Albeit remarkable achievements in anti-cancer endeavors, the prevention and treatment of cancer remain unresolved challenges. Hence, there is an urgent need to explore new and efficacious natural compounds with potential anti-cancer therapeutic agents. One such group of compounds is alisols, tetracyclic triterpene alcohols extracted from alisma orientale. Alisols play a significant role in cancer therapy as they can suppress cancer cell proliferation and migration by regulating signaling pathways such as mTOR, Bax/Bcl-2, CHOP, caspase, NF-kB and IRE1. Pharmacokinetic studies showed that alisols can be absorbed entirely, rapidly, and evenly distributed in vivo. Moreover, alisols are low in toxicity and relatively safe to take. Remarkably, each alisol can be converted into many compounds with different pathways to their anti-cancer effects in the body. Thus, alisols are regarded as promising anti-cancer agents with minimal side effects and low drug resistance. This review will examine and discuss alisols' anti-cancer molecular mechanism, pharmacokinetics and metabolism. Based on a comprehensive analysis of nearly 20 years of research, we evaluate the therapeutic potential of alisols for various types of cancer and offer insights and strategies for developing new cancer treatments.