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Crystal Structures and Human Leukemia Cell Apoptosis Inducible Activities of Parthenolide Analogues Isolated from Piptocoma rufescens

The molecular structures of three parthenolide analogues, (−)-goyazensolide (1), (−)-15-deoxygoyazensolide (2), and (−)-ereglomerulide (3), isolated from the leaves of Piptocoma rufescens in a previous study were determined by X-ray analysis, and the absolute configuration of (−)-goyazensolide (1) was confirmed crystallographically using Cu Kα radiation at low temperature. Compounds 1–3, (+)-rufesolide A (4), and commercial parthenolide were found to be growth inhibitory toward MOLM-13 and EOL-1 human acute myeloid leukemia cells using PKC412 (midostaurin) as the positive control, with 1–3 being more active than parthenolide. Also, compounds 1–4 exhibited synergistic effects when tested with PKC412, but parthenolide did not show this type of activity. At a concentration lower than 2.0 μM, both 1 and 2 induced approximately 50% of the cells to become apoptotic at a late stage of the cell cycle, but no similar apoptotic effects were observed for 3, 4, or parthenolide. Leukemia cell apoptosis was induced by ...

Authors:   Yulin Ren; Judith C. Gallucci; Xinxin Li; Lichao Chen; Jianhua Yu; A. Douglas Kinghorn
Journal:   Journal of Natural Products
Year:   2018
DOI:   10.1021/acs.jnatprod.7b01079
Publication date:   19-Jan-2018
Facts, background information, dossiers
  • crystal structures
  • concentration
  • cells
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