Ear edema assay

Three new oxepin-containing natural products oxepinamides A-C 166-168 and two new fumiquinazoline metabolites fumiquinazolines H-I 169-170 were isolated from organic extracts of the culture broth and mycelia of Acremonium sp., a fungus obtained from the surface of the Caribbean tunicate Ecteinascidia turbinata Compound 166 exhibited good anti-inflammatory activity in a topical RTX-induced mouse ear edema assay. Compounds 169 and 170 both exhibited weak anti-fungal activity towards Candida albicans in a broth microdilution assay. Total... 

Tolypodiol (13) is a meroditerpene that was isolated from a cultured sample of Tolypothrix nodosa originally collected in a soil sample from Nan Madol, Pohnpei. Its structure was determined by a combination of mass spectral analysis and NMR of the parent compound as well as its acetylated analogue. Tolypodiol was found to possess anti-inflammatory activity in the mouse ear edema assay with an ED50 = 30 pg per ear, which rivals that of the standard, hydrocortisone (20 pg per ear). ... 

From a taxonomically distinct and still unidentified specie of the Pseudopterogorgia genus, a related series of pseudopterosins containing bicyclic diterpenoid glycosides, 7 seco A-D, were also isolated and their structures elucidated by Look and Fenical [18]. Compounds 7 seco A-D possess potent anti-inflammatory and analgesic activities that are similar to the pseudopterosins, and also show antimicrobial activity towards the bacteria. Staphylococcus aureus. For example 7 seco-A, pseudopterosin exhibited a 69% reduction of inflammation in the mouse ear edema assay at a minimum inhibitory concentration (MIC) of 50 pg/ear. 

Assay for Iinhibition of TPA-induced Inflammatory Ear Edema in Mice... 

In vivo primary screening assay CRO Inhibition of croton oil induced ear edema... 

The anti-inflammatory activity of the hydroalcoholic extract of P. cocos against some acute and chronic inflammatory processes was established recently. It reduced the TPA-induced edema (80% inhibition at 0.5 mg/ear), but its effect was milder against the AA-induced ear edema (40% inhibition at 0.5 mg/ear). When the extract was assayed in chronic experimental model of inflammation, it caused a 53% reduction in ear thickness together with a 73% decrease in myeloperoxidase (MPO) activity, which shows that leukocyte infiltration into the inflammation site could be prevented by a repeated dose of 1 mg/ear. The main constituents isolated from the extract were identified as pachymic and dehydrotumulosic acids. Topical administration of these lanostanes inhibited the TPA-induced edema with ID50 of 2.48 and 0.31 pg/ear, respectively. Reasons for the greater activity of dehydrotumulosic acid... 

Different assays related with inflammation have been developed on different iridoids. Some iridoids appear to be efficient on subacute processes but not or only slightly active in acute processes. On paw and ear edema, has been established different relationships Recio and cols.[30] have published the modest relevance of iridoids as systemic antiinflammatory agents. However, some of them, are very active when were locally administrated. This could be due to the weak acidic nature of the iridoids, that makes them more lipophilic in acidic environments such as inflamed tissues. 

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]. 

Uttley and Van Abbey (1973) mouse ear test - undiluted shampoos were applied to one ear daily for 4 days. The degree of inflammation was quantified visually as vessel dilation, erythema and edema. A reference material was tested on another group of mice and the two were compared. The use of anesthetic may be a confounding factor in this assay as it may alter inflammation development. 

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