Aphios Corporation

Marine Anti-Plaque Compound – Asterias™

Aphios Corporation is developing a marine anti-plaque compound, Asterias,™ for use in toothpastes and rinses for oral care [US Patent Pending].

Epidemiological surveys indicate that about 50% of the adult population of the United States has gingivitis, which can lead to a number of life threatening illnesses such as heart disease. Most anti-gingivitis compounds, e.g. triclosan, chlorhexidine and fluorine, are halogenated.

Marine microorganisms are a unique source of novel genotypes and chemical entities, which can generate compounds that integrate halogens such as chlorine and bromine. Marine microorganisms, because of their intrinsic capability to metabolize halogens, can thus be an important resource for the discovery of bioactive secondary metabolites and compounds with antimicrobial, anti-cariogenic and anti-plaque forming properties.

Aphios Corporation has developed a unique collection of marine microorganisms isolated from diverse environments such as: (i) marine invertebrates including bryozoans, sponges, corals, tunicates; (ii) deep sea sediments and shallow mangrove swamps; (iii) hypersaline ponds; (iv) hydrothermal vents; (v) marine vertebrates like fish and shark; (vi) tropical and temperate oceans; and (vii) plants including macroalgae.

Marine microbes are first fermented by methods that mimic the natural saline marine environment in order to enhance isolation of bioactive compounds. The microorganisms are fermented in at least four different saline media designed to maximize the diversity of secondary metabolites and enzymes. The media are high or low in particular nutrients, specifically carbon and nitrogen. Carbon sources are glucose, glycerol, or Na acetate. Nitrogen sources are peptone, yeast extract, and beef extract. Marine fermentation media are prepared in artificial sea water.

Through screening of its marine molecules library for anti-plaque activity against microbes relevant to the flora of the oral cavity, Aphios has discovered and identified bioactive components derived from an obligate marine microorganism (APP-214), and scaled up manufacturing of the active ingredient Asterias.™ This compound is being further developed by medicinal chemistry to maximize effectiveness and substantivity against orally relevant microorganisms. In this research effort, Aphios is collaborating with renowned scientists from University of California, Los Angeles (UCLA), Los Angeles, CA, Massachusetts Institute of Technology, Cambridge, MA, Tufts University, Boston, MA and Scripps Institution of Oceanography, La Jolla, CA. This research is partially funded by the National Institute of Dentistry and Craniofacial Research (NIDCR), National Institutes of Health (NIH) through a Small Business Innovative Research (SBIR) grant.