Neuroprotective activity of Hypericum perforatum and its major components

Hypericum perforatum is a perennial plant, with worldwide distribution, commonly known as St. Johns wort. It has been used for centuries in traditional medicine for the treatment of several disorders, such as minor burns, anxiety, and mild to moderate depression. In the past years, its antidepressant properties have been extensively studied. Despite that, other H. perforatum biological activities, as its neuroprotective properties have also been evaluated. The present review aims to provide a comprehensive summary of the main biologically active compounds of H. perforatum, as for its chemistry, pharmacological activities, drug interactions and adverse reactions and gather scattered information about its neuroprotective abilities. As for this, it has been demonstrated that H. perforatum extracts and several of its major molecular components have the ability to protect against toxic insults, either directly, through neuroprotective mechanisms, or indirectly, through is antioxidant properties. H. perforatum has therefore the potential to become an effective neuroprotective therapeutic agent, despite further studies that need to be carried out.This work was supported by Fundacao para a Ciencia e Tecnologia (FCT), projects PTDC/AGR-ALI/105169/2008, PEst-OE/AGR/UI4033/2014. AO was supported by Escola Superior de Tecnologia da Saude do Porto and Instituto Politecnico do Porto (Programa de Formacao Avancada de Docentes).info:eu-repo/semantics/publishedVersio

3-Hydroxytyrosol as a phenolic cholinesterase inhibitor with antiamnesic activity: a multimethodological study of selected plant phenolics

BackgroundPlant phenolics are increasingly being investigated for their diverse biological activities, including neuroprotective effects relevant to conditions like Alzheimer’s disease.ObjectiveThe neurobiological potential of 37 plant phenolics was screened through a multifaceted approach encompassing in vitro enzyme inhibition and antioxidant assays, in vivo antiamnesic evaluation, and in silico molecular docking and toxicity predictions.MethodsThe compounds were tested for their cholinesterase (ChE) inhibition potentials, metal-chelation activities, and copper-reducing antioxidant capacities (CUPRACs) using a microtiter assay as well as ferric-reducing antioxidant power assays. Additionally, the in silico ADME, pharmacokinetic, and toxicokinetic profiles of the compounds were predicted using computational platforms.ResultsSeveral compounds exhibited significant inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities. Of these, quercetin was found to be the most active inhibitor, with IC50 values of 1.22 ± 0.79 mM against AChE and 2.51 ± 0.04 mM against BChE. Some of the other compounds, including caffeic acid (IC50: 3.51 ± 0.62 mM), apigenin (IC50: 3.52 ± 0.08 mM), and taxifolin (IC50: 7.18 ± 2.05 mM), also showed AChE inhibition. Then, oleuropein, rosmarinic acid, gallic acid, epigallocatechin gallate, and 3-hydroxytyrosol were further investigated for their antiamnesic activities using a passive avoidance test in scopolamine-induced mice; our data showed that these compounds were effective considering the latency time of the mice and that 3-hydroxytyrosol showed the highest antiamnesic effect. The dual inhibitory compounds were subjected to molecular docking experiments with ChEs, and the in silico toxicities of three compounds were assessed using the PASS and SwissADME prediction programs.ConclusionOur data provide compelling evidence for the neuroprotective potentials of several plant phenolics. Notably, 3-hydroxytyrosol was identified for the first time as a ChE inhibitor with significant in vivo antiamnesic activity and warrants further investigation

Polygala anatolica Boiss. et Heldr.: Is A Potential Remedy for Inflammation and Pain?

Species of Polygala genus have been used for the treatment of inflamation and pain in Turkish traditional medicine. The aim of the present study is to assess the anti-inflammatory and analgesic activities of P. anatolica. n-Hexane, ethyl acetate and methanol extracts of the aerial parts and roots of P. anatolica were investigated for their anti-inflammatory and analgesic effects. The methanol extracts prepared from the aerial parts and roots of P. anatolica were found to be active in carrageenan- and PGE(2)-induced paw edema models and in Whittle method. Methanolic extract of the aerial part inhibited serotonin-induced hind paw edema, while the root extract did not exert inhibitory effect in the same model. In addition, Fr. B and C obtained from the methanol extract of P. anatolica aerial parts showed significant anti-inflammatory activity. Morover, the analgesic effect of the methanol extracts prepared from the roots and aerial parts and Fr.B and Fr.C were found to be statistically significant without inducing ulceration. The methanol extract obtained from the aerial parts of the plant and its saponoside and flavonoid fractions showed anti-inflammatory and analgesic activities in the trials