Novel mangiferin derivatives attenuate adipogenesis in 3T3-L1 preadipocytes and ameliorate diet induced obesity in C57BL/6J mice
文献类型： 外文期刊
作者： Gu, Dong-Quan 1 ; Li, Yin 1 ; Wu, Liu-Shun 1 ; Lyu, Meng-Ting 1 ; Li, Ying 1 ; Huang, Sheng-Zhuo 4 ; Xu, Feng-Qing 1 ; Wu, De-Ling 1 ; Zhou, Wu-Xi 1 ;
作者机构： 1.Anhui Univ Chinese Med, Sch Pharm, Hefei 230012, Peoples R China
2.Anhui Prov Key Lab Bioact Nat Prod, Hefei 230012, Peoples R China
3.Anhui Prov Key Lab New Mfg Technol Tradit Chinese, Hefei 230012, Peoples R China
4.Chinese Acad Trop Agr Sci, Inst Trop Biosci & Biotechnol, Key Lab Res & Dev Nat Prod Li Folk Med Hainan Prov, Haikou 571101, Peoples R China
期刊名称：RSC MEDICINAL CHEMISTRY （ 影响因子：3.6； 五年影响因子：4.2 ）
ISSN：
年卷期： 2025 年
页码：
收录情况： SCI
摘要： Mangiferin with a xanthone scaffold exhibited potent anti-obesity activities and thus has attracted interest. However, some shortcomings, including limited solubility and moderate potency, restrict its application. To develop novel and efficient anti-obesity agents, a series of mangiferin (MGF) amino acid derivatives were synthesized, optimized and evaluated for anti-obesity activities in vitro and in vivo. Among these derivatives, G1 was identified to be a promising compound. G1 showed better liposolubility compared to MGF. In 3T3-L1 preadipocytes, G1 significantly inhibited cell differentiation and reduced fat accumulation by increasing inhibitory activity on fatty acid synthase, and triggering G0/G1 phase cell cycle arrest and production of intracellular reactive oxygen species. The intraperitoneal administration of G1 (30, 60 mg kg-1/2 days) significantly inhibited body, liver and fat tissue weight gain, reduced lipid dysfunction, and ameliorated pathological characteristics in high-fat diet induced C57BL/6J obese mice. These results suggest that compound G1 may warrant further investigation as a promising anti-obesity agent for the treatment of human obesity.
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