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Many studies have demonstrated the herbicidal effects of several essential oils and their possible use as substitutes for chemical herbicides. Several enzymes play a very significant role in seed germination: among these, α-amylase could be involved in essential oil phytotoxic processes. The aims of this study were to compare the chemical composition of the essential oils of two ecotypes of O. heracleoticum growing in Cilento (Southern Italy) and to study their possible use as natural herbicide using Raphanus sativus , Sinapis arvensis and Lolium multiflorum seeds. Moreover, a possible inhibitory activity on the α-amylase enzyme extracted from germinating seeds was evaluated as a possible mechanism of action. Both oils, characterized by GC-MS, belonged to a carvacrol chemotype. The alpha-amylase activity was determined using DNSA (dinitrosalicylic acid) assay quantifying the reducing sugar produced. Furthermore, the essential oils demonstrated phytotoxicity at the highest dose tested, and an inhibitory effect on α-amylase, probably correlated with the phytotoxic effects, was registered. The oils showed interesting phytotoxic and alpha-amylase inhibitory activities, which deserve to be further investigated.

We studied the total polyphenols, flavonoids, vitamin C, the antioxidant and anti-inflammatory activity of six Citrus monofloral honey, and the in vitro inhibitory effect against cholinesterases and tyrosinase. Finally, we assessed their effect against the biofilm of some pathogenic bacteria. Lime honey showed the best antioxidant activity and the highest content of polyphenols and vitamin C. Lemon and tangerine honey contained almost exclusively flavonoids. Lemon honey better preserved the bovine serum albumin against denaturation (IC 50  = 48.47 mg). Honeys inhibited acetylcholinesterase, butyrylcholinesterase, and tyrosinase up to 12.04% (tangerine), 19.11% (bergamot), and 94.1% (lemon), respectively. Lime and clementine honey better inhibited the Listeria monocytogenes biofilm. Bergamot honey acted mainly against the Staphylococcus aureus and Acinetobacter baumannii biofilm; bergamot and tangerine honey inhibited the Pseudomonas aeruginosa biofilm particularly. Bergamot, clementine, and tangerine honey acted against Escherichia coli sessile cell metabolism. This Citrus honey exhibited in vitro prospective health benefits and is applicable for future in vivo studies., (© 2023. The Author(s).)

In the present study, the chemical composition of the volatile oil and methanolic extract from Ducrosia flabellifolia Boiss. was investigated. The antimicrobial, antioxidant, and anticancer activities of the methanolic extract from D. flabellifolia aerial parts were screened using experimental and computational approaches. Results have reported the identification of decanal (28.31%) and dodecanal (16.93%) as major compounds in the essential oil obtained through hydrodistillation. Farnesyl pyrophosphate, Methyl 7-desoxypurpurogallin-7-carboxylate trimethyl ether, Dihydro-Obliquin, Gummiferol, 2-Phenylaminoadenosine, and 2,4,6,8,10-dodecapentaenal, on the other hand, were the dominant compounds in the methanolic extract. Moreover, the tested extract was active against a large collection of bacteria and yeast strains with diameter of growth inhibition ranging from 6.67 ± 0.57 mm to 17.00 ± 1.73 mm, with bacteriostatic and fungicidal activities against almost all tested microorganisms. In addition, D. flabellifolia methanolic extract was dominated by phenolic compounds (33.85 ± 1.63 mg of gallic acid equivalent per gram of extract) and was able to trap DPPH• and ABTS•+ radicals with IC 50 about 0.05 ± 0 mg/mL and 0.105 ± 0 mg/mL, respectively. The highest percentages of anticancer activity were recorded at 500 µg/mL for all cancer cell lines with IC 50 about 240. 56 µg/mL (A-549), 202.94 µg/mL (HCT-116), and 154.44 µg/mL (MCF-7). The in-silico approach showed that D. flabellifolia identified compounds bound 1HD2, 2XCT, 2QZW, and 3LN1 with high affinities, which together with molecular interactions and the bond network satisfactorily explain the experimental results using antimicrobial, antioxidant, and anticancer assays. The obtained results highlighted the ethnopharmacological properties of the rare desertic D. flabellifolia plant species growing wild in Hail region (Saudi Arabia).

The composition, herbicidal, larvicidal, and toxic activities of Juniperus horizontalis Moench essential oil and sabinene, its main component, were evaluated. The seed germination percentage and root length of eight different plant species (crops and weeds) were measured for in vitro herbicidal activity tests. Different doses (100, 50, 10, 5, 1, 0.5 µg/mL) of the samples were applied to seeds for 120 h. The same doses were applied to test the toxicity of the samples on Tubifex tubifex (sludge worm) and Chironomus aprilinus (blood worm). Four doses (435, 652.5, 870, and 1740) of samples were in a larvicidal test on Tenebrio molitor L. (mealworm), and bioassays were checked after 24 and 48 h. The analysis of the oil allowed for the identification of dominant components as sabinene (38.7%), α-pinene (10.0%), elemol (8.6%), γ-terpinene (8.3%), limonene (7.8%) and α-thujene (5.3%). The results showed that the effect of oil on root length inhibition was significant in all crop species. The doses which affected root growth were not toxic to Tubifex tubifex and Chironomus aprilinus . Finally, the obtained results in the larvicidal bioassay indicate that the potential of J. horizontalis in yellow mealworm survivorship limitation can be a starting point for future research.

This study was carried out to characterize the chemical composition of the essential oils from seven Eucalyptus species (E. griffithsii, E. hemiphloia, E. lesouefii, E. longicornis, E. pyriformis, E. viminalis, and E. wandoo), as well as their phytotoxic and antibacterial activities. The essential oils were analyzed by GC/MS and the potential in vitro phytotoxicity was evaluated against germination and radical elongation of Raphanus sativus, Lolium multiflorum, and Sinapis arvensis seeds. The antibiofilm activity was studied against both Gram-negative (Pseudomonas aeruginosa, Escherichia coli and Acinetobacter baumannii) and Gram-positive (Staphylococcus aureus and Listeria monocytogenes) bacteria. The inhibition of biofilm formation and its metabolism was determined at different times. Eucalyptol was the most abundant component in all essential oils studied (ranging from 40.8% for E. lesouefii EO to 73.6% for E. wandoo) except for that of E. pyriformis where it was present but at 15.1%. E. pyriformis was the most active against both germination and radical elongation of S. arvensis. The action of all essential oils proved to be highly effective in inhibiting the bacterial adhesion process of the five strains considered. In light of these results, these essential oils could have potential applications both in the agricultural and health fields.

Eucalyptus species are characterized by their richness in essential oils (EOs) with a great diversity of biological activities. This study reports the chemical composition and the phytotoxic and antibiofilm activities of the EOs of six Eucalyptus species growing in Tunisia: E. bicostata, E. gigantea, E. intertexta, E. obliqua, E. pauciflora and E. tereticornis . Four EOs were rich above all in oxygenated monoterpenes (25.3-91.4%), with eucalyptol as the main constituent. However, in the EOs of E. pauciflora and E. tereticornis, sesquiterpene hydrocarbons (28.8-54.0%) were the main class of constituents; piperitone was the main constituent of both EOs. The phytotoxicity of the EOs was tested against germination and radicle elongation of the weeds Sinapis arvensis and Lolium multiflorum and the crop Raphanus sativus , resulting in the different inhibition of seed germination and radicle elongation depending on both chemical composition and the seed tested, with remarkable phytotoxicity towards S. arvensis and R. sativus . Furthermore, almost all EOs showed antibacterial potential, resulting in significant inhibition of bacterial biofilm formation and the metabolism of Gram-positive ( Staphylococcus aureus subsp. aureus and Listeria monocytogenes ) and Gram-negative ( Acinetobacter baumannii , Pseudomonas aeruginosa and Escherichia coli ) bacterial strains, in addition to acting on mature biofilms. The EOs were inhibitory against all bacterial strains tested and usually reluctant to undergo the action of conventional antibiotics. Therefore, these EOs may be considered for applications both as herbicides and in food and health fields.

The cultivation of different species of Eucalyptus has recently expanded in Liguria (Italy) due to the growing demand of the North European floricultural market. Eucalyptus tree branches are cut and selected for their quality, resulting in large amounts of waste biomass to be disposed of. The aim of our study was to evaluate the phytotoxic and antimicrobial activities of essential oils (EOs) from pruning wastes of E. cinerea (EC) and E. nicholii (EN), for potential applications in agriculture. Phytochemical analyses showed eucalyptol (1,8-cineole) as the major component in both EOs, but the EO yield of EN was higher than that of EC, in agreement with a significantly higher oil gland density on EN leaves. EOs from both species showed phytotoxicity on both weeds tested, but no significant inhibition on horticultural crop seed germination, except for Raphanus sativus . The EO from EC showed the strongest antibacterial activity, while the EO from EN showed the strongest antifungal activity. Concluding, EOs from Eucalyptus pruning may be used as possible alternatives to synthetic herbicides and pesticides, acting as antimicrobial and antifungal agents, thus representing a safe strategy for crop management programs.

The complex taxonomy of Eucalyptus genus, the renewed interest in natural compounds able to combat microbial strains, the overuse of synthetic pesticides, the consequent request for alternative control methods were the reasons for this research. The essential oils (Eos) of Eucalyptus bosistoana , Eucalyptus melliodora , Eucalyptus odorata , Eucalyptus paniculata , Eucalyptus salmonopholia, and Eucalyptus transcontinentalis were analyzed by GC/MS and their potential phytotoxic activity was evaluated against the germination and radicle elongation of Sinapis arvensis , Raphanus sativus and Lolium multiflorum . The antibiofilm activity was assayed against both Gram-positive ( Staphylococcus aureus and Listeria monocytogenes ) and Gram-negative ( Pseudomonas aeruginosa, Escherichia coli, and Acinetobacter baumannii) bacteria. Monoterpenoids were the most representative constituents in all EOs and eucalyptol was the dominant component except in E. melliodora EO, in which p -cymene was the most abundant. In phytotoxic assays, the EOs from E. odorata and E. paniculata were the most active against germination and radical elongation of the tested seeds. Finally, the Eucalyptus EOs proved their capacity to effectively inhibit the adhesion process of all five pathogen strains, with percentages often reaching and exceeding 90%. These Eucalytpus EOs could have possible employments in the food, health and agricultural fields.

The Eucalyptus genus (Myrtaceae) is characterized by a richness in essential oils (EO) with multiple biological activities. This study reports the chemical composition and the phytotoxic and antimicrobial activities of the EOs from Tunisian E. occidentalis , E. striaticalyx and E. stricklandii . The EOs were analyzed using GC/MS and their phytotoxicities were assessed against the germination and seedling growth of Sinapis arvensis , Trifolium campestre and Lolium rigidum . Antimicrobial activity was investigated against both Gram-negative ( Pseudomonas aeruginosa, Escherichia coli and Acinetobacter baumannii) and Gram-positive ( Staphylococcus aureus and Listeria monocytogenes ) bacteria. The inhibition of biofilm formation and its metabolism was determined at different times. All EOs were rich in oxygenated monoterpenes (36.3-84.8%); the EO of E. occidentalis was rich in sesquiterpenes, both oxygenated and hydrocarbon (40.0% and 15.0%, respectively). Eucalyptol was the main constituent in all samples. The EOs showed phytotoxic activity on seed germination and seedling growth, depending both on chemical composition and weed. The EOs show a remarkable antibacterial potential resulting in a significant inhibition of the formation of bacterial biofilm and its metabolism, depending on the EO and the strain, with activity on the mature biofilm as well. Therefore, these Eucalyptus EOs could have potential applications both in the food and health fields.

Acetaminophen (APAP) is the most common prescription medicine around the world for the treatment of pain and fever and is considered to be a safe drug at its therapeutic dose. However, a single overdose or frequent use of APAP can cause severe acute liver injury. APAP hepatotoxicity is a prevalent cause of acute liver disease around the world and the lack of suitable treatment makes it a serious problem. In recent years, there has been a surge in interest in using probiotics and probiotic-derived products, known as postbiotics, as health and disease negotiators. A growing body of evidence revealed that they can be equally effective against APAP hepatotoxicity. Different probiotic bacteria were found to be pre-clinically effective against APAP hepatotoxicity. Different postbiotics have also shown exciting results in preclinical models of APAP hepatotoxicity. This review summarized the protective roles and mechanisms of the different probiotic bacteria and postbiotics against APAP hepatotoxicity, with critical discussion. A brief discussion on potential novel probiotics and postbiotics for oxidative liver injury was also included. This review was written in an attempt to pique the interest of researchers in developing a safe therapeutic option against oxidative liver damage using probiotics and/or postbiotics as dietary supplements.

This work aimed to evaluate the chemical composition of the essential oils (EOs) of two cultivars of Allium sativum and their antibiofilm activity against the food pathogens Acinetobacter baumannii , Escherichia coli , Listeria monocytogenes , and Staphylococcus aureus . The crystal violet assay ascertained the susceptibility of the bacterial biofilms, while the MTT assay let to evaluations of the metabolic changes occurring in the bacterial cells within biofilms. Their chemical composition indicated some sulfuric compounds (i.e., allicin, diallyl disulfide, and allyl propyl disulfide), and decene as some of the main components of the EOs. The aerial parts and bulbs' EOs from the two cultivars showed chemical differences, which seemed to affect the antibiofilm activity. The EOs from aerial parts of 'Bianco del Veneto' inhibited the biofilm formation of L. monocytogenes and E. coli (60.55% and 40.33%, respectively). In comparison, the 'Staravec' EO inhibited the cellular metabolism of E. coli (62.44%) and S. aureus (51.52%) sessile cells. These results indicate their possible use as preserving agents in the food industry and suggest their potential exploitation in the development of new formulations to avoid or limit nosocomial infections.

Background: The potential of essential oils (EOs) and of their principal constituents for eradication of biofilm and at the same time the research of new potential acetylcholinesterase inhibitors is gaining increasing interest in last years. The aims of this study were to determine the chemical composition and to evaluate the antibacterial, cytotoxic, and anti-acetylcholinesterase properties of Myrtus communis leaves essential oil and its main constituents., Methods: Essential oil was obtained by hydrodistillation of M. communis L. leaves and was analyzed by GC and GC-MS. The antimicrobial activity was carried out against both gram-negative and gram-positive bacteria. The microdilution method was used to estimate the minimum inhibitory concentrations (MICs). Then, the capacity of essential oil and its main constituent to inhibit biofilm growth, with the method of O'Toole and Kolterand, and the metabolic activity of biofilm cells through the MTT colorimetric method were evaluated at different times. Moreover, was studied the potential cytotoxic activity against SH-SY5Y cell line with MTT assay and the anti-acetylcholinesterase activity using Ellman's assay., Results: Myrtenyl-acetate, 1,8 cineole, α-pinene, and linalool were the main components in the EO. The myrtle EO, at the minimum tested dose (0.4 mg/ml), inhibited S. aureus biofilm by 42.1% and was capable of inhibiting the biofilm cell metabolism in all tested strains, except Staphylococcus aureus. Moreover, the EO showed good cytotoxic and anti-acetylcholinesterase activities IC 50 of 209.1 and 32.8 μg/ml, respectively., Conclusions: The results suggest that myrtle EO and its main constituents could be used as possible products that could act against the resistant pathogenic species E. coli, P. aeruginosa, L. monocytogenes and S. aureus, on the other hand, as possible coadjutants in the treatment of neurological diseases., (© 2022. The Author(s).)

Alzheimer's disease (AD) is a chronic, complex neurodegenerative disorder mainly characterized by the irreversible loss of memory and cognitive functions. Different hypotheses have been proposed thus far to explain the etiology of this devastating disorder, including those centered on the Amyloid-β (Aβ) peptide aggregation, Tau hyperphosphorylation, neuroinflammation and oxidative stress. Nonetheless, the therapeutic strategies conceived thus far to treat AD neurodegeneration have proven unsuccessful, probably due to the use of single-target drugs unable to arrest the progressive deterioration of brain functions. For this reason, the theoretical description of the AD etiology has recently switched from over-emphasizing a single deleterious process to considering AD neurodegeneration as the result of different pathogenic mechanisms and their interplay. Moreover, much relevance has recently been conferred to several comorbidities inducing insulin resistance and brain energy hypometabolism, including diabetes and obesity. As consequence, much interest is currently accorded in AD treatment to a multi-target approach interfering with different pathways at the same time, and to life-style interventions aimed at preventing the modifiable risk-factors strictly associated with aging. In this context, phytochemical compounds are emerging as an enormous source to draw on in the search for multi-target agents completing or assisting the traditional pharmacological medicine. Intriguingly, many plant-derived compounds have proven their efficacy in counteracting several pathogenic processes such as the Aβ aggregation, neuroinflammation, oxidative stress and insulin resistance. Many strategies have also been conceived to overcome the limitations of some promising phytochemicals related to their poor pharmacokinetic profiles, including nanotechnology and synthetic routes. Considering the emerging therapeutic potential of natural medicine, the aim of the present review is therefore to highlight the most promising phytochemical compounds belonging to two major classes, polyphenols and monoterpenes, and to report the main findings about their mechanisms of action relating to the AD pathogenesis., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2022 Piccialli, Tedeschi, Caputo, D’Errico, Ciccone, De Feo, Secondo and Pannaccione.)

Edible herbs are widely used in the human diet due to their pleasant flavors and countless health benefits associated with their components having, mainly, antioxidant and anti-inflammatory therapeutic functions. Since herbs are highly perishable materials because of their high water content, to guarantee products are safe and stable over time, it is necessary that they undergo stabilization operations. The application of microwave-assisted drying, a promising technique in terms of process sustainability, for the stabilization of the aromatic herb, Ocimum basilicum L., was investigated. The activities were carried out by applying different operating conditions in order to evaluate the impact of the time/temperature combination on the final quality of dried basil. The latter was investigated via the chemical characterization of extracted essential oils and tissue damages. Conventional convective processes were also applied to perform comparisons between dried basil products both under production and the quality preservation points of view. Results showed that microwave heating is suitable as a drying method, as expected, due to the well-known interaction between vegetable tissue (rich in water) and the electromagnetic field; and that drying methods have a different influence on the chemical composition of the essential oils extracted from dried products, in terms of the number (ranging from 41 to 18 components in different dried samples) and percentage (until 67% in linalool and 21% in α- trans -bergamotene in different dried samples) of its' constituents.

In this work, we aimed to study the chemical composition of the essential oils from bulbs and leaves of two cultivars of Allium sativum L. and two of A. ampeloprasum L. var. holmense. Moreover, we investigated their activity against four common bacterial strains responsible for food contamination (Listeria monocytogenes, Escherichia coli, Acinetobacter baumannii, and Staphylococcus aureus) by formation of biofilms. The susceptibility of bacterial biofilms was evaluated by crystal violet assay, whereas the metabolic changes occurring in the bacterial cells were ascertained through the MTT test. The essential oils were characterized by the presence of most characteristic components, although with different composition between the species and the cultivars. The essential oils inhibited the capacity of the pathogenic bacteria to form biofilms (up to 79.85 against L. monocytogenes) and/or acted on their cell metabolism (with inhibition of 68.57% and 68.89% against L. monocytogenes and S. aureus, respectively). The capacity of the essential oils to act against these foodborne bacteria could suggests further ideas for industrial applications and confirms the versatility of these essential oils as food preservatives.

Oregano (Origanum vulgare L.) is mainly cultivated, both as fresh and dried herb, for several purposes, such as ailments, drugs, and spices. To evaluate the influence of some drying methods on the chemical composition of the essential oil of oregano, its aerial parts were dehydrated by convective drying techniques (shade, static oven), microwave-assisted heating (three different treatments) and osmotic treatment. The oils were analyzed by GC-FID and GC-MS. The highest essential oil yield was achieved from microwave and shade drying methods. In total, 39 components were found, with carvacrol (ranging from 56.2 to 81.4%) being the main constituent; other compounds present in lower amounts were p-cymene (1.6-17.7%), γ-terpinene (0.8-14.2%), α-pinene (0.1-2.1%), thymol methyl ether (0.4-1.8%) and thimoquinone (0.5-3.5%). The essential oil yields varied among the different treatments as well as the relative compositions. The percentages of p-cymene, γ-terpinene and α-pinene decreased significantly in the dried sample compared with the fresh sample; on the other hand, carvacrol, isoborneol and linalool increased significantly in the dried materials. The choice of the drying method for obtaining the essential oil therefore appears crucial not only in relation to the higher yield but also and above all in reference to the percentage presence of components that can direct the essential oil toward an appropriate use., (© 2022. The Author(s).)

The unexpected emergence of the new Coronavirus disease (COVID-19) has affected more than three hundred million individuals and resulted in more than five million deaths worldwide. The ongoing pandemic has underscored the urgent need for effective preventive and therapeutic measures to develop anti-viral therapy. The natural compounds possess various pharmaceutical properties and are reported as effective anti-virals. The interest to develop an anti-viral drug against the novel severe acute respiratory syndrome Coronavirus (SARS-CoV-2) from natural compounds has increased globally. Here, we investigated the anti-viral potential of selected promising natural products. Sources of data for this paper are current literature published in the context of therapeutic uses of phytoconstituents and their mechanism of action published in various reputed peer-reviewed journals. An extensive literature survey was done and data were critically analyzed to get deeper insights into the mechanism of action of a few important phytoconstituents. The consumption of natural products such as thymoquinone, quercetin, caffeic acid, ursolic acid, ellagic acid, vanillin, thymol, and rosmarinic acid could improve our immune response and thus possesses excellent therapeutic potential. This review focuses on the anti-viral functions of various phytoconstituent and alkaloids and their potential therapeutic implications against SARS-CoV-2. Our comprehensive analysis provides mechanistic insights into phytoconstituents to restrain viral infection and provide a better solution through natural, therapeutically active agents., (Copyright © 2022 The Authors. Published by Elsevier Masson SAS.. All rights reserved.)

The present study was the first to evaluate the phytochemical composition, antioxidant, antimicrobial, antibiofilm, and anti-quorum sensing potential of Allium subhirsutum L. (hairy garlic) aqueous extract through in vitro and in silico studies. The phytochemical profile revealed the presence of saponins, terpenes, flavonols/flavonones, flavonoids, and fatty acids, particularly with flavonoids (231 ± 0.022 mg QE/g extract), tannins (159 ± 0.006 mg TAE/g extract), and phenols (4 ± 0.004 mg GAE/g extract). Gas chromatography-mass spectrometry (GC-MS) analysis identified 15 bioactive compounds, such as 5-hydroxymethylfurfural (37.04%), methyl methanethiolsulfonate (21.33%), furfural (7.64%), beta-D-glucopyranose, 1,6-anhydro- (6.17%), 1,6-anhydro-beta-D-glucofuranose (3.6%), trisulfide, di-2-propenyl (2.70%), and diallyl disulfide (1.93%). The extract was found to be non-toxic with 50% cytotoxic concentration higher than 30,000 µg/mL. The investigation of the antioxidant activity via DPPH (2, 2-diphenyl-1-picrylhydrazyl) and FRAP (IC 50 = 1 μg/mL), ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid); IC 50 = 0.698 ± 0.107 μg/mL), and β-carotene (IC 50 = 0.811 ± 0.036 mg/mL) was assessed. Nevertheless, good antimicrobial potential against a diverse panel of microorganisms with bacteriostatic and fungistatic effect was observed. Quorum sensing inhibition effects were also assessed, and the data showed the ability of the extract to inhibit the production of violacein by the mutant C. violaceum strain in concentration-dependent manner. Similarly, the biofilm formation by all tested strains was inhibited at low concentrations. In silico pharmacokinetic and toxicological prediction indicated that, out of the sixteen identified compounds, fourteen showed promising drug ability and could be used as lead compounds for further development and drug design. Hence, these findings support the popular use of hairy garlic as a source of bioactive compounds with potential application for human health.

Due to the emergency and uncontrolled situation caused by the COVID-19 pandemic that arising in the entire world, it is necessary to choose available drugs that can inhibit or prevent the disease. Therefore, the repurposing of the commercial antibiotic, dirithromycin has been screened for the first time against fifteen receptors and compared to the azithromycin using a molecular docking approach to identify possible SARS-CoV-2 inhibitors. Our docking results showed that dirithromycin fit significantly in the Furin catalytic pocket having the lowest binding score (-9.9 Kcal/mol) with respect to azithromycin (-9.4 Kcal/mol) and can interact and block both Asp154 and Ser368 residues by Van der Walls interaction as well as bound to His194 and Ser368 residues via hydrogen bonds. Good results were also obtained with the Tmprss-2 receptor. A Molecular Dynamic simulation was assessed to confirm this interaction. Additionally, detailed receptor-ligand interactions with SARS-CoV-2 and pro-inflammatory mediators were investigated suggesting more target information with interesting results. The findings of this study are very efficient and provide a basis for the development of dirithromycin for clinical trial applications to be efficient in treating SARS-CoV-2 infections.

Developing new prophylactic and therapeutic agents with broad-spectrum antiviral activities is urgently needed to combat emerging human severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Since no available clinically antiviral drugs have been approved to eradicate COVID-19 as of the writing of this report, this study aimed to investigate bioactive short peptides from Allium subhirsutum L. (Hairy garlic) extracts identified through HR-LC/MS analysis that could potentially hinder the multiplication cycle of SARS-CoV-2 via molecular docking study. The obtained promising results showed that the peptides (Asn-Asn-Asn) possess the highest binding affinities of -8.4 kcal/mol against S protein, (His-Phe-Gln) of -9.8 kcal/mol and (Gln-His-Phe) of -9.7 kcal/mol towards hACE2, (Thr-Leu-Trp) of -10.3 kcal/mol and (Gln-Phe-Tyr) of -9.8 kcal/mol against furin. Additionally, the identified peptides show strong interactions with the targeted and pro-inflammatory ranging from -8.1 to -10.5 kcal/mol for NF-κB-inducing kinase (NIK), from -8.2 to -10 kcal/mol for phospholipase A2 (PLA2), from -8.0 to -10.7 kcal/mol for interleukin-1 receptor-associated kinase 4 (IRAK-4), and from -8.6 to -11.6 kcal/mol for the cyclooxygenase 2 (COX2) with Gln-Phe-Tyr model seems to be the most prominent. Results from pharmacophore, drug-likeness and ADMET prediction analyses clearly evidenced the usability of the peptides to be developed as an effective drug, beneficial for COVID-19 treatment.

Lavandula angustifolia Mill. (lavender) and Origanum heracleoticum L. (greek oregano) are aromatic plants used in traditional medicine for relief of convulsion, anxiety, insomnia and in the treatment of neurological disorders. On the basis of literature, we evaluated the changing in glutathione enzymatic activities provoked by the essential oils and pure components, linalool, carvacrol and limonene to study the mechanisms of action, responsible for several activities. Activities of SOD (superoxide dismutase) and GPx (glutathione peroxidase) tend to increase respect to control. SOD maximal increase reached up to 117% for carvacrol and limonene. Increase in GPx activity reached even up to value 1.229 for origanum oil in comparison to control 0.125 μkat/mg prot. Activities of GR (glutathione reductase), except for lavender, showed a biphasic response. Like for GR, the administration of compounds, resulted in a biphasic response in GST (glutathione-S-transferase) activities (with a consistent increase in activity at concentration 125 μg/mL for all compounds except lavender). Moreover, the changes in GSH (reduced glutathione), are no significant for different concentrations of essential oils. So, the biological properties of essential oils and specifically, the antioxidant ones, can be related to their capacity to modify the glutathione enzymatic activities.

The main objective of this study is to find out the anti-SARS-CoV-2 potential of emetine by using molecular docking and dynamic simulation approaches. Interestingly, molecular docking studies suggest that Emetine showed significant binding affinity toward Nsp15 (-10.8   kcal/mol) followed by Nsp12 (-9.5   kcal/mol), RNA-dependent RNA polymerase, RdRp (-9.5   kcal/mol), Nsp16 (-9.4   kcal/mol), Nsp10 (-9.2   kcal/mol), Papain-like protein (-9.0   kcal/mol), Nsp13 (-9.0   kcal/mol), Nsp14 (-8.9   kcal/mol) and Spike Protein Receptor Domain (-8.8   kcal/mol) and chymotrypsin-like protease, 3CLpro (-8.5   kcal/mol), respectively, which are essential for viral infection and replication. In addition, molecular dynamic simulation (MD) was also performed for 140   ns to explore the stability behavior of the main targets and inhibitor complexes as well as the binding mechanics of the ligand to the target proteins. The obtained MD results followed by absolute binding energy calculation confirm that the binding of emetine at the level of the various receptors is more stable. The complex EmetineNSP15, mechanistically was stabilized as follows: Emetine first binds to the monomer, after, binds to the second inducing the formation of a dimer which in turn leading to the formation of complex that simulation stabilizes it at a value less than 5   Å. Overall, supported by the powerful and good pharmacokinetic data of Emetine, our findings with clinical trials may be helpful to confirm that Emetine could be promoted in the prevention and eradication of COVID-19 by reducing the severity in the infected persons and therefore can open possible new strategies for drug repositioning. Communicated by Ramaswamy H. Sarma.

The emergence of a novel coronavirus viz., severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in late 2019 and its subsequent substantial spread produced the coronavirus disease 2019 (COVID-19) pandemic worldwide. Given its unprecedented infectivity and pathogenicity, the COVID-19 pandemic had a devastating impact on human health, and its clinical management has been a great challenge, which has led to the development and speedy trials of several vaccine candidates against SARS-CoV-2 at an exceptional pace. As a result, several COVID-19 vaccines were made commercially available in the first half of 2021. Although several COVID-19 vaccines showed promising results, crucial insights into their epidemiology, protective mechanisms, and the propensities of reinfection are not largely reviewed. In the present report, we provided insights into the prospects of vaccination against COVID-19 and assessed diverse vaccination strategies including DNA, mRNA, protein subunits, vector-based, live attenuated, and inactivated whole/viral particle-based vaccines. Next, we reviewed major aspects of various available vaccines approved by the World Health Organization and by the local administrations to use against COVID-19. Moreover, we comprehensively assessed the success of these approved vaccines and also their untoward effects, including the possibility of reinfection. We also provided an update on the vaccines that are under development and could be promising candidates in the future. Conclusively, we provided insights into the COVID-19 vaccine epidemiology, their potency, and propensity for SARS-CoV-2 reinfection, while a careful review of their current status, strategies, success, and future challenges was also presented.

Cucumis sativus L. is globally cultivated as an edible vegetable. Besides its nutritional benefits, it is used in traditional medicines against various ailments. The current study was designed to elucidate the multi-target mechanisms of a C. sativus seeds extract against asthma and diarrhea using network pharmacology along with a molecular docking approach. Furthermore, in-vitro and in-vivo experiments were conducted to verify the mechanistic insight of in silico studies. LC-ESI-MS/MS was performed to identify the bioactive compounds in the extract; later, some compounds were quantified by HPLC. C. sativus seed. EtOH has kaempferol in higher concentration 783.02 µg/g, followed by quercetin (693.83 µg/g) and luteolin (617.17 µg/g). In silico studies showed that bioactive compounds interfered with asthma and diarrhea-associated target genes, which are members of calcium-mediated signaling to exert a calcium channel blocker activity. The seeds extract exerted a concentration-dependent spasmolytic response on isolated jejunum, trachea, and urinary bladder preparations and caused relaxation of spastic contraction of K + (80 mM) with suppressed calcium concentration-response curves at dose 0.3 and 1 mg/mL. It also showed antiperistalsis, antidiarrheal and antisecretory activity in animal models. Thus, C. sativus seeds have therapeutic effects by regulating the contractile response through a calcium-mediated signaling pathway.

Background/Aim: Sweet almond ( Prunus amygdalus dulcis ) oil is one of the most famous cold-pressed seed oils. However, other species of Prunus can provide oils with healthy properties. We analyzed the fatty acid (FA) composition, as well as the antioxidant, the in vitro anti-inflammatory properties, and the antibiofilm activity of five commercial vegetable cold-pressed seed oils of apricot, peach, plum, cherry, and black cherry. Methods: Gas Chromatography-Mass Spectrometry was performed for the analysis of FAs The antioxidant property of the oils was carried using different tests [2, 2-diphenyl-1-picrylhydrazyl (DPPH assay)], Ferric Reducing Antioxidant Power (FRAP), and the 2, 20 -azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS·+). The denaturation assay performed on bovine serum albumin (BSA) was used to evaluate the in vitro anti-inflammatory activity. The anti-biofilm activity was assessed using five pathogenic strains, namely, Acinetobacter baumannii, Escherichia coli, Listeria monocytogenes, Pseudomonas aeruginosa , and Staphylococcus aureus , through the crystal violet test and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), used to evaluate the metabolism of the microbial cells present within the biofilm. Results: Oleic acid and linoleic acids were the most abundant FAs. Black cherry seed oil exhibited the best antioxidant activity, but in general, the amount of oil needed to inhibit the activity of 1 ml of DPPH assay at 50% did not exceed 10 μg. The extract concentration for the 50% inhibition of the denaturation of the protein (IC50) did not exceed 4.4 μg. Linoleic and stearic acids affected the antioxidant activity of the oils; oleic acid, linolenic, and palmitoleic acids exhibited beneficial effects in preserving the BSA denaturation, as shown by the correlation data. The oils were able to inhibit the biofilm formation of the pathogens (up to 71.40% of inhibition) as well as act against their mature biofilm, although with different strengths, with values up to 61.54%. Concurrently, they also acted on the pathogen metabolism. Conclusion: The oils represent a valuable source of some healthy FAs. They showed potential antioxidant and anti-inflammatory in vitro activity, in addition, their potential effect on the biofilm can offer important ideas for research and reflection on their use as functional foods and/or ingredients., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2021 Fratianni, d'Acierno, Ombra, Amato, De Feo, Ayala-Zavala, Coppola and Nazzaro.)

The phytotoxicity and eco-compatibility of essential oils (EOs) from Eucalyptus gunnii (EG) and E. pulverulenta 'Baby Blue' (EP), cultivated in Italy for their cut foliage, were investigated. Leaf micromorphology, EOs phytochemical characterization, and phytotoxicity were analysed. EP revealed a significantly higher oil gland density and a higher EO yield with respect to EG. In both EOs, 1,8-cineole was the major compound (~75%), followed by α-pinene in EG (13.1%) and eugenol in EP (7.5%). EO phytotoxicity was tested on both weeds ( Lolium multiflorum , Portulaca oleracea ) and crops ( Raphanus sativus , Lactuca sativa , Lepidium sativum , Solanum lycopersicum , Pisum sativum, Cucumis sativus ). EG EO inhibited germination of P. oleracea , R. sativus , and S. lycopersicum seeds (ranging from 61.5 to 94.6% for the higher dose used), while affecting only radical elongation in S. lycopersicum (ranging from 66.7 to 82.6%). EP EO inhibited germination of P. oleracea and R. sativus (ranging from 41.3 to 74.7%) and affected radical elongation of L. sativum and L. multiflorum (ranging from 57.4 to 76.0%). None of the EOs affected the germination and radical growing of L. sativa , P. sativum , and C. sativus . Moreover, EP EO was more active than EG EO in inhibiting α-amylase, a key enzyme for seed growth regulation. Brine shrimp lethality assay showed that both EOs are safe for aquatic organisms, suggesting their high eco-compatibility. The data collected provide useful information for future applications of these EOs in agriculture as safe and selective bioherbicides.

Alzheimer's disease (AD) is one of the most prominent neurodegenerative diseases, which impairs cognitive function in afflicted individuals. AD results in gradual decay of neuronal function as a consequence of diverse degenerating events. Several neuroimmune players (such as cytokines and growth factors that are key players in maintaining CNS homeostasis) turn aberrant during crosstalk between the innate and adaptive immunities. This aberrance underlies neuroinflammation and drives neuronal cells toward apoptotic decline. Neuroinflammation involves microglial activation and has been shown to exacerbate AD. This review attempted to elucidate the role of cytokines, growth factors, and associated mechanisms implicated in the course of AD, especially with neuroinflammation. We also evaluated the propensities and specific mechanism(s) of cytokines and growth factors impacting neuron upon apoptotic decline and further shed light on the availability and accessibility of cytokines across the blood-brain barrier and choroid plexus in AD pathophysiology. The pathogenic and the protective roles of macrophage migration and inhibitory factors, neurotrophic factors, hematopoietic-related growth factors, TAU phosphorylation, advanced glycation end products, complement system, and glial cells in AD and neuropsychiatric pathology were also discussed. Taken together, the emerging roles of these factors in AD pathology emphasize the importance of building novel strategies for an effective therapeutic/neuropsychiatric management of AD in clinics.

Membrane-bound CD200 is overexpressed in chronic lymphocytic leukemia (CLL), and there is some evidence that its soluble ectodomain (sCD200) could also be involved in the pathophysiology and the disease. However, very little is known about sCD200's prognostic significance. sCD200 was tested at diagnosis in 272 patients with CLL and in 78 age- and sex-matched healthy subjects using a specific human CD200 (OX-2 membrane glycoprotein) ELISA kit. A significantly higher concentration of sCD200 was found in CLL patients compared to controls. In our cohort, sCD200 was significantly higher in patients who were older than 66 years, with Binet stage C, unmutated IgVH and unfavorable (del11q or del17p) FISH. Time-to-first treatment and overall survival were significantly shorter in patients with higher sCD200 concentration, using as a cut-off 1281 pg/mL, the median value for sCD200 concentration in the whole CLL cohort. However, the prognostic impact of sCD200 was not confirmed in multivariate analysis. Baseline sCD200 values appeared to have an impact on the response to chemotherapy or chemo-immunotherapy, but not to targeted agents. Collectively, our data show that sCD200 serum levels correlate with more aggressive clinical and biological features and are able to predict a worse prognosis. This work supports the relevant role of CD200 not only as a diagnostic tool but also as a prognostic indicator and a potential therapeutic target in CLL.

We evaluated the polyphenol content and the α-glucosidase activity exhibited by different monofloral honeys of Italian origin. Their capacity to act on different pathogenic ( Acinetobacter baumannii , Escherichia coli , Listeria monocytogenes , Pseudomonas aeruginosa , and Staphylococcus aureus) as well as probiotic bacteria ( Lacticaseibacillus casei , Lactobacillus   acidophilus , Lactiplantibacillus plantarum , Lactobacillus gasseri , and Lacticaseibacillus rhamnosus ) was also assessed. Total polyphenols varied between 110.46 μg/g of fresh product (rhododendron honey) and 552.29 μg/g of fresh product (strawberry tree honey). Such result did not correspond to a parallel inhibitory α-glycosidase activity that, in each case was never higher than 33 μg/mL. Honeys were differently capable to fight the biofilm formation of the pathogens (inhibition up to 93.27%); they inhibited the in vitro adhesive process (inhibition up to 84.27%), and acted on mature biofilm (with values up to 76.64%). Their effect on bacterial metabolism was different too. Honeys were ineffective to inhibit E. coli mature biofilm nor to act on its metabolism. The action of the honey on probiotic strains seemed almost always stimulate their growth. Thus, these monofloral honeys might exhibit effects on human health and act positively as prebiotics.

Many natural-derived compounds, including the essential oils from plants, are investigated to find new potential protective agents in several neurodegenerative disorders such as Alzheimer's disease (AD). In the present study, we tested the neuroprotective effect of limonene, one of the main components of the genus Citrus , against the neurotoxicity elicited by Aβ 1-42 oligomers, currently considered a triggering factor in AD. To this aim, we assessed the acetylcholinesterase activity by Ellman's colorimetric method, the mitochondrial dehydrogenase activity by MTT assay, the nuclear morphology by Hoechst 33258, the generation of reactive oxygen species (ROS) by DCFH-DA fluorescent dye, and the electrophysiological activity of K V 3.4 potassium channel subunits by patch-clamp electrophysiology. Interestingly, the monoterpene limonene showed a specific activity against acetylcholinesterase with an IC 50 almost comparable to that of galantamine, used as positive control. Moreover, at the concentration of 10 µg/mL, limonene counteracted the increase of ROS production triggered by Aβ 1-42 oligomers, thus preventing the upregulation of K V 3.4 activity. This, in turn, prevented cell death in primary cortical neurons, showing an interesting neuroprotective profile against Aβ 1-42 -induced toxicity. Collectively, the present results showed that the antioxidant properties of the main component of the genus Citrus , limonene, may be useful to prevent neuronal suffering induced by Aβ 1-42 oligomers preventing the hyperactivity of K V 3.4.

Diabetes mellitus (DM) is one of the principal manifestations of metabolic syndrome and its prevalence with modern lifestyle is increasing incessantly. Chronic hyperglycemia can induce several vascular complications that were referred to be the major cause of morbidity and mortality in DM. Although several therapeutic targets have been identified and accessed clinically, the imminent risk of DM and its prevalence are still ascending. Substantial pieces of evidence revealed that histone deacetylase (HDAC) isoforms can regulate various molecular activities in DM via epigenetic and post-translational regulation of several transcription factors. To date, 18 HDAC isoforms have been identified in mammals that were categorized into four different classes. Classes I, II, and IV are regarded as classical HDACs, which operate through a Zn-based mechanism. In contrast, class III HDACs or Sirtuins depend on nicotinamide adenine dinucleotide (NAD + ) for their molecular activity. Functionally, most of the HDAC isoforms can regulate β cell fate, insulin release, insulin expression and signaling, and glucose metabolism. Moreover, the roles of HDAC members have been implicated in the regulation of oxidative stress, inflammation, apoptosis, fibrosis, and other pathological events, which substantially contribute to diabetes-related vascular dysfunctions. Therefore, HDACs could serve as the potential therapeutic target in DM towards developing novel intervention strategies. This review sheds light on the emerging role of HDACs/isoforms in diabetic pathophysiology and emphasized the scope of their targeting in DM for constituting novel interventional strategies for metabolic disorders/complications.

The aim of the study was to investigate the micromorphology of Mentha pulegium leaves and flowers harvested in three different Sicilian (Italy) areas with peculiar pedo-climatic conditions, and to characterize the phytochemical profile, the phytotoxic activity, and the eco-compatibility of their essential oils (EOs) for potential use as safe bioherbicides. Light microscopy (LM) and scanning electron microscopy (SEM) highlighted that M. pulegium indumentum consists of non-glandular and glandular trichomes of different types. Peltate trichomes of plants from the different sites showed few significant differences in dimension and abundance, but they were characterized by a surprisingly high number of secretory cells both in leaves and flowers. Phytochemical analyses showed that oxygenated monoterpenes were the most abundant class in all the EOs investigated (92.2-97.7%), but two different chemotypes, pulegone/isomenthone and piperitone/isomenthone, were found. The complex of morphological and phytochemical data indicates that soil salinity strongly affects the expression of the toxic metabolite pulegone, rather than the EO yield. Phytotoxicity tests showed a moderate activity of EOs against the selected species as confirmed by α-amylase assay. Moreover, the low toxicity on brine shrimp provided a rationale for the possible use of investigated EOs as eco-friendly herbicides.

In this study, we investigated the bioactive potential (antibacterial and antioxidant), anticancer activity and detailed phytochemical analysis of Selaginella repanda (S. repanda) ethanolic crude extract for the very first time using different in vitro approaches. Furthermore, computer-aided prediction of pharmacokinetic properties and safety profile of the identified phytoconstituents were also employed in order to provide some useful insights for drug discovery. S. repanda , which is a rich source of potent natural bioactive compounds, showed promising antibacterial activity against the tested pathogenic bacteria ( S. aureus , P. aeruginosa , E. coli and S. flexneri ). The crude extract displayed favorable antioxidant activity against both 2,2-diphenyl-1-picrylhydrazyl (DPPH) (IC 50 = 231.6 μg/mL) and H 2 O 2 (IC 50 = 288.3 μg/mL) molecules. S. repanda also showed favorable and effective anticancer activity against all three malignant cancer cells in a dose/time dependent manner. Higher activity was found against lung (A549) (IC 50 = 341.1 μg/mL), followed by colon (HCT-116) (IC 50 = 378.8 μg/mL) and breast (MCF-7) (IC 50 = 428.3 μg/mL) cancer cells. High resolution-liquid chromatography-mass spectrometry (HR-LC-MS) data of S. repanda crude extract revealed the presence of diverse bioactive/chemical components, including fatty acids, alcohol, sugar, flavonoids, alkaloids, terpenoids, coumarins and phenolics, which can be the basis and major cause for its bioactive potential. Therefore, achieved results from this study confirmed the efficacy of S. repanda and a prospective source of naturally active biomolecules with antibacterial, antioxidant and anticancer potential. These phytocompounds alone with their favorable pharmacokinetics profile suggests good lead and efficiency of S. repanda with no toxicity risks. Finally, further in vivo experimental investigations can be promoted as probable candidates for various therapeutic functions, drug discovery and development.

Pomegranate ( Punica granatum L.) fruits are important sources of vitamins and minerals and widely used in the dietary supplement industry. An aqueous extract of its leathery exocarp (LEP) was obtained by a solid-phase micro-extraction method. The antifungal activity was examined against the phytopathogenic fungi, Fusarium oxysporum , Phytophthora cinnamomi , Penicillium digitatum and Botrytis cinerea , and the antibacterial activity was evaluated against Escherichia coli , Xanthomonas campestris, Bacillus megaterium and Clavibacter michiganensis . The antimicrobial assays showed, in some cases, a promising antimicrobial effect compared to the synthetic drugs. The possible anti-acetylcholinesterase and antioxidant activities of the LEP extract were investigated by the Ellman's assay and 2,2-diphenyl-1-picrylhydrazyl (DPPH) test, respectively, and their results showed that the LEP extract has an effective anti-acetylcholinesterase inhibitory effect and an antioxidant activity. Thus, the LEP extract could be valid as a candidate for further studies on the use of pomegranate in neurodegenerative diseases as a food preservative and a suitable substitute to control several phytopathogens.

The essential oil (EO) from basil- Ocimum basilicum -was characterized, microencapsulated by vibration technology, and used to prepare a new type of packaging system designed to extend the food shelf life. The basil essential oil (BEO) chemical composition and antimicrobial activity were analyzed, as well as the morphological and biological properties of the derived BEO microcapsules (BEOMC). Analysis of BEO by gas chromatography demonstrated that the main component was linalool, whereas the study of its antimicrobial activity showed a significant inhibitory effect against all the microorganisms tested, mostly Gram-positive bacteria. Moreover, the prepared BEOMC showed a spheroidal shape and retained the EO antimicrobial activity. Finally, chitosan-based edible films were produced, grafted with BEOMC, and characterized for their physicochemical and biological properties. Since their effective antimicrobial activity was demonstrated, these films were tested as packaging system by wrapping cooked ham samples during 10 days of storage, with the aim of their possible use to extend the shelf life of the product. It was demonstrated that the obtained active film can both control the bacterial growth of the cooked ham and markedly inhibit the pH increase of the packaged food.

The present study evaluated the therapeutic potential of myricitrin (Myr), a glycosyloxyflavone extracted from Myrica esculenta bark, against diabetic nephropathy. Myr exhibited a significant hypoglycemic effect in high fat-fed and a single low-dose streptozotocin-induced type 2 diabetic (T2D) rats. Myr was found to improve glucose uptake by the skeletal muscle via activating IRS-1/PI3K/Akt/GLUT4 signaling in vitro and in vivo. Myr significantly attenuated high glucose (HG)-induced toxicity in NRK cells and in the kidneys of T2D rats. In this study, hyperglycemia caused nephrotoxicity via endorsing oxidative stress and inflammation resulting in the induction of apoptosis, fibrosis, and inflammatory damages. Myr was found to attenuate oxidative stress via scavenging/neutralizing oxidative radicals and improving endogenous redox defense through Nrf-2 activation in both in vitro and in vivo systems. Myr was also found to attenuate diabetes-triggered renal inflammation via suppressing NF-κB activation. Myr inhibited hyperglycemia-induced apoptosis and fibrosis in renal cells evidenced by the changes in the expressions of the apoptotic and fibrotic factors. The molecular docking predicted the interactions between Myr and different signal proteins. An in silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) study predicted the drug-likeness character of Myr. Results suggested the possibility of Myr to be a potential therapeutic agent for diabetic nephropathy in the future.

Alzheimer's disease (AD) is a neurodegenerative disorder leading to cognitive deficits and cognitive decline. Since no cure or preventing therapy is currently available to counteract AD, natural-derived compounds are investigated to find new potential neuroprotective agents for its treatment. In the present study, we tested the neuroprotective effect of lavender and coriander essential oils (EOs) and their main active constituent linalool, against the neurotoxicity elicited by Aβ 1-42 oligomers, a key molecular factor in the neurodegeneration of AD. Importantly, our findings on neuronally differentiated PC12 cells exposed to Aβ 1-42 oligomers are in accordance with previous in vivo studies reporting the neuroprotective potential of lavender and coriander EOs and linalool. We found that lavender and coriander EOs at the concentration of 10 μg/mL as well as linalool at the same concentration were able to improve viability and to reduce nuclear morphological abnormalities in cells treated with Aβ 1-42 oligomers for 24 hours. Lavender and coriander EOs and linalool also showed to counteract the increase of intracellular reactive oxygen species production and the activation of the pro-apoptotic enzyme caspase-3 induced by Aβ 1-42 oligomers. Our findings provide further evidence that these EOs and their main constituent linalool could be natural agents of therapeutic interest against Aβ 1-42 -induced neurotoxicity., (© 2020 John Wiley & Sons Ltd.)

CD200, a transmembrane type Ia glycoprotein belonging to the immunoglobulin protein superfamily, is broadly expressed on a wide variety of cell types, such as B lymphocytes, a subset of T lymphocytes, dendritic cells, endothelial and neuronal cells. It delivers immunosuppressive signals through its receptor CD200R, which is expressed on monocytes/myeloid cells and T lymphocytes. Moreover, interaction of CD200 with CD200R has also been reported to play a role in the regulation of tumor immunity. Overexpression of CD200 has been reported in chronic lymphocytic leukemia (CLL) and hairy cell leukemia but not in mantle cell lymphoma, thus helping to better discriminate between these different B cell malignancies with different prognosis. In this review, we focus on the role of CD200 expression in the differential diagnosis of mature B-cell neoplasms and on the prognostic significance of CD200 expression in CLL, where conflicting results have been published so far. Of interest, increasing evidences indicate that anti-CD200 treatment might be therapeutically beneficial for treating CD200-expressing malignancies, such as CLL., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2020 D’Arena, De Feo, Pietrantuono, Seneca, Mansueto, Villani, La Rocca, D’Auria, Statuto, Valvano, Arruga, Deaglio, Efremov, Sgambato and Laurenti.)

The present study was carried out to determine some biochemical characteristics, in particular the total polyphenol content and the free radical scavenging activity, of the extracts recovered from bulbs and aerial parts (these last often considered as by-products) of two landraces of A. ampeloprasum var. holmense cultivated in Southern Italy. For the first time, the capacity of the extracts of these landraces to inhibit the formation of biofilm of different Gram-negative and Gram-positive bacteria and to affect the metabolism of the cells present within the bacterial biofilm was evaluated. All extracts exhibited an amount of total polyphenols not lower than 2.86 mg/g of dried product and revealed a noteworthy antioxidant activity, with EC 50 values not exceeding 4.95 mg. In both cases, the aerial parts extracts were more effective than the bulb extracts, which also showed a minor amount of total polyphenols. The extracts inhibited mainly the adhesive capability of Pseudomonas aeruginosa and Staphylococcus aureus , by 95.78% and 85.01%, respectively. The extracts demonstrated to inhibit also the metabolism of the bacterial cells reaching levels up to 90%. Finally, as assessed by the assays performed on the 24-h preformed biofilms, all the extracts were also capable to cause a reduction in bacterial biomass and to affect their metabolism.

In this study, we investigate the phytochemical profile, anticancer, and antioxidant activities of Teucrium polium methanolic extract using both in vitro and in silico approaches. The results showed the identification of 29 phytochemical compounds belonging to 13 classes of compounds and 20 tripeptides using High Resolution-Liquid Chromatography Mass Spectrometry (HR-LCMS). 13R-hydroxy-9E,11Z octadecadienoic acid, dihydrosamidin, valtratum, and cepharantine were the main compounds identified. The tested extract showed promising antioxidant activities (ABTS-IC 50 = 0.042 mg/mL; 1,1-diphenyl-2-picrylhydrazyl (DPPH)-IC 50 = 0.087 mg/mL, β-carotene-IC 50 = 0.101 mg/mL and FRAP-IC 50 = 0.292 mg/mL). Using both malignant Walker 256/B and MatLyLu cell lines, T. polium methanolic extract showed a dose/time-dependent antitumor activity. The molecular docking approach revealed that most of the identified molecules were specifically binding with human peroxiredoxin 5, human androgen, and human progesterone receptors with high binding affinity scores. The obtained results confirmed that T. polium is a rich source of bioactive molecules with antioxidant and antitumor potential.

Solidago canadensis L. (SC) (Canadian goldenrod) is a dangerous plant invader in Europe, which suppress the indigenous flora. Essential oils (EOs) are considered biological control agents. GC-MS analysis for identification of main components was conducted and the potential phytotoxicity of six EOs were also evaluated. Limonene and β-thujone were dominant components in Salvia officinalis L., menthone and menthol in Mentha × piperita L., carvacrol in Origanum vulgare L., estragole/anisole and anethole in Foeniculum vulgare Mill., limonene and carvone in Anethum graveolens L., and anethole in Pimpinella anisum L. Along with EOs, anethole, anisole, camphor, carvone, estragole, limonene, menthol, menthone, thujone and thymol were used independently to evaluate phytotoxic effect against Canadian goldenrod seed germination. A significant inhibitory effect was registered for origanum (1.250 µg.ml -1 ). The influence of single components was significant. The highest phytotoxic activity was registered with anethole and estragole. Phenolic compounds were the inhibitoriest, followed by oxygenated and hydrocarbon monoterpenes.

The chemical profile of Teucrium polium L. ( T. polium ) methanolic extract was tested using liquid chromatography coupled with high resolution mass spectrometry (HR-LCMS). Disc diffusion and microdilution assays were used for the antimicrobial activities. Coxsackievirus B-3 (CVB3) and Herpes simplex virus type 2 (HSV-2) were used for the antiviral activities. Chromobacterium violaceum (ATCC 12472 and CV026) and Pseudomonas aeruginosa PAO1 were used as starter strains for the anti-quorum sensing tests. Isoprenoids are the main class of compounds identified, and 13R-hydroxy-9E,11Z-octadecadienoic acid, valtratum, rhoifolin, sericetin diacetate, and dihydrosamidin were the dominant phytoconstituents. The highest mean diameter of growth inhibition zone was recorded for Acinetobacter baumannii (19.33 ± 1.15 mm). The minimal inhibitory concentrations were ranging from 6.25 to 25 mg/mL for bacterial strains, and from 6.25 to 25 mg/mL for Candida species. The 50% cytotoxic concentration on VERO (African Green Monkey Kidney) cell lines was estimated at 209 µg/mL. No antiviral activity was recorded. Additionally, T. polium extract was able to inhibit P. aeruginosa PAO1 motility in a concentration-dependent manner. However, the tested extract was able to inhibit 23.66% of the swarming and 35.25% of swimming capacities of PAO1 at 100 µg/mL. These results highlighted the role of germander as a potent antimicrobial agent that can interfere with the virulence factors controlled by the quorum-sensing systems.

This study investigated Allium subhirsutum L. (AS) anticancer and antioxidant effects and inhibition of tumor angiogenesis in a murine model of skeletal metastases due to inoculation of Walker 256/B cells. Phytochemical composition of AS extract (ASE) was studied by High Resolution-Liquid Chromatography Mass Spectroscopy (HR-LCMS). Total phenolic and flavonoid contents (TPC and TFC) were determined. In vitro, the antioxidant properties were evaluated by reducing power and antiradical activity against DPPH. Cancer cells' proliferation, apoptosis, metastatic development and angiogenesis were evaluated using Walker 256/B and MatLyLu cells. The p-coumaric acid was the major phenolic acid (1700 µg/g extract). ASE showed high levels of TPC and TFC and proved potent antioxidant effects. ASE inhibited Walker 256/B and MatLyLu cells' proliferation (Half-maximal inhibitory concentration: IC 50 ≃ 150 µg/mL) and induced apoptosis. In silico and in vivo assays confirmed these findings. ASE effectively acts as a chemo-preventive compound, induces apoptosis and attenuates angiogenesis and osteolytic metastases due to Walker 256/B malignant cells.

Cell phones, smartphones, and tablets are extensively used in social and professional life, so they are frequently exposed to bacteria. The main goal of the present work was to isolate and characterize Staphylococci strains from students' cell phone mobiles. Subsequently, 24 Staphylococci strains were tested against a wide range of antibiotics, for the distribution of some virulence-related genes and their ability to form biofilm. Staphylococcus spp. were cultured from all studied devices on chromogenic medium and identified using the matrix-assisted laser desorption/ionization (MALDI), time-of-flight (TOF) mass spectrometry (MS) technique (MALDI-TOF-MS). The results obtained showed that S. aureus was the dominant species (19 strains, 79.1%), followed by S. warneri (3 strains, 12.5%), and S. haemolyticus (2 strains, 8.3%). Isolated strains showed high percentages of hydrolytic enzymes production, resistance to many tested antibiotics, and 37.5% expressed the mec A gene. The tested strains were highly adhesive to polystyrene and glass and expressed implicated ica A (62.5%) and ica D (66.6%) genes. All Staphylococcus spp. strains tested were found to possess proteases and the α-hemolysin gene. Our results highlighted the importance of mobile phones as a great source of Staphylococcus spp., and these species were found to be resistant to many antibiotics with multiple antibiotic resistance (MAR) index ranging from (0.444) to (0.812). Most of the studied strains are able to form biofilm and expressed many virulence genes. Phylogenetic analysis based on the phenotypic and genetic characters highlighted the phenotypic and genetic heterogeneity of the S . aureus population studied. Further analyses are needed to elucidate the human health risks associated with the identified Staphylococci strains., Competing Interests: The authors declare no conflict of interest.

Melanin is the main pigment of human skin, playing the primary role of protection from ultraviolet radiation. Alteration of the melanin production may lead to hyperpigmentation diseases, with both aesthetic and health consequences. Thus, suppressors of melanogenesis are considered useful tools for medical and cosmetic treatments. A great interest is focused on natural sources, aimed at finding safe and quantitatively available depigmenting substances. Lichens are thought to be possible sources of this kind of compounds, as the occurrence of many phenolic molecules suggests possible effects on phenolase enzymes involved in melanin synthesis, like tyrosinase. In this work, we used four lichen species, Cetraria islandica Ach., Flavoparmelia caperata Hale, Letharia vulpina (L.) Hue, and Parmotrema perlatum (Hudson) M. Choisy, to obtain extracts in solvents of increasing polarity, viz. chloroform, chloroform-methanol, methanol, and water. Cell-free, tyrosinase inhibition experiments showed highest inhibition for L. vulpina methanol extract, followed by C. islandica chloroform-methanol one. Comparable results for depigmenting activities were observed by means of in vitro and in vivo systems, such as MeWo melanoma cells and zebrafish larvae. Our study provides first evidence of depigmenting effects of lichen extracts, from tyrosinase inhibition to cell and in vivo models, suggesting that L. vulpina and C. islandica extracts deserve to be further studied for developing skin-whitening products., Competing Interests: Paolo Giordani is an Academic Editor for PeerJ., (©2020 Malaspina et al.)

Adiantum philippense ( A. philippense ), an ethnomedicinally important fern, has become an interesting herb in the search for novel bioactive metabolites, which can also be used as therapeutic agents. Primarily, in this study, A. philippense crude extract was screened for its phytochemical constituents, antagonistic potential, and effect on bacterial adhesion and biofilm formation against common food pathogens. Phytochemical profiling of A. philippense was carried out by using High Resolution-Liquid Chromatography and Mass Spectroscopy (HR-LCMS) followed by antibacterial activity via agar cup/well diffusion, broth microdilution susceptibility methods, and growth curve analysis. Antibiofilm potency and efficacy were assessed on the development, formation, and texture of biofilms through light microscopy, fluorescent microscopy, scanning electron microscopy, and the assessment of exopolysaccharide production. Correspondingly, a checkerboard test was performed to evaluate the combinatorial effect of A. philippense and chloramphenicol. Lastly, molecular docking studies of identified phytochemicals with adhesin proteins of tested food pathogens, which helps the bacteria in surface attachment and leads to biofilm formation, were assessed. A. philippense crude extract was found to be active against all tested food pathogens, displaying the rapid time-dependent kinetics of bacterial killing. A. philippense crude extract also impedes the biofilm matrix by reducing the total content of exopolysaccharide, and, likewise, the microscopic images revealed a great extent of disruption in the architecture of biofilms. A synergy was observed between A. philippense crude extract and chloramphenicol for E. coli, S. aureus , and P. aeruginosa , whereas an additive effect was observed for S. flexneri . Various bioactive phytochemicals were categorized from A. philippense crude extract using HR-LCMS. The molecular docking of these identified phytochemicals was interrelated with the active site residues of adhesin proteins, IcsA, Sortase A, OprD, EspA, and FimH from S. flexneri, S. aureus, P. aeruginosa , and E. coli , respectively. Thus, our findings represent the bioactivity and potency of A. philippense crude extract against food pathogens not only in their planktonic forms but also against/in biofilms for the first time. We have also correlated these findings with the possible mechanism of biofilm inhibition via targeting adhesin proteins, which could be explored further to design new bioactive compounds against biofilm producing foodborne bacterial pathogens., (Copyright © 2020 Adnan, Patel, Deshpande, Alreshidi, Siddiqui, Reddy, Emira and De Feo.)

Background: Fruit peels are generally underutilized byproducts of the food industry, although they are valuable sources of bioactive compounds. The aim of this study is to evaluate a new application for three Citrus peel EOs as bio-herbicides., Methods: After a micro-morphological evaluation of Citrus peels by SEM analysis, the phytochemical composition of the EOs of Citrus × bergamia Risso & Poit., Citrus × myrtifolia Raf., and Citrus limon (L.) Osbeck was characterized by GC/FID and GC/MS analyses. The in vitro phytotoxicity against germination and initial radical elongation of several crop and weed species was evaluated. Furthermore, the eco-compatibility of these EOs has been assessed by the brine shrimp ( Artemia salina ) lethality assay., Results: SEM analysis highlighted the morphometric differences of the schizolysigenous pockets among the peels of the three Citrus species. Oxygenated monoterpenes are the main constituents in C. × bergamia (51.09%), whereas monoterpene hydrocarbons represent the most abundant compounds in C. × myrtifolia (82.15%) and C. limon (80.33%) EOs. They showed marked and selective phytotoxic activity in vitro, often at very low concentration (0.1 μg/mL) against all plant species investigated, without showing any toxicity on Artemia salina , opening the perspective of their use as safe bio-herbicides.