Display omitted •The pharmacological effects of isorhamnetin are reviewed comprehensively.•Isorhamnetin is mainly contained in Hippophae rhamnoides and Ginkgo biloba.•Isorhamnetin protects cardio-cerebral vessels and nerves.•Investigations on the mechanism of action of isorhamnetin are limited.•The research on the target of isorhamnetin is missing. Isorhamnetin is one of the most important active ingredients in the fruits of Hippophae rhamnoides L. and the leaves of Ginkgo biloba L., which possesses extensive pharmacological activities. At present, there have been numerous investigations on isorhamnetin, which has the effects of cardiovascular and cerebrovascular protection, anti-tumor, anti-inflammatory, anti-oxidation, organ protection, prevention of obesity, etc. The related mechanisms involve the regulation of PI3K/AKT/PKB, NF-κB, MAPK and other signaling pathways as well as the expression of related cytokines and kinases. Isorhamnetin has a high value of development and application. However, the investigations on its mechanism of action are limited and lack of detailed scientific validation. The manuscript reviewed the pharmacological effects of isorhamnetin and related mechanisms of action for the development of its medicinal properties further.