A library of extracted natural materials (Korea Bioactive Natural Material Bank) have been screened to discover candidates for the treatment of non-alcoholic liver disease (NAFLD), and the 70% ethanol extract of Sicyos angulatus was found to inhibit hepatic lipid accumulation. Bioassay-guided fractionation of this bioactive extract yielded five previously undescribed flavonoid glycosides and one previously undescribed flavonolignan glycoside along with seven known flavonoid glycosides. The chemical structures of these compounds were elucidated by a combination of extensive spectroscopic analysis, including MS, NMR and UV techniques. Eight compounds of all isolated compounds showed inhibitory effects on the lipid accumulation induced by high concentrations of palmitic acid and glucose in HepG2 cells. Four selected compounds were tested for lipid content in a dose-dependent manner (10, 20 and 40 μM), and among those compounds, kaempferol 3-O-β-d-glucopyranosyl-7-O-α-l-rhamnopyranoside showed the strongest inhibition of hepatic lipid production in HepG2 cells. In an oil-red O staining assay, five compounds were shown to reduce hepatic lipid accumulation better than what was observed in the vehicle control group. The present study suggests a new class of chemical entities for developing bioactive agents for the treatment of diseases caused by fat accumulation in the liver.

中文翻译：

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角鲀黄酮苷及其对肝脏脂质积累的抑制作用

已经筛选了提取的天然材料库（韩国生物活性天然材料库）以发现治疗非酒精性肝病 (NAFLD) 的候选药物，并且发现 70% 的长角海参的乙醇提取物可抑制肝脏脂质积累。这种生物活性提取物的生物测定引导分馏产生了五种以前未描述的黄酮苷和一种以前未描述的黄酮木脂素苷以及七种已知的黄酮苷。这些化合物的化学结构通过广泛的光谱分析（包括 MS、NMR 和 UV 技术）的组合阐明。所有分离化合物中的八种化合物对高浓度棕榈酸和葡萄糖在 HepG2 细胞中诱导的脂质积累显示出抑制作用。以剂量依赖性方式（10、20 和 40 μM）测试了四种选定化合物的脂质含量，在这些化合物中，山奈酚 3-O-β-d-吡喃葡萄糖基-7-O-α-l-rhamnopyranoside 显示出对 HepG2 细胞中肝脏脂质产生的最强抑制。在油红 O 染色试验中，五种化合物显示出比在载体对照组中观察到的更好地减少肝脏脂质积累。本研究提出了一类新的化学实体，用于开发生物活性剂，用于治疗由肝脏脂肪堆积引起的疾病。与在载体对照组中观察到的相比，五种化合物显示出更好地减少肝脏脂质积累。本研究提出了一类新的化学实体，用于开发生物活性剂，用于治疗由肝脏脂肪堆积引起的疾病。与在载体对照组中观察到的相比，五种化合物显示出更好地减少肝脏脂质积累。本研究提出了一类新的化学实体，用于开发生物活性剂，用于治疗由肝脏脂肪堆积引起的疾病。