Tenidap inhibits 5-lipoxygenase product formation in vitro, but this activity is not observed in three animal models

Carty, Thomas J.; Sweeney, Francis J.; Griffiths, R.; Eskra, James D.; Ernest, Michael J.; Pillar, J.; Cheng, Jianbo; Loose, L D; Joseph, P.; Pazoles, P. P.; Moore, Peter F.; Nagahisa, Atsushi; Murase, Saori; Kadin, Saul B.

doi:10.1007/s000110050163

Cited by 7 publications

(2 citation statements)

References 48 publications

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“…Although some drugs may have shown the capacity to inhibit both 5-LO and COX in vitro, this did not always translate in vivo (42). LTB 4 , a product of the 5-LO pathway, is known to be an important mediator of a number of inflammatory responses.…”

Section: Discussionmentioning

confidence: 99%

In vivo dual inhibition of cyclooxygenase and lipoxygenase by ML-3000 reduces the progression of experimental osteoarthritis: Suppression of collagenase 1 and interleukin-1? synthesis

Jovanović

Fernandes

Martel‐Pelletier

et al. 2001

Arthritis & Rheumatism

103

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Section: Discussionmentioning

confidence: 99%

In vivo dual inhibition of cyclooxygenase and lipoxygenase by ML-3000 reduces the progression of experimental osteoarthritis: Suppression of collagenase 1 and interleukin-1? synthesis

Jovanović

Fernandes

Martel‐Pelletier

et al. 2001

Arthritis & Rheumatism

103

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“…In order to measure peritoneal leukotriene B 4 levels a modification of a previously described procedure was followed 17 . Animals received a 5‐mL intraperitoneal injection of saline containing 50 μg/mL heparin; 10 min later a laparotomy was performed and the peritoneal fluid was collected and centrifuged.…”

Section: Methodsmentioning

confidence: 99%

Tepoxalin inhibits inflammation and microvascular dysfunction induced by abdominal irradiation in rats

Panés

Mollà

Casadevall

et al. 2000

Aliment Pharmacol Ther

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INTRODUCTIONRadiation therapy for malignant pelvic, abdominal, or retroperitoneal diseases has the concurrent problem of radiation-induced bowel injury. Such injuries complicate current treatment regimens and preclude the use of larger radiation dosage and potentially more curable treatment schedules. The response of the microvasculature to radiation is widely regarded as the doselimiting factor for untoward effects to the intestine. Recent morphological and intravital microscopic studies have documented an early in¯ammatory response, appearing only a few hours after irradiation and characterized by leucocyte in®ltration into the irradiated organs. 1±3 This in¯ammatory response has been implicated in the vascular alterations that result from SUMMARY Background: In¯ammatory cells contribute to the acute and sub-acute sequelae of radiation therapy. Tepoxalin, an inhibitor of cyclooxygenase and 5-lipoxygenase that suppresses NF±jB activation, has potent anti-in¯am-matory activity. Aims: To assess the effects of tepoxalin on radiationinduced in¯ammatory damage, and determine its mechanisms of action. Methods: Leucocyte rolling, adhesion and emigration, and albumin leakage were determined by intra-vital microscopy in rat mesenteric venules. NF±jB activation was measured by electrophoretic mobility shift assays, and endothelial intercellular adhesion molecule-1 expression by the radiolabelled antibody technique. Groups of irradiated rats were treated with tepoxalin, Nacetyl-L-cysteine, zileuton (lipoxygenase inhibitor), or vehicle.

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3‐Alkenyl‐oxindoles: Natural Products, Pharmaceuticals, and Recent Synthetic Advances in Tandem/Telescoped Approaches

2010

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The structures and biological activities of naturally occurring 3‐alkenyl‐oxindoles are reviewed. Important man‐made3‐alkenyl‐oxindoles are covered, particularly those with pharmaceutical applications such as sunitinib (SU11248), the orally active receptor tyrosine kinase inhibitor marketed by Pfizer as Sutent®. Traditional synthetic approaches to 3‐alkenyl‐oxindoles are summarised and then recently developed tandem/telescoped synthetic routes are described.

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Tenidap inhibits 5-lipoxygenase product formation in vitro, but this activity is not observed in three animal models

Cited by 7 publications

References 48 publications

In vivo dual inhibition of cyclooxygenase and lipoxygenase by ML-3000 reduces the progression of experimental osteoarthritis: Suppression of collagenase 1 and interleukin-1? synthesis

In vivo dual inhibition of cyclooxygenase and lipoxygenase by ML-3000 reduces the progression of experimental osteoarthritis: Suppression of collagenase 1 and interleukin-1? synthesis

Tepoxalin inhibits inflammation and microvascular dysfunction induced by abdominal irradiation in rats

3‐Alkenyl‐oxindoles: Natural Products, Pharmaceuticals, and Recent Synthetic Advances in Tandem/Telescoped Approaches

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