红厚壳中的两个新卡莎烷型二萜 Erythrofordins D 和 E。
Erythrofordins D and E, two new cassaine-type diterpenes from Erythrophleum suaveolens.
机构信息
Natural Products Support Group, Leidos Biomedical Research Inc., Frederick National Laboratory for Cancer Research Sponsored by the National Cancer Institute, Frederick, MD 21702, United States.
Data Management Services Inc., Frederick National Laboratory for Cancer Research, Frederick, MD 21702, United States; Natural Products Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Frederick, MD 21702, United States.
出版信息
Bioorg Med Chem Lett. 2019 Jan 15;29(2):134-137. doi: 10.1016/j.bmcl.2018.12.019. Epub 2018 Dec 10.
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 value of 2.45 and 0.71 µM, mean TGI value of 9.77 and 2.29 µM, and a mean LC 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.
两种新的卡山烷型二萜类化合物，即 erythrofordins D（1）和 E（2），来源于喀麦隆收集的非洲铁木 Erythrophleum suaveolens，被分离并评估其抗肿瘤活性。在 NCI-60 癌细胞测定中，erythrofordins D（1）和 E（2）在低微摩尔范围内具有细胞毒性，平均 GI 值分别为 2.45 和 0.71 µM，平均 TGI 值分别为 9.77 和 2.29 µM，平均 LC 值分别为 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 strophanthin 具有相似的 NCI-60 反应谱。此外，在一项检查源自诱导多能干细胞的人心肌细胞活力和收缩功能的测定中，erythrofordins 在低至 0.03 µg/mL 的浓度下显示出心脏毒性作用。
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