Congratulations to the Loesgen and Strother Labs on their recent publication in the Journal of Natural Products, titled “Antinociceptive Benzothiazine and Benzothiazole Natural Products from Marine Croceibacter atlanticus."
Previous Loesgen Lab graduate student Erin Marshall discovered and characterized new analgesic/anti-nociceptive compounds from a marine bacterium, isolated from the Arctic Ocean.
Abstract
With the goal of identifying new therapeutic leads to treat pain, we screened a library of microbial chemical extracts using the Embryonic Zebrafish Irritant-evoked Hyperlocomotion (EZIH) assay, an in vivo phenotypic assay for analgesic/antinociceptive activity. We found that extracts from the bacterium Croceibacter atlanticus substantially altered behavioral responses. Using behavior-guided fractionation to identify the active partitions, we determined that the known 1,4-benzothiazin-3-one BPSS2111–2113:C and the new benzothiazole croceithiazole A suppress behavioral responses to painful and/or nociceptive stimuli without apparent acute toxicity. Further investigation with radioligand binding assays revealed that BPSS2111–2113:C shows selective binding to both the serotonin receptor 5-HT2B and the benzodiazepine site of GABAA receptors, while croceithiazole A appears to bind the peripheral benzodiazepine receptor. These results suggest that BPSS2111–2113:C and croceithiazole A are interesting leads as analgesics, sedatives, anesthetics, or molecular probes.
Full Paper: Antinociceptive Benzothiazine and Benzothiazole Natural Products from Marine Croceibacter atlanticus
Public depository version: NSF PAR https://nsfpar.research.gov/services/metadata/file/10676363