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PXD066787-1
PXD066787 is an original dataset announced via ProteomeXchange.
Dataset Summary
| Title | Potent and Pleiotropic Effects of Preussin B on Inhibition of Intestinal Cholesterol Absorption: Integrative Mechanisms of Action and Proteomic Analysis |
| Description | Preussin (Asperidine B) has recently shown its lipid-lowering effects by inhibiting intestinal absorption in human colorectal adenocarcinoma (Caco-2) cells and ex vivo intestinal loop in rats. While statins are widely prescribed as the primary line drug of choice for lowering hyperlipidemia, ezetimibe is the only drug that reduces intestinal cholesterol absorption, and is also optional for statin-nonresponsive individuals. To gain more understanding of the mechanisms of action and lead compounds, the derivatives of preussin: TP3, TP4, TP5, TP6, and TP7 have recently been synthesized, and the structures were confirmed using 1D and 2D nuclear magnetic resonance (NMR) spectroscopy. However, whether these derivatives exhibited inhibitory effects on cholesterol absorption is unknown. Thus, this study aims to investigate the most potent inhibitory effect of cholesterol absorption of preussin derivatives using fluorescent-micelle cholesterol transport in intestinal Caco-2 cells, confirmed by an in vivo cholesterol absorption assay. Possible targets of the lead compounds were identified using a protein binding assay and label-free quantification using proteomic analyses. Results showed that all tested preussin derivatives markedly inhibited cholesterol absorption in the intestinal Caco2 cells to a similar extent to preussin and ezetimibe. TP5 (preussin B) consistently displayed a significant reduction of plasma cholesterol, identical to preussin and ezetimibe, with the same potency in rats. In addition, the proteomic analysis found that substantial differentially expressed changes in six proteins are involved in the lipid metabolism pathway. Interestingly, GOT2, as one of these six proteins in the lipid transport pathway, consistently interacts with TP5. The molecular docking and dynamic prediction showed that TP5 coupled with GOT2 at a pocket comparable to its cofactor. These findings suggest that preussin B has therapeutic potential as a candidate for a cholesterol absorption inhibitor to treat hyperlipidemia. |
| HostingRepository | jPOST |
| AnnounceDate | 2025-12-04 |
| AnnouncementXML | Submission_2025-12-04_02:58:51.813.xml |
| DigitalObjectIdentifier | |
| ReviewLevel | Non peer-reviewed dataset |
| DatasetOrigin | Original dataset |
| RepositorySupport | Unsupported dataset by repository |
| PrimarySubmitter | Dr.Wararat Chiangjong |
| SpeciesList | scientific name: Homo sapiens (Human); NCBI TaxID: 9606; |
| ModificationList | S-carboxamidomethyl-L-cysteine; L-methionine sulfoxide |
| Instrument | TripleTOF 5600 |
Dataset History
| Revision | Datetime | Status | ChangeLog Entry |
|---|---|---|---|
| 0 | 2025-07-30 19:27:13 | ID requested | |
| ⏵ 1 | 2025-12-04 02:58:52 | announced |
Publication List
| Dataset with its publication pending |
Keyword List
| submitter keyword: cholesterol absorption, preussin, preussin B, preussin analogues, proteomics, lipid-lowering, hypercholesterolemia |
Contact List
| Chutima S. Vaddhanaphuti | |
|---|---|
| lab head | |
| Dr.Wararat Chiangjong | |
| contact affiliation | Mahidol University |
| dataset submitter | |
Full Dataset Link List
| jPOST dataset URI |
| Dataset FTP location NOTE: Most web browsers have now discontinued native support for FTP access within the browser window. But you can usually install another FTP app (we recommend FileZilla) and configure your browser to launch the external application when you click on this FTP link. Or otherwise, launch an app that supports FTP (like FileZilla) and use this address: ftp://ftp.jpostdb.org/JPST003966/ |
