Escin, a natural mixture of triterpenoid saponins isolated from horse chestnut (Aesculus hippocastanum) seeds, is used and studied as a vasoprotective anti-inflammatory, anti-edematous and anti-nociceptive agent. In traditional Chinese medicine, Escin is widely used for the treatment of cerebral edema, and chronic venous insufficiency, among other conditions while recent studies showed Escin might have antitumor effects as well. Escin reduced cell proliferation and induces apoptosis on glioma and lung adenocarcinoma cell lines. Escin suppressed the metastasis of triple‐negative breast cancer cells through inhibiting epithelial–mesenchymal transition. Furthermore, the study also showed Escin can reverse multidrug resistance through inhibition of the GSK3β/β–catenin pathway in cholangiocarcinoma cells. Escin has been proved to be well tolerated and efficiency on improving the gastrointestinal motility in patients with colorectal cancer.