Shi Mengting, Ma Guanhua, Yang Xiulan
Department of Pharmacology, The School of Basic Medicine, Health Science Center, Yangtze University, Jingzhou 434023, China.
Pharmaceutics. 2025 Feb 25;17(3):299. doi: 10.3390/pharmaceutics17030299.
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.
青蒿琥酯(ART)是一种从青蒿素衍生而来的半合成倍半萜内酯,以其独特的内过氧化物基团为特征,已成为临床抗疟治疗的基石。最近的研究表明它具有广泛的药理学特性,包括强大的抗疟、抗炎、抗肿瘤、抗糖尿病、免疫调节和抗纤维化特性。这些发现显著拓宽了青蒿琥酯的治疗范围,并为其在治疗胃肠道疾病中的潜在应用提供了新的视角。从机制上讲,青蒿琥酯通过多模式机制对多种胃肠道疾病,如胃溃疡、溃疡性结肠炎(UC)、肝纤维化(HF)、胃癌、肝细胞癌和结直肠癌,发挥显著的治疗作用,这些机制包括细胞周期调节、诱导凋亡、抑制肿瘤细胞侵袭和迁移、抑制增殖、激活铁死亡和免疫调节。本综述评估了关于青蒿琥酯在消化系统疾病中的治疗应用和分子机制的现有证据,旨在阐明其临床转化潜力。青蒿琥酯作为一种有前景的多靶点药物,在改善胃肠道疾病管理方面具有重要前景。