State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.
J Nat Prod. 2012 Jun 22;75(6):1145-59. doi: 10.1021/np300225t. Epub 2012 May 18.
Twenty-six new diterpenoid alkaloids, 1-26 (1-4: hetisan-type C(20)-diterpenoid alkaloids; 5-26: aconitane C(19)-diterpenoid alkaloids), and two known analogues, hypaconitine 27 and benzoylmesaconine 28, have been isolated from a water extract of the lateral root of Aconitum carmichaelii. Compounds 7 and 8 are rare examples of conformational isomers obtained from the same material. The conformation and conformational transformation of ring A in the C(19)-diterpenoid alkaloids are discussed on the basis of NMR data analysis in combination with single-crystal X-ray crystallography of 6 and 27 by anomalous scattering of Cu Kα radiation. In preliminary analgesic and toxicity assays, the isomer with ring A in the chair conformation (8 or 27) was found to be more active than that with ring A in the boat conformation (7 or 27a). In addition, 15, 16, and 19 showed neuroprotective activity.
从乌头（Aconitum carmichaelii）侧根的水提取物中分离得到了 26 种新的二萜生物碱 1-26（1-4：hetisan 型 C(20)-二萜生物碱；5-26：乌头烷 C(19)-二萜生物碱）和 2 种已知类似物，即 Hypaconitine 27 和 Benzoylmesaconine 28。化合物 7 和 8 是从同一物质中获得的罕见构象异构体实例。根据 NMR 数据分析，并结合单晶 X 射线衍射对 6 和 27 的铜 Kα 辐射异常散射，讨论了 C(19)-二萜生物碱中环 A 的构象和构象转化。在初步的镇痛和毒性试验中，发现具有椅式构象的环 A 的异构体（8 或 27）比具有船式构象的环 A 的异构体（7 或 27a）更具活性。此外，15、16 和 19 表现出神经保护活性。
