Kokanova-Nedialkova Zlatina, Nedialkov Paraskev, Kondeva-Burdina Magdalena, Simeonova Rumyana, Tzankova Virginia, Aluani Denitsa
Department of Pharmacognosy, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Str., 1000 Sofia, Bulgaria.
Laboratory of drug metabolism and drug toxicity, Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Str., 1000 Sofia, Bulgaria.
Fitoterapia. 2017 Apr;118:13-20. doi: 10.1016/j.fitote.2017.02.001. Epub 2017 Feb 14.
Three new flavonoid glycosides (7-9) named patuletin-3-O-(5″'-О-Е-feruloyl)-β-d-apiofuranosyl(1→2)[β-d-glucopyranosyl (1→6)]-β-d-glucopyranoside (7), spinacetin-3-O-(5″'-О-Е-feruloyl)-β-d-apiofuranosyl (1→2)[β-d-glucopyranosyl(1→6)]-β-d-glucopyranoside (8) and 6-methoxykaempferol-3-O-(5″'-О-Е-feruloyl)-β-d-apiofuranosyl(1→2)[β-d-glucopyranosyl (1→6)]-β-d-glucopyranoside (9) together with six known flavonoid glycosides of patuletin, spinacetin and 6-methoxykaempferol (1-6) were isolated from the aerial parts of C. bonus-henricus and identified with spectroscopic methods (1D and 2D NMR, UV, IR, HRESIMS). The MeOH extract exerts hepatoprotective and antioxidant activities comparable to those of flavonoid complex silymarin in in vitro (60μg/mL) and in vivo (100mg/kg/daily for 7days) models of hepatotoxicity, induced by CCl. Flavonoids (1-9) (100μM), compared to silybin, significantly reduced the cellular damage caused by CCl in rat hepatocytes, preserved cell viability and GSH level, decreased LDH leakage and reduced lipid damage. High concentrations of compounds (1-9) showed marginal or no cytotoxicity on HepG2 cell line. The experiment data suggest that the glycosides of 6-methoxykaempferol, spinacetin and patuletin are a promising and safe class of hepatoprotective agents.
从滨海刺芹地上部分分离得到三种新的黄酮苷（7 - 9），分别命名为紫铆亭 - 3 - O -（5″'- O - E - 阿魏酰基）-β - d - 芹菜呋喃糖基（1→2）[β - d - 吡喃葡萄糖基（1→6）]-β - d - 吡喃葡萄糖苷（7）、菠菜黄素 - 3 - O -（5″'- O - E - 阿魏酰基）-β - d - 芹菜呋喃糖基（1→2）[β - d - 吡喃葡萄糖基（1→6）]-β - d - 吡喃葡萄糖苷（8）和6 - 甲氧基山奈酚 - 3 - O -（5″'- O - E - 阿魏酰基）-β - d - 芹菜呋喃糖基（1→2）[β - d - 吡喃葡萄糖基（1→6）]-β - d - 吡喃葡萄糖苷（9），以及六种已知的紫铆亭、菠菜黄素和6 - 甲氧基山奈酚的黄酮苷（1 - 6），并通过光谱方法（1D和2D NMR、UV、IR、HRESIMS）进行了鉴定。在体外（60μg/mL）和体内（100mg/kg/每日，共7天）由CCl诱导的肝毒性模型中，甲醇提取物表现出与黄酮类化合物复合物水飞蓟宾相当的肝保护和抗氧化活性。与水飞蓟宾相比，黄酮类化合物（1 - 9）（100μM）显著降低了CCl对大鼠肝细胞造成的细胞损伤，维持了细胞活力和谷胱甘肽水平，减少了乳酸脱氢酶泄漏并减轻了脂质损伤。高浓度的化合物（1 - 9）对HepG2细胞系显示出轻微或无细胞毒性。实验数据表明，6 - 甲氧基山奈酚、菠菜黄素和紫铆亭的苷是一类有前景且安全的肝保护剂。
