Shionone is a triterpenoid that is the primary constituent of an important ancient Chinese medicine named Radix Asteris. It has emerged as an attractive candidate against different important diseases, including interstitial cystitis, colitis, cancer, Parkinson’s disease, and urinary tract infections, and was found to have a protective effect on multiple organs, including the colon, kidneys, lungs, brain, and bladder. The anti-inflammation activity of shionone may be considered an important property that imparts the positive health outcomes of shionone. Important molecular targets and markers such as TNF-α, STAT3, NLRP3, and NF-κB were also found to be targeted by shionone and were verified in different diseases. This suggests the possible potential of shionone against other diseases associated with these targets. Pharmacokinetic studies also support the therapeutic potential of shionone and provide the initial track that may be pursued for its development. Yet, the compilation of the pharmacological activities of shionone and its important genes and pathway targets are absent in the existing literature, which would direct its development as a therapeutic and/or supplement. Hence, the present review provides a compilation of information concerning pharmacological activities, highlights the existing holes, and proposes a specific direction for the expansion of shionone as a therapeutic against different diseases and conditions.