ABSTRACT
The root of Angelica gigas [gigantus] Nakai (AGN) is a medicinal herbal in Korea. AGN root ethanolic extract dietary supplements are marketed for memory health and pain management. More than a dozen preclinical in vivo bioactivities of AGN extracts, including anti-cancer and sleep promotion, have been reported. Significant progress has been made in understanding the pharmacokinetics (PK) and metabolism of signature phytochemicals decursin and decursinol angelate and their botanical synthesis precursor and mammalian hepatic metabolite, decursinol, including human PK studies. This chapter summarizes PK and metabolism of pyranocoumarins and preclinical in vivo anti-cancer efficacy. For human clinical translation, significant challenges include sourcing of AGN extracts and product consistency. Human clinical trial design and AGN dose optimization are paramount in unlocking the anti-cancer potential. An open label Phase I/II trial is under way to estimate the effect size in a niche patient cohort with biochemically recurrent prostate cancer.
