their substituted heterocyclic residues, which is unprecedented in such types of meroterpenoids. Gauge-invariant atomic orbital NMR chemical shift calculations were employed to investigate stereochemical details with support of the application of advanced statistics such as CP3 and DP4. Compounds 2 and 8 and the mixture of 3 and 4 suppressed β-catenin response transcription (CRT) via degrading β-catenin and exhibited cytotoxic activity on colon cancer cells, implying that their anti-CRT potential is, at least in part, one of their underlying antineoplastic mechanisms.
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| Authors | In Hyun Hwang, Joonseok Oh, Wei Zhou, Seoyoung Park, Joo-Hyun Kim, Amar G Chittiboyina, Daneel Ferreira, Gyu Yong Song, Sangtaek Oh, MinKyun Na, Mark T Hamann |
| Journal | Journal of natural products (J Nat Prod) Vol. 78 Issue 3 Pg. 453-61 (Mar 27 2015) ISSN: 1520-6025 [Electronic] United States |
| PMID | 25590830 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't) |
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