Abstract
Artesunate (ART), an artemisinin-derived semi-synthetic sesquiterpene lactone distinguished by its unique endoperoxide group, has become a cornerstone of clinical antimalarial therapy. Recent research has demonstrated its broad pharmacological profile, including its potent antimalarial, anti-inflammatory, anti-tumor, antidiabetic, immunomodulatory, and anti-fibrotic properties. These discoveries have significantly broadened the therapeutic scope of ART and offer new perspectives for its potential use in treating gastrointestinal disorders. Mechanistically, ART exerts significant therapeutic effects against diverse gastrointestinal pathologies-such as gastric ulcers, ulcerative colitis (UC), hepatic fibrosis (HF), gastric cancer, hepatocellular carcinoma, and colorectal cancer-via multimodal mechanisms, including cell cycle modulation, apoptosis induction, the suppression of tumor cell invasion and migration, proliferation inhibition, ferroptosis activation, and immune regulation. This review evaluates existing evidence on ART's therapeutic applications and molecular mechanisms in digestive diseases, intending to elucidate its clinical translation potential. ART emerges as a promising multi-target agent with significant prospects for improving the management of gastrointestinal disorders.