Your browser doesn't support javascript.
loading
Erythrofordins D and E, two new cassaine-type diterpenes from Erythrophleum suaveolens.
Grkovic, Tanja; Evans, Jason R; Akee, Rhone K; Guo, Liang; Davis, Myrtle; Jato, Johnson; Grothaus, Paul G; Ahalt-Gottholm, Michelle; Hollingshead, Melinda; Collins, Jerry M; Newman, David J; O'Keefe, Barry R.
Afiliação
  • Grkovic T; Natural Products Support Group, Leidos Biomedical Research Inc., Frederick National Laboratory for Cancer Research Sponsored by the National Cancer Institute, Frederick, MD 21702, United States. Electronic address: tanja.grkovic@nih.gov.
  • Evans JR; Data Management Services Inc., Frederick National Laboratory for Cancer Research, Frederick, MD 21702, United States; Natural Products Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, MD 21702, United States.
  • Akee RK; Natural Products Support Group, Leidos Biomedical Research Inc., Frederick National Laboratory for Cancer Research Sponsored by the National Cancer Institute, Frederick, MD 21702, United States.
  • Guo L; Laboratory of Investigative Toxicology, Leidos Biomedical Research Inc., Frederick National Laboratory for Cancer Research Sponsored by the National Cancer Institute, Frederick, MD 21702, United States.
  • Davis M; Toxicology and Pharmacology Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Bethesda, MD 20892, United States.
  • Jato J; Faculty of Medicine and Biomedical Sciences, B. P. 92, University of Yaounde, Yaounde, Cameroon.
  • Grothaus PG; Natural Products Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, MD 21702, United States.
  • Ahalt-Gottholm M; Biological Testing Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, MD 21702, United States.
  • Hollingshead M; Biological Testing Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, MD 21702, United States.
  • Collins JM; Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, MD 21702, United States.
  • Newman DJ; Natural Products Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, MD 21702, United States.
  • O'Keefe BR; Natural Products Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, MD 21702, United States; Molecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, United States. Electronic add
Bioorg Med Chem Lett ; 29(2): 134-137, 2019 01 15.
Article em En | MEDLINE | ID: mdl-30553734
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 GI50 value of 2.45 and 0.71 µM, mean TGI value of 9.77 and 2.29 µM, and a mean LC50 of 26.92 and 11.48 µM 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 µg/mL.
Assuntos
Palavras-chave

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Caesalpinia / Miócitos Cardíacos / Diterpenos Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Caesalpinia / Miócitos Cardíacos / Diterpenos Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article