ABSTRACT
Since its role in inflammatory diseases was recognized, nitric oxide (NO) has become an important mediator to evaluate anti-inflammatory agents. Sesquiterpene lactones, which occur in several medicinal plants, inhibit the NO production in macrophage-like cells. This action is probably due to a 1,4 addition reaction between its alpha,beta-unsaturated carbonyl group with sulfhydryl (SH)-containing compounds. For this reason it is believed that these compounds are cytotoxic, which restricts their therapeutic use. In this contribution, the ability of the ambrosanolide-type sesquiterpene lactone cumanin (from the Asteraceae Ambrosia psilostachya) to inhibit NO biosynthesis was evaluated in lipopolisaccharide-induced peritoneal murine macrophages and its cytotoxicity was assessed in the MTT assay. Cumanin showed a potent inhibitory effect in NO production (IC(50) = 9.38+/-0.38 microM) with low cytotoxicity. The 1,4-addition reaction of thiols was slow, which does not explain the inhibition of NO production but does explain the low cytotoxicity of cumanin with respect to other lactones.
Subject(s)
Ambrosia , Macrophages, Peritoneal/drug effects , Nitric Oxide/antagonists & inhibitors , Nitric Oxide/biosynthesis , Animals , Cell Survival/drug effects , Cell Survival/physiology , Macrophages, Peritoneal/metabolism , Male , Mice , Plant Components, Aerial , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Sesquiterpenes/chemistry , Sesquiterpenes/isolation & purification , Sesquiterpenes/pharmacologyABSTRACT
The dried aqueous extract of aerial parts of Cirsium subcoriaceum (Asteraceae) and its major flavonoid glycoside, pectolinarin, have been evaluated for analgesic and anti-inflammatory effects in mice and rats, respectively. Both the extract and pectolinarin exerted significant and dose-dependent analgesic and anti-inflammatory activities. Also, the anti-inflammatory activities of an aqueous extract of Buddleia cordata and its principal glycoside linarin were evaluated. The results of pharmacological testing proved that linarin is a better anti-inflammatory agent than pectolinarin and indomethacin. On the other hand, pectolinarin exerted a better analgesic effect than linarin.
