Gentiopicroside isolated from Gentiana scabra Bge. inhibits adipogenesis in 3T3-L1 cells and reduces body weight in diet-induced obese mice

Gentiopicroside isolated from Gentiana scabra Bge. inhibits adipogenesis in 3T3-L1 cells and reduces body weight in diet-induced obese mice
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DOI:
10.1016/j.bmcl.2019.05.038
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发表时间:
2019-07-15
影响因子:
2.7
通讯作者:
Lee, Mi-Kyung
Lee, Mi-Kyung
中科院分区:
医学4区
文献类型:
--
作者:
Choi, Ra-Yeong;Nam, Sang-Jip;Lee, Mi-Kyung

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龙胆苦苷是龙胆的主要活性成分,其通常用作亚洲治疗炎症的草药。龙胆苦苷显著下调成脂关键转录因子的表达(PPAR γ、C/EBP α、SREBP-1c)并剂量依赖性地抑制脂质摄取相关基因(LPL)、脂肪酸转运相关基因(FABP 4)和甘油三酯(TG)合成相关基因(DGAT 2),以及脂肪酸合成相关基因(FAS,SCD 1),这导致3 T3-L1细胞中细胞内脂滴积累和TG含量降低。龙胆苦苷还下调炎症细胞因子基因(NF κ B1,TNF α,IL 6)的表达与车辆相比。与对照组相比,高脂饮食喂养12周的小鼠口服龙胆苦苷(50 mg/kg)导致体重和内脏脂肪量减少。总之,本研究的结果表明,龙胆苦苷通过调节3 T3-L1中脂肪生成/脂肪生成相关基因和炎症基因的表达具有积极的减肥作用,并且在体内有效地降低体重和内脏脂肪量。
Gentiopicroside is a major active component of the Gentiana scabra Bge., which is commonly used as herbal medicine for the treatment of inflammation in Asia. Gentiopicroside significantly down-regulated expression of key adipogenic transcription factors (PPAR gamma, C/EBP alpha, SREBP-1c) and dose-dependently inhibited the lipid uptake- related gene (LPL), fatty acid transport-related gene (FABP4) and triglyceride (TG) synthesis-related gene (DGAT2), as well as fatty acid synthesis-related genes (FAS, SCD1), which resulted in reduced intracellular lipid droplet accumulation and TG content in 3T3-L1 cells. Gentiopicroside also down-regulated expression of inflammatory cytokine genes (NF kappa B1, TNF alpha, IL6) compared with vehicle. Oral administration of gentiopicroside (50 mg/kg) in mice fed with high-fat diet for 12 weeks resulted in reduced body weight and visceral fat mass compared with the control group. Overall, the results of this study showed that gentiopicroside had positive antiobesity effects by regulating the expression of adipogenesis/lipogenesis-related genes and inflammatory genes in 3T3-L1, and that it effectively reduced body weight and visceral fat mass in vivo.