Boesenbergia rotunda (the family Zingiberaceae) is a well-known medicinal plant from Southeast
Asia and China. Its parts, especially the roots, were used as an alternative in cuisine, and flavoring. Many attempts
tend to explore its phytochemistry and pharmacological values. The ultimate goal of this review is to
critically offer the pharmacological values and mechanisms of action of B. rotunda crude extracts and their isolated
compounds. Phytochemical investigation and pharmacokinetics were also discussed.On the basis of the
most effective keyword “Boesenbergia rotunda”, the relevant data have been gathered from international electronic
sources, including Sci-Finder, Google Scholar, PubMed, and reputation publishers. B. rotunda species
was reported to contain two main chemical classes of phenolics and terpenoids. Its constituents have great biological
values and spread out to drug development, including anticancer, anti-inflammatory, antimicrobacterial,
antioxidative, ani-viral, anti-insect, antidiabetic, anti-allergic, anti-obesity, hepatoprotective, neuroprotective,
rhenoprotective, gastroprotective, skin protective, vasorelaxant, and aphrodisiac activities. Various pharmacological
actions were successfully proven by the underlying mechanisms. (–)-Panduratin A seems to be the most
active compound with an oral bioavailability of 7-9%. B. rotunda plant extracts are safe in use with LD50 > 4.0
g/kg. Pharmacokinetic studies indicated that the metabolism of B. rotunda constituents may be related to the
oxidation and glucuronidation of its phenolic compounds. Further phytochemical and pharmacological studies
are expected, as well as clinical applications are urgently needed.