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桃儿七皂苷对 HepG2 细胞和小鼠肝组织极低密度脂蛋白分泌的抑制作用。

Inhibitory effect of trans-tiliroside on very low-density lipoprotein secretion in HepG2 cells and mouse liver.

机构信息

Pharmaceutical Research and Technology Institute, Kindai University, 3-4-1 Kowakae, Higashi-osaka, Osaka, 577-8502, Japan.

Morishita Jintan Co., Ltd., 11-1 Tsudayamate 2-Chome, Hirakata, Osaka, 573-0128, Japan.

出版信息

J Nat Med. 2024 Jan;78(1):180-190. doi: 10.1007/s11418-023-01756-0. Epub 2023 Nov 16.

DOI:10.1007/s11418-023-01756-0
PMID:37973705
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10764534/
Abstract

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.

摘要

一种酰化黄酮醇糖苷,反式杜鹃素(1),存在于某些不同草药的部分,包括玫瑰果(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)代谢上,包括其抗肥胖和细胞内 TG 减少的作用。在本研究中,使用人肝癌衍生的 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 可降低 HepG2 细胞中 CHO 的分泌,这种作用可被甲羟戊酸浓度依赖性增强,并降低载脂蛋白 B(apoB)-100 的分泌,后者是极低密度脂蛋白(VLDL)的标志物。化合物 1 还抑制了微粒体甘油三酯转移蛋白的活性,后者介导了肝脏中胆固醇和甘油三酯形成 VLDL。在体内,化合物 1 抑制了禁食小鼠中 Triton WR-1339 诱导的 TG 在血液中的积累,并维持 apoB-100 的低水平。这些结果表明,化合物 1 抑制了 CHO 作为 VLDL 从肝脏中的分泌,具有预防血脂异常的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/c483d90862b7/11418_2023_1756_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/22677bd50834/11418_2023_1756_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/92c60250d975/11418_2023_1756_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/47bc5b1b3e15/11418_2023_1756_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/fa52714bc5d0/11418_2023_1756_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/c483d90862b7/11418_2023_1756_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/22677bd50834/11418_2023_1756_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/92c60250d975/11418_2023_1756_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/47bc5b1b3e15/11418_2023_1756_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/fa52714bc5d0/11418_2023_1756_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0abf/10764534/c483d90862b7/11418_2023_1756_Fig5_HTML.jpg

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