CARE & CRCP, Biomedical, Center, P. Universidad Católica de Chile, P.O. Box 114-D, Santiago, Chile.
Curr Med Chem. 2010;17(5):391-406. doi: 10.2174/092986710790226156.
St. John's Wort (SJW) has been used medicinally for over 5,000 years. Relatively recently, one of its phloroglucinol derivatives, hyperforin, has emerged as a compound of interest. Hyperforin first gained attention as the constituent of SJW responsible for its antidepressant effects. Since then, several of its neurobiological effects have been described, including neurotransmitter re-uptake inhibition, the ability to increase intracellular sodium and calcium levels, canonical transient receptor potential 6 (TRPC6) activation, N-methyl-D-aspartic acid (NMDA) receptor antagonism as well as antioxidant and anti-inflammatory properties. Until recently, its pharmacological actions outside of depression had not been investigated. However, hyperforin has been shown to have cognitive enhancing and memory facilitating properties. Importantly, it has been shown to have neuroprotective effects against Alzheimer's disease (AD) neuropathology, including the ability to disassemble amyloid-beta (Abeta) aggregates in vitro, decrease astrogliosis and microglia activation, as well as improve spatial memory in vivo. This review will examine some of the early studies involving hyperforin and its effects in the central nervous system (CNS), with an emphasis on its potential use in AD therapy. With further investigation, hyperforin could emerge to be a likely therapeutical candidate in the treatment of this disease.
贯叶连翘（SJW）已被用于医学治疗超过 5000 年。最近，其苯丙素葡萄糖苷衍生物之一——金丝桃素，作为一种具有研究意义的化合物开始崭露头角。金丝桃素最初作为 SJW 中负责抗抑郁作用的成分而受到关注。此后，其多种神经生物学作用已被描述，包括神经递质再摄取抑制、增加细胞内钠和钙水平的能力、经典瞬时受体电位 6（TRPC6）激活、N-甲基-D-天冬氨酸（NMDA）受体拮抗作用以及抗氧化和抗炎特性。直到最近，其在抑郁症以外的药理学作用尚未得到研究。然而，金丝桃素已被证明具有增强认知和促进记忆的特性。重要的是，它已被证明具有神经保护作用，可对抗阿尔茨海默病（AD）的神经病理学，包括在体外分解淀粉样β（Abeta）聚集体、减少星形胶质细胞和小胶质细胞激活，以及改善体内空间记忆的能力。本综述将探讨一些涉及金丝桃素及其在中枢神经系统（CNS）中的作用的早期研究，重点关注其在 AD 治疗中的潜在用途。随着进一步的研究，金丝桃素可能会成为治疗这种疾病的一种有希望的治疗候选药物。
