An acylated flavonol glycoside, trans-tiliroside (1), is found in certain parts of different herbs, including the seeds of Rosa canina (Rosaceae). Previous studies on compound 1 have focused on triglyceride (TG) metabolism, including its anti-obesity and intracellular TG reduction effects. In the present study, the effects of compound 1 on cholesterol (CHO) metabolism were investigated using human hepatocellular carcinoma-derived HepG2 cells and mice. Compound 1 decreased CHO secretion in HepG2 cells, which was enhanced by mevalonate in a concentration-dependent manner and decreased the secretion of apoprotein B (apoB)-100, a marker of very low-density lipoprotein (VLDL). Compound 1 also inhibited the activity of microsomal triglyceride transfer proteins, which mediate VLDL formation from cholesterol and triglycerides in the liver. In vivo, compound 1 inhibited the accumulation of Triton WR-1339-induced TG in the blood of fasted mice and maintained low levels of apoB-100. These results suggest that compound 1 inhibits the secretion of CHO as VLDL from the liver and has the potential for use for the prevention of dyslipidemia.

Graphical abstract

中文翻译：

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反式替罗甙对HepG2细胞和小鼠肝脏极低密度脂蛋白分泌的抑制作用

一种酰化黄酮醇糖苷，反式-tiliroside ( 1 )，存在于不同草药的某些部分，包括犬蔷薇（蔷薇科）的种子。先前对化合物1 的研究主要集中在甘油三酯 (TG) 代谢，包括其抗肥胖和细胞内 TG 降低作用。在本研究中，使用人肝细胞癌衍生的 HepG2 细胞和小鼠研究了化合物1对胆固醇 (CHO) 代谢的影响。化合物1减少 HepG2 细胞中的 CHO 分泌，甲羟戊酸以浓度依赖性方式增强这种分泌，并减少脱辅基蛋白 B (apoB)-100（极低密度脂蛋白 (VLDL) 的标志物）的分泌。化合物1还抑制微粒体甘油三酯转移蛋白的活性，该蛋白介导肝脏中胆固醇和甘油三酯形成 VLDL。在体内，化合物1抑制 Triton WR-1339 诱导的 TG 在禁食小鼠血液中的积累，并维持较低的 apoB-100 水平。这些结果表明，化合物1抑制肝脏以VLDL形式分泌CHO，并具有用于预防血脂异常的潜力。

图形概要