NLRP3 inhibitors: Unleashing their therapeutic potential against inflammatory diseases

Ramalingam, Vaikundamoorthy

doi:10.1016/j.bcp.2023.115915

Cited by 4 publications

(1 citation statement)

References 184 publications

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“…After caspase-1 is activated, NLRP3 serves as a platform for the maturation of inflammatory cytokines, such as IL-1β and IL-18 . The activation of the NLRP3 inflammasome regulates autophagy, mitochondrial metabolism, and the epithelial–mesenchymal transition, which in turn promotes tumor cell growth, survival, migration, and invasion in prostate cancer . In this study, FCN and its cocrystals downregulate the expression of NLRP3 protein as compared with control DU145 prostate cancer cells.…”

Section: Resultsmentioning

confidence: 95%

Repurposing of Antifungal Drug Flucytosine/Flucytosine Cocrystals for Anticancer Activity against Prostate Cancer Targeting Apoptosis and Inflammatory Signaling Pathways

Kanagavel,

Sparjan Samuvel,

Ramalingam

et al. 2024

Mol. Pharmaceutics

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This study aimed to repurpose the antifungal drug flucytosine (FCN) for anticancer activity together with cocrystals of nutraceutical coformers sinapic acid (SNP) and syringic acid (SYA). The cocrystal screening experiments with SNP resulted in three cocrystal hydrate forms in which two are polymorphs, namely, FCN-SNP F−I and FCN-SNP F−II, and the third one with different stoichiometry in the asymmetric unit (1:2:1 ratio of FCN:SNP:H 2 O, FCN-SNP F−III). Cocrystallization with SYA resulted in two hydrated cocrystal polymorphs, namely, FCN-SYA F−I and FCN-SYA F−II. All the cocrystal polymorphs were obtained concomitantly during the slow evaporation method, and one of the polymorphs of each system was produced in bulk by the slurry method. The interaction energy and lattice energies of all cocrystal polymorphs were established using solid-state DFT calculations, and the outcomes correlated with the experimental results. Further, the in vitro cytotoxic activity of the cocrystals was determined against DU145 prostate cancer and the results showed that the FCN-based cocrystals (FCN-SNP F−III and FCN-SYA F−I) have excellent growth inhibitory activity at lower concentrations compared with parent FCN molecules. The prepared cocrystals induce apoptosis by generating oxidative stress and causing nuclear damage in prostate cancer cells. The Western blot analysis also depicted that the cocrystals downregulate the inflammatory markers such as NLRP3 and caspase-1 and upregulate the intrinsic apoptosis signaling pathway marker proteins, such as Bax, p53, and caspase-3. These findings suggest that the antifungal drug FCN can be repurposed for anticancer activity.

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Section: Resultsmentioning

confidence: 95%

Repurposing of Antifungal Drug Flucytosine/Flucytosine Cocrystals for Anticancer Activity against Prostate Cancer Targeting Apoptosis and Inflammatory Signaling Pathways

Kanagavel,

Sparjan Samuvel,

Ramalingam

et al. 2024

Mol. Pharmaceutics

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Natural products: A potential immunomodulators against inflammatory-related diseases

Sai Priya,

Ramalingam,

Suresh Babu

2024

Inflammopharmacol

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Inflammatory and Immune Mechanisms in COPD: Current Status and Therapeutic Prospects

Qi,

Yan,

Tang

et al. 2024

JIR

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Background Chronic obstructive pulmonary disease (COPD) currently ranks among the top three causes of mortality worldwide, presenting as a prevalent and complex respiratory ailment. Ongoing research has underscored the pivotal role of immune function in the onset and progression of COPD. The immune response in COPD patients exhibits abnormalities, characterized by diminished anti-infection capacity due to immune senescence, heightened activation of neutrophils and macrophages, T cell infiltration, and aberrant B cell activity, collectively contributing to airway inflammation and lung injury in COPD. Objective This review aimed to explore the pivotal role of the immune system in COPD and its therapeutic potential. Methods We conducted a review of immunity and COPD published within the past decade in the Web of Science and PubMed databases, sorting through and summarizing relevant literature. Results This article examines the pivotal roles of the immune system in COPD. Understanding the specific functions and interactions of these immune cells could facilitate the development of novel therapeutic strategies and interventions aimed at controlling inflammation, enhancing immune function, and mitigating the impact of respiratory infections in COPD patients.

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NLRP3 inhibitors: Unleashing their therapeutic potential against inflammatory diseases

Cited by 4 publications

References 184 publications

Repurposing of Antifungal Drug Flucytosine/Flucytosine Cocrystals for Anticancer Activity against Prostate Cancer Targeting Apoptosis and Inflammatory Signaling Pathways

Repurposing of Antifungal Drug Flucytosine/Flucytosine Cocrystals for Anticancer Activity against Prostate Cancer Targeting Apoptosis and Inflammatory Signaling Pathways

Natural products: A potential immunomodulators against inflammatory-related diseases

Inflammatory and Immune Mechanisms in COPD: Current Status and Therapeutic Prospects

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