Identification and mechanism of hepatoprotective saponins and metabolites in the sweet variant of
文献类型：期刊论文
| 作者 | Wang, Hanghang5; Chen, Chen5; Xue, Mingzhen5; Zhang, Yu5; Chen, Keming5; Sun, Bingjie5; Wang, Peipei4; Tong, Xinyi3; Yu, Xiong2; Li, Han5 |
| 刊名 | BIOORGANIC CHEMISTRY
 |
| 出版日期 | 2025-10-01 |
| 卷号 | 165页码:13 |
| 关键词 | Gynostemma pentaphyllum Gypenoside Gut metabolite Liver protection Hepatic stellate cells |
| ISSN号 | 0045-2068 |
| DOI | 10.1016/j.bioorg.2025.108996 |
| 通讯作者 | Zhao, Linguo(lgzhao@njfu.edu.cn) ; Wang, Xiachang(xiachangwang@njucm.edu.cn) ; Zhang, Yinan(yinanzhang@njucm.edu.cn) |
| 英文摘要 | Gynostemma pentaphyllum (Thunb.) Makino has been traditionally utilized as medicinal herb and function food in traditional Chinese medicine for treating chronic hepatic disorders. Sweet variants of G. pentaphyllum collected from different regions of China are cultivated as the primary resources for the preparation of curative products. We and other groups identified a series of dammarane-type triterpenoids enriched in the plant, such as gypenosides LVI and XLVI, as the bioactive components responsible for the hepatoprotective effect. However, their therapeutic potential may be constrained by low oral bioavailability and complex metabolic pathways. This study applied an in vitro analysis of gut microbiome-based metabolism to determine the major pathway of the gypenosides. Structure-activity relationships, pharmacokinetic studies, and pharmacodynamic results revealed that the removal of the C-3 saccharide chain is not only the main metabolic pathway in the intestinal tract but also generates the active hepatoprotective ingredient with higher bioavailability and potency than the proteotype. Notably, the investigation of underlying the mechanism demonstrated that the compounds inhibited the activation of hepatic stellate cells via the AMPK/P300/Smad3 signaling pathway. Collectively, these findings demonstrate that in vivo metabolism is critical for unlocking the therapeutic potential of orally administered sweet variant G. pentaphyllum, as this metabolic process releases active ingredients that overcome the bioavailability limitations of the parent gypenoside. |
| WOS关键词 | LIVER FIBROSIS ; IN-VITRO ; ANTIOXIDANT |
| 资助项目 | Science Foundation of China[22177052] ; Key Industrial and Research Program of Jiangsu Provincial 333 Talent[2022-2-245] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001575371200002 |
| 出版者 | ACADEMIC PRESS INC ELSEVIER SCIENCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/321534]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhao, Linguo; Wang, Xiachang; Zhang, Yinan |
| 作者单位 | 1.Lingang Lab, Shanghai 201203, Peoples R China 2.Ocean Univ China, Sch Med & Pharm, Qingdao 266003, Peoples R China 3.Nanjing Forestry Univ, Jiangsu Coinnovat Ctr Efficient Proc & Utilizat Fo, Nanjing 210037, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201210, Peoples R China 5.Nanjing Univ Chinese Med, Jiangsu Key Lab Funct Subst Chinese Med, Nanjing 210023, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Hanghang,Chen, Chen,Xue, Mingzhen,et al. Identification and mechanism of hepatoprotective saponins and metabolites in the sweet variant of[J]. BIOORGANIC CHEMISTRY,2025,165:13. |
| APA | Wang, Hanghang.,Chen, Chen.,Xue, Mingzhen.,Zhang, Yu.,Chen, Keming.,...&Zhang, Yinan.(2025).Identification and mechanism of hepatoprotective saponins and metabolites in the sweet variant of.BIOORGANIC CHEMISTRY,165,13. |
| MLA | Wang, Hanghang,et al."Identification and mechanism of hepatoprotective saponins and metabolites in the sweet variant of".BIOORGANIC CHEMISTRY 165(2025):13. |
入库方式： OAI收割
来源：上海药物研究所
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