ArticlePloS one2025
Cytotoxic, anti-inflammatory, antioxidant, and anti-glyoxalase-I evaluation of chelating substances: In silico and in vitro study.
Article in PloS one, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
3 citing papers in PubMed.
- 7-azaindole as privileged scaffold: Advances in drug design and structural modification.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- Lactylation enzymes in cancer: Mechanisms and novel therapeutic approaches (Review).Oncology letters · 2026Review
- Discovery of hydroxytriazole as a potential glyoxalase-I inhibitor utilizing computer-aided drug design techniques.Scientific reports · 2026Article
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
introductionGlyoxalase I is a crucial target in cancer treatment due to its involvement in detoxifying methylglyoxal. Suppressing the activity of Glyoxalase I has great potential for disrupting the pathways that allow cancer cells to survive, creating a new route for cancer treatment. METHODOLOGY: This study aims to investigate several substances as inhibitors of glyoxalase-I. After demonstrating their efficacy, additional inquiry will concentrate on assessing their cytotoxic and anti-inflammatory capabilities, yielding significant insights for prospective medicinal uses. The selection of these chemicals as potential Glyoxalase I inhibitors was based on their ability to bind metals, in crucial enzymes. These compounds consist of catechol, dihydroxy, trihydroxy benzene, and functional groups such hydroxamic acid, sulfur, carboxylic acid, amide, and 3-hydroxy-4-pyridone with the aim to suppress Glyoxalase I in vitro. Docking protocol was employed to examine the binding interactions with the active site. These auspicious compounds have been subjected to cytotoxicity assay testing employing Sulforhodamine B in eleven distinct cell lines, as well as anti-inflammatory and antioxidant evaluations.
resultsGlyoxalase I inhibition revealed that 4-hydroxy-estradiol exhibited the highest efficacy with an IC50 value of 0.226 µM. Trichostatin A demonstrated a significant anti-proliferation effect in colorectal cancer cells (CACO2, HCT116, SW620, HT29) with IC50 values ranging from 14.0 µM to 27.0 µM. Furthermore, it exhibited substantial decreases in viability, ranging from 1.4 µM to 14.7 µM, in cancer cell cultures of skin (A375), lung (A549), prostate (PC3), breast (MCF7 and T47D), and cervical (HeLa). Except for 4-hydroxyestrdiol, the other phytochemicals demonstrated considerable selectivity in reducing the viability of cancer cells in monolayers of colorectal, cervical, mammary, lung, and skin tissues. In comparison to indomethacin and vitamin C, all of the studied natural compounds exhibited excellent anti-inflammatory properties in LPS-primed RAW 264.7 murine macrophages and had moderate antioxidant abilities comparable to ascorbic acid, with IC50 values from 26.0 µM to 99.0 µM.
conclusionFurther assessment of molecular action mechanisms and structural betterments/enhancements and/or derivatization of promising potent agents with antiglyoxylase - antiinflammation duality along with differential cytotoxicity and reductive capacities are advisably warranted with appropriately matched downstream in vivo validation modalities.
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