Department of Biochemistry, Center for Biological Sciences, Universidade Federal de Santa Catarina, Florianópolis, SC, 88040-900, Brazil.
CNS Drugs. 2017 Dec;31(12):1029-1041. doi: 10.1007/s40263-017-0474-4.
Ursolic acid is a pentacyclic triterpenoid found in several plants. Despite its initial use as a pharmacologically inactive emulsifier in pharmaceutical, cosmetic and food industries, several biological activities have been reported for this compound so far, including anti-tumoural, anti-diabetic, cardioprotective and hepatoprotective properties. The biological effects of ursolic acid have been evaluated in vitro, in different cell types and against several toxic insults (i.e. 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, amyloid-β peptides, kainic acid and others); in animal models of brain-related disorders (Alzheimer disease, Parkinson disease, depression, traumatic brain injury) and ageing; and in clinical studies with cancer patients and for muscle atrophy. Most of the protective effects of ursolic acid are related to its ability to prevent oxidative damage and excessive inflammation, common mechanisms associated with multiple brain disorders. Additionally, ursolic acid is capable of modulating the monoaminergic system, an effect that might be involved in its ability to prevent mood and cognitive dysfunctions associated with neurodegenerative and psychiatric conditions. This review presents and discusses the available evidence of the possible beneficial effects of ursolic acid for the management of neurodegenerative and psychiatric disorders. We also discuss the chemical features, major sources and potential limitations of the use of ursolic acid as a pharmacological treatment for brain-related diseases.
熊果酸是一种五环三萜,存在于多种植物中。尽管最初作为一种在制药、化妆品和食品工业中无药理活性的乳化剂使用,但迄今为止,已有多种生物活性被报道,包括抗肿瘤、抗糖尿病、心脏保护和肝脏保护作用。熊果酸的生物学效应已在体外、不同细胞类型和针对多种毒性损伤(如 1-甲基-4-苯基-1,2,3,6-四氢吡啶、淀粉样β肽、海人酸等)、与脑相关的疾病(阿尔茨海默病、帕金森病、抑郁症、创伤性脑损伤)和衰老的动物模型中,以及癌症患者和肌肉萎缩的临床研究中进行了评估。熊果酸的大多数保护作用与其预防氧化损伤和过度炎症的能力有关,这是与多种脑部疾病相关的常见机制。此外,熊果酸能够调节单胺能系统,这种作用可能与其预防与神经退行性和精神疾病相关的情绪和认知功能障碍的能力有关。本文综述了熊果酸在管理神经退行性和精神疾病方面可能具有的有益作用的现有证据。我们还讨论了熊果酸作为治疗脑部相关疾病的药理学治疗的化学特征、主要来源和潜在局限性。