Natural celecoxib

There are at least two factors that could influence the turnover rate, the site of metabolism (hot spot) and the affinity of a compound toward these enzymes the protein/ligand (substrate or inhibitor) interaction and the chemical reactivity of the compound towards oxidation. Because of the interaction of the protein with the potential ligand, certain atoms of the compound could be exposed to the heme group, and depending on the chemical nature of these moieties the oxidative reaction will take place at different rates, for example celecoxib is metabolized by CYP2C9 at the... 

Two case reports have suggested a potential association between the sulfonamide group in celecoxib and the development of acute pancreatitis (99,100). The cause of acute pancreatitis in patients taking celecoxib is speculative, but sulfonamides are known to cause pancreatitis, and one of these patients reported an allergy to sulfa medication. Thus, the reaction might have been allergic in nature. 

Not many pyrazoles and indazoles exist in nature. However, many synthetic medicines do contain pyrazoles, pyrazolones, and indazoles. For instance, an anti-inflammatory cyclooxygenase-2 (COX-2) selective inhibitor celecoxib (Celebrex) has the tri-substituted pyrazole as its core structure. A fully substituted pyrazole, rimonabant (Acomplia), is a selective inverse agonist for the cannabinoid receptor type 1 (CBi). Acomplia was marketed in 56 countries for the treatment of obesity by Sanofi-Aventis starting in... 

Celecoxib is extensively distributed in tissues and is 97% protein-bound. It is bound primarily to albumin and to a lesser extent alpha-1-acid glycoprotein. The approximate volume of distribution at steady state is 400 liters, suggesting extensive distribution into the tissues. This extensive volume of distribution may be related to the lipophilic nature of celecoxib as well as to its high PKa (11.1). The effective plasma is approximately 11 hours under fasting conditions [1]. 

Ibrahim, M.M., et al. Natural bioadhesive biodegradable nanoparticles-based topical ophthalmic formulations for sustained celecoxib release. J. Pharm. Tech. Drug. Res. 2(1), 7 (2013)... 

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