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

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.

SUBMITTER: Grkovic T 

PROVIDER: S-EPMC6330894 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature

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

Grkovic Tanja T   Evans Jason R JR   Akee Rhone K RK   Guo Liang L   Davis Myrtle M   Jato Johnson J   Grothaus Paul G PG   Ahalt-Gottholm Michelle M   Hollingshead Melinda M   Collins Jerry M JM   Newman David J DJ   O'Keefe Barry R BR  

Bioorganic & medicinal chemistry letters 20181210 2

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<sub>50</sub> value of 2.45 and 0.71 µM, mean TGI value of 9.77 and 2.29 µM, and a mean LC<sub>50</sub> of 26.92 and 11.48 µM for 1 and 2 respectively. Using the COMPARE algor  ...[more]

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