Martin-Luther-University Halle-Wittenberg Organic Chemistry, Kurt-Mothes-Str. 2, D-06120, Halle (Saale), Germany.
University of Innsbruck, Institute of Pharmacy/Pharmacognosy, Center for Molecular Biosciences Innsbruck (CMBI), Center for Chemistry and Biomedicine, Innrain 80-82, A-6020, Innsbruck, Austria.
Eur J Med Chem. 2019 Oct 15;180:457-464. doi: 10.1016/j.ejmech.2019.07.049. Epub 2019 Jul 16.
Depending on the conditions of the reactions, maslinic acid can be converted into the corresponding 2-O-, 3-O-, or 2,3-di-O-acylated compounds in good yields. These compounds showed in SRB assays a significantly increased cytotoxicity as compared to the parent compound maslinic acid. For the most active compound of this series, i.e. 2-O-(2-chlorobenzoyl) maslinic acid (5), more detailed cell biological tests (i.e. AO/PI dye exclusion experiments, an annexin V assay, and microscopic investigations) on A2780 (human ovarian carcinoma cells) revealed that this compound triggers apoptosis.
根据反应条件的不同，齐墩果酸可以转化为相应的 2-O-、3-O-或 2,3-二酰化化合物，收率良好。与母体化合物齐墩果酸相比，这些化合物在 SRB 测定中表现出明显增加的细胞毒性。对于该系列中最活跃的化合物，即 2-O-(2-氯苯甲酰基)齐墩果酸（5），对 A2780（人卵巢癌细胞）进行了更详细的细胞生物学测试（即 AO/PI 染料排除实验、Annexin V 测定和显微镜研究），表明该化合物触发了细胞凋亡。
