Anti-inflammatory assay

Among five triterpenoids isolated from Calendula officinalis flowers, P-amyrin (119), faradiol (232), i /-taraxasterol (238), taraxasterol (239), and lupeol (238), the diol 232 was the most active. It showed a dose-dependent effect with a potency that equals that of indomethacin (5) in the topical anti-inflammatory assay with croton oil [33]. Esterification at C-3 of 232 with a fatty acid reduced the activity by more than 50% [33] consistent with our observation in the TPA-induced assay described above. The anti-inflammatory properties, as determined by croton oil-induced edema of mouse ear, of faradiol-3-O-myristate (233) and its 3-O-palmitate (234), the main components of lipophilic extracts of C. officinalis flowers, were shown to be contribute significantly to the pronounced antiphlogistic activity of the lipophilic extracts of C. officinalis flowers [34]. 

Prior to the identification of the COX-2 enzyme, researchers at DuPont identified a potent anti-inflammatory compound, DuP-697 (1) which was a relatively weak inhibitor of bovine seminal vesicle prostaglandin synthesis, but potent in a variety of anti-inflammatory assays [22]. It was later found that this compound possessed selective inhibitory activity against COX-2. A structurally dissimilar compound, NS-398 (2), was also established to be... 

Tolmetin sodium is rapidly and almost completely absorbed on oral administration, with peak plasma levels being attained within the first hour of administration. It has a relatively short plasma half-life of approximately 1 hour because of extensive first-pass metabolism, involving hydroxylation of the p-methyl group to the primary alcohol, which is subsequently oxidized to the dicarboxylic acid shown below. This metabolite is inactive in standard in vivo anti-inflammatory assays. The free acid (pKa = 3.5) is highly bound to plasma proteins (99%), and excretion of tolmetin and its metabolites occurs primarily in the urine. 

The anti-inflammatory effect of the EO from the leaves of indigenous Cinnamomum osmophloeum Kaneh. (camphor tree, Lauraceae) was studied by Chao et al. (2005). Twenty-one components, among which the monoterpenes 1,8-cineole (17%) and santolina triene (14.2%) and the sesquiterpenes spathulenol (15.7%) and caryophyUene oxide (11.2%), were analyzed as main constituents. In the anti-inflammatory assay it was found that the EO exerted a high capacity to suppress pro-IL-l i protein expression induced by LPS-treated J774A.1 murine macrophage at dosages of 60 xg/mL. Additionally, IL-lp and IL-6 production was reduced at the same dose. The TNE-a production could not be influenced by this dose of the EO. 

Analgesic Anti-inflammatory Agents - Inasmuch as a CNS component is involved in the development of inflammatory response, it.is not surprising that morphine, chloropromazine, anti-depressants and related structures are highly active in the edema, granuloma and other anti-inflammatory assays. l f 3 a recent exan le was the alkaloid cryogenine equipotent to phenylbutazone. These compounds usually produce less gastrointestinal irritation, but their application is more effective in acute inflammatory disorders and limited by other CMS effects associated with them. 

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