title: Synthesis and characterization of norbelladine, a precursor of  Amaryllidaceae alkaloid, as an anti-inflammatory/anti-COX  compound.
abstract: Rising ROS and systemic inflammation is often a serious concern in many disease conditions including obesity. Therefore, compounds with both anti-oxidant and anti-inflammatory activities are considered beneficial in preventing/treating several human chronic diseases. Norbelladine is an amine compound, a precursor for Amaryllidaceae alkaloids (e.g., belladine, crinamine, lycorine, and galanthamine) found in plants traditionally used for treating a variety of human diseases. However, little information is available about its potential health effects. Therefore, the amine was first synthesized, and its anti-oxidant and anti-inflammatory activities were investigated in this study. Also, the potential effects of the amine on NF-κB activation were investigated due to the critical involvement of ROS in the activation. Norbelladine was synthesized with more than 60% yield, analyzed by a HPLC method, and verified using NMR spectroscopic method. Then, its radical scavenging activity was investigated using DPPH- and superoxide radical assays. At the concentration of 10 μM, norbelladine was a compound able to quench DPPH-radical by 31% (P < 0.05) and reduce superoxide radicals from xanthine oxidase by 33% (P < 0.05). At the concentration of 0.25 μM, the amine also inhibited both COX-1 and COX-2 enzymes by 51% and 25% (P < 0.05), respectively. Furthermore, at the concentration of 10 μM, norbelladine inhibited NF-κB activation by 23% (P < 0.05). In summary, the data suggests that norbelladine may be a compound to quench radicals, inhibit COX enzymes as well as suppress NF-κB activation at relatively lower concentrations.
authors.forename: Jae B
authors.initials: JB
authors.lastname: Park
mesh_terms: D000470:Alkaloids / Q000737:chemistry*; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D006801:Humans; D019668:Liliaceae / Q000737:chemistry*
chemical_list: D000470:Alkaloids; D000893:Anti-Inflammatory Agents