The stable cyclic adenosine monophosphate analogue, dibutyryl cyclo-adenosine monophosphate (bucladesine), is active in a model of acute skin inflammation.

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  • Author(s): Rundfeldt C; Steckel H; Sörensen T; Wlaź P
  • Source:
    Archives of dermatological research [Arch Dermatol Res] 2012 May; Vol. 304 (4), pp. 313-7.
  • Publication Type:
    Journal Article
  • Language:
    English
  • Additional Information
    • Source:
      Publisher: Springer Verlag Country of Publication: Germany NLM ID: 8000462 Publication Model: Print Cited Medium: Internet ISSN: 1432-069X (Electronic) Linking ISSN: 03403696 NLM ISO Abbreviation: Arch Dermatol Res Subsets: MEDLINE
    • Publication Information:
      Original Publication: Berlin : Springer Verlag
    • Subject Terms:
      Anti-Inflammatory Agents/*therapeutic use ; Bucladesine/*therapeutic use ; Dermatitis/*drug therapy; Administration, Topical ; Animals ; Arachidonic Acid/toxicity ; Bucladesine/adverse effects ; Cyclic AMP/analogs & derivatives ; Disease Models, Animal ; Edema/chemically induced ; Edema/drug therapy ; Emulsions ; Humans ; Male ; Mice ; Treatment Outcome
    • Abstract:
      Anti-inflammatory therapeutic options for the topical treatment of skin diseases with inflammatory or allergic contribution are mostly limited to topical glucocorticoids and calcineurin inhibitors. Both compound classes induce adverse effects. Elevation of intracellular cyclic adenosine monophosphate (cAMP) by inhibition of phosphodiesterase 4 was shown to induce potent anti-inflammatory effects, but the safety profile of currently available compounds is not sufficient. A different approach to increase intracellular cAMP is the substitution of chemically stabilized cAMP analogues. Bucladesine is a stabilized cAMP analogue with an excellent safety profile which had been marketed as topical treatment of impaired wound healing. In the current study, a novel water free emulsion containing bucladesine was evaluated for anti-inflammatory effects. In the arachidonic acid induced ear oedema model in mice, single or multiple administration of an emulsion containing 1.5% was capable of significantly reducing the inflammatory oedema. The data indicate that bucladesine represents an interesting treatment option for skin diseases where an anti-inflammatory activity is indicated. Due to the established clinical safety, this agent may bridge the gap between potent agents such as glucocorticoids or calcineurin inhibitors and emollients without active compounds.
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    • Accession Number:
      0 (Anti-Inflammatory Agents)
      0 (Emulsions)
      27YG812J1I (Arachidonic Acid)
      63X7MBT2LQ (Bucladesine)
      E0399OZS9N (Cyclic AMP)
    • Publication Date:
      Date Created: 20120204 Date Completed: 20140718 Latest Revision: 20211021
    • Publication Date:
      20240829
    • Accession Number:
      PMC3332354
    • Accession Number:
      10.1007/s00403-012-1216-6
    • Accession Number:
      22302126