Shen Yi, Cui Shu-Jun, Chen Hao, Shen Lei, Wang Min, Dong Xiang, Xiao Chao-Jiang, Jiang Bei
J Nat Prod. 2020 Apr 24;83(4):927-936. doi: 10.1021/acs.jnatprod.9b00761. Epub 2020 Apr 1.
Eleven new angeloylated eudesmane sesquiterpenoids, dobinins D-N (, , , , , , and -), and four known compounds (, , , and ) were isolated from the roots of . A new oxidation product () was also obtained from dobinin H (). Their structures were elucidated by spectroscopic data and single-crystal X-ray diffraction analyses. Dobinins K-N (-) are the first examples of rearrangement noreudesmane analogue sesquiterpenoids with a unique 6/5-fused carbon skeleton. A putative biosynthetic pathway of compounds - is proposed. Compound exhibited significant antimalarial activity superior to artemisinin with the inhibition ratio of 59.1%, and compounds , , and exhibited moderate antimalarial activities against BY265RFP with inhibition ratios ranging from 14.5% to 18.5% at a dose of 30 mg/kg/day. In addition, the apoptosis of BY265RFP by the depolarization of mitochondrial membrane potential with striking ROS production, after parasitized erythrocyte lysis mediated by cytokines IL-12 and IFN-γ, may be a possible mechanism of antimalarial action of compound against BY265RFP.
从[植物名称]的根部分离出了11种新的当归酰化桉叶烷倍半萜类化合物，多宾宁D - N（[具体化合物名称1]、[具体化合物名称2]、[具体化合物名称3]、[具体化合物名称4]、[具体化合物名称5]、[具体化合物名称6]、[具体化合物名称7]和[具体化合物名称8]），以及4种已知化合物（[具体化合物名称9]、[具体化合物名称10]、[具体化合物名称11]和[具体化合物名称12]）。还从多宾宁H（[具体化合物名称]）中获得了一种新的氧化产物（[具体化合物名称]）。通过光谱数据和单晶X射线衍射分析阐明了它们的结构。多宾宁K - N（[具体化合物名称5] - [具体化合物名称8]）是具有独特6/5稠合碳骨架的重排去甲桉叶烷类似物倍半萜类化合物的首个实例。提出了化合物[具体化合物名称1] - [具体化合物名称8]的推测生物合成途径。化合物[具体化合物名称1]表现出显著的抗疟活性，优于青蒿素，抑制率为59.1%，化合物[具体化合物名称2]、[具体化合物名称3]和[具体化合物名称4]在剂量为30 mg/kg/天时，对[疟原虫名称]BY265RFP表现出中等抗疟活性，抑制率在14.5%至18.5%之间。此外，在细胞因子IL - 12和IFN - γ介导的被寄生红细胞裂解后，通过线粒体膜电位去极化并产生大量活性氧导致[疟原虫名称]BY265RFP凋亡，可能是化合物[具体化合物名称1]对[疟原虫名称]BY265RFP抗疟作用的一种可能机制。
