Celecoxib, a tricyclic compound having pyrazole ring exhibits an excellent level of antiinflammatory action against COX-2 enzymes and some of its analogs act as anticancer and antibacterial agents. Various efficient routes and different improved processes for the synthesis of this drug have already been disclosed in the literature. However, there is a need for further developments in the present scenario of achieving cost effective synthetic technologies to celecoxib with high purity accompanied by excellent yield. Therefore, an effort has been made to summarize briefly the different methods of preparation of Celecoxib with their advantages or disadvantages that have been reported in various patents up to 2013. The present review would be beneficial for scientific community for further developments in the synthetic methodologies for Celecoxib and to explore some novel celecoxib based biologically active agents.
Physiologically dropped immature Citrus reticulata Blanco fruits are regarded as waste and discarded in the citrus orchard but are a good source of bioactive compounds including flavonoids, antioxidants and total phenols. A study was undertaken to identify and quantify these bioactive compounds and to investigate the influence of different drying techniques, namely freeze drying and hot air oven drying, on flavonoids namely flavanone glycosides, antioxidant potential and total phenol content in immature dropped fruits of Citrus reticulata Blanco. Flavonoids were quantified in high-performance liquid chromatography (HPLC). The antioxidant activity were investigated with three assays azino-bis [3-ethylbenzthiazoline-6-sulfonic acid]) (ABTS), 2,2-diphenyl-1-picrylhydrazyl radical (DPPH), Ferric Reducing Ability of Plasma (FRAP) and total phenol content was determined. Freeze dried samples of 12 and 14 mm size retained maximum hesperidin flavonoid content (27.03% and 27.20%) as compared to the hot air dried samples (17.99%) and retained higher phenolic content ranged from 50.54–54.19 mg GAEL−1. The antioxidant activity in freeze dried fruits was from 12.21–13.55 mM L−1 Trolox and 15.27–16.72 mM L−1 Trolox with ABTS, DPPH assay and FRAP values ranging from 7.31–9.07 mM L−1 Trolox. Significant positive correlation was found between the flavonoid hesperidin with antioxidant assays and total phenolic content (TPC). The results showed that waste citrus fruits can act as potential source of bioflavonoids, especially hesperidin, and antioxidants for pharmaceutical as well as nutraceutical industry.
Purpose Pain is an unpleasant sensation, but a protective mechanism of our body. It is the most common medical complaint requiring a visit to a physician. The new non-steroidal anti-inflammatory drug (NSAID) – zaltoprofen, is a preferential COX-2 inhibitor. It also inhibits bradykinin-induced nociceptive responses by blocking the B2 receptor-mediated pathway in the primary sensory neurons. The present study was conducted to evaluate and compare the anti-nociceptive activity of zaltoprofen with a conventional NSAID – piroxicam, in a mouse model of acute pain using hot plate and tail flick tests. Materials and methods Twenty-four adult Swiss albino mice (20–25 g) of either sex were used in this study. Oral zaltoprofen and piroxicam were used as test and standard drugs respectively. Anti-nociceptive activity was evaluated and compared using hot plate and tail flick tests. Results In comparison to the control group (vehicle), zaltoprofen showed a significant increase in reaction time at various time periods in the hot plate and tail flick tests. In the hot plate method, zaltoprofen groups (15 and 20 mg/kg) showed a significant elevation in pain threshold in comparison to control group (vehicle) ( p <0.001). In the tail flick model also, zaltoprofen groups (15 and 20 mg/kg) showed a significant increase in the reaction time in comparison to control group (vehicle). In both the analgesiometer assays, zaltoprofen was found to be non-inferior compared to a standard drug – piroxicam (positive control). Conclusion Our study concludes that zaltoprofen is an effective analgesic agent in various pain models. Our results support that zaltoprofen has therapeutic potential for treating pain disorders and is non-inferior to a standard drug – piroxicam.
Citrus fruits are famous for nutritional value and studies are there for extraction of secondary metabolites from citrus waste. An attempt was made to quantify antioxidants, flavonoids and phenols from dropped fruits of 8–24 mm size, to find the impact of freeze and hot-air oven drying techniques on extraction. Flavonoids (hesperidin, narirutin/isonaringin, diosmin and didymin/neoponcirin) were quantified through high performance liquid chromatography (HPLC) and total phenols (TPC) were estimated by Folin-Ciocalteu method. Antioxidant capacity was adjudged by azino-bis [3-ethylbenzthiazoline-6-sulfonic acid] (ABTS), 2, 2-diphenyl-1-picrylhydrazyl radical (DPPH) and Ferric Reducing Antioxidant Power (FRAP). Freeze dried fruits of 10 mm and 12 mm retained maximum hesperidin content (22.383% and 21.560%) in comparison to hot-air oven counterparts (18.377% and 15.090%). Narirutin/isonaringin (1.343% and 1.191%), diosmin (5.293% and 3.234%) and didymin/neoponcirin (1.187% and 1.113%) content were found higher in 8 mm and 10 mm freeze dried fruits. The antioxidant capacity (7.548–11.643 mmol L−1 Trolox, 8.164–14.710 mmol L−1 Trolox, 4.008–5.863 mmol L−1 Trolox by ABTS, DPPH and FRAP assays) and TPC were found higher in freeze dried samples. Significant correlation was found between antioxidant capacity, TPC and flavonoids at p < 0.01. Freeze drying technique can be adopted for retaining and quality extraction of bioactive compounds from immature dropped fruits for further use in nutraceutical industries.
Children with Down syndrome have elevated levels of oxidative stress . Hence antioxidant therapy can be beneficial among them.
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