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.

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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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Selectivity of a drug becomes a major problem in the treatment of a clinical disease and many nonsteroidal anti‐inflammatory drugs (NSAID's) are classic examples of this conundrum. In the present study, we designed a set of hybrid compounds (11 a‐p, 12 a‐i) that compose new N‐acyl hydrazones (NAH) linked with isoxazoles, using rational drug design approach. The binding affinities of newly designed compounds were calculated and compared with known non anti‐inflammatory NAH and cyclooxygenase‐2 (COX‐2) inhibitors (coxibs) at the active sites of cyclooxygenase‐1 (COX‐1) and COX‐2. The comparison revealed that the hybrid compounds bind with COX‐2 active site in a fashion quite similar to known non anti‐inflammatory compounds (4). Based on these findings, we further synthesized the compounds (11 a‐p, 12 a‐i) and subjected them to in vitro, in vivo anti‐inflammatory studies. Compound 11 l (IC50=5.8 μM) and 12 c (IC50 = 4.1 μM) were found to be active COX‐2 inhibitors. Compounds 12 a, 12 b and 12 e displayed COX‐2 enzyme inhibition at lower micro molar concentrations. The compounds were also evaluated for antioxidant activity and compound 11 h exhibited an effective antioxidant activity when compared with ascorbic acid. Additionally, these compounds were screened for anti‐bacterial activities and compound 11 l and 12 h were exhibited greater anti‐bacterial activity against gram +ve and ‐ve than standards Ciprofloxacin and Flucloxacillin.

Introduction: Pre-diabetes is a condition that persists for a considerable duration before progressing into type 2 diabetes mellitus (T2DM). Development of resistance to insulin is the underlying cause of pre-diabetes, preventive measures such as diagnosis, treatment and exercise will preclude its development into T2DM. The present study aims at studying the effect of pre-treatment and post-treatment with isolated fraction of Costus igneus on pre-diabetes and diabetes in neonatal streptozotocin (STZ) induced T2DM.Methods: Neonatal rats were treated with STZ and differentiated for pre-treatment and post-treatment. Rats of pre-treated group were treated with isolated fraction of Costus igneus (CIF) from 4th week after STZ administration and after 12th week in non-treated rats of post-treatment group. The antihyperglycemic was studied on 7th and 12th week after STZ treatment using oral glucose tolerance test and the hypoglycemic effect was studied on day 1, 7, 14 and 21 of treatment after 12th week of STZ treatment in both pre and post treated groups.Results: Oral glucose tolerance test on 7th and 12th week had shown a protective effect against increase in blood glucose levels in pre-treated groups whereas, no such significant decrease was observed in non-treated groups. In the effect on hypoglycemia, a reduction in blood glucose levels was observed on treatment with CIF in both pre and post treated rats on 14th and 21st day.Conclusions: Treatment with CIF in pre-diabetic stage could reduce the chances of progression into T2DM and is also beneficial in diabetic rats, which could be due to increase in the peripheral utilization of glucose and the insulin mimetic effect of Costus igneus.

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