School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; State Key Laboratory of Southwestern Chinese Medicine Resources, 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.
Bioorg Chem. 2021 Oct;115:105252. doi: 10.1016/j.bioorg.2021.105252. Epub 2021 Aug 8.
Twelve tetrahydrofuran lignans (1-12), including six new compounds (1-6), were isolated from the 70% EtOH extract of the fruits of Leonurus japonicus. Spectroscopic analyses and ECD and OR calculations were used to determine their structures. Compounds 5 and 6 were unusual alkaloidal lignans with a butyrolactam unit. Based on the beneficial effects of the fruits of L. japonicus (Chongweizi in Chinese) on the liver in traditional Chinese medicine (TCM), the hepatocyte protective activities of the isolates were studied by MTT, Hoechst 33,342 staining, and western blotting. The MTT results revealed that compounds 1, 2, 7, and 8 significantly increased the survival rates of HL-7702 cells injured by acetaminophen, with EC values of 10.41 ± 0.90 μM, 19.86 ± 3.13 μM, 9.68 ± 1.93 μM, and 21.35 ± 3.58 μM, respectively. In the Hoechst 33,342 fluorescence staining, compounds 1 and 7 suppressed the apoptosis of the injured HL-7702 cells. Furthermore, the western blot analysis showed that compounds 1 and 7 increased the Bcl-2/Bax protein expression ratio and procaspase-3 protein expression, indicating that compounds 1 and 7 may exert hepatoprotective activity by regulating the mitochondrial apoptotic pathway.
从益母草的 70%乙醇提取物中分离得到了 12 种四氢呋喃木脂素（1-12），包括 6 种新化合物（1-6）。通过光谱分析和 ECD 和 OR 计算确定了它们的结构。化合物 5 和 6 是具有丁内酯单元的不寻常的生物碱木脂素。根据益母草（Chongweizi 在中文中的名称）在中国传统医学中对肝脏的有益作用，通过 MTT、Hoechst 33,342 染色和 Western blot 研究了分离物的肝细胞保护活性。MTT 结果表明，化合物 1、2、7 和 8 显著提高了对乙酰氨基酚损伤的 HL-7702 细胞的存活率，EC 值分别为 10.41±0.90μM、19.86±3.13μM、9.68±1.93μM 和 21.35±3.58μM。在 Hoechst 33,342 荧光染色中，化合物 1 和 7 抑制了损伤的 HL-7702 细胞的凋亡。此外，Western blot 分析表明，化合物 1 和 7 增加了 Bcl-2/Bax 蛋白表达比和 procaspase-3 蛋白表达，表明化合物 1 和 7 可能通过调节线粒体凋亡途径发挥肝细胞保护活性。
