Scale up isolation, characterization and in vivo evaluation of aaptamine from A. aaptos suggests its anti‐depressant effects are linked to the DOP receptor

Abstract

Recently we discovered that the aaptamine class of marine sponge derived natural products exhibit selective agonist activity in vitro for the delta opioid receptor (DOR) versus mu opioid receptor (MOR). Our findings may explain reports by others that aaptamine (1) demonstrates in vivo anti-depressant effects in mouse models using the Porsolt Forced Swim Test. This project involved the extraction of the sponge Aaptos aaptos (a source of 1), establishing a scale up purification procedure to provide sufficient amounts of 1 (30 mg) for a follow up in vivo evaluation and ultimately confirmation of the structure of 1 using LC-MS and 1H NMR. The results of our purification scheme, chemical analysis and in vivo evaluation of 1 using assays measuring anti-depressant like activity are reported here in and suggest that the in vivo anti-depressant effects of 1 are linked directly to its agonist effects on the DOR receptor. Support or Funding Information Fletcher Jones Fund of Dominican University of California, Grants from NIH, R01DA015232 (J.L.W), R01DA019958 (J.L.W), R21DA031574 (J.L.W.), R01CA47135 (P.C.), and NSF MS Instrument Grant UCSC CHE-147922 (P.C.) This abstract is from the Experimental Biology 2018 Meeting. There is no full text article associated with this abstract published in The FASEB Journal.