Background: Palestine is a rich land with wild edible plants which used from the ancient times as food and medicine. Arum is a valuable genus of medicinal plants which is used in the ethnic medicine for treatment of cancer or consumed as integrated food. This work aimed to evaluate and compare the phytoconstituents, total phenols contents and free radical scavenging potential for Arum dioscoridis, Arum elongatum, Arum hygrophilum and Arum palaestinum a members of Palestinian flora. Methods: Phytoconstituents screened by using standard analytical methods, total phenols determined by using Folin Ciocalteu's method and antioxidant activities were assessed by DPPH assay. Results: The crude extracts of Arum plant studied species revealed the presence of several biologically active phytochemicals with the highest quantity of saponin, alkaloid, phenols and flavonoids. For A. dioscoridis, A. elongatum, A. hygrophilum and A. palaestinum free radical scavenging activities were 6.7±0.75µg/ml, 19.9±0.63µg/ml, 9.9±0.49µg/ml, and 6.9±0.62µg/ml respectively, while the IC50 for Trolox was 4.8±0.39µg/ml as well as the total phenols contents for these species were 60.07 ±0.12, 27.49 ±0.32, 41.75±0.12 and 53.17±0.22 (mg GAE/g extract), ±SD respectively. Conclusion: The antioxidant activities in the studied Arum plant species showed a marked correlation with their total phenols contents. A. dioscoridis and A. palaestinum had the highest antioxidant activities with high contents of total phenols and they can be used as perfect choices for manufacturing of pharmaceutical, cosmeticeuticals and nutraceutical formulations.
Series of diaryl-based pyrazole and triazole derivatives were designed and synthesized in a facile synthetic approach in order to produce selective COX-2 inhibitor. ese series of derivatives were synthesized by different reactions like Vilsmeier-Haack reaction and click reaction. In vitro COX-1 and COX-2 inhibition studies showed that five compounds were potent and selective inhibitors of the COX-2 isozyme with IC 50 values in 0.551-0.002 μM range. In the diarylpyrazole derivatives, compound 4b showed the best inhibitory activity against COX-2 with IC 50 � 0.017 μM as one of the N-aromatic rings was substituted with sulfonamide and the other aromatic ring was unsubstituted. However, when the N-aromatic ring was substituted with sulfonamide and the other aromatic ring was substituted with sulfone (compound 4d), best COX-2 selectivity was achieved (IC 50 � 0.098 μM, SI � 54.847). In the diaryltriazole derivatives, compound 15a showed the best inhibitory activity in comparison to all synthesized compounds including the reference celecoxib with IC 50 � 0.002 μM and SI � 162.5 as it could better fit the extra hydrophobic pocket which is present in the COX-2 enzyme. Moreover, the docking study supports the obtained SAR data and binding similarities and differences on both isozymes.
Antioxidant activity of natural compounds in food and in dietary supplements plays an important role in healthy life. Scientific evidences suggest that antioxidants reduce the risk for chronic diseases including cancer, diabetes mellitus and heart diseases. The antioxidant activity of wild Cyclamen persicum, Malva sylvestris and Urtica pilulifera leaves and their cultivated species were studied using 2, 2-diphenylpicrylhydrazyl (DPPH) radical scavenging activity and compared to Trolox antioxidant activity. The exhaustive extractions yields for these samples were estimated by using polar and nonpolar solvents. The results showed that the wild Cyclamen persicum, Malva sylvestris and Urtica pilulifera leaves have higher exhaustive extraction yield and as well the higher antioxidant activity (IC50) comparing with their cultivated species. Both of cultivated, as well the wild natural growing forms of Cyclamen persicum, Malva sylvestris and Urtica pilulifera are a good source for natural foods supplements, pharmaceutical industry purposes and for organic food rich with antioxidant compounds.
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