Tricosanthin (TCS), a type Ⅰ ribosome-inactivating protein that has been used for midterm abortion in traditional Chinese medicine, can depurinate rRNA and inhibit protein synthesis, thus efficiently arresting tumor growth.However, it has poor targeting and stability, low cellular uptake and strong immunogenicity in vivo, which constrain its clinical applications.Chemical modification of TCS is an effective method to improve its drugability.