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

Basic Information

ID: ALA4371064

Journal: Bioorg Med Chem Lett

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

Authors: Grkovic T, Evans JR, Akee RK, Guo L, Davis M, Jato J, Grothaus PG, Ahalt-Gottholm M, Hollingshead M, Collins JM, Newman DJ, O'Keefe BR.

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.

CiteXplore: 30553734

DOI: 10.1016/j.bmcl.2018.12.019

Patent ID: