Academic Journal
Electron density engineering of chalcone derivatives towards synergistically strengthened lipid droplet probes for fluorescence diagnosis and drug evaluation of non-alcoholic fatty liver disease.
| Τίτλος: | Electron density engineering of chalcone derivatives towards synergistically strengthened lipid droplet probes for fluorescence diagnosis and drug evaluation of non-alcoholic fatty liver disease. |
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| Συγγραφείς: | Luo Y; Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China., Zhao Q; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China., Jiang X; Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China., Chen Y; Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China., Kuang X; Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China., Huang R; Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China., Qu J; Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China., Liu J; Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China., Zhang Q; Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China., Yu C; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; Chongqing Key Laboratory for Pharmaceutical Metabolism Research, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China., Cai Y; Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China. Electronic address: ycai@cqmu.edu.cn. |
| Πηγή: | Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy [Spectrochim Acta A Mol Biomol Spectrosc] 2026 Aug 05; Vol. 356, pp. 127744. Date of Electronic Publication: 2026 Mar 18. |
| Τύπος έκδοσης: | Journal Article |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Elsevier Country of Publication: England NLM ID: 9602533 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-3557 (Electronic) Linking ISSN: 13861425 NLM ISO Abbreviation: Spectrochim Acta A Mol Biomol Spectrosc Subsets: MEDLINE |
| Imprint Name(s): | Publication: Original Publication: [Kidlington, Oxford, U.K. ; Tarrytown, NY] : Pergamon, c1994- |
| Ιατρικοί όροι (MeSH): | Non-alcoholic Fatty Liver Disease*/drug therapy , Non-alcoholic Fatty Liver Disease*/diagnosis , Non-alcoholic Fatty Liver Disease*/diagnostic imaging , Lipid Droplets*/chemistry , Lipid Droplets*/metabolism , Fluorescent Dyes*/chemistry , Chalcone*/chemistry, Optical Imaging/methods ; Humans ; Animals ; Spectrometry, Fluorescence ; Electrons ; Fluorescent Chemosensor Compounds ; Hep G2 Cells |
| Περίληψη: | Detecting abnormal lipid levels and timely intervention have great potential for diagnosis and treatment of non-alcoholic fatty liver disease (NAFLD). Herein, a novel molecular electron density engineering strategy for synergistically strengthened lipid droplets (LDs) fluorescence probes based on the chalcone skeleton is presented for simultaneous fluorescence diagnosis and drug evaluation of NAFLD. Specifically, a series of novel chalcone derivatives (C1-C7) with controlled intrinsic electron density distribution are rationally fabricated via introducing various push-pull electronic groups into triphenylamine-fused chalcones. Notably, the optical properties including polarity sensibility, Stokes shift, fluorescence emission, photostability, and aggregation-induced emission (AIE) characteristics are all synergistically boosted upon transforming from D-π-A-π-D to D-π-A-π-A architectures. C2 is identified as the optimal probe for LDs-targeted dynamic high-fidelity fluorescence monitoring in live cells, revealing a novel LDs motion pattern termed "Sequential Separation". Further, C2 permits multiscale fluorescence imaging diagnosis of NAFLD in vitro/vivo. Moreover, two LDs-based drug evaluation protocols utilizing C2 for NAFLD intervention are first established, and sesamol is identified as a potential NAFLD therapeutic agent through these assays. Overall, this work not only provides a rational design strategy and novel probe toolbox for the early diagnosis of NAFLD, but also develops pioneering drug screening methodologies for exploiting potential NAFLD therapeutic drugs. (Copyright © 2026. Published by Elsevier B.V.) |
| Competing Interests: | Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. |
| Contributed Indexing: | Keywords: Chalcone; Drug evaluation; Electron density engineering; Fluorescence imaging; Lipid droplets; Non-alcoholic fatty liver disease |
| Substance Nomenclature: | 0 (Fluorescent Dyes) 5S5A2Q39HX (Chalcone) 0 (Fluorescent Chemosensor Compounds) |
| Entry Date(s): | Date Created: 20260322 Date Completed: 20260713 Latest Revision: 20260713 |
| Update Code: | 20260714 |
| DOI: | 10.1016/j.saa.2026.127744 |
| PMID: | 41865636 |
| Βάση Δεδομένων: | MEDLINE |
| ISSN: | 1873-3557 |
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| DOI: | 10.1016/j.saa.2026.127744 |