Anti-inflammatory activity of orpanoxin administered orally and topically to rodents

Brooks, Robert R.; Bonk, Kenneth R.; Decker, George E.; Miller, Kim E.

doi:10.1007/bf01982875

Cited by 24 publications

(12 citation statements)

References 11 publications

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“…While it is not clear if the effects of oral and topical application of other NSAIDs are similar, it is clear that the vehicle employed could have a significant effect on the activity of the topically applied drug. The effects for topically applied piroxicam and indomethacin reported here are less impressive than those reported in the literature [6,8,18,21], but this may be due to differences in the vehicles used. Those studies used agents (propylene glycol, urea, alcohol solutions) in the vehicles which might promote penetration through the skin.…”

Section: Discussioncontrasting

confidence: 72%

“…Piroxicam [8,19], bendazac [3], aspirin [7], etoclofene [5], orpanoxin [6], BRL-20459 [17], indomethacin [18], ketoprofen [20], suprofen [4], and steroids [21,22] have all shown to possess efficacy or bioavailability when used topically in animal models of inflammation. In general, preparations of these drugs in the 3-10% range were required to achieve significant activity.…”

Section: Discussionmentioning

confidence: 99%

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The topical anti-inflammatory and analgesic properties of bromfenac in rodents

Nolan¹,

Wagner²,

Gathright³

et al. 1988

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Bromfenac [2-amino-3-(4-bromobenzoyl)benzeneacetic acid sodium salt sesquihydrate] is an anti-inflammatory/analgesic agent that possesses potent topical activity in rats, guinea pigs, and mice. In rat models of acute (carrageenan paw edema) and chronic (adjuvant arthritis) inflammation, preparations of bromfenac at concentrations as low as 0.01-0.32% (0.01-0.32 mg bromfenac) produced significant anti-inflammatory activity when applied to the injected paw or to the backs of rats. In the acute paw edema test, topical bromfenac was more potent than indomethacin or hydrocortisone and about as active as triamcinolone acetonide. Bromfenac, at concentrations of 0.1-0.32%, showed topical analgesic activity in the acetylcholine-induced abdominal constriction test in mice. In this test, bromfenac was more potent than indomethacin (24.9X), more potent than ketoprofen (approximately 14.9X), and superior to piroxicam. In the guinea pig UV-erythema test, bromfenac was active (26.1X indomethacin) when applied to the UV-exposed site, but not when applied away from the site. The results suggest that bromfenac has activity topically because of a local and a systemic effect. Test results obtained with a long (4-7 hr) pretreatment time (paw edema, adjuvant arthritis, abdominal constriction) are due in great part to a systemic effect of topically applied bromfenac, while the UV-erythema test (1-hr treatment time) clearly indicates a local effect.

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Section: Discussioncontrasting

confidence: 72%

Section: Discussionmentioning

confidence: 99%

The topical anti-inflammatory and analgesic properties of bromfenac in rodents

Nolan¹,

Wagner²,

Gathright³

et al. 1988

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“…Croton oil irritant solution (0.1 ml) prepared according to Brooks et al (1985) was applied to the inner surface of the right ear of mice. The mice were divided into three groups of 6 animals in each group.…”

Section: Croton-oil Induced Ear Inflammationmentioning

confidence: 99%

Anti-inflammatory activity of tea (Camellia sinensis) root extract

et al. 2004

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“…1980Brooks et al 1985a. It also suppresses carrageenan-induced paw oedema in the dog (Brooks et al 1985b).…”

mentioning

confidence: 94%

EFFECTS OF ORPANOXIN ON ARACHIDONIC ACID METABOLISM OF HUMAN POLYMORPHONUCLEAR LEUCOCYTES AND PLATELETS IN VITRO

Doerr

Kaufman

Brooks

1988

Clin Exp Pharma Physio

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1. The effect of orpanoxin, a nonsteroidal anti-inflammatory drug, on cyclo-oxygenase and lipoxygenase activity in human polymorphonuclear leucocytes (PMNL) and platelets was studied ex vivo to see if lipoxygenase inhibition contributed to orpanoxin's mechanism of action. 2. In PMNL, orpanoxin (50, 100, and 200 mumols/l), like indomethacin (100 mumols/l), had little effect on synthesis of leukotriene B4 or 5S-hydroxy-6-trans,8,11,14-cis-eicosatetraenoic acid. BW755c at 100 mumols/l inhibited synthesis of both. 3. In PLT, orpanoxin (100 mumols/l) inhibited formation of cyclo-oxygenase products (thromboxanes, prostaglandins, and 12-L-hydroxy-5,8,10-heptadecatrienoic acid) and increased synthesis of the lipoxygenase product, 12S-hydroxy-5,8-cis,10-trans,14-cis-eicosatetraenoic acid. Effects of indomethacin (100 mumols/l) and benoxaprofen (100 mumols/l) in platelets were qualitatively similar to those of orpanoxin. 4. These results indicate that the discrepancy between the low potency of orpanoxin in inhibiting bovine seminal vesicle cyclo-oxygenase in vitro and its high potency as an anti-inflammatory agent in vivo is not explained by its having an additional lipoxygenase inhibitory mechanism.

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Anti-inflammatory activity of orpanoxin administered orally and topically to rodents

Cited by 24 publications

References 11 publications

The topical anti-inflammatory and analgesic properties of bromfenac in rodents

The topical anti-inflammatory and analgesic properties of bromfenac in rodents

Anti-inflammatory activity of tea (Camellia sinensis) root extract

EFFECTS OF ORPANOXIN ON ARACHIDONIC ACID METABOLISM OF HUMAN POLYMORPHONUCLEAR LEUCOCYTES AND PLATELETS IN VITRO

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