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Flavonoids from Eight Tropical Plant Species That Inhibit the Multidrug Resistance Transporter ABCG2

  1. Author:
    Versiani, M. A.
    Diyabalanage, T.
    Ratnayake, R.
    Henrich, C. J.
    Bates, S. E.
    McMahon, J. B.
    Gustafson, K. R.
  2. Author Address

    [Versiani, Muhammad Ali; Diyabalanage, Thushara; Ratnayake, Ranjala; Henrich, Curtis J.; McMahon, James B.; Gustafson, Kirk R.] NCI Frederick, Mol Targets Lab, Ctr Canc Res, Frederick, MD 21702 USA. [Henrich, Curtis J.] NCI Frederick, SAIC Frederick, Frederick, MD 21702 USA. [Bates, Susan E.] NCI, Med Oncol Branch, Ctr Canc Res, Bethesda, MD 20892 USA.;Gustafson, KR, NCI Frederick, Mol Targets Lab, Ctr Canc Res, Frederick, MD 21702 USA.;gustafki@mail.nih.gov
    1. Year: 2011
    2. Date: Feb
  1. Journal: Journal of Natural Products
    1. 74
    2. 2
    3. Pages: 262-266
  2. Type of Article: Article
  3. ISSN: 0163-3864
  1. Abstract:

    Overexpression of ABCG2, a membrane-bound multidrug transporter, can make tumor cells resistant to treatment with conventional chemotherapeutic agents. A high-throughput screening effort with the NCI repository of natural product extracts revealed that eight tropical plant extracts significantly inhibited the function of ABCG2. This activity was tracked throughout the extract fractionation process to a series of ABCG2 inhibitory flavonoids (1-13). Their structures were identified by a combination of NMR, mass spectrometry, and circular dichroism studies, and this resulted in the elucidation of (2S)-5,7,3'-trihydroxy-4'-methoxy-8-(3 ''-methylbut-2 ''-enyl)-flavonone (1), (2S)-5,7,3',5'-tetrahydroxy-8-[3 '',8 ''-dimethylocta-2 ''(E),7 ''-dienyl]flavonone (3), and 5,7,3'-trihydroxy-3,5'-dimethoxy-2'-(3'-methylbut-2-enyl)flavone (12,) as new compounds.

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External Sources

  1. DOI: 10.1021/np100797y
  2. WOS: 000287637300022

Library Notes

  1. Fiscal Year: FY2010-2011
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