Faculty of Pharmaceutical Sciences, Toho University, Miyama 2-2-1, Funabashi, Chiba, 274-8510, Japan.
School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, 110016, People's Republic of China.
J Nat Med. 2021 Sep;75(4):1058-1066. doi: 10.1007/s11418-021-01551-9. Epub 2021 Jul 21.
Macrocyclic daphnane orthoesters (MDOs) have attracted significant research interest for the drug discovery to cure HIV infection based on the "Shock and Kill" strategy. In the present study, the first chemical study on Wikstroemia ligustrina (Thymelaeaceae) was carried out by LC-MS analysis and phytochemical investigation. Nine daphnane diterpenoids (1-9) including seven MDOs were detected by LC-MS analysis. Further phytochemical investigation resulted in the isolation and structural elucidation of five daphnanes (1, 2, 5, 8, and 9) with potent anti-HIV activity. Taking the isolated MDO (1) as a model compound, the MS/MS fragmentation pathway was also elucidated.
大环达芙烷原酯（MDOs）因其基于“休克和杀伤”策略治疗 HIV 感染的药物发现而引起了极大的研究兴趣。在本研究中，通过 LC-MS 分析和植物化学研究对腊梅科（腊梅科）的腊梅进行了首次化学研究。通过 LC-MS 分析检测到 9 种达芙烷二萜（1-9），包括 7 种 MDOs。进一步的植物化学研究导致分离和结构阐明了具有强大抗 HIV 活性的 5 种达芙烷（1、2、5、8 和 9）。以分离的 MDO（1）为模型化合物，还阐明了 MS/MS 碎裂途径。
