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Design and synthesis of novel saponin-triazole derivatives in the regu-lation of adipogenesis

摘要Saponins associated with Panax notoginseng(P.notoginseng)demonstrate significant thera-peutic efficacy across multiple diseases.However,certain high-yield saponins face limited clinical applications due to their reduced pharmacological efficacy.This study synthesized and evaluated 36 saponin-1,2,3-triazole derivatives of ginsenosides Rg1/Rb1 and notoginsenos-ide R1 for anti-adipogenesis activity in vitro.The research revealed that the ginsenosides Rg1-1,2,3-triazole derivative a17 demonstrates superior adipogenesis inhibitory effects.Structure-activity relationships(SARs)analysis indicates that incorporating an amidyl-substituted 1,2,3-triazole into the saponin side chain via Click reaction enhances anti-adipogenesis activity.Ad-ditionally,several other derivatives exhibit general adipogenesis inhibition.Compound a17 demonstrated enhanced potency compared to the parent ginsenoside Rg1.Mechanistic in-vestigations revealed that a17 exhibits dose-dependent inhibition of adipogenesis in vitro,ac-companied by decreased expression of preadipocytes.Peroxisome proliferator-activated re-ceptor γ(PPARγ),fatty acid synthase(FAS),and fatty acid binding protein 4(FABP4)adipo-genesis regulators.These findings establish the ginsenoside Rg1-1,2,3-triazole derivative a17 as a promising adipocyte differentiation inhibitor and potential therapeutic agent for obesity and associated metabolic disorders.This research provides a foundation for developing ef-fective therapeutic approaches for various metabolic syndromes.

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作者 Yongsheng Fang [1] Zhiyun Zhu [1] Chun Xie [1] Dazhen Xia [1] Huimin Zhao [1] Zihui Wang [1] Qian Lu [1] Caimei Zhang [1] Wenyong Xiong [1] Xiaodong Yang [1] 学术成果认领
作者单位 Key Laboratory of Medicinal Chemistry for Natural Resource,Ministry of Education;Yunnan Key Laboratory of Research and Development for Natural Products,School of Phar-macy;Yunnan University,Kunming 650500,China [1]
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DOI 10.1016/S1875-5364(25)60830-2
发布时间 2025-08-13(万方平台首次上网日期,不代表论文的发表时间)
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中国天然药物

中国天然药物

2025年23卷8期

920-931页

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