A neuroprotective sulfone of marine origin and the in vivo anti-inflammatory activity of an analogue

Our continuing effort of searching bioactive substances from the Formosan soft coral Cladiella australis has led to the isolation of a bioactive substance austrasulfone (1), which possesses significant neuroprotective activities. A straightforward synthesis of 1 was achieved by a two-step reaction sequence. Dihydroaustrasulfone alcohol (3), the synthetic precursor of 1, not only exhibited in vitro anti-inflammatory activity, but also showed potent therapeutic ability in the treatment of neuropathic pain, atherosclerosis, and multiple sclerosis in rats.

Isolation, activity, and synthesis of a new soft coral metabolite, austrasulfone (1), were described. Its synthetic intermediate, dihydroaustrasulfone alcohol (3), also exhibited promising in vitro and in vivo anti-inflammatory activity.Figure optionsDownload as PowerPoint slideResearch highlights
► A neuroprotective agent, austrasulfone (1), has been isolated from marine soft coral Cladiella australis.
► A straightforward synthesis of 1 was achieved by a two-step reaction sequence.
► Its synthetic intermediate, dihydroaustrasulfone alcohol (3), not only exhibited in vitro anti-inflammatory activity, but also showed potent therapeutic ability in the treatment of neuropathic pain, atherosclerosis, and multiple sclerosis in rats.