Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China.
Mar Drugs. 2018 Jan 12;16(1):25. doi: 10.3390/md16010025.
Seven new polyketides, named tanzawaic acids R-X (-, ), along with seven known analogues (- and -), were isolated from HDN13-279. Their structures, including the absolute configurations, were elucidated by NMR, MS, X-ray diffraction, circular dichroism (CD) analyses and chemical derivatization. Five compounds (, , , and ) significantly decreased the oleic acid (OA)-elicited lipid accumulation in HepG2 liver cells at the concentration of 10 μM, among which, four compounds (, , and ) significantly decreased intracellular total cholesterol (TC) levels and three Compounds (, , and ) significantly decreased intracellular triglyceride (TG) levels. Moreover, the TG-lowering capacities of compounds and were comparable with those of simvastatin, with the TG levels being nearly equal to blank control. This is the first report on the lipid-lowering activity of tanzawaic acid derivatives.
从 HDN13-279 中分离得到 7 个新的聚酮化合物，命名为坦扎瓦酸 R-X (-, )，以及 7 个已知类似物 (- 和 -)。通过 NMR、MS、X 射线衍射、圆二色性 (CD) 分析和化学衍生化等方法阐明了它们的结构，包括绝对构型。在 10 μM 的浓度下，有 5 种化合物 (,,, 和 ) 显著降低了油酸 (OA) 诱导的 HepG2 肝细胞内脂质积累，其中 4 种化合物 (,, 和 ) 显著降低了细胞内总胆固醇 (TC) 水平，3 种化合物 (,, 和 ) 显著降低了细胞内甘油三酯 (TG) 水平。此外，化合物 和 的降低 TG 能力与辛伐他汀相当，TG 水平几乎与空白对照相等。这是坦扎瓦酸衍生物具有降脂活性的首次报道。
