Background/introduction: 4-aryl-4H-chromenes have attracted attention as potential anticancer agents.
Objective: In an effort to discover effective compounds, we designed a new series of these chromenes with methoxy substitution at 2, 3, 4, 5, and 6 positions.
Methods: The synthesized compounds were tested for anticancer properties against two human cancer cell lines (MCF- 7 and PC3) as well as a normal cell line. Furthermore, induction of apoptosis was explored through various methods, such as flow cytometry analysis, morphological changes, activation of caspase 3, ROS, and MMP.
Results: The MTT assay showed that the 5g derivative, with methoxy groups at and positions, exhibited the highest potency (IC = 40 μM) against the PC3 cell line. Our findings revealed that compound 5g induced apoptosis in the PC3 cell line, which was demonstrated by activation of caspase 3, an increase in ROS levels, and early apoptosis percentage.
Conclusion: These results suggest that compound 5g holds promise as a potential therapeutic approach to cancer treatment.
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http://dx.doi.org/10.2174/1871520623666230504101651 | DOI Listing |
J Biochem Mol Toxicol
January 2025
Medical Experiment Center, Shaanxi University of Chinese Medicine, Xianyang, China.
Bisphenol A (BPA), an environmental endocrine disrupting chemical, is one of the most widely used chemicals in the world and is widely distributed in the external environment, specifically in food, water, dust, and soil. BPA exposure is associated with abnormal cognitive behaviors. However, the underlying mechanism remains unclear.
View Article and Find Full Text PDFCell Mol Biol (Noisy-le-grand)
January 2025
Department of Pharmacology, Faculty of Pharmacy, Mersin University, Mersin, Türkiye.
Increasing evidence suggests that inhibition of receptor-interacting serine/threonine-protein kinase (RIPK) 1/RIPK3/mixed lineage kinase domain-like pseudokinase (MLKL) necrosome has protective effects in vivo models of painful conditions seen in humans associated with inflammation and demyelination in the central nervous system. However, the contribution of RIPK1-driven necroptosis to inflammatory pain remains unknown. Therefore, this study aims to determine the effect of necrostatin (Nec) -1s, a selective RIPK1 inhibitor, on lipopolysaccharide (LPS)-induced inflammatory pain and related underlying mechanisms.
View Article and Find Full Text PDFToxicon
January 2025
College of Traditional Chinese Medicine, Shandong University of Traditional Chinese Medicine, Jinan 250355, China. Electronic address:
Strychni Semen is the dried ripe seeds of the plant Strychnos nux-vomica L, and has great medicinal value and developmental potential.However, Strychni Semen is severely toxic, with adverse effects on the central nervous system, urinary system, and other organ systems, and severe cases can be life-threatening. The present study was to reveal the mechanism of nephrotoxicity induced by Strychni Semen and its alkaloid components using experiments.
View Article and Find Full Text PDFExp Eye Res
January 2025
State Key Laboratory of Ophthalmology, Zhongshan Ophthalmic center, Sun Yat-sen University, Guangzhou 510000, Guangdong, China. Electronic address:
Currently, research on optic nerve injury predominantly focuses on the retina and optic nerve, but emerging evidence suggests that optic nerve injury also affects advanced visual structures like the superior colliculus (SC) and primary visual cortex (V1 region). However, the exact mechanisms have not been fully explored. This study aims to investigate the characteristics and mechanisms of pathology in the SC and V1 region after optic nerve crush (ONC) to deepen our understanding of the central mechanism of visual injury.
View Article and Find Full Text PDFInt J Biol Macromol
January 2025
Department of Veterinary Medicine, College of Animal Sciences, Zhejiang University, Hangzhou, China; Institute of Preventive Veterinary Medicine, Zhejiang Provincial Key Laboratory of Preventive Veterinary Medicine, Zhejiang University, Hangzhou, China; Key Laboratory of Animal Virology of Ministry of Agriculture, Center for Veterinary Sciences, Zhejiang University, Hangzhou, China; Hainan Institute of Zhejiang University, Sanya, China; Zhejiang University-Xinchang Joint Innovation Centre (TianMu Laboratory), Gaochuang Hi-Tech Park, Xinchang, China. Electronic address:
Viral infections trigger inflammasome-mediated caspase-1 activation. Nevertheless, limited understanding exists regarding how viruses use the active caspase-1 to evade host immune response. Here, we use porcine epidemic diarrhea virus (PEDV) as a model of coronaviruses (CoVs) to illustrate the intricate regulation of CoVs to combat IFN-I signaling and pyroptosis.
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