Neurobiological effects of hyperforin and its potential in Alzheimer's disease therapy

T. N. Griffith, L. Varela-Nallar, M. C. Dinamarca, N. C. Inestrosa

Research output: Contribution to journalReview articlepeer-review

68 Citations (Scopus)

Abstract

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-β (Aβ) 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.

Original languageEnglish
Pages (from-to)391-406
Number of pages16
JournalCurrent Medicinal Chemistry
Volume17
Issue number5
DOIs
Publication statusPublished - Feb 2010

Keywords

  • Alzheimer's transgenic mice
  • Amyloid aggregates
  • NMDA receptors
  • St. John's Wort
  • TRPC6 channels

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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