Wang Xiao-Ya, Zhou Qin-Mei, Guo Li, Dai Ou, Meng Chun-Wang, Miao Lu-Lin, Liu Jie, Lin Qiao, Peng Cheng, Xiong Liang
School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; Institute of Innovative Medicine Ingredients of Southwest Specialty Medicinal Materials, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.
School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; Institute of Innovative Medicine Ingredients of Southwest Specialty Medicinal Materials, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; Innovative Institute of Chinese Medicine and Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
Fitoterapia. 2021 Mar;149:104822. doi: 10.1016/j.fitote.2020.104822. Epub 2020 Dec 31.
Fuzi, a well-known traditional Chinese medicine developed from the lateral roots of Aconitum carmichaelii Debx., has been widely used for the treatment of heart failure. In order to search for active compounds from Fuzi, a phytochemical study was performed, which resulted in the isolation of 14 aminoalcohol-diterpenoid alkaloids, including one new compound (1). Their cardioprotective effects against doxorubicin-induced toxicity in H9c2 cells were evaluated. All of the alkaloids showed cardioprotective effects in a nonmonotonic concentration-response manner, with the maximum protection rates ranging from 17.96 ± 2.93% to 98.31 ± 0.35%. Compound 5 exhibited the most potent cardioprotective activity. Taking the maximum protection rate as an indicator, the preliminary structure-activity relationship analysis indicated that the substitutions of C-1, C-13, C-15, C-16, and N and the configurations of OMe-6 and OH-15 are important structural features for the cardioprotective activities of the aminoalcohol-diterpenoid alkaloids.
附子是一种由乌头的侧根所制的著名中药，已被广泛用于治疗心力衰竭。为了从附子中寻找活性化合物，开展了一项植物化学研究，从中分离出14种氨基醇二萜生物碱，包括一种新化合物（1）。评估了它们对阿霉素诱导的H9c2细胞毒性的心脏保护作用。所有生物碱均以非单调浓度 - 反应方式表现出心脏保护作用，最大保护率在17.96±2.93%至98.31±0.35%之间。化合物5表现出最强的心脏保护活性。以最大保护率为指标，初步的构效关系分析表明，C-1、C-13、C-15、C-16和N的取代以及OMe-6和OH-15的构型是氨基醇二萜生物碱心脏保护活性的重要结构特征。
