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A New Hypoxia Inducible Factor-2 Inhibitory Pyrrolinone Alkaloid from Roots and Stems of Piper sarmentosum

  1. Author:
    Bokesch, H. R.
    Gardella, R. S.
    Rabe, D. C.
    Bottaro, D. P.
    Linehan, W. M.
    McMahon, J. B.
    McKee, T. C.

  2. Author Address

    [Bokesch, HR; Gardella, RS; McMahon, JB; McKee, TC] NCI, Mol Targets Lab, Ctr Canc Res, Frederick, MD 21702 USA. [Bokesch, HR; Gardella, RS] NCI, SAIC Frederick Inc, Frederick, MD 21702 USA. [Rabe, DC; Bottaro, DP; Linehan, WM] NCI, Urol Oncol Branch, Ctr Canc Res, Bethesda, MD 21702 USA.;McKee, TC (reprint author), NCI, Mol Targets Lab, Ctr Canc Res, Frederick, MD 21702 USA;mckeeta@mail.nih.gov
    1. Year: 2011
    2. Date: Sep
  2. Journal: Chemical & Pharmaceutical Bulletin
    1. 59
    2. 9
    3. Pages: 1178-1179
  4. Type of Article: Article
  5. ISSN: 0009-2363
  1. Abstract:

    A new trimethoxycinnamoyl-2-pyrrolinone alkaloid, langkamide (1), along with the known compounds piplartine (2) and 3,4,5-trimethoxycinnamic acid (3) were isolated from the roots and stems of the shrub Piper sarmentosum ROXB. The structures were established by spectroscopic analyses and comparison of their spectral data with values reported in the literature. The compounds were tested for their ability to modulate hypoxia inducible factor-2 (HIF-2) transcription activity and all three showed HIF-2 inhibitory activity with EC(50) values of 14.0, 4.8, and 60.6 mu m, respectively, for compounds 1, 2, and 3.

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External Sources

  1. View record in Web of Science®
  2. WOS: 000294387500019

Library Notes

  1. Fiscal Year: FY2011-2012
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