Zhao Meng-Jie, Wang Shan-Shan, Jiang Yao, Wang Ying, Shen Hong, Xu Pei, Xiang Hua, Xiao Hong
Nanjing Medical University, Affiliated Nanjing Brain Hospital, No. 264 Guangzhou Road, Nanjing, Jiangsu, 210029, People's Republic of China.
Department of Pharmaceutical Chemistry, China Pharmaceutical University, No. 24 Tong Jia Xiang, Nanjing, China.
Lipids Health Dis. 2017 May 2;16(1):85. doi: 10.1186/s12944-017-0472-z.
The novel compound XH601 is a synthesized derivative of formononetin. The present study was to investigate the hypolipidemia effect and potential mechanism of XH601.
Male Golden Syrian hamsters were induced by high-fat diet (HFD) for eight weeks and the hyperlipidemic model was established successfully. After XH601 treatment, serum and hepatic biochemistry parameters of hamsters were detected and the effect of XH601 on adipose tissue was also analyzed. Furthermore, 3 T3-L1 cell differentiation by Oil-Red-O staining was observed and the mRNA and protein expression of peroxisome proliferator-activated receptors (PPARs) were measured by qRT-PCR and Western-blot in mature adipocytes.
The in vivo results suggest that XH601 significantly decreased the adipose weight and levels of serum triglyceride (TG), total cholesterol (TC), low-density lipoprotein (LDL-C), apolipoprotein B (Apo-B), apolipoprotein E (Apo-E), while increased serum high-density lipoprotein (HDL-C). The in vitro results implied that XH601 up-regulated the mRNA and protein expression of both PPARα and PPARβ/δ in a dose-dependent manner.
The study suggests that XH601 exhibited strong ability to improve the dyslipidemia in hamsters fed with high-fat diet. The potential mechanism of XH601 was associated with the up-regulation of PPARα and PPARβ/δ mRNA and protein expression.
新型化合物XH601是刺芒柄花素的合成衍生物。本研究旨在探讨XH601的降血脂作用及其潜在机制。
雄性叙利亚金仓鼠用高脂饮食(HFD)诱导8周,成功建立高脂血症模型。XH601处理后,检测仓鼠的血清和肝脏生化参数,并分析XH601对脂肪组织的影响。此外,通过油红O染色观察3T3-L1细胞分化情况,并采用qRT-PCR和Western blot检测成熟脂肪细胞中过氧化物酶体增殖物激活受体(PPARs)的mRNA和蛋白表达。
体内实验结果表明,XH601显著降低了脂肪重量以及血清甘油三酯(TG)、总胆固醇(TC)、低密度脂蛋白(LDL-C)、载脂蛋白B(Apo-B)、载脂蛋白E(Apo-E)水平,同时提高了血清高密度脂蛋白(HDL-C)水平。体外实验结果表明,XH601以剂量依赖的方式上调PPARα和PPARβ/δ的mRNA和蛋白表达。
该研究表明,XH601对高脂饮食喂养的仓鼠具有较强的改善血脂异常的能力。XH601的潜在机制与PPARα和PPARβ/δ mRNA及蛋白表达上调有关。