Anthraquinone-2,6-disulfonic acid as a disease-modifying osteoarthritis drug: An in vitro and in vivo study

Lucia Savarino, Antonella Fioravanti, Graziana Leo, Ruggero Aloisi, Maurizio Mian

Research output: Contribution to journalArticle


Pharmacologic treatment of osteoarthritis has been confined mostly to analgesic or nonsteroidal antiinflammatory drugs that only modify the symptoms. We asked whether anthraquinone-2,6-disulfonic acid might act as a disease-modifying osteoarthritis drug. We evaluated the in vitro inhibitory effect of anthraquinone-2,6-disulfonic acid on cathepsin B activity and proteoglycan release from cultured rabbit cartilage challenged with interleukin-1β in comparison with diacerhein, the prodrug of rhein. We studied the in vivo activity in an experimental osteoarthritis model induced by medial monolateral meniscectomy in rabbits. After 3 months of treatment with oral anthraquinone-2,6-disulfonic acid or diacerhein at 25 mg/kg/day, the animals were sacrificed and the knees were retrieved; cluster chondrocytes, fibrillations, fissures, and osteophytes were studied on cartilage biopsies. The evidence for disease-modifying activity of anthraqui-none-2,6-disulfonic acid was (1) the in vitro dose-dependent inhibition of cathepsin B activity, (2) the in vitro time- and dose-dependent inhibition of interleukin-1β-stimulated proteoglycan release from the cartilage matrix, and (3) the in vivo reduction of all cartilage degeneration parameters. Our data suggest anthraquinone-2,6- disulfonic acid is worth exploring for treating osteoarthritis.

Original languageEnglish
Pages (from-to)231-237
Number of pages7
JournalClinical Orthopaedics and Related Research
Issue number461
Publication statusPublished - Aug 2007

ASJC Scopus subject areas

  • Surgery
  • Orthopedics and Sports Medicine

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