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Erythrofordins D and E, two new cassaine-type diterpenes from Erythrophleum suaveolens.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-12-10 , DOI: 10.1016/j.bmcl.2018.12.019
Tanja Grkovic 1 , Jason R Evans 2 , Rhone K Akee 1 , Liang Guo 3 , Myrtle Davis 4 , Johnson Jato 5 , Paul G Grothaus 6 , Michelle Ahalt-Gottholm 7 , Melinda Hollingshead 7 , Jerry M Collins 8 , David J Newman 6 , Barry R O'Keefe 9
Affiliation  

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.

中文翻译:


Erythrofordins D 和 E,是来自 Erythrophleum suaveolens 的两种新的木薯碱型二萜。



分离并评估了两种新的木薯碱型二萜类化合物,即 erythrofordins D (1) 和 E (2),它们源自喀麦隆的 Erythrophleum suaveolens 收藏品,并评估了其抗肿瘤活性。在 NCI-60 癌细胞测定中,发现赤霉素 D (1) 和 E (2) 在低微摩尔范围内具有细胞毒性,平均 GI50 值为 2.45 和 0.71 µM,平均 TGI 值为 9.77 和 2.29 µM, 1 和 2 的平均 LC50 分别为 26.92 和 11.48 µM。使用 COMPARE 算法,发现新化合物与已知的强心苷 hyrcanoside 和 stropanthin 具有相似的 NCI-60 响应曲线。此外,在一项检查源自诱导多能干细胞的人心肌细胞的活力和收缩功能的测定中,赤霉素在浓度低至 0.03 µg/mL 时显示出心脏毒性作用。
更新日期:2018-12-10
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