Academy of Integrative Medicine, College of Pharmacy, Department of Biochemistry and Molecular Biology, Dalian Medical University, Dalian 116044, People's Republic of China.
Academy of Integrative Medicine, College of Pharmacy, Department of Biochemistry and Molecular Biology, Dalian Medical University, Dalian 116044, People's Republic of China.
Bioorg Chem. 2018 Apr;77:471-477. doi: 10.1016/j.bioorg.2018.02.007. Epub 2018 Feb 12.
Euphorbia ebracteolata was a natural medicine for the treatment of tuberculosis. The present work has performed the investigation of bioactive chemical substances from the roots of E. ebracteolata. Using various chromatographic techniques, 15 compounds were obtained from the roots of E. ebracteolata. On the basis of widely spectroscopic data analyses, the isolated compounds were determined to be diterpenoids, including rosane derivatives (1-12), isopimarane (13), abietane (14), and lathyrane (15), among which compounds 1-4, and 9 were undescribed previously. The inhibitory effects of isolated diterpenoids against Mycobacterium tuberculosis were evaluated using an Alamar blue cell viability assay. And two rosane-type diterpenoids 3 and 8 displayed moderate inhibitory effects on with the MIC values of 18 μg/mL and 25 μg/mL, respectively. For the potential inhibitor 3, the inhibitory effect against the target enzyme GlmU was evaluated, which displayed a moderate inhibitory effect with the IC 12.5 μg/mL. Therefore, the diterpenoids from the roots of E. ebracteolata displayed anti-tuberculosis effects, which would be pay more attentions for the anti-tuberculosis agents.
麻叶Euphorbia ebracteolata 是一种治疗肺结核的天然药物。本工作对麻叶Euphorbia ebracteolata 的根的生物活性化学成分进行了研究。采用各种色谱技术，从麻叶Euphorbia ebracteolata 的根中得到了 15 种化合物。根据广泛的光谱数据分析，分离得到的化合物被确定为二萜类化合物，包括 Rosane 衍生物（1-12）、异松脂烷（13）、松香烷（14）和拉坦烷（15），其中化合物 1-4 和 9 以前未被描述过。采用 Alamar blue 细胞活力测定法评价分离得到的二萜类化合物对结核分枝杆菌的抑制作用。两种 Rosane 型二萜类化合物 3 和 8 对 MIC 值分别为 18μg/mL 和 25μg/mL 的结核分枝杆菌具有中等抑制作用。对于潜在的抑制剂 3，评估了其对靶酶 GlmU 的抑制作用，结果显示其对 GlmU 的抑制作用 IC 12.5μg/mL。因此，麻叶Euphorbia ebracteolata 的根中二萜类化合物具有抗结核作用，可能成为抗结核药物的研究热点。
