Immunopharmacology and immunotoxicology · 2026
Silver nanoparticle-conjugated pyrimidine-based BN6 methanimine derivative improves DSS-induced inflammatory bowel disease in zebrafish.
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Ramamurthy Karthikeyan, Santhanakrishnan Magesh, Kannan Jagan, Cibikeerthivas Coimbatore Ravindran, Chitra Vellapandian, Rajagopal Rajakrishnan, Alfarhan Ahmed, Almutairi Bader O, Choi Ki Choon, Muthu Kumaradoss Kathiravan, Palaniappan Senthilkumar, Arockiaraj Jesu
Аннотация
BACKGROUND: Treatment for inflammatory bowel diseases (IBD) include immunosuppressant and steroids for managing the inflammation. Also, these treatments have many negative complications, limited efficacy, and development of drug resistance.
OBJECTIVE: To synthesize the (Z)-N-(4-(2-chlorophenyl)-6-(4-nitrophenyl)pyrimidin-2-yl)-1-(furan-2-yl)methanimine (named BN6) derivative and examines its anti-inflammatory, antioxidant, and drug-delivery effectiveness of silver nanoparticle (AgNPs) nanoconjugates against dextran sulfate sodium (DSS) induced IBD in an in-vivo zebrafish model.
METHODS: The synthesis and evaluation of AgNPs-BN6 derivatives conducted through in vitro studies. The drug release profile was studied at pH 7.0, simulating intestinal conditions, and the entrapment efficiency was evaluated across a range of concentrations, from 10 to 160 μM. Inflammatory marker levels (tnf-α, il-1β, cox-2, and il-10), biochemical changes (SOD, CAT, GSH, and LDH), macrophage localization, oxidative stress and cellular damages were measured in a following AgNPs-BN6 treatment at concentrations of 40 μM, 80 μM, and BN6 (100 μM).
RESULTS: AgNPs-BN6 conjugate drug release at 80 μM peaked at over 80% within 5 h under intestinal pH, with a slight decrease noted at 10 h. The highest entrapment efficiency, 82.30 ± 0.25, was observed at 80 μM, showcasing a dose-dependent increase until that concentration. In the model group, inflammatory markers tnf-α, il-1β, and cox-2 were particularly elevated, signaling inflammation, whereas AgNPs-BN6 treatment at 80 μM effectively lowered these markers, reinstating balance with inflammatory genes. Additionally, AgNPs-BN6 treatment reduces oxidative stress markers, demonstrating its antioxidant properties.
CONCLUSION: AgNPs-BN6 derivatives, especially at 80 μM, possess substantial anti-inflammatory and antioxidant properties, emphasizing their potential as effective therapeutic agents for inflammatory disease.
CLINICAL TRAIL: Not Applicable.
OBJECTIVE: To synthesize the (Z)-N-(4-(2-chlorophenyl)-6-(4-nitrophenyl)pyrimidin-2-yl)-1-(furan-2-yl)methanimine (named BN6) derivative and examines its anti-inflammatory, antioxidant, and drug-delivery effectiveness of silver nanoparticle (AgNPs) nanoconjugates against dextran sulfate sodium (DSS) induced IBD in an in-vivo zebrafish model.
METHODS: The synthesis and evaluation of AgNPs-BN6 derivatives conducted through in vitro studies. The drug release profile was studied at pH 7.0, simulating intestinal conditions, and the entrapment efficiency was evaluated across a range of concentrations, from 10 to 160 μM. Inflammatory marker levels (tnf-α, il-1β, cox-2, and il-10), biochemical changes (SOD, CAT, GSH, and LDH), macrophage localization, oxidative stress and cellular damages were measured in a following AgNPs-BN6 treatment at concentrations of 40 μM, 80 μM, and BN6 (100 μM).
RESULTS: AgNPs-BN6 conjugate drug release at 80 μM peaked at over 80% within 5 h under intestinal pH, with a slight decrease noted at 10 h. The highest entrapment efficiency, 82.30 ± 0.25, was observed at 80 μM, showcasing a dose-dependent increase until that concentration. In the model group, inflammatory markers tnf-α, il-1β, and cox-2 were particularly elevated, signaling inflammation, whereas AgNPs-BN6 treatment at 80 μM effectively lowered these markers, reinstating balance with inflammatory genes. Additionally, AgNPs-BN6 treatment reduces oxidative stress markers, demonstrating its antioxidant properties.
CONCLUSION: AgNPs-BN6 derivatives, especially at 80 μM, possess substantial anti-inflammatory and antioxidant properties, emphasizing their potential as effective therapeutic agents for inflammatory disease.
CLINICAL TRAIL: Not Applicable.