| Literature DB >> 30553734 |
Tanja Grkovic1, Jason R Evans2, Rhone K Akee3, Liang Guo4, Myrtle Davis5, Johnson Jato6, Paul G Grothaus7, Michelle Ahalt-Gottholm8, Melinda Hollingshead8, Jerry M Collins9, David J Newman7, Barry R O'Keefe10.
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.Entities:
Keywords: COMPARE; Cardiotoxicity; Erythrofordin; NCI-60; Natural product
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Year: 2018 PMID： 30553734 PMCID： PMC6330894 DOI： 10.1016/j.bmcl.2018.12.019
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823