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Literature DB >> 2117339

Biochemical and pharmacological properties of a new topical anti-inflammatory compound, 9-phenylnonanohydroxamic acid (BMY 30094).

K M Tramposch¹, F C Zusi, S A Marathe, P L Stanley, X Nair, S A Steiner, J W Quigley.

Abstract

Drugs which block the biosynthesis of leukotrienes and prostaglandins may have potential in the treatment of psoriasis and other skin diseases. The biochemical and anti-inflammatory activity of 9-phenylnonanohydroxamic acid (BMY 30094) is described. BMY 30094 inhibited human neutrophil 5-lipoxygenase with an IC50 of 5.7 microM. BMY 30094 also blocked human platelet cyclooxygenase and lipoxygenase with IC50 values of 15.2 and 15.0 microM, respectively. Topical application of this compound blocked arachidonic acid and 12-O-tetradecanoylphorbol ester-induced mouse skin inflammation with activity comparable to that observed for lonapalene. The topical ED50 for BMY 30094 in the arachidonic acid-induced inflammation model is 2.2 mumoles/ear. In the sub-cutaneous carrageenan sponge assay in rats, BMY 30094 blocked LTB4 and PGE2 production and inhibited neutrophil migration. This compound would be a useful tool to determine the role of arachidonic acid metabolites in the etiology of inflammatory dermatoses.

Entities: Chemical Disease Species

Mesh：

Substances：

Year: 1990 PMID： 2117339 DOI： 10.1007/bf01966310

Source DB: PubMed Journal: Agents Actions ISSN： 0065-4299

27 in total

1. A new approach to anti-inflammatory drugs.

Authors: G A Higgs; R J Flower; J R Vane
Journal: Biochem Pharmacol Date: 1979-06-15 Impact factor: 5.858

2. Arachidonic acid in psoriasis. Pathogenic role and pharmacological regulation.

Authors: K Kragballe; J J Voorhees
Journal: Acta Derm Venereol Suppl (Stockh) Date: 1985

3. Local vascular changes induced by the cocarcinogen, phorbol myristate acetate.

Authors: A Janoff; A Klassen; W Troll
Journal: Cancer Res Date: 1970-10 Impact factor: 12.701

4. Arachidonic acid and leukotrienes in dermatology.

Authors: K Kragballe; J J Voorhees
Journal: J Invest Dermatol Date: 1983-10 Impact factor: 8.551

5. Prostaglandin E and F levels in mouse epidermis are increased by tumor-promoting phorbol esters.

Authors: C L Ashendel; R K Boutwell
Journal: Biochem Biophys Res Commun Date: 1979-09-27 Impact factor: 3.575

6. Selective inhibition of arachidonate 5-lipoxygenase by novel acetohydroxamic acids: effects on acute inflammatory responses.

Authors: G A Higgs; R L Follenfant; L G Garland
Journal: Br J Pharmacol Date: 1988-06 Impact factor: 8.739

2. Combination of a dual 5-lipoxygenase/cyclooxygenase inhibitor with a glucocorticoid results in synergistic topical antiinflammatory activity without inducing skin atrophy.

Authors: K M Tramposch
Journal: Inflammation Date: 1993-10 Impact factor: 4.092

2 in total

Biochemical and pharmacological properties of a new topical anti-inflammatory compound, 9-phenylnonanohydroxamic acid (BMY 30094).

1. A new approach to anti-inflammatory drugs.

2. Arachidonic acid in psoriasis. Pathogenic role and pharmacological regulation.

3. Local vascular changes induced by the cocarcinogen, phorbol myristate acetate.

4. Arachidonic acid and leukotrienes in dermatology.

5. Prostaglandin E and F levels in mouse epidermis are increased by tumor-promoting phorbol esters.

6. Selective inhibition of arachidonate 5-lipoxygenase by novel acetohydroxamic acids: effects on acute inflammatory responses.

7. Determination of ibuproxam and its metabolites in the plasma and urine of rats.

8. Prostaglandin and leukotriene synthesis in mouse ears inflamed by arachidonic acid.

9. Tachyphylaxis in 12-0-tetradecanoylphorbol acetate- and arachidonic acid-induced ear edema.

10. Modulation of mouse ear edema by cyclooxygenase and lipoxygenase inhibitors and other pharmacologic agents.

1. Temporal infiltration of leukocyte subsets into mouse skin inflamed with phorbol ester.

2. Combination of a dual 5-lipoxygenase/cyclooxygenase inhibitor with a glucocorticoid results in synergistic topical antiinflammatory activity without inducing skin atrophy.