Department of Medicinal Chemistry, Virginia Commonwealth University, Richmond, Virginia, USA.
The Institute for Structural Biology, Drug Discovery and Development, School of Pharmacy, Virginia Commonwealth University, Richmond, Virginia, USA.
Med Res Rev. 2024 Nov;44(6):2707-2729. doi: 10.1002/med.22062. Epub 2024 Jun 6.
For the last two decades, the aromatic aldehyde 5-hydroxymethyl-furfural (5-HMF) has been the subject of several investigations for its pharmacologic potential. In 2004, the Safo group reported that 5-HMF has potent antisickling activity by targeting and ameliorating the primary pathophysiology of hypoxia-induced sickling of erythrocytes (red blood cells [RBC]). Following the encouraging outcome of the preclinical and phase I/II clinical studies of 5-HMF for the treatment of sickle cell disease (SCD), there have been multiple studies suggesting 5-HMF has several other biological or pharmacologic activities, including anti-allergic, antioxidant, anti-hypoxic, anti-ischemic, cognitive improvement, anti-tyrosinase, anti-proliferation, cytoprotective, and anti-inflammatory activities. The wide range of its effects makes 5-HMF a potential candidate for treating a variety of diseases including cognitive disorders, gout, allergic disorders, anemia, hypoxia, cancers, ischemia, hemorrhagic shock, liver fibrosis, and oxidative injury. Several of these therapeutic claims are currently under investigation and, while promising, vary in terms of the strength of their evidence. This review presents the research regarding the therapeutic potential of 5-HMF in addition to its sources, physicochemical properties, safety, absorption, distribution, metabolism, and excretion (ADME) profiles.
在过去的二十年中，芳香醛 5-羟甲基糠醛（5-HMF）因其潜在的药理学特性而受到了多项研究的关注。2004 年，Safo 小组报道称，5-HMF 通过靶向和改善缺氧诱导的红细胞（红细胞[RBC]镰状化的主要病理生理学，具有很强的抗镰状化活性。在 5-HMF 治疗镰状细胞病（SCD）的临床前和 I/II 期临床试验取得令人鼓舞的结果后，多项研究表明 5-HMF 具有其他几种生物学或药理学活性，包括抗过敏、抗氧化、抗缺氧、抗缺血、认知改善、抗酪氨酸酶、抗增殖、细胞保护和抗炎活性。其广泛的作用使其成为治疗多种疾病的潜在候选药物，包括认知障碍、痛风、过敏疾病、贫血、缺氧、癌症、缺血、出血性休克、肝纤维化和氧化损伤。其中一些治疗主张目前正在研究中，虽然有希望，但它们的证据强度不同。除了其来源、物理化学性质、安全性、吸收、分布、代谢和排泄（ADME）特征外，本综述还介绍了 5-HMF 在治疗中的潜在作用。
