Semisynthesis and Kappa-Opioid Receptor Activity of Derivatives of Columbin, a Furanolactone Diterpene.
Journal of natural products July 28, 2017 Anil Yilmaz, Rachel Saylor Crowley, Alexander M Sherwood et al.
Columbin, a natural compound from plants used in traditional medicine, was modified to create derivatives that might activate the kappa-opioid receptor (KOR), a target for conditions like anxiety, depression, and addiction. The derivatives showed slightly improved activity at the KOR compared to the original columbin, but neither the parent compound nor its derivatives were potent KOR ligands. This study is the first to test columbin at the KOR and explores chemical modifications that can be made to the columbin molecule.