The purpose of the present study was to estimate the protective effects of curcumin against anxiety and memory impairment, which are often comorbid in patients with anxiety disorders who are on standard anxiolytic therapy. The effects of curcumin on brain monoamine levels were also determined. We used the elevated plus maze (EPM), a standard animal model of anxiety, to determine the effects of subacute administration (14 days) of curcumin at doses of 5 and 10 mg/kg (p.o.) against pentylenetetrazole (PTZ; 20 mg/kg, i.p.)-induced anxiety-like behavior, followed by an evaluation of the effects of curcumin on cognitive deficits induced by PTZ using the passive avoidance retention task. Rats were exposed to the passive avoidance learning task before the initiation of treatment, and the effects on memory retention were studied 24 h after the EPM trial. A marked increase in the time spent in the open arms, an index of anxiety, and an increase in the step-down latency, an index of memory retention, were observed in curcumin-treated rats. Curcumin increased the levels of serotonin, norepinephrine, and dopamine in various regions of the rat brain. These results confirm the anxiolytic and memory-retentive effects of curcumin, and alterations in brain monoamine levels may have contributed to the present findings.
The oxadiazole linked benzoxazoles derivatives were designed using scaffold hopping approach and their molecular level interactions with both isoforms of cyclooxygenases, Cyclo OXygenase‐1 (COX‐1) and CycloOXygenase‐2 (COX‐2), were carried out using docking protocols. Mini library of oxadiazole linked benzoxazoles derivatives were synthesized and tested for their COX inhibitory activity by in vitro enzyme assay. The results indicated that compound 2‐(((5‐(2,4‐dichlorophenyl)‐1,2,4‐oxadiazol‐3‐yl)methyl)thio)benzo[d]oxazole (5 h), 2‐(((5‐(4‐nitrophenyl)‐1,2,4‐oxadiazol‐3‐yl)methyl)thio)benzo[d]oxazole (5 j) and 2‐(((5‐(4‐(trifluoromethyl)phenyl)‐1,2,4‐oxadiazol‐3‐yl)methyl)thio)benzo[d]oxazole (5 k) selectively inhibited COX‐2 enzyme. The compound 5 j exhibited strong selective COX‐2 inhibition (IC50=4.83 μM) followed by compound 5 h (IC50=5.10 μM) and 5 k (IC50=6.70 μM). The in vivo anti‐inflammatory activity of compound 5 j was found to have better efficiency than the standard drug Ibuprofen at both 3 h and 5 h intervals. The significant molecular level interactions with respect to position of benzoxazole, 1,2,4‐oxadiazole and substituted aryl groups in both COX‐1 and COX‐2 active sites were discussed. Subsequently, 2,2‐diphenyl‐2‐picrylhydrazyl (DPPH) anti‐oxidant activity was also checked for all the compounds and the compound 5 j was found to be good anti‐oxidant among the series with an IC50 of 34.5 μM.
The design, synthesis and biological evaluation of the anti-inflammatory activities of novel N-phenyl sulfonamide linked N-acylhydrazones (NPS–NAH) have been reported.
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