Search Results (207)

Background/Objectives: There is evidence concerning herbal medicines and plant-based compounds, including Lamiaceae species, as putative senolytic agents; however, there are only a few reports on Ocimum americanum properties using rat models. The aim of this study was to investigate the neuroprotective effects and potential modes of action of Ocimum americanum L. using ex vivo and in vivo assays to assess the effects of OAEE on hippocampal tissue from young adult and late middle-aged Wistar rats, with a focus on oxidative stress, cholinesterase activity, and neuroinflammatory markers. Methods: Ocimum americanum ethanol extract (OAEE) was incubated with hippocampal slices of young adult and late middle-aged male Wistar rats exposed to H₂O₂; an acute treatment with OAEE was evaluated in aversive memory performance and neurochemical parameters, such as hippocampal cellular oxidative state, and anticholinesterase activity, and a diet supplementation of OAEE were evaluated on several hippocampal biochemical parameters, such as oxidative state, anticholinesterase activity, and neuroinflammatory parameters in young adult and late middle-aged male rats. Results: OAEE reversed the H₂O₂-induced impaired cellular viability in hippocampal slices from young adult rats, as well as protected hippocampal slices against H₂O₂-induced damage in both young adult and late middle-aged Wistar rats, indicating its neuroprotective action. Chronic dietary OAEE supplementation reduced aging-induced increases in reactive species and lipid peroxidation levels in the hippocampus. Indeed, this supplementation reduced the TNF-α content in hippocampus from both ages, and IL-1β levels in young adult rats. Conclusions: The antioxidant actions of OAEE here observed, preventing the lipoperoxidation, as well as its anti-neuroinflammatory effect, might be related to neuroprotective effect. Our findings add evidence to support the idea of the potential use of Ocimum americanum as a nutraceutical or functional food in the aging process. Full article

Aloysia triphylla is widely used in traditional medicine from Peru for its sedative, digestive and anti-inflammatory properties. However, comprehensive studies on the biological activities of its essential oil (EO), particularly from Peruvian sources, remain limited. This study aimed to analyze the chemical composition and enantiomeric profile of A. triphylla EO and evaluate its antibacterial, antioxidant, anticholinesterase, and cytotoxic activities. The EO was obtained by steam distillation and analyzed using gas chromatography–mass spectrometry (GC-MS). A total of 62 compounds were identified, with (E)-caryophyllene (16.80%), β-pinene (9.96%), and germacrene D (10.00%) being the major components. Enantiomeric analysis revealed specific chiral signatures, including (−)-α-pinene, (+)-limonene, and (R)-(−)-linalool. The EO exhibited significant antibacterial activity, particularly against Bacillus subtilis (MIC = 5 µg/mL), and weak antioxidant activity (IC₅₀ = 7720 and 4648 µg/mL for DPPH and ABTS, respectively). Additionally, the EO demonstrated moderate acetylcholinesterase inhibition (IC₅₀ = 87.8 µg/mL) and cytotoxicity in the Artemia salina assay (LC₅₀ = 964 µg/mL). These findings suggest that A. triphylla EO possesses promising bioactivities with potential applications in pharmaceutical and cosmetic fields. Full article

An important field of research in medicinal and organic chemistry involves halogen-containing heterocyclic synthones, which form the backbone of more complex organic compounds. This study aimed to design and synthesize 28 novel derivatives of 7-aryl-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one. The derivatives were created from 7-bromoquinoline intermediates to evaluate their potential as cholinesterase inhibitors for treating neurodegenerative diseases such as Alzheimer’s disease. The conditions for the Suzuki–Miyaura cross-coupling reaction were optimized to improve yield and purity. The derivatives were evaluated for their anticholinesterase activity using Ellman’s method, revealing that it most effectively inhibited cholinesterase within the micromolar range. 7-(3-Chloro-4-fluorophenyl)-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one derivative exhibited the highest inhibitory potency, with an IC₅₀ value of 6.084 ± 0.26 μM. Additionally, molecular dynamics simulations provided insight into how this lead compound interacts with the enzyme, suggesting its potential as a drug candidate for Alzheimer’s disease. Full article

Chemical analysis of the hydroethanolic Hypericum repens L. extracts was performed using the LC/Q-TοF/HRMS technique. The majority of compounds identified belonged to phenolics, particularly flavonoids. The extract was also studied for its possible bioactivities, demonstrating high antioxidant properties compared to the control (IC₅₀ values ranging from 4.6 to 9.42 μg/mL). Significant antibacterial activity was also detected against Escherichia coli, Staphylococcus aureus, Enterococcus faecalis, and Salmonella enteritidis, with MIC values from 125 to 625 μg/mL. S. aureus presented the highest susceptibility among all bacteria tested. Additionally, the extract showed very mild anticholinesterase activity in the AChE and BChE inhibition assays. These findings provide the first insights into the phytochemical composition, as well as the antioxidant, antimicrobial, and anticholinesterase activities of H. repens extract, suggesting that the endemic Cyprus H. repens is a valuable natural rich source of bioactive compounds with a potentially broad range of bioactivities. Full article

In Argentina and globally, pistachio (Pistacia vera) production has significantly grown, driven by its high nutritional value and food industry demand. Its harvesting and processing generate about 40% of pistachio waste (PW), including leaves, twigs, seed coats, green, and empty kernels. Underutilized PW has led to environmental problems, including soil and water contamination by landfill accumulation. However, it could be a potential source of undiscovered bioactive compounds. This study aimed to characterize the chemical profile and to evaluate the bioactive properties of PW. The dried pistachio waste (dPW) was used to prepare the pistachio waste decoction (PWD) (10% w/v). The total phenolic content (TPC) and flavonoid content (FC) were quantified, and the chemical profile was analyzed using UPLC-DAD-ESI-MS/MS. Nematicidal activity against Meloidogyne incognita (J2), acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition, antioxidant capacity (ABTS, DPPH, FRAP), and phytotoxicity on Allium cepa, Lactuca sativa, and Raphanus sativus were evaluated. The UPLC-DAD-ESI-MS/MS analysis identified 26 compounds, including phenolics, flavonoids, and unsaturated fatty acids. The main compounds were gallic acid, anacardic acid, and quercetin derivatives. The TPC and FC were 212.65 mg GAE/g dPW and 0.022 mg QE/g dPW, respectively, displaying strong antioxidant activity across the assays DPPH, ABTS, and FRAP. PWD exhibited nematicidal activity against M. incognita (J2) (LC₅₀ = 0.12% at 24 h). Alterations in the cuticle were observed, including structural disorganization and detachment from internal tissues. Additionally, a remarkable cholinesterase inhibitory effect was detected at 2.0% PWD (42.65% for AChE and 58.90% for BuChE). PWD showed low phytotoxic effects across the tested species, and the germination percentage (GP) and the mean germination time (MGT) were not significantly affected (GP > 79%). These findings highlight the potential of PW as a sustainable alternative for M. incognita control, the remarkable nematicidal, anticholinesterase, and antioxidant properties, and the low phytotoxicity, supporting its use in sustainable agricultural practices. Full article

Peach, apricot, chokeberry, blueberry, cranberry, raspberry, and wild strawberry fruits were used to create a polyphenolic preparation (PP) after enzyme-assisted extraction, ultrafiltration, and concentration. The composition of PP was determined using LC-MS. Gelatin jellies produced with PP, as well as liquid PP, were “digested” in an in vitro model. The entrapment of PP in the gelatin matrix delayed the release of total polyphenolics, flavonoids, flavanols, condensed tannins, and anthocyanins (predominantly during the “small intestinal” phase). PP entrapped in the jelly more effectively (p < 0.05) decreased the activity of acetylcholinesterase, butyrylcholinesterase, cyclooxygenase-2 and catalase (during the “small intestinal” phase). However, no significant (p < 0.05) effects on superoxide dismutase, glutathione peroxidase, and glutathione reductase activities were observed. FRAP, CUPRAC, HORAC, oxidation of linoleic acid, and ABTS-reducing activities were higher during the “intestinal” phase; however, the DPPH test and β-carotene bleaching tests did not confirm these results. The presented findings may be useful for designing nutraceuticals with programmed release of bioactive compounds during digestion. Full article

Amaryllidaceae alkaloids from the Amaryllidoideae subfamily exhibit broad pharmacological activities, including neuroprotection and anticancer effects. Galanthamine is a key compound for Alzheimer’s therapy. The Hippeastrum genus, particularly in Bolivia, offers significant potential for novel drug discovery, emphasising the need for conservation and further phytochemical research. Twenty-seven samples from Bolivian Hippeastrum species were investigated in terms of their alkaloid profile and anticholinesterase activity. The phytochemical analysis of Bolivian Hippeastrum species via GC-MS identified 48 Amaryllidaceae alkaloids, displaying diverse structural groups with potential pharmacological significance. Lycorine- and Homolycorine-type alkaloids were predominant, particularly in H. chionedyanthum and H. haywardii, with high concentrations of lycorine, a promising anticancer compound. The species H. evansiarum and H. mollevillquense contained notable quantities of Galanthamine type alkaloids, relevant for Alzheimer’s treatment. This study also highlights variability in acetylcholinesterase and butyrylcholinesterase inhibitory activities, with H. lara-ricoi and H. haywardii demonstrating strong inhibition. These findings suggest that Hippeastrum species are a valuable source of bioactive compounds, warranting further research into their therapeutic applications. Full article

This study investigates the therapeutic potential of Lippia origanoides essential oil (LOEO) in neurological and pharmaceutical applications. The chemical composition of LOEO was analyzed using gas chromatography–mass spectrometry (GC-MS), revealing major constituents, such as carvacrol, thymol, and γ-gurjunene, known for their antioxidant and antimicrobial properties. LOEO demonstrated significant acetylcholinesterase (AChE)-inhibitory activity, particularly in a nanoformulation that enhances bioavailability and stability. Additionally, the major constituent carvacrol, when tested in isolation, also exhibited AChE-inhibitory activity comparable to that of the nanoformulation. Molecular docking analysis indicated strong binding affinities between LOEO compounds and AChE, supporting its therapeutic potential for neurodegenerative diseases like Alzheimer’s. Additionally, in silico pharmacokinetic predictions revealed favorable absorption and blood–brain barrier penetration profiles for key constituents. Despite promising results, this study acknowledges the need for in vivo validation and long-term stability assessments of the nanoformulation. Future research should focus on pharmacodynamic studies and evaluating the oil’s effectiveness in animal models. These findings highlight LOEO as a valuable candidate for developing natural therapies for neurodegenerative diseases. Full article

Citrus x limonia is an aromatic species, known locally in Ecuador as limón mandarina or limón chino. In the present study, the chemical composition and biological activity of the essential oil isolated from this species were determined. The essential oil was extracted through hydrodistillation. The chemical composition and enantiomeric distribution of the essential oil were determined by gas chromatography. Antimicrobial activity was determined using the broth microdilution method against tree Gram-positive cocci, a Gram-positive bacillus, four Gram-negative bacilli, a fungus, and a yeast. The antioxidant activity was determined through ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) and DPPH (2,2-diphenyl-1-picrylhydrazyl) methods. The spectrophotometric method was used to determine anticholinesterase activity. In the essential oil, thirty-nine compounds were identified, which represented 99.35% of the total composition. Monoterpene hydrocarbons were the most representative group in terms of number of compounds (thirteen) and in terms of relative abundance (91.39%). The main constituents were found to be limonene (57.38 ± 1.09%), γ-terpinene (13.01 ± 0.37%), and β-pinene (12.04 ± 0.63%). Five pairs of enantiomers were identified in the essential oil from fruits of Citrus x limonia. The essential oil presented a minimum inhibitory concentration of 4000 μg/mL against Aspergillus niger. The antioxidant activity of essential oil was weak per the ABTS method, with a SC₅₀ of 1.26 mg/mL. Additionally, the essential oil exhibited moderate anticholinesterase activity, with an IC₅₀ of 203.9 ± 1.03 µg/mL. This study provides the first comprehensive analysis of the chemical composition and biological activities of the essential oil from fruits of Citrus x limonia. Full article

Objective: In this study, the chemical composition and biological activities of the essential oils extracted from the leaves and fruits of Zanthoxylum mantaro were analyzed. Methods: The essential oils were obtained through hydrodistillation using a Clevenger-type apparatus. Chemical composition was determined by gas chromatography coupled with mass spectrometry (GC-MS) and gas chromatography with a flame ionization detector (GC-FID). The antimicrobial activity was evaluated against four Gram-positive bacteria, three Gram-negative bacteria, and two fungi using the broth microdilution method. Antioxidant activity was assessed using the ABTS (2,2′-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid) and DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging assays. Additionally, the acetylcholinesterase inhibitory effect of the essential oils was measured by a spectrophotometric method. Results and Conclusions: A total of 23 compounds were identified in the essential oil from the fruits, while 47 compounds were found in the essential oil from the leaves. The major constituents of the fruit essential oil were α-thujone (39.85%), β-thujone (25.04%), sabinene (10.71%), and terpinen-4-ol (4.38%), whereas the main compounds in the leaf essential oil were germacrene D (21.75%), nerolidol (E) (12.39%), and pentadecanal (7.14%). The essential oil from the fruits exhibited antifungal activity against Aspergillus niger (ATCC 6275), with a minimum inhibitory concentration (MIC) of 1000 μg/mL. Both the fruit and leaf essential oils showed moderate antioxidant activity in the ABTS assay, with SC₅₀ values of 274.14 ± 1.06 μg/mL and 2798.85 ± 15.69 μg/mL, respectively. Furthermore, the fruit essential oil demonstrated considerable acetylcholinesterase inhibitory activity with an IC₅₀ value of 65.46 ± 1.01 μg/mL, while the leaf essential oil exhibited an IC₅₀ value of 158.2 ± 1.02 μg/mL. Full article

Citrus x limonia is an aromatic species belonging to the Rutaceae family. In the present study, the chemical composition, enantiomeric distribution, and biological activity of the essential oil isolated from leaves of Citrus x limonia were determined. The essential oil was extracted through hydrodistillation. The chemical composition of the essential oil was determined by gas chromatography (GC) coupled to a flame ionization detector (GC-FID), and a mass spectrometer detector (GC-MS) using a nonpolar column. The enantiomeric distribution was performed using two enantioselective chromatographic columns. Antimicrobial activity was determined using the broth microdilution method. The antimicrobial activity was tested against eight bacteria and two fungi. The antioxidant activity was determined through ABTS and DPPH methods. The spectrophotometric method was used to determine anticholinesterase activity. In the essential oil, forty-three compounds were identified. These compounds represent 99.13% of the total composition. Monoterpene hydrocarbons were the most representative group in number of compounds (fourteen) and in terms of relative abundance (65.67%). The main constituent is found to be limonene (25.37 ± 0.80%), β-pinene (23.29 ± 0.15%) and sabinene (8.35 ± 0.10%). Six pairs of enantiomers were identified in the essential oil from fruits of Citrus x limonia. The essential oil showed moderate antibacterial activity against Gram-positive cocci Enterococcus faecalis, and Gram-positive bacillus Lysteria monocytogenes with a MIC of 1000 μg/mL. The oil exhibited strong antifungal activity against fungi Aspergillus niger, and yeasts Candida albicans with a MIC of 250 and 500 μg/mL, respectively. The antioxidant activity of essential oil was weak in ABTS method with a SC₅₀ of 9.12 mg/mL. Additionally, the essential oil presented moderate anticholinesterase activity with an IC₅₀ of 71.02 ± 1.02 µg/mL. Full article

Evernia prunastri (L.) Ach. (Parmeliaceae), an edible lichen commonly known as oakmoss, was traditionally used by Egyptians to make bread. In this study, the ethyl-acetate (EtOAc) extract of E. prunastri was investigated for its potential therapeutic applications in diabetes mellitus, Alzheimer’s and Parkinson’s diseases, oxidative stress, and bacterial infections. The extract exhibited significant in vitro enzyme inhibition activities, including anti-amylase and anti-glucosidase activities linked to diabetes and anti-cholinesterase and anti-tyrosinase activities associated with Alzheimer’s and Parkinson’s diseases. The antioxidant activity was evaluated through multiple assays, including free radical scavenging (DPPH and ABTS), reducing power (CUPRAC and FRAP), metal chelation, and phosphomolybdenum methods, demonstrating strong oxidative stress relief potential. The antibacterial properties were also confirmed through antibacterial testing, showing efficacy against a range of bacterial strains. Total phenolic and flavonoid contents were quantified, while the chemical profile of the EtOAc extract was determined by LC-HRMS/MS analysis. The chemical composition was predominantly characterized by depsides (evernic acid and atranorin), phenolic acids (orsellinic acid), and dibenzofurans, revealing a diverse array of bioactive secondary metabolites. The extract demonstrated a broad spectrum of biological activities, including enzyme inhibition, antioxidant effects, and antibacterial properties. This study highlights the potential of E. prunastri as a functional food, providing a rich source of bioactive compounds with numerous health-promoting effects, and it suggests its relevance in therapeutic applications for chronic diseases such as diabetes, Alzheimer’s, and bacterial infections. Full article

Background: Meroterpenoids represent a remarkably diverse class of natural secondary metabolites, some of which are synthesized via terpenoid biosynthetic pathways. Over the past ten years, these compounds have gained interest because of their wide range of biological activities, such as anti-cholinesterase, COX-2 inhibitory, antibacterial, antiviral, antidiabetic, antioxidant, anti-inflammatory, antineoplastic, and cardioprotective properties. This review aims to consolidate the recognized neuroprotective effects of meroterpenoids from marine and terrestrial fungi. Methods: Data compiled from several databases, including PubMed, Science Direct, Scopus, and Google Scholar, include articles published since 2000 using keywords such as “neuroprotective”, “fungi”, “mushroom”, “marine sponge”, “neurodegeneration”, and “dementia” in connection with “meroterpenoids”. Results: Meroterpenoids modulate different cell signaling pathways and exhibit different and often combined mechanisms of action to ameliorate neuronal damage and dysfunction. Reported activities include anti-cholinesterase, antioxidant, BACE1 inhibition, and anti-inflammatory activities, all of which have potential in the treatment of dementia associated with neurodegenerative diseases such as Alzheimer’s and Parkinson’s. Conclusions: Meroterpenoids have the potential to be developed as effective tools for neuropathological diseases. Ongoing research to elucidate the various neuroprotective pathways remains essential and requires further investigation. Full article

This study investigated, for the first time, the phenolic acid profile along with the in vitro antioxidant and acetylcholinesterase (AChE) inhibitory activities of leaves and fruits from five Romanian wild-grown Acer spp. (Sapindaceae): A. campestre L., A. monspessulanum L., A. platanoides L., A. pseudoplatanus L., and A. tataricum L. High-performance liquid chromatography coupled with ultraviolet and mass spectrometry (HPLC/UV/MS) was employed to identify and quantify key phenolic acids, including gallic, caffeic, protocatechuic, chlorogenic, and p-coumaric acids. Total phenolic content (TPC) ranged from 61.48 ± 3.76 to 512.8 ± 20.54 µg gallic acid equivalents (GAE)/mL. Antioxidant activities, assessed through 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays, demonstrated the strongest radical scavenging capacities for A. tataricum fruits, with half maximal inhibitory concentration (IC₅₀) values of 10.88 ± 3.39 µg/mL and 10.39 ± 2.86 µg/mL, respectively. The ferric-reducing antioxidant power (FRAP) assay revealed the highest reducing power for A. tataricum fruits (1158 ± 48.98 µmol Fe²⁺/L) and leaves (1119 ± 164.6 µmol Fe²⁺/L). AChE inhibition was only found in A. tataricum, with an IC₅₀ of 7.91 ± 7.50 mg/mL for leaves and 15.95 ± 8.52 mg/mL for fruits. These results highlight A. tataricum as a promising source of natural antioxidants and neuroprotective agents. Full article

Hieronymiella peruviana, a recently described endemic species from southern Peru, belongs to the Amaryllidaceae family and is known for its diversity of alkaloids. Amaryllidoideae have been studied for their diverse biological activities, particularly for their properties in treating neurodegenerative diseases. This work examines the alkaloidal profile using GC-MS and UPLC-MS/MS of alkaloid-enriched extracts obtained from the leaves and bulbs of H. peruviana and their inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. In addition, the phenolic and flavonoid content in the methanolic extract from bulbs was quantified and the antioxidant capacity was evaluated. Moreover, the seed germination was investigated under four temperature conditions (15, 20, 25, and 30 °C). Twenty-two alkaloids, most of them of the homolycorine- and galanthamine-type, including galanthamine, were identified in the alkaloid extracts by means of GC-MS and UPLC-MS/MS analysis. Lycorine and 8-O-Demethylhomolycorine were the most abundant alkaloids in the bulbs and leaves, respectively. The leaves and bulbs alkaloid extracts demonstrated strong AChE inhibition (IC₅₀ = 5.20–8.60 µg/mL) and moderate BuChE inhibition (IC₅₀ = 90.20–122.76 µg/mL). The bulbs’ methanolic extract exhibited mild antioxidant activity, showing 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) values of 16.36% at 500 μg/mL and 58.31 mg Trolox equivalents (TE)/g, respectively. Seed germination was most effective at 20 °C and 25 °C. Finally, 60 days after germination, the survival rate of H. peruviana seedlings was 48.33%. These findings establish H. peruviana as a promising source of bioactive alkaloids with potential pharmacological and therapeutic applications, as well as providing critical insights for its propagation and conservation. Full article