Details

Autor(en) / Beteiligte

• 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.

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2019-01, Vol.29 (2), p.134-137

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2019

Quelle

ScienceDirect

Beschreibungen/Notizen

• [Display omitted] 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.