New lignans from the fruits of Leonurus japonicus and their hepatoprotective activities
| Autor: | Yu-Lin He, Fang Peng, Fei Liu, Sheng Lin, Zhi-Hao Tian, Jin-Feng Chen, Hong-Zhen Shu, Cheng Peng, Liang Xiong |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Apoptosis
Protective Agents Biochemistry Lignans Cell Line Structure-Activity Relationship Western blot Drug Discovery medicine Humans Molecular Biology EC50 medicine.diagnostic_test biology Traditional medicine Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry Leonurus japonicus biology.organism_classification Staining Acetaminophen Blot medicine.anatomical_structure Leonurus Hepatocyte Fruit Hepatocytes medicine.drug |
| Zdroj: | Bioorganic chemistry. 115 |
| ISSN: | 1090-2120 |
| Popis: | 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 EC50 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. |
| Databáze: | OpenAIRE |
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