Abstract
Six halogenated alkaloids have been semi-synthesized from natural boldine as starting material. Their antioxidant activity toward reactive oxygen species (ROS) generation by neutrophils stimulated with N-formyl-methionyl-leucyl-phenylalanine and in the hypoxanthine–xanthine oxidase system was evaluated. Most of the alkaloids synthesized inhibited ROS generation in both systems in a concentration-dependent manner. The alkaloids with phenolic substituents displayed more powerful anti-oxidative activity than those containing methoxylated groups. None of the alkaloids assayed had any effect on xanthine oxidase activity. Therefore, halogenated phenanthrene alkaloids can become in promising candidates for the development of novel and potent anti-inflammatory drugs.
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