Background: Since primitive times, man has gone in different ways to search for cures and relief from various diseases by using several plants, plant products and plant-derived products. Recently, there is a scientific curiosity and certain popularity with regard to screening essential oils and extracts from plants used medicinally all over the world. Objective: This study design to evaluate the component of ginger extracts in different solvents by HPLC in addition to evaluate the in vitro effects of it on microorganisms , especially the plant is used in Iraqi folk medicine as anti-inflammatory, antipyretic, anti-diabetic, relieving rheumatic pains and for treating stomach discomfort. Methods: The extraction of soluble compounds from ginger by the soxhlet method was performed by using methanol and n-hexane as solvents and the main composition of ginger extracts were analyzed by HPLC. Agarwell diffusion method tested antimicrobial activities of two crud extracts in different concentrations of plant on seven types of bacteria strains and one fungus. Results: Seven components were identified from the separation of ginger extracts by HPLC. The two extracts had antimicrobial activity, methanol extract was superior than n-hexane extract against the same tested microorganisms. Conclusion: The results of this study revealed that this plant possesses some antimicrobial properties as antibiotics and antifungal, therefore they can be used as a potential source of active ingredients for food, pharmaceutical industry or preservatives.
A series of six pyrazoline ring derivatives as a pharmacophore were incorporated to the naproxen; to increase its size were synthesized and preliminarly evaluated as antiinflammatory agents with expected selectivity toward COX-2 enzyme. In vivo acute antiinflammatory effects of the final compounds (5a-f) were evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug (naproxen) produced significant reduction of paw edema with respect to the effect of control group (propylene glycol 50%, v:v). However, compound 5d and 5e show comparable effect to naproxen at all experimental time while compounds 5a, 5b and 5c produced significantly lower inhibitory effect than naproxen at time 120-240 minutes. Furthermore, compound 5f exert significantly higher paw edema reduction than naproxen at 60-240 min. Also the antibacterial activities of the final compounds were evaluated by Well Diffusion Method. All tested compounds exert significant antibacterial activity against tested Gram positive and Gram negative bacteria in comparison to dimethyl sulfoxide as control group. In comparison the antibacterial results among the tested compound 5e may regard the best one and compound 5c the lower one.
Background: Undoubtedly, cancer is regarded as a major concern for researchers alongside the whole humanity for its high mortality rates. At this moment, there must be some researchers working hard to design, synthesize, and biologically investigate the effects of some potential candidates to fight back cancer. Materials and methods: In previous unpublished work, the authors successfully designed, synthesized, characterized a potential two spebrutinib analogues. Consequently, these analogues were evaluated with the employment of MCF-7, HCT116, and MDCK cell lines. Results: In respect to the spebrutinib standard, one of these analogues has superior activity against MCF-7 cell line (IC50; 10.744 µg/mL against 13.566 µg/mL for spebrutinib) and an enhanced toxicity profile on MDCK cell line (IC50; 8.653 mg/mL against 4.011 mg/mL for spebrutinib). Conclusion: The two compounds showed good activity against breast and colon cell lines and enhanced toxicity profile against normal kidney cell line in respect to spebrutinib standard.
A new series of trisubstituted pyrazoline bearing benzenesulfonamide moiety (6a,b-10a,b) were designed, synthesised and evaluated for their anti-inflammatory in vitro. Before starting the synthesis, docking study has been used to insert compounds within the COX-2 structure active site using celecoxib drug as a reference. Final compounds (6a,b-10a,b) were synthesised by condensing chalcones bearing pyridine moiety (1a,b-5a,b) with 4-hydrazinyl benzenesulfonamide hydrochloride.In vitro, their anti-inflammatory activity was assessed using egg-white paw edema method, they showed moderate to strong inhibitory activity. Notably, Compounds 6a (29.78%), 7a (28.43%), 9a (27.92%) and 10a (27.92%) exhibited significant percentage inhibition at 300 minutes and results are comparable with percentage inhibition drug celecoxib (22.67%) and this result is highly agreement with docking scoring study.
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