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Erythrofordins D and E, two new cassaine-type diterpenes from Erythrophleum suaveolens

  1. Author:
    Grkovic, Tanja
    Evans, Jason
    Akee, Rhone
    Guo, Liang
    Davis, Myrtle
    Jato, Johnson
    Grothaus, Paul
    Gottholm Ahalt, Michelle
    Hollingshead, Melinda
    Collins, Jerry
    Newman, Dave
    O'Keefe, Barry
  2. Author Address

    NCI, Nat Prod Support Grp, Leidos Biomed Res Inc, Frederick Natl Lab Canc Res, Frederick, MD 21702 USA.Frederick Natl Lab Canc Res, Data Management Serv Inc, Frederick, MD 21702 USA.NCI, Nat Prod Branch, Dev Therapeut Program, Div Canc Treatment & Diag, Frederick, MD 21702 USA.NCI, Lab Invest Toxicol, Leidos Biomed Res Inc, Frederick Natl Lab Canc Res, Frederick, MD 21702 USA.NCI, Toxicol & Pharmacol Branch, Dev Therapeut Program, Bethesda, MD 20892 USA.Univ Yaounde, Fac Med & Biomed Sci, BP 92, Yaounde, Cameroon.NCI, Biol Testing Branch, Dev Therapeut Program, Div Canc Treatment & Diag, Frederick, MD 21702 USA.NCI, Dev Therapeut Program, Div Canc Treatment & Diag, Frederick, MD 21702 USA.NCI, Mol Targets Program, Ctr Canc Res, Frederick, MD 21702 USA.
    1. Year: 2019
    2. Date: Jan 15
    3. Epub Date: 2018 12 10
  1. Journal: Bioorganic & medicinal chemistry letters
  2. PERGAMON-ELSEVIER SCIENCE LTD,
    1. 29
    2. 2
    3. Pages: 134-137
  3. Type of Article: Article
  4. ISSN: 0960-894X
  1. Abstract:

    Two new cassaine-type diterpenoids, namely erythrofordins D (1) and E (2), sourced from a Cameroon collection of Erythrophleum suaveolens were isolated and assessed for anti-tumor activity. In the NCI-60 cancer cell assay, erythrofordins D (1) and E (2) were found to be cytotoxic in the low micro molar ranges with a mean GI(50) value of 2.45 and 0.71 mu M, mean TGI value of 9.77 and 2.29 mu M, and a mean LC50 of 26.92 and 11.48 mu M for 1 and 2 respectively. Using the COMPARE algorithm, the new compounds were found to have similar NCI-60 response profiles to the known cardiac glycosides hyrcanoside and strophanthin. In addition, in an assay examining the viability and contractile function in human cardiomyocytes derived from induced pluripotent stem-cells, erythrofordins showed cardiotoxicity effects at concentrations as low as 0.03 mu g/mL.

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External Sources

  1. DOI: 10.1016/j.bmcl.2018.12.019
  2. PMID: 30553734
  3. WOS: 000454616600002

Library Notes

  1. Fiscal Year: FY2018-2019
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