Dual-state emissive fluorogens (DSE-gens) are currently defining their importance as a transpiring tool in biological and biomedical applications. This work focuses on designing and synthesizing indole-anthracene-based solid-state emitting twisted π-conjugates using a metal-free protocol to achieve AIE-active DSE-gens, expanding their scope in biological applications. Special effort has been made to introduce proficient and photo/thermostable DSE-gens that inhibit cancer but not normal cells. Here, the lead DSE-gen initially detects cancer and normal cells by bioimaging; however, it could also confirm and distinguish cancer cells from normal cells by its abated fluorescence signal after killing cancer cells. In contrast, the fluorescence signals for a normal cell remain unscathed. Surprisingly, these molecules displayed decent anticancer properties against FaDu and 4T1 but not MCF-7 cell lines. From a series of newly designed indole-based molecules, we report one single 2,3,4-trimethoxybenzene-linked DSE-gen (the lead), exhibiting high ROS generation, less haemolysis, and less cytotoxicity than doxorubicin (DOX) for normal cells, crucial parameters for a biocompatible anticancer probe. Thus, we present a potentially applicable anticancer drug, offering a bioactive material with bioimaging efficacy and a way to detect dead cancer cells selectively. The primary mechanism behind the identified outcomes is deciphered with the support of experimental (steady-state and time-resolved fluorescence, biological assays, cellular uptake) and molecular docking studies.
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http://dx.doi.org/10.1039/d2tb02078e | DOI Listing |
Drug Dev Res
February 2025
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.
Five series of new 1,3,4-thiadiazole hybrids were designed and synthesized as promising EGFR inhibitors. Three human cancer cell lines were employed for testing each hybrid's in vitro antiproliferative efficacy; colon HCT-116, liver HepG-2 and breast MCF-7 using MTT assay. Comparing compound 9a to the reference doxorubicin, 9a shown superior activity to that of Dox with respect to MCF-7 (IC 3.
View Article and Find Full Text PDFJ Biochem Mol Toxicol
January 2025
Anqing Medical College Clinical Research Center, Anqing Municipal Hospital, Anqing, Anhui, P.R. China.
Our previous research identified that lncRNA PVT1 is upregulated in patients with IA. However, the precise functions of PVT1 in IA remain unclear. We compared the levels of PVT1, caspase-3, caspase-1, and NLRP3 in normal and IA patients.
View Article and Find Full Text PDFElife
December 2024
Department of Dermatology, First Affiliated Hospital of Nanjing Medical University, Nanjing, China.
Psoriasis is a multifactorial immune-mediated inflammatory disease. Its pathogenesis involves abnormal accumulation of neutrophils and T-cell-related abnormalities. Pyroptosis is a type of regulated cell death associated with innate immunity, but its role in psoriasis is unclear.
View Article and Find Full Text PDFPlast Reconstr Surg Glob Open
December 2024
From the Department of Plastic, Reconstructive and Aesthetic Surgery, Nippon Medical School Hospital, Tokyo, Japan.
Background: Keloids are growing scars that arise from injury to the reticular dermis and subsequent chronic local inflammation. The latter may be promoted by vascular hyperpermeability, which permits the ingress of chronic inflammatory cells/factors. Cutaneous capillaries consist of endothelial cells that generate, and are anchored by, a vascular basement membrane (VBM).
View Article and Find Full Text PDFGenes Dis
March 2025
Center for Pancreatic Cancer Research, The South China University of Technology School of Medicine, Guangzhou, Guangdong 510006, China.
Pancreatic ductal adenocarcinoma (PDA) is a lethal malignancy characterized by insidious onset and lack of effective therapy. The molecular pathogenesis of PDA remains to be understood fully. Transcriptional factor GATA6 is an important transcriptional regulator in normal pancreas development, particularly in the initial specification and differentiation of the pancreas.
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