Curcumin has been widely reported as an anti-inflammatory agent isolated from the plant Curcuma longa L. (turmeric). This anti-inflammatory activity was associated with the ability of this compound to inhibit the activity of both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) in arachidonic acid metabolism. Dual COX-1 and COX-2 inhibitors are preferred to be employed in the therapy of chronic inflammatory diseases compared to selective inhibitors, since it was reported that the use of selective inhibitors led to severe adverse side effect. In the present study, in vitro and in silico assays on curcumin and its analogues as dual inhibitors for both COX-1 and COX-2 were performed. The results provide theoretical contribution in understanding the ligand-protein interactions at the molecular level to develop new curcumin analogues which possess better anti-inflammatory activity as well as to avoid unsolicited side effects.
Synthesis of Tetrahydrohexagamavunon-5 (THHGV-5) and Tetrahydrohexagamavunone-7 (THHGV-7) were prepared by catalytic hydrogenation reaction on Hexagamavunon-5 (HGV-5) and Hexagamavunone-7 (HGV-7) by using gas H 2 as source of hydrogen gas, Pd/C 10 % as metal catalyst and methanol as solvent at room temperature. According to previous study, Pd/C catalyst is more specific than other metal catalyst to reduce α,β-unsaturated double bond without reduction of its carbonyl functional group.
Purpose: To examine the chemopreventive activity of curcumin analogues, hexagamavunone-0 (HGV-0) and gamavutone-0 (GVT-0), compared to curcumin in a colorectal cancer model in Wistar rats.
Methods: Rats (n = 25) were assigned to one of five groups (n = 5 in each group). Colorectal cancer was induced in the control group with subcutaneous injection of 1,2-dimethylhydrazine (DMH) 60 mg/kg once a week for 15 weeks. In addition to DMH injection, treatment groups were treated with curcumin (20, 40, or 80 mg/kg),20, 40, or 80 mg/kg), and hexagamavunone 20, 40, or 80 mg/kg)
orally twice a week for 15 weeks. The number and volume of nodules in the colorectal area were observed after laparatomy. Histopathological analysis was performed using H & E staining and immunohistochemistry with antibodies against adenomatous polyposis coli (APC) and cyclooxygenase 2 (COX-2).
Results: All treatments reduced colorectal nodule volume, but only HGV-0 significantly decreased the numbers of nodules compared to DMH controls (p < 0.05). The reduction was 96.1 % with 40 mg/kg HGV-0. Mutated APC expression was inhibited by curcumin, GVT-0, and HGV-0 at a dose of 40 mg/kg, whereas COX-2 expression was mostly inhibited by
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