Korean Angelica gigas Nakai (AGN) is a major medicinal herb used in Asian countries such as Korea and China.
Traditionally, its dried root has been used to treat anemia, pain, infection and articular rheumatism in Korea, most often through boiling
in water to prepare the dosage forms. The pyranocoumarin compound decursin and its isomer decursinol angelate (DA) are the major
chemical components in the alcoholic extracts of the root of AGN. The in vitro anti-tumor activities of decursin and/or DA against
prostate cancer, lung cancer, breast cancer, colon cancer, bladder cancer, sarcoma, myeloma and leukemia have been increasingly
reported in the past decade whereas the in vivo efficacy in mouse models was established only for a few organ sites. Preliminary
pharmacokinetic studies by us and others in rodent models indicated that decursinol (DOH), which has much less in vitro direct anticancer
activities by itself, is the major and rapid in vivo hydrolysis metabolite of both decursin and DA. Besides decursin, DA and DOH,
other chemical components in AGN such as polysaccharides and polyacetylenes have been reported to exert anti-cancer and antiinflammation
activities as well. We systematically reviewed the published literature on the anti-cancer and other bio-activities effects of
AGN extract and decursin, DA and DOH, as well as other chemicals identified from AGN. Although a number of areas are identified that
merit further investigation, one critical need is first-in-human studies of the pharmacokinetics of decursin/DA to determine whether
humans differ from rodents in absorption and metabolism of these compounds.