Non-Steroidal FXR Agonistic Dimeric 2-Methyl-4-(1-glycerol)furan with Lipid-Lowering Activities from Marine-Derived sp. ZSN1.
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| Main Authors: | , , , , |
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| Format: | Artículo científico |
| Language: | en |
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Marine drugs
2025
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| _version_ | 1868266226135859201 |
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| author | Jiang, Yongjun Lei, Zhen Fang, Jiebin Wu, Yanping Sun, Chengpeng |
| author_facet | Jiang, Yongjun Lei, Zhen Fang, Jiebin Wu, Yanping Sun, Chengpeng Jiang, Yongjun Lei, Zhen Fang, Jiebin Wu, Yanping Sun, Chengpeng |
| collection | PubMed - marine biology |
| contents | Non-Steroidal FXR Agonistic Dimeric 2-Methyl-4-(1-glycerol)furan with Lipid-Lowering Activities from Marine-Derived sp. ZSN1. Jiang, Yongjun Lei, Zhen Fang, Jiebin Wu, Yanping Sun, Chengpeng Receptors, Cytoplasmic and Nuclear Humans Furans Aquatic Organisms Hypolipidemic Agents Hep G2 Cells Molecular Structure Fermentation Animals Receptor, Farnesoid X-Activated Five novel 2-methyl-4-(1-glycerol)furan (MGF) dimers, namely nocardifuran A (), 13--nocardifuran A (), 15--nocardifuran A (), nocardifuran B (), and nocardifuran C (), were isolated from the Gause liquid fermentation of the marine-derived sp. ZSN1. Their structures were elucidated through HRESIMS, 1D and 2D NMR spectroscopic data analysis, and ECD calculations. Compounds - were identified as derivatives of MGF with its rearrangement of furan or pyran derivatives, while compound was identified as the derivative of MGF with an indole derivative. These MGF dimers, representing a new structural class, were isolated from a marine microorganism for the first time, thereby enhancing chemical diversity. Screening for farnesoid X receptor (FXR) agonistic activity revealed that MGF dimers could activate FXR. Furthermore, bioactivity evaluations demonstrated that these types of compounds exhibited lipid-lowering activity with lower cytotoxicity in vitro. Consequently, our findings not only contribute to the chemical diversity of marine-derived MGF-type natural products but also offer potential insights into the development of MGF dimers as lead compounds for FXR agonists in the dysregulation of hepatic lipid metabolism. |
| format | Artículo científico |
| id | pubmed_40137278 |
| institution | PubMed |
| language | en |
| publishDate | 2025 |
| publisher | Marine drugs |
| record_format | pubmed |
| spellingShingle | Non-Steroidal FXR Agonistic Dimeric 2-Methyl-4-(1-glycerol)furan with Lipid-Lowering Activities from Marine-Derived sp. ZSN1. Jiang, Yongjun Lei, Zhen Fang, Jiebin Wu, Yanping Sun, Chengpeng Receptors, Cytoplasmic and Nuclear Humans Furans Aquatic Organisms Hypolipidemic Agents Hep G2 Cells Molecular Structure Fermentation Animals Receptor, Farnesoid X-Activated Non-Steroidal FXR Agonistic Dimeric 2-Methyl-4-(1-glycerol)furan with Lipid-Lowering Activities from Marine-Derived sp. ZSN1. Jiang, Yongjun Lei, Zhen Fang, Jiebin Wu, Yanping Sun, Chengpeng Receptors, Cytoplasmic and Nuclear Humans Furans Aquatic Organisms Hypolipidemic Agents Hep G2 Cells Molecular Structure Fermentation Animals Receptor, Farnesoid X-Activated Five novel 2-methyl-4-(1-glycerol)furan (MGF) dimers, namely nocardifuran A (), 13--nocardifuran A (), 15--nocardifuran A (), nocardifuran B (), and nocardifuran C (), were isolated from the Gause liquid fermentation of the marine-derived sp. ZSN1. Their structures were elucidated through HRESIMS, 1D and 2D NMR spectroscopic data analysis, and ECD calculations. Compounds - were identified as derivatives of MGF with its rearrangement of furan or pyran derivatives, while compound was identified as the derivative of MGF with an indole derivative. These MGF dimers, representing a new structural class, were isolated from a marine microorganism for the first time, thereby enhancing chemical diversity. Screening for farnesoid X receptor (FXR) agonistic activity revealed that MGF dimers could activate FXR. Furthermore, bioactivity evaluations demonstrated that these types of compounds exhibited lipid-lowering activity with lower cytotoxicity in vitro. Consequently, our findings not only contribute to the chemical diversity of marine-derived MGF-type natural products but also offer potential insights into the development of MGF dimers as lead compounds for FXR agonists in the dysregulation of hepatic lipid metabolism. |
| title | Non-Steroidal FXR Agonistic Dimeric 2-Methyl-4-(1-glycerol)furan with Lipid-Lowering Activities from Marine-Derived sp. ZSN1. |
| topic | Receptors, Cytoplasmic and Nuclear Humans Furans Aquatic Organisms Hypolipidemic Agents Hep G2 Cells Molecular Structure Fermentation Animals Receptor, Farnesoid X-Activated |
| url | https://pubmed.ncbi.nlm.nih.gov/40137278/ |