Life sciences · 2025
Improvement of the stability of ginsenoside Rg5 and its pharmacological efficacy in nonalcoholic steatohepatitis.
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Ma Jiahui, Bai Xue, Duan Zhiguang, Fu Rongzhan, Zeng Wen, Li Yang, Guan Zhenghui, Zhu Chenhui
Аннотация
AIMS: Ginsenoside Rg5 (Rg5) has been certified to have superior activity in relieving the symptoms of non-alcoholic steatohepatitis (NASH). Nevertheless, the potential application of Rg5 is limited owing to its instability during storage. This study aims to enhance the stability of Rg5 through structural modification and evaluate its efficacy in treating NASH.
MATERIALS AND METHODS: The modification involved the hydrogenation of the double bonds at C-20 (22) and C-24 (25) to form 2H-ginsenoside Rg5 (2HRg5). We used spectroscopic techniques including H-NMR, C-NMR, and high-resolution mass spectrometry to characterize the structure of 2HRg5. In addition, we used High-performance liquid chromatography (HPLC) to study the stability changes through stability experiments at 25 or 60°C for 25 days. We created NASH models in vitro and in vivo and used transcriptomics, molecular docking, and molecular dynamics simulations to examine the impact of 2HRg5 on NASH lipid accumulation, fibrosis, and liver inflammation.
KEY FINDINGS: After 25 days at 60°C, 2HRg5 retained 82.7% of the active content compared to 9.4% for Rg5, with superior reduction in lipid accumulation, inflammation, and fibrosis in NASH mice. 2HRg5 inhibits the STING-TBK1-IRF3 pathway and reduces type I interferon release and inflammation. Moreover, the high binding efficiency and remarkable system stability between 2HRg5 and STING further support our findings.
SIGNIFICANCE: 2HRg5 provides improved storage stability and efficacy, making it a promising therapeutic candidate for NASH.
MATERIALS AND METHODS: The modification involved the hydrogenation of the double bonds at C-20 (22) and C-24 (25) to form 2H-ginsenoside Rg5 (2HRg5). We used spectroscopic techniques including H-NMR, C-NMR, and high-resolution mass spectrometry to characterize the structure of 2HRg5. In addition, we used High-performance liquid chromatography (HPLC) to study the stability changes through stability experiments at 25 or 60°C for 25 days. We created NASH models in vitro and in vivo and used transcriptomics, molecular docking, and molecular dynamics simulations to examine the impact of 2HRg5 on NASH lipid accumulation, fibrosis, and liver inflammation.
KEY FINDINGS: After 25 days at 60°C, 2HRg5 retained 82.7% of the active content compared to 9.4% for Rg5, with superior reduction in lipid accumulation, inflammation, and fibrosis in NASH mice. 2HRg5 inhibits the STING-TBK1-IRF3 pathway and reduces type I interferon release and inflammation. Moreover, the high binding efficiency and remarkable system stability between 2HRg5 and STING further support our findings.
SIGNIFICANCE: 2HRg5 provides improved storage stability and efficacy, making it a promising therapeutic candidate for NASH.