Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
Centre for NMR & Structural Chemistry, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad 500607, India.
Eur J Med Chem. 2017 Aug 18;136:74-84. doi: 10.1016/j.ejmech.2017.04.065. Epub 2017 Apr 24.
A comprehensive re-investigation of aerial parts of Caragana sukiensis resulted in the isolation of twelve compounds (1-12) including three new cycloartane type triterpenoids (3-5) respectively. Chemical structures of the isolated compounds were established by analysis of their IR, HRMSESI, 1D and 2D NMR spectroscopic data. In addition, these compounds were evaluated for their cytotoxic activity against cancer lines (HeLa, A549, MCF-7, DU-145) and Human embryonic kidney cell line (HEK-293). The results indicated that compound 8 showed potent cytotoxic activity against A549 with IC value of 1.54 μM which is comparable to standard drug, doxorubicin. Further, flow cytometric analysis showed that compound 8 arrested the cell cycle in the Go/G1 phase leading to apoptotic cell death. In addition, Hoechst 33258 staining, Annexin V-FITC assay and measurement of mitochondrial membrane potential also suggested that 8 induced cell death by apoptosis. Further, all the isolates were also screened for their antifeedant and insecticidal activity against tobacco caterpillar (Spodoptera litura), using no-choice leaf disk method. Among screened compounds 1, 3, 4, and 6 showed potent antifeedancy with ED values of 0.59, 1.19, 0.67, and 1.68 μg/cm. Overall, this study identified a novel class of cycloartane tritepenoids as potent cyotoxic agents as well as antifeedants.
对锦鸡儿属植物的地上部分进行了全面的再研究，结果分离得到了 12 种化合物（1-12），包括 3 种新型环阿屯烷型三萜类化合物（3-5）。通过分析它们的 IR、HRMSESI、1D 和 2D NMR 波谱数据，确定了分离化合物的化学结构。此外，还评估了这些化合物对癌细胞系（HeLa、A549、MCF-7、DU-145）和人胚肾细胞系（HEK-293）的细胞毒性活性。结果表明，化合物 8 对 A549 具有很强的细胞毒性活性，IC 值为 1.54 μM，与标准药物阿霉素相当。此外，流式细胞术分析表明，化合物 8 将细胞周期阻滞在 G0/G1 期，导致细胞凋亡。此外，Hoechst 33258 染色、Annexin V-FITC 检测和线粒体膜电位测量也表明，8 通过凋亡诱导细胞死亡。此外，还采用非选择性叶盘法，对所有分离物进行了对烟草夜蛾（Spodoptera litura）的拒食和杀虫活性筛选。在所筛选的化合物 1、3、4 和 6 中，具有 0.59、1.19、0.67 和 1.68 μg/cm 的 ED 值，表现出很强的拒食活性。总的来说，这项研究发现了一类新型的环阿屯烷三萜类化合物，它们具有很强的细胞毒性活性和拒食活性。
