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Biological activities of six under-utilized medicinal leafy vegetable plants indigenous to Africa, i.e., Basella alba, Crassocephalum rubens, Gnetum africanum, Launaea taraxacifolia, Solanecio biafrae, and Solanum macrocarpon, were investigated via two independent techniques. The total phenolic content (TPC) was determined, and six microtiter plate assays were applied after extraction and fractionation. Three were antioxidant in vitro assays, i.e., ferric reducing antioxidant power (FRAP), cupric reduction antioxidant capacity (CUPRAC), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging, and the others were enzyme (acetylcholinesterase, butyrylcholinesterase, and tyrosinase) inhibition assays. The highest TPC and antioxidant activity from all the methods were obtained from polar and medium polar fractions of C. rubens, S. biafrae, and S. macrocarpon. The highest acetyl- and butyrylcholinesterase inhibition was exhibited by polar fractions of S. biafrae, C. rubens, and L. taraxacifolia, the latter comparable to galantamine. The highest tyrosinase inhibition was observed in the n-butanol fraction of C. rubens and ethyl acetate fraction of S. biafrae. In vitro assay results of the different extracts and fractions were mostly in agreement with the bioactivity profiling via high-performance thin-layer chromatography–multi-imaging–effect-directed analysis, exploiting nine different planar assays. Several separated compounds of the plant extracts showed antioxidant, α-glucosidase, α-amylase, acetyl- and butyrylcholinesterase-inhibiting, Gram-positive/-negative antimicrobial, cytotoxic, and genotoxic activities. A prominent apolar bioactive compound zone was tentatively assigned to fatty acids, in particular linolenic acid, via electrospray ionization high-resolution mass spectrometry. The detected antioxidant, antimicrobial, antidiabetic, anticholinesterase, cytotoxic, and genotoxic potentials of these vegetable plants, in particular C. rubens, S. biafrae, and S. macrocarpon, may validate some of their ethnomedicinal uses. [ABSTRACT FROM AUTHOR]

• Insecticidal activity of 47 macroalgae mostly from Mediterranean Sea was examined. • Cholinesterase and tyrosinase inhibitory effect of the alga extracts was investigated. • D. dichotoma var. intricata was the only one exhibiting BChE inhibition over 50%. • BChE inhibition by four diterpenes in DDI was investigated in silico. • The macroalgae and their metabolites might be new sources of novel insecticides. Ethanolic extracts prepared from forty-seven macroalgae species collected from the Mediterranean Sea, Aegean Sea, and Sea of Marmara were tested at 200 μg/mL against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase (TYR), crucial for insect vivacity. Only one alga extract, e.g. Dictyota dichotoma var. intricata (C.Agardh) Greville 1830, had a notable inhibition of BChE (72.0 ± 0.07%), whereas the rest of the macroalgae possessed no or low inhibition of AChE (2.20 ± 0.39% - 14.20 ± 2.16%), BChE (0.62 ± 0.07% - 41.20 ± 3.07%), and TYR (< 10%). Several known diterpenes (isoamijiol, 14-deoxyamijiol, amijidictyol, dictyodial, and 4α-acetoxydictyodial) found earlier in this species were proceeded to molecular docking experiments to figure out its interactions with BChE. Eleven of the 47 macroalgal extracts were selected based on sufficient availability for testing in larvicidal and adulticidal activity assays against female Aedes aegypti "Orlando1952" the mosquito vector of yellow fever and dengue. The selected extracts displayed a high adulticidal activity ranging between 80–100% activity at 5 μg/mosquito. In contrast, only the ethanol extract of Ceramium siliquosum var. elegans showed larvicidal mortality of 93.3 ± 11.5% at 0.5 μg/mL. Our findings show that the macroalgae and their metabolites could be sources of novel insecticidal agents. [ABSTRACT FROM AUTHOR]

• Isoquinoline alkaloids were tested against cholinesterases in vitro and in silico. • N -norgalanthamine is the most active one inhibiting both cholinesterases. • 8-Hydroxy-9-methoxycrinine was a strong inhibitor of AChE. • (+)-9- O -demethylhomolycorine displayed a moderate BChE inhibition. • This is the first report on ChE inhibition by three off the tested alkaloids. All cholinesterase (ChE) inhibitory drugs in clinical use are nitrogenous compounds and among them, galanthamine as the latest anticholinesterase drug, contains a tetrahydroisoquinoline structure. For this reason, isoquinoline alkaloids seem to be attractive in search for novel drug candidates towards Alzheimer's disease (AD). Therefore, in the current work, we investigated inhibitory capacity of several alkaloids representing expanding group of biogenetically-related isoquinoline alkaloids from the Amaryllidaceae including lycorine, (+)-9- O -demethylhomolycorine, 6-hydroxybuphanisine, 9- O -demethoxymontanine, 3- epi- hydroxy-bulbispermine, tazettine, haemanthamine, (+)-haemanthidine, (-)-crinine, 8-hydroxy-9-methoxycrinine, and N -norgalanthamine against ChEs by microtiter enzyme inhibition assays. Our findings indicated that N -norgalanthamine is the most active one inhibiting both acetylcholinesterase (AChE, IC 50 = 2.42 ± 0.16 µg/mL) and butyrylcholinesterase (BChE, IC 50 = 20.87 ± 1.01 µg/mL) at 100 μg/mL, whereas IC 50 values of galanthamine used as the reference were 1.33 ± 0.11 µg/mL and 37.69 ± 2.93 µg/mL for AChE and BChE, respectively. Beside this, 8-hydroxy-9-methoxycrinine was a strong inhibitor of AChE (IC 50 = 6.92 ± 0.51 µg/mL), while (+)-9- O -demethylhomolycorine displayed a moderate BChE inhibition (IC 50 = 83.57 ± 1.36 µg/mL). Relevantly, 8-hydroxy-9-methoxycrinine and N -norgalanthamine were docked into active gorges of hAChE (PDB: 4EY6) and hBChE (PDB: 4TPK), which pointed out the detail that N -norgalanthamine displayed a very similar binding mode of to that of galanthamine. Moreover, both AChE-inhibiting alkaloids were found to stably bind to hAChE active site occupying the middle of the gorge between the catalytic site and the peripheral anionic site. 8-Hydroxy-9-methoxycrinine was also docked into the active site of BChE. We can conclude that among the tested alkaloids, N -norgalanthamine with dual ChE inhibitory effect seems to be the most promising anti-Alzheimer candidate molecule for future experiments. [ABSTRACT FROM AUTHOR]

COVID-19 caused by a new type of coronavirus (SARS-CoV-2) originated in China has speedily become a frightening pandemic all over the world. Despite of intense efforts relevant to experimental and clinical studies since the start of the COVID-19 pandemic, no disease-specific drug or vaccine is available, yet. Several treatment strategies including already known antiviral drugs, interpherons, interleukin inhibitors, and other drugs acting through different mechanims are being implemented in COVID-19 patients. On the other hand, natural products especially pythocompounds have been proven to be lead molecules for drug design and development research. Among them, curcumin as the main constituent of Curcuma longa L. (turmeric), is the reputed compound displaying remarkable biological activities for human health. It has been shown to have a inhibiting effect against a wide range of viruses such as HCV, HIV, PEDV, HSV, Ebola, dengue, influenza, Zika, SARS-CoV, etc. Therefore, curcumin could be considered as a structural model for designing new molecules against COVID-19. In the present review, antiviral activity of curcumin is scrutinized thorugh the literature data relevant to its enzyme and receptor interactions, in vitro, in vivo, in silico, and cell-based assays. [ABSTRACT FROM AUTHOR]

Berberine is an alkaloid with a wide range of reported beneficial health effects. The current work provides an extensive literature analysis on berberine. Bibliometric data were identified by means of the search string TOPIC=(“berberin*” OR “umbellatine*”), which yielded 5,547 publications indexed in the Web of Science Core Collection electronic database. The VOSviewer software generated bubble maps to visualize semantic terms with citation results. The ratio of original articles to reviews was 13.6:1. The literature has been growing more quickly since the 2010s. Major contributing countries were China, the United States, India, Japan, and South Korea. Most of the publications appeared in journals specialized in pharmacology pharmacy, biochemistry molecular biology, chemistry, and plant science. Some of the frequently mentioned chemicals/chemical classes were alkaloid, palmatine, jatrorrhizine, coptisine, isoquinoline, and sanguinarine. The prevalent medical conditions under investigation included Alzheimer’s disease, cancer, diabetes, and obesity. [ABSTRACT FROM AUTHOR]

Graphical abstract Highlights • 26 O-alkylcoumarins were synthesized and tested at 100 µM for their in vitro inhibitory potential against cholinesterases. • 12 of them exerted a potent and selective inhibition against BChE. • None of them possessed any potential to inhibit AChE. • MetaCore/MetaDrug analysis and docking simulations were applied the active compounds. Abstract Coumarins of synthetic or natural origins are an important chemical class exerting diverse pharmacological activities. In the present study, 26 novel O-alkylcoumarin derivatives were synthesized and have been tested at 100 µM for their in vitro inhibitory potential against acetylcholinesterase (AChE) and butyrlcholinesterase (BChE) targets which are the key enzymes playing role in the pathogenesis of Alzheimer's disease. Among the tested coumarins, none of them could inhibit AChE, whereas 12 of them exerted a marked and selective inhibition against BChE as compared to the reference (galanthamine, IC 50 = 46.58 ± 0.91 µM). In fact, 10 of the active coumarins showed higher inhibition (IC 50 = 7.01 ± 0.28 µM – 43.31 ± 3.63 µM) than that of galanthamine. The most active ones were revealed to be 7-styryloxycoumarin (IC 50 = 7.01 ± 0.28 µM) and 7-isopentenyloxy-4-methylcoumarin (IC 50 = 8.18 ± 0.74 µM). In addition to the in vitro tests, MetaCore/MetaDrug binary QSAR models and docking simulations were applied to evaluate the active compounds by ligand-based and target-driven approaches. The predicted pharmacokinetic profiles of the compounds suggested that the compounds reveal lipophilic character and permeate blood brain barrier (BBB) and the ADME models predict higher human serum protein binding percentages (>50%) for the compounds. The calculated docking scores indicated that the coumarins showing remarkable BChE inhibition possessed favorable free binding energies in interacting with the ligand-binding domain of the target. Therefore, our results disclose that O-alkylcoumarins are promising selective inhibitors of cholinesterase enzymes, particularly BChE in our case, which definitely deserve further studies. [ABSTRACT FROM AUTHOR]

Pteryxin is a dihydropyranocoumarin derivative found in Apiaceae family. In this study, pteryxin, which was previously isolated from the fruits of Mutellina purpurea , was investigated for its inhibitory potential against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), which are the key enzymes in the pathology of Alzheimer's disease (AD). The compound was tested in vitro using ELISA microplate reader at 100 μg/ml and found to cause 9.30 ± 1.86% and 91.62 ± 1.53% inhibition against AChE and BChE, respectively. According to our results, pteryxin (IC 50 = 12.96 ± 0.70 μg/ml) was found to be a more active inhibitor of BChE than galanthamine (IC 50 = 22.16 ± 0.91 μg/ml; 81.93± 2.52% of inhibition at 100 μg/ml). Further study on pteryxin using molecular docking experiments revealed different possible binding modes with both polar and hydrophobic interactions inside the binding pocket of BChE. Top docking solution points out to the formation of two hydrogen bonds with the catalytic residues S198 and H438 of BChE as well as a strong π - π stacking with W231. Therefore, pteryxin as a natural coumarin seems to be a strong BChE inhibitor, which could be considered as a lead compound to develop novel BChE inhibitors for AD treatment. [ABSTRACT FROM AUTHOR]

The article discusses a study which assessed the antioxidant potential of various extracts obtained from the leaf and fruit of Maclura pomifera, Schneider and its major isoflavonoids. Topics covered include findings which show the antioxidant capacity of iso-osajin, iso-pomiferin, and macluraxanthone, and indications that pomiferin is a natural possible antioxidant agent.

Context:Xeranthemum annuumL. (Asteraceae) (XA) is an ornamental and medicinal species with limited bioactivity and phytochemical data. Objective:Identification of anticholinesterase, antioxidant, anti-inflammatory and analgesic effects of the flower and root–stem (R-S) extracts of XA. Materials and methods:Anticholinesterase (at 100 μg mL−1) and antioxidant (at 1000 μg mL−1) effects of various extracts were evaluated via microtiter assays, while anti-inflammatory and analgesic effects of the R-S extracts were tested using carrageenan-induced hind paw oedema (100 and 200 mg kg−1) andp-benzoquinone (PBQ) writhing models (200 mg kg−1) in male Swiss albino mice. The R-S ethanol extract of XA was subjected to isolation studies using conventional chromatographic methods. Results:Most of the extracts showed inhibition over 85% against butyrylcholinesterase and no inhibition towards acetylcholinesterase. The flower chloroform and the R-S ethyl acetate extracts were most effective (97.85 ± 0.94% and 96.89 ± 1.09%, respectively). The R-S ethanol extract displayed a remarkable scavenging activity against DPPH (77.33 ± 1.99%) and in FRAP assay, while the hexane extract of the R-S parts possessed the highest metal-chelating capacity (72.79 ± 0.33%). The chloroform extract of the R-S caused a significant analgesic effect (24.4%) in PBQ writhing model. No anti-inflammatory effect was observed. Isolation of zierin and zierin xyloside, which were inactive in anticholinesterase assays, was achieved from the R-S ethanol extract. Discussion and conclusion:This is the first report of anticholinesterase, antioxidant, analgesic and anti-inflammatory activities and isolation of zierin and zierin xyloside from XA. Therefore, XA seems to contain antioxidant and BChE-inhibiting compounds. [ABSTRACT FROM AUTHOR]

Thymol (2-isopropyl-5-methylphenol) is the main monoterpene phenol occurring in essential oils isolated from plants belonging to the Lamiaceae family ( Thymus , Ocimum , Origanum, and Monarda genera), and other plants such as those belonging to the Verbenaceae, Scrophulariaceae, Ranunculaceae, and Apiaceae families. These essential oils are used in the food industry for their flavouring and preservative properties, in commercial mosquito repellent formulations for their natural repellent effect, in aromatherapy, and in traditional medicine for the treatment of headaches, coughs, and diarrhea. Many different activities of thymol such as antioxidant, anti-inflammatory, local anaesthetic, antinociceptive, cicatrizing, antiseptic, and especially antibacterial and antifungal properties have been shown. This review aims to critically evaluate the available literature regarding the antibacterial and antifungal effects of thymol. [ABSTRACT FROM AUTHOR]

The neurobiological activity of the methanol extracts of thirteen Umbelliferae (Apiaceae) plants was tested against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase (TYR) using a high-throughput screening technique. Although the extracts displayed no to a low inhibition profile against the enzymes, the highest cholinesterase inhibition was observed with Heracleum platytaenium (32.52±3.27 % for AChE and 46.16±1.42 % for BChE) at 100 μg mL-1. Since neurodegeneration is linked to oxidative damage, the antioxidant potential of the extracts were examined through radical scavenging, metal-chelating capacity, and reducing power experiments and they exerted modest levels of activity varying according to the method. The extracts had a better ability to scavenge the nitric oxide radical (19.47±2.09 to 54.91±1.98 %). Since these species are known to be rich in coumarins, quantitative high-performance liquid chromatography (HPLC) analysis indicated the presence of xanthotoxin, angelicin, isopimpinellin, bergapten, and pimpinellin in Heracleum platytaenium and angelicin and imperatorin in Angelica sylvestris var. sylvestris. [ABSTRACT FROM AUTHOR]

Randomly selected essential oils and some terpene and phenolic derivatives were evaluated for their ability to modulate human cellular immune responses using various inflammatory parameters including reactive oxygen species (ROS) generation from whole blood phagocytes and isolated polymorphonuclear neutrophils (PMNs), proliferation of T-cells, IL-2. and TNF-α cytokine production. The essential oils from Foeniculum vulgare , Saturea cuneifolia , and Origanum munitiflorum inhibited ROS produced from whole blood phagocytes, while thymol, carvacrol, rosmarinic acid, caffeic acid, quercetin, and kaempferol glycoside potently inhibited the ROS production from whole blood as well as from isolated PMNs, among which caffeic acid, quercetin, and kaempferol glycoside exhibited a better inhibitory effect than that of ibuprofen. The compounds rosmarinic acid, caffeic acid, quercetin, kaempferol glycoside, genistein, and apigenin (IC 50 7.0 ± 0.5, <3.12, <3.12, 4.3 ± 1.0, 5.8 ± 0.5, and <3.12 μg/mL) were found to exert potent inhibition on proliferation of T-cells. On the other hand, quercetin (IC 50 2.9 ± 0.3 μg/mL) and apigenin (IC 50 <1.0 μg/mL), were also found to be the potent inhibitor of IL-2 cytokine. The essential oils of Mentha species, and compounds quercetin and apigenin were found to potently inhibit the production of pro-inflammatory cytokine TNF-α. The results indicated that essential oils and phenolics might be considered as promising immunomodulatory agents. [ABSTRACT FROM AUTHOR]

Coumarins are widely distributed, plant-derived, 2 H -1-benzopyran-2-one derivatives which have attracted intense interest in recent years as a result of their diverse and potent pharmacological properties. Particularly, their effects on the central nervous system (CNS) have been established. The present review discusses the most important pharmacological effects of natural and synthetic coumarins on the CNS, including their interactions with benzodiazepine receptors, their dopaminergic and serotonergic affinity, and their ability to inhibit cholinesterases and monoamine oxidases. The structure-activity relationships pertaining to these effects are also discussed. This review posits that natural or synthetic coumarins have the potential for development in the therapy of psychiatric and neurodegenerative disorders, including Alzheimer’s and Parkinson’s diseases, schizophrenia, anxiety, epilepsy, and depression. [ABSTRACT FROM AUTHOR]

The extracts from 25 plant species from Salvia , Hypericum , Onosma , Thymus , Origanum , Rosa , and Prunus with eight isolated compounds were screened for their memory-vitalizing potential against the enzymes, i.e., acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase (TYR) along with DPPH, DMPD, and NO radicals and iron-chelation capacity using spectrophotometric microtiter assays. The n -hexane:dichloromethane (1:1) extract of Onosma nigricaule roots (63.18 ± 0.56%) and the ethyl acetate extract of the aerial parts of Hypericum capitatum var. capitatum (50.79 ± 3.88%) were the most active toward AChE and BChE, respectively. The highest iron-chelating capacity was found in the n -hexane extract of Thymus sipyleus subsp. sipyleus var. sipyleus , where mostly Labiatae species exhibited better radical scavenging effect. Among the extracts, the roots of O. nigricaule , the aerial parts of Hypericum capitatum var. capitatum and T . sipyleus subsp. sipyleus var. sipyleus could be further evaluated for their memory-vitalizing properties based on different mechanisms. [ABSTRACT FROM AUTHOR]

Hypericum perforatum L. (St. John's Wort) is a reputed plant with a long service to humankind. In the current study, antioxidant activity of the methanol extract of the aerial parts of H. perforatum growing in Turkey along with hyperoside and hyperforin was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, metal-chelation, and ferric-reducing antioxidant power (FRAP) assays. The major components including chlorogenic acid, the flavonoid derivatives; rutin, hyperoside, quercitrin, quercetin, and biapigenin, the naphthodianthrons; pseudohypericin and hypericin, and the phloroglucinol derivatives; hyperforin and adhyperforin were quantified in the extract by LC-DAD-MS. Hypericin (16 ± 0.08 μg/g) and hiperforin (1164 ± 0.02 μg/g) contents in H. perforatum were found to be in accordance with the amounts required by the European Pharmacopeia. The extract and hyperoside exerted a remarkable antioxidant activity in DPPH radical scavenging and FRAP assays, whereas they did not have metal-chelation capacity. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance The oil macerates of Hypericum perforatum L. (St. John׳s Wort=SJW) have a long history of medicinal use and SJW has been used in traditional medicine both orally and topically for centuries worldwide mainly for wound healing, ulcer and inflammation. Materials and methods We analyzed the fatty acid composition of 10 traditionally (home-made) and 13 commercially (ready-made) prepared SJW oil macerates by GC–MS. The acid, peroxide, iodine, saponification values, and the unsaponifiable matters of the samples were determined according to the European Pharmacopoeia. We also explored potential mechanism of wound healing effect of the samples, i.e. TNFα-induced NF-κB activation. Results The most home-made oil samples contained oleic acid predominantly and complied with the requirements set for olive oil by European Pharmacopoeia. However, majority of the ready-made samples appeared to have adulteration with some other oils. Moderate NF-κB inhibitory effects have been observed with some of the oil samples. Conclusion This study sheds light on the fact that application of the proper traditional method to prepare olive oil macerates from Hypericum perforatum is able to get bioactive constituents in the oil. Besides, inhibition of TNFα-induced NF-κB activation appears to be a potential mechanism for topical wound healing activity of SJW oil macerates. [ABSTRACT FROM AUTHOR]

Highlights: [•] In Sudan, people consume sorghum grain as fermented flat bread known as kisra. [•] Fermentation and baking increased the bioavailability of phenols in sorghum grains. [•] Kisra prepared from Tabat and Wad Ahmed cultivars showed effective DPPH and FRAP activity. [ABSTRACT FROM AUTHOR]

Ethnopharmacology has been an important starting point in medical and pharmaceutical sciences for discovering drug candidates from natural sources. In this regard, the genus Salvia L., commonly known as sage, is one of the best-known medicinal and aromatic plants of the Lamiaceae family; it has been recorded as being used for memory enhancement in European folk medicine. Despite the various uses of sage in folk medicines, the records that have pointed out sage's memory-enhancing properties have paved the way for the aforementioned effect to be proven on scientific grounds. There are many preclinical studies and excellent reviews referring to the favorable effect of different species of sage against the cognitive dysfunction that is related to Alzheimer's disease (AD). Hence, the current review discusses clinical studies that provide evidence for the effect of Salvia species on cognitive dysfunction. Clinical studies have shown that some Salvia species, i.e., hydroalcoholic extracts and essential oils of S. officinalis L. and S. lavandulaefolia leaves in particular, have been the most prominently effective species in patients with mild to moderate AD, and these species have shown positive effects on the memory of young and healthy people. However, the numbers of subjects in the studies were small, and standardized extracts were not used for the most part. Our review points out to the need for longer-term clinical studies with higher numbers of subjects being administered standardized sage preparations. [ABSTRACT FROM AUTHOR]

Abstract: In the current study, neuroprotective effect of the essential oil and aromatic waters of rose was investigated by in vitro and in silico methods. The samples were tested for their inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Since oxidative damage is associated with neurodegeneration, antioxidant activity of the samples was determined by DPPH radical scavenging, metal-chelation, and ferric-reducing antioxidant power (FRAP) assays. Their chemical composition was elucidated by GC–MS. Anti-cholinesterase effects of the main components (citronellol, geraniol, nerol, and phenylethyl alcohol) were also examined. The rose oil showed a noteworthy inhibition against AChE (60.86±1.99%) and BChE (51.08±1.70%) at 1000μg/mL and low activity in DPPH radical scavenging and FRAP tests. Phenylethyl alcohol exerted higher cholinesterase inhibition than other components and applied further to molecular docking simulations. Docking and binding energies supporting experimental results show that the compound is more selective towards BChE than AChE. [Copyright &y& Elsevier]

Abstract: Twenty-one samples of traditionally-prepared (home-made) and ready-made (commercial) St. John’s Wort olive oil macerates were profiled for their in vitro antimicrobial and antiprotozoal activity. Their cytotoxic potential was evaluated on MRC-5 fibroblasts. In the antiprotozoal assays, ten of the oils inhibited Trypanosoma brucei rhodesiense (IC50 15.9–64.5μg/mL), while only one oil exerted antimicrobial activity towards Staphylococcus aureus (IC50 =88.7μg/mL). LC–DAD–MS data revealed the presence of pseudohypericin (0.135–3.280μg/g) and hypericin (0.277–6.634μg/g) in all the oils, whereas chlorogenic acid (1.063μg/g) was detected only in one oil sample. Hyperforin was detected in four (0.977–2.399μg/g) and adhyperforin in six samples (0.005–3.165μg/g). Hypericin and pseudohypericin were common in the active oils, whereas hyperforin, adhyperforin, and chlorogenic acid were absent in these samples. Our results indicated that if the correct plant material is used, the infused oils from Hypericum perforatum may contain active components. [Copyright &y& Elsevier]

Highlights: [•] Enzyme inhibitory and antioxidant activity of Centella asiatica was investigated. [•] The extracts showed notable inhibition against butyrylcholinesterase and tyrosinase. [•] Phenolic acids of the extracts from Turkey and India were identified by HPLC. [•] Essential oil composition of the plant from Turkey was established. [•] This is the first study on Centella asiatica cultivated in Turkey [Copyright &y& Elsevier]

Abstract: In this study, cholinesterase inhibitory potential relevant to Alzheimer''s disease and antioxidant activities of the dichloromethane, ethyl acetate, and ethanol extracts from the aerial parts and/or roots of fourteen Salvia (sage) species (S. argentea, S. bracteata, S. caespitosa, S. cryptantha, S. glutinosa, S. indica, S. microstegia, S. multicaulis, S. pinnata, S. quezelii, S. syriaca, S. tobeyi, S. verticillata subsp. amasiaca, and S. viscosa) were investigated. Cholinesterase inhibition was determined by Ellman method at 25, 50, and 100μgml−1. Their antioxidant activity was assessed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, metal-chelation capacity, and ferric-reducing antioxidant power (FRAP) assays. Total phenol and flavonoid contents of the extracts were also determined. The dichloromethane and ethanol extracts of the aerial parts of S. cryptantha were the most active ones against AChE (56.22±1.07%) and BChE (33.80±4.18%), respectively. The ethanol extracts exhibited better scavenging activity and FRAP. Anticholinesterase activity of 9 Salvia species (S. argentea, S. bracteata, S. caespitosa, S. indica, S. pinnata, S. quezelii, S. syriaca, S. tobeyi, and S. viscosa) is reported for the first time in the current study. [Copyright &y& Elsevier]

Abstract: The petroleum ether, chloroform, ethyl acetate, and methanol extracts of the aerial parts of Buxus sempervirens growing naturally in Turkey were investigated against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) as well as tyrosinase (TYRO) enzymes for their inhibitory activity using ELISA microplate reader. Antiprotozoal activity of the extracts was tested against the parasites; Plasmodium falciparum (malaria) and Trypanosoma brucei rhodesiense (human African trypanosomiasis) at 0.81 and 4.85μg/mL concentrations. As antioxidant activity contributes to antimalarial activity, the extracts were also tested for their 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, iron-chelating capacity, and ferric-reducing antioxidant power (FRAP). Total phenol and flavonoid contents in the extracts were determined spectrophotometrically. The alkaloid fraction of the chloroform extract afforded two major alkaloids named (+)-buxabenzamidienine (1) and (+)-buxamidine (2). Our results showed that, except for the petroleum ether extract, the extracts displayed high antimalarial and anti-BChE effects as well as quite high iron-chelation capacity. Therefore, we suggest that the active extracts in the antimalarial tests might be showing their effects through the mechanism of BChE inhibition and additionally iron-chelation ability. [Copyright &y& Elsevier]

The extracts of various marine sponges (Agelas oroides and Axinella damicornis, Axinella cannabina, Ircinia spinulosa, I. fasciculata, and I. variabilis, Dysidea avara, and Sarcotragus spinulosus) collected from different spots of the Turkish cost of the Mediterranean Sea have been evaluated for their antibacterial, antifungal, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, and acetylcholinesterase (AChE) inhibitory activities. Three compounds (oroidin, 4,5-dibromopyrrol-2-carboxylic acid, and 25-hydroxy-24-methylcholesterol) were isolated from A. oroides and tested in the same manner. The sponge extracts showed notable antimicrobial and anti-AChE activity and low DPPH scavenging activity. Oroidin was found to have moderate anti-AChE and strong radical scavenging activities. The results demonstrated that the sponge extracts exerted a variable degree of antibacterial, anti-radical, and anti-AChE activity, whereas they seemed to have similar antifungal effect. Our findings point out to the fact that the collection site has an important influence on bioactivity of the sponges. [ABSTRACT FROM AUTHOR]

In this study, antibacterial, antifungal, insecticidal and genotoxic activities of the fruit and leaf extracts of Melia azedarach of Turkish origin were evaluated for the first time. The antimicrobial activity was assessed against Gram (+) and ( − ) bacteria, four Candida species and three dermatophytic fungus ( Trichophyton rubrum, Epidermophyton floccosum and Microsporum gypseum). The insecticidal activity of the methanolic fruit extract was performed against the larvae of Aedes aegpyti, Culex pipiens and Culex quinquefasciatus. The genotoxicity of this extract was evaluated against Drosophila melanogaster by somatic mutation and recombination test. The extracts showed higher antibacterial effect against Gram ( − ) strains (16-32 μg ml− 1 of minimal inhibition concentration, MIC), while the leaf extracts were more effective on Candida albicans (32 μg ml− 1 of MIC). The extracts did not exhibit insecticidal activity and genotoxicity. Total phenol and flavonoid contents of the extracts were determined spectrophotometrically, and the ethyl acetate extract of the leaves was the richest in total flavonoids. [ABSTRACT FROM AUTHOR]

Abstract: The ethyl acetate and methanol extracts from 16 Salvia L. species were screened for their inhibitory activity against acetylcholinesterase, butyrylcholinesterase, lipoxygenase, and tyrosinase; the enzymes linked to neurodegeneration. Their antioxidant activity was also tested using DPPH radical scavenging, metal-chelation, and ferric-reducing antioxidant power (FRAP) assays. Total flavonoid content of the extracts was determined by AlCl3 reagent, while HPLC technique was applied for analysis of various phenolic acids in the extracts. The extracts exerted weak cholinesterase and tyrosinase inhibition, and remarkable inhibition against lipoxygenase (13.07±2.73–74.21±5.61%) at 100μgml−1. The methanol extracts showed higher antioxidant activity in DPPH radical scavenging and FRAP assays. The extracts were analyzed for their gallic, protocateuchic, p-hydroxy-benzoic, vanillic, caffeic, chlorogenic, syringic, o- and p-coumaric, ferulic, rosmarinic, and tr-cinnamic acid contents and the methanol extract of Salvia ekimiana (153.50mg100g−1) was revealed to be the richest in terms of rosmarinic acid. [Copyright &y& Elsevier]

Abstract: In the current study, the n-hexane, chloroform, ethyl acetate, water, and n-butanol fractions obtained from the main ethanol extract of Cistus laurifolius L. were evaluated for their cholinesterase inhibitory effects against acetyl- (AChE) and butyrylcholinesterase (BChE), at 50, 100, and 200μg/ml, using an ELISA microplate reader. The antioxidative effect of the extract and fractions was also determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, ferrous ion-chelation capacity, and ferric-reducing antioxidant power (FRAP) test systems. Total phenol and flavonoid contents of the extract and fractions were calculated using Folin-Ciocalteau and aluminium chloride reagents. Three flavonoid derivatives; 3-O-methylquercetin (1), 3,7-O-dimethylquercetin (2), and 3,7-O-dimethylkaempferol (3) isolated from the CHCl3 fraction were also tested in the same manner. Our experimental findings indicated that the ethanol extract exerted the highest AChE inhibition (80.07±1.06% at 200μg/ml). The ethyl acetate and n-butanol fractions displayed the best activity against DPPH and FRAP assays. [Copyright &y& Elsevier]

Abstract: In the current study, neuroprotective effects of the ethyl acetate and methanol extracts of four terebinth coffee brands and the fruits of Pistacia terebinthus L. were investigated through enzyme inhibition tests against acetylcholinesterase, butyrylcholinesterase, and tyrosinase as well as antioxidant test systems. Antioxidant activity was measured using radical scavenging activity tests and metal-related tests including metal-chelation capacity, ferric-reducing antioxidant power (FRAP), and phosphomolybdenum reducing power (PRAP). The fatty oils of the coffee brands and the fruits and the fruit essential oil were examined by GC–MS. Total phenol and flavonoid contents were calculated spectrophotometrically. The extracts had moderate inhibition against butyrylcholinesterase (9.78–45.74% at 200μgmL−1) and potent scavenging activity against DPPH. They exerted strong activity in FRAP and metal-chelation tests and modest activity in PRAP test. Oleic acid was identified as the major fatty acid in the fatty oils, while α-pinene (26.31%) was dominant in the essential oil. [Copyright &y& Elsevier]

This paper covers the studies relevant to neuroprotective activity of Centella asiatica (L.) Urban, also known as "Gotu Kola." The plant is native to the Southeast Asia and has been used traditionally as brain tonic in ayurvedic medicine. The neuroprotective effect of C. asiatica has been searched using the key words "Centella, Centella asiatica, gotu kola, Asiatic pennywort, neuroprotection, and memory" through the electronic databases including Sciencedirect, Web of Science, Scopus, Pubmed, and Google Scholar. According to the literature survey, C. asiatica (gotu kola) has been reported to have a comprehensive neuroprotection by different modes of action such as enzyme inhibition, prevention of amyloid plaque formation in Alzheimer's disease, dopamine neurotoxicity in Parkinson's disease, and decreasing oxidative stress. Therefore, C. asiatica could be suggested to be a desired phytopharmaceutical with neuroprotective effect emerged from traditional medicine. [ABSTRACT FROM AUTHOR]

Several extracts of the leaves and fruits of Juglans regia L. were assessed for their neuroprotective effects through antioxidant and anti-cholinesterase methods. Anticholinesterase activity was determined against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the enzymes vital for Alzheimer's disease, at 50, 100 and 200 μg ml− 1. Antioxidant activity was tested using radical scavenging activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH), N, N-dimethyl- p-phenylenediamine (DMPD), superoxide (SO), nitric oxide (NO) and hydrogen peroxide (H2O2) radicals, as well as ferric ion-chelating capacity, ferric- and phosphomolybdenum-reducing antioxidant power at 500, 1000 and 2000 μg ml− 1. Total phenol and flavonoid quantification of the extracts was calculated. The extracts scavenged DPPH radical in varying degrees; however, they did not scavenge DPMD and H2O2. Only the dichloromethane and water extracts were able to quench SO (10.09 ± 1.38%) and NO (24.09 ± 2.19%) radicals, respectively, at low level. The extracts showed either low or no BChE inhibition and no AChE inhibition. [ABSTRACT FROM AUTHOR]

In the current study, in vitro inhibitory activity of several essential oils obtained from the cultivated plants, Foeniculum vulgare, Mentha piperita and M. spicata, Ocimum basilicum, Origanum majorana, O. onites, O. vulgare, Satureja cuneifolia, and a number of individual essential oil components of terpene and aromatic types were screened against 10 isolated strains of Klebsiella pneumoniae producing extended-spectrum beta-lactamase (ESBL) enzyme, which makes this microorganism quite resistant against the antibiotics: trimetoprime-sulfametoksazol, sulbactam-ampicilin, clavulonate-amoxicilin, ceftriaxon, cefepime, imipenem, ceftazidime, tobramicine, gentamisine, ofloxacin, and ciprofloksasin. All of the essential oils and the components exerted a remarkable inhibition ranging between 32 and 64 μg/mL against all of these strains as strong as the references (ampicilin and oflaxocin) inhibiting at 32 μg/mL. Besides, chemical compositions of the essential oils were elucidated by gas chromatography-mass spectrometry (GC-MS). The essential oils and the pure components widely found in essential oils screened herein have shown remarkable inhibition against ESBL-producing K. pneumoniae strains, which leads to the suggestion that they may be used as food preservatives for this purpose. Practical Application: The essential oils obtained from Foeniculum vulgare, Mentha piperita and M. spicata, O.cimum basilicum, Origanum majorana, O. onites, O. vulgare, and Satureja cuneifolia as well as common essential oil components have shown notable inhibitory effects against 10 isolated strains of Klebsiella pneumoniae producing extended-spectrum beta-lactamase (ESBL) enzyme and they might be used as food preservative or ingredient. [ABSTRACT FROM AUTHOR]

Abstract: In vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory and antioxidant activities of the aqueous and ethanol extracts of the leaves, ripe fruits, and unripe fruits of Juniperus communis ssp. nana, Juniperus oxycedrus ssp. oxycedrus, Juniperus sabina, Juniperus foetidissima, and Juniperus excelsa were investigated in the present study. Cholinesterase inhibition of the extracts was screened using ELISA microplate reader. Antioxidant activity of the extracts was tested by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radical scavenging, ferrous ion-chelating, and ferric-reducing antioxidant power (FRAP) assays. Total phenol and flavonoid contents of the extracts were determined spectrophotometrically. The extracts had low or no inhibition towards AChE, whereas the leaf aqueous extract of J. foetidissima showed the highest BChE inhibition (93.94±0.01%). The leaf extracts usually exerted higher antioxidant activity. We herein describe the first study on anticholinesterase and antioxidant activity by the methods of ferrous ion-chelating, superoxide radical scavenging, and ferric-reducing antioxidant power (FRAP) assays of the mentioned Juniperus species. [Copyright &y& Elsevier]

In the current study, we examined anti-acetylcholinesterase (AChE) and antioxidant activities of the ethyl acetate, methanol, and water extracts from the bulbs of Turkish Sternbergia Waldst. & Kit. (Amaryllidaceae) species; S. candida, S. clusiana, S. fisheriana, S. lutea subsp. lutea, and S. lutea subsp. sicula. Anti-AChE activity was tested by spectrophotometric method of Ellman using ELISA microplate reader at 50, 100, and 200 µg mL-1 concentrations. Antioxidant activity of the extracts was evaluated by DPPH radical scavenging activity, ferrous ion-chelating capacity, ferric-reducing antioxidant power, and beta-carotene bleaching assays at 500, 1000, and 2000 µg mL-1. Total phenol and flavonoid contents of the extracts were determined via Folin-Ciocalteau's and AlCl3 reagents, respectively. The ethyl acetate extract of S. fischeriana was the most active in anti-AChE assay (90.94% and 98.02% of inhibitions at 100 and 200 µg mL-1 concentrations, respectively. Antioxidant activity of the extracts was found to be not significant. [ABSTRACT FROM AUTHOR]

Abstract: Dichloromethane, ethyl acetate, acetone, methanol, and water extracts prepared from the fruits and leaves of Laurocerasus officinalis Roem. (LO) (Rosaceae) were screened for their cholinesterase inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the key enzymes in pathogenesis of Alzheimer''s disease (AD), using ELISA microplate reader at 50, 100, and 200μgmL−1. As AD is associated with oxidative stress, the antioxidant activity of the extracts was also tested by radical-forming methods against 2,2-diphenyl-1-picrylhydrazyl (DPPH), N,N-dimethyl-p-phenylendiamine (DMPD), and superoxide radicals as well as iron-related methods; iron-chelating capacity and ferric-reducing antioxidant power (FRAP) assays. Total phenol and flavonoid quantification was achieved using Folin–Ciocalteau and AlCl3 reagents, respectively. The highest AChE (44.01±1.75%) and BChE (19.91±0.37%) inhibition was caused by the LO-leaf-methanol extract 200μgmL−1, while it showed the best radical-scavenging activity against DPPH at 2000μgmL−1. Only, the dichloromethane and water extracts of the fruits and the leaf water extract had an iron-chelating capacity, while the leaf methanol extract displayed the highest FRAP. The leaf methanol extract (113.45±0.71mgg−1 extract) was found to be the richest in total phenols, while the leaf acetone extract (139.90±4.64mgg−1 extract) had the most abundant amount of total flavonoids. [Copyright &y& Elsevier]

The EtOH extracts of the leaves of two new cultivars (Uysal-SFU and Turgut-SFT) of Salvia fruticosa Mill. was tested against acetylcholinesterase (IC50: 30.62 ± 3.27 and 32.97 ± 2.33 µg/mL for SFU and SFT, respectively) and butyrylcholinesterase (IC50: 69.91 ± 1.08 µg/mL and 86.55 ± 1.26 µg/mL), respectively, relevant to Alzheimer's disease. The essential oils showed a stumpy inhibition against AChE and no inhibition against BChE. DPPH radical scavenging activity of the extracts (86.70 ± 0.17% and 86.14 ± 1.13% for SFU and SFT, respectively) was stronger than that of quercetin (85.51 ± 0.17%): Their (1.24 ± 0.05 and 1.04 ± 0.16 for SFU and SFT, respectively) ferric-reducing antioxidant power were close to that of the reference (e.g. quercetin, 1.42 ± 0.14). Molecular docking simulations were performed on their major monoterpenes. Our findings revealed that the leaf EtOH extracts of two cultivars are promising inhibitors of both AChE and BChE. [ABSTRACT FROM AUTHOR]

• There is a complex interplay between gut microbiota, nervous and immune system. • This relationship leads to introduce the concept of the gut-brain-immune axis. • Evidence reported the role of polyphenols in modulating the gut-brain-immune axis. • Polyphenols may be effective in management of gut-brain-immune axis-related diseases. Neurodegenerative disorders, particularly in the elderly population, represent one of the most pressing social and health-care problems in the world. Besides the well-established role of both oxidative stress and inflammation, alterations of the immune response have been found to be closely linked to the development of neurodegenerative diseases. Interestingly, various scientific evidence reported that an altered gut microbiota composition may contribute to the development of neuroinflammatory disorders. This leads to the proposal of the concept of the gut-brain-immune axis. In this scenario, polyphenols play a pivotal role due to their ability to exert neuroprotective, immunomodulatory and microbiota-remodeling activities. In the present review, we summarized the available literature to provide a scientific evidence regarding this neuroprotective and immunomodulatory effects and the interaction with gut microbiota of polyphenols and, the main signaling pathways involved that can explain their potential therapeutic application in neurodegenerative diseases. [ABSTRACT FROM AUTHOR]

Natural products are always important in finding new drug candidates and natural product chemistry research has been a mainstay in drug discovery and development. Enzyme inhibitors are known as one of the strongest therapy strategies against a wide range of diseases. In other words, enzyme inhibitors are one of the vital classes of drugs clinically available. In search novel enzyme inhibitors from natural sources being mostly plants, we have been screening many medicinal plants and pure natural compounds using microplate assays against a number of enzymes including cholinesterase family, elastase, collagenase, tyrosinase, xanthine oxidase, phosphodiesterase-I, carbonic anhydrase-II, lipoxygenase, HMG CoA reductase, etc. Since some of these enzymes are related to cosmetics, we have been also studying developing new formulations for anti-aging cosmetics. The active inhibitors found by our group are further investigated by in silico methods using molecular docking experiments. During these studies, we found many promising compounds such as coumarins and other polyphenolics such as flavonoids have been identified as active inhibitors through our results. In this study, examples of natural products as promising inhibitors determined by our group against different enzymes will be underlined. [ABSTRACT FROM AUTHOR]

Pharmacognosy deals with the natural drugs obtained from organisms such as most plants, microbes, and animals. Up to date, many important drugs including morphine, atropine, galanthamine, etc. have originated from natural sources which continue to be good model molecules in drug discovery. Traditional medicine is also a part of pharmacognosy and most of the third world countries still depend on the use of herbal medicines. Consequently, pharmacognosy always keeps its popularity in pharmaceutical sciences and plays a critical role in drug discovery. [ABSTRACT FROM AUTHOR]

Abstract Background Allicin is an organosulfur and defensive compound found in garlic (Allium sativum L.) and other Allium species. Its unique odor is easily detectable, and its effects on human health have been studied since ancient times. Scope and approach In this compressive review we report the presence of allicin in different Allium species, their biosynthesis, pharmacokinetics, absorption, and safety profile. Among the main allicin applications highlight its antimicrobial and antiparasitic properties, reviewed in the present work from in vitro evidence and in vivo studies. Finally, special attention was also given to the allicin state of the art in human health, including in vitro and in vivo assays, and clinical trials, on antioxidant, anticancer, antidiabetic and immunomodulatory effects, besides to its contribution as a cardioprotective agent. Key findings and conclusions The promising capacity of allicin to interact with thiol groups seems to be directly related to its antimicrobial potential, showing both antibacterial and antifungal activities. Allicin also displayed an interesting potential in the prevention and treatment of several diseases including diabetes mellitus, cardiovascular disease, and cancer. Indeed, its antioxidant and immunomodulatory effects are some of the mechanisms that may explain their biological activities. Future applications should be directed to allicin pharmaceutical formulation, its delivery and its compatibility with food matrices and other drugs due to allicin biosynthesis, instability, reactivity, and volatility. Highlights • Allicin is an organosulfur compound mainly found in garlic. • Allicin has antimicrobial, nematocidal and anthelmintic activity. • Its effects are due its antioxidant and immunomodulatory activities. • Allicin is a promising therapeutic compound. • Its instability requires future research on pharmaceutical formulations. [ABSTRACT FROM AUTHOR]

An introduction is presented in which the authors discuss several reports in the issue on topics including neurological activity of traditional Chinese medicine against diabetic peripheral neuropathy, neuroprotective effect of a Chinese medicine, and spinal cord injuries.

Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione) is a is an important consituitents present in Curcuma longa L. (turmeric) rhizome. It is also a lipophilic molecule that rapidly permeates cell membrane. Curcumin has been used as pharmacological traditional medicinal agent in Ayurvedic medicine for ∼6000 years. Being chemopreventive agent, curcumin has been found to modulate multiple molecular pathways through several mechanisms, e.g. induction of apoptosis, inhibition survival signals, and prevention from reactive oxidative species (ROS). Curcumin significantly caused reduction in lung cancer stem cells markers (CD133, ALDHA1, CD44, Nanog, and Oct4) and the number of CD133-positive cells as well as efficiently decreased the tumorsphere formation, inhibited proliferation, and induced apoptotic cell death. It also suppressed the activation of both Wnt/β-catenin and Sonic Hedgehog pathways. Curcumin has been also reported to diminish renal hypertrophy, reduce mesangial matrix expansion, and cause a lower level of albuminuria. It also inhibited the upregulated protein and mRNA expressions of collagen IV and fibronectin in the renal cortices as well as significantly reduced the mature interleukin-1 β , cleaved caspase-1, and NLRP3 protein levels in the renal cortices of db/db mice as well as in HK-2 cells. It also ameliorated the defective insulin signalling pathway by upregulating insulin-like growth factor (IGF)-1R, IRS-2, PI3K, p-PI3K, Akt and p-Akt protein expression while downregulating IR and IRS-1. Besides, curcumin lowered the heart MDA and DNA fragmentation levels, increased concentration of SOD, catalase, and gluathione levels, decreased the percentage of TUNEL-positive cells and γH2AX protein expression, while it lowered the percentage (%) of capspase 3 positive cells and improved the percentage of Bcl-2 positive cells. The current review article presents effective role of curcumin against cancer, diabetes, oxidative stress, cardiovascular, obesity, and aging. [ABSTRACT FROM AUTHOR]

The popularity of herbal medicines and dietary supplements is increasing all over the world due to the many side-effects assigned to synthetic drugs. Herbal remedies should be considered as safe, with no side-effects, but unfortunately, even if they are labelled as natural, large numbers of adulterants, not only with toxic heavy metals but also with undeclared synthetic substances, have been detected up to date. In this review, the most frequent instances of adulteration of herbal medicines and dietary supplements acting as sexual enhancers and slimming products are thoroughly discussed. The great success of synthetic phosphodiesterase type-5 (PDE-5) inhibitory drugs like sildenafil, vardenafil and tadalafil, used for the treatment of erectile dysfunction has made them, as well as their unapproved analogues, popular as adulterants in herbal dietary supplements. The second group among blockbuster products are herbal preparations for slimming purpose, as obesity and gaining weight are major problems worldwide. Here, sibutramine hydrochloride monohydrate, an anti-obesity drug which inhibits serotonergic and noradrenergic reuptake, seems to be the most common adulterant. Together with large numbers of its analogues, thyroid hormones, anorexigens, diuretics, stimulants, and laxative agents are also detected in most of tested diet supplements. [ABSTRACT FROM AUTHOR]

Plant tannins are a unique class of polyphenols with relatively high molecular weights. Within the ellagitannins group, agrimoniin--dimeric ellagitannin--is one of the most representative compounds found in many plant materials belonging to the Rosaceae family. Agrimoniin was first isolated in 1982 from roots of Agrimonia pilosa Ledeb. (Rosaceae), a plant traditionally used in Japan and China as an antidiarrheal, hemostatic, and antiparasitic agent. Agrimoniin is a constituent of medicinal plants, which are often applied orally in the form of infusions, decoctions, or tinctures. It is also present in commonly consumed food products, such as strawberries and raspberries. It is metabolized by human gut microbiota into a series of low-molecular-weight urolithins with proven anti-inflammatory and anticancer in vivo and in vitro bioactivities. The compound has received widespread interest owing to some interesting biological effects and therapeutic activities, which we elaborate in the present review. Additionally, we present an overview of the techniques used for the analysis, isolation, and separation of agrimoniin from the practical perspective. [ABSTRACT FROM AUTHOR]

Based on our continuous effort to investigate chemistry and biology of the plant secondary metabolites, we were able to isolate a glycosidal flavonoid 1 from the Wild Egyptian Artichoke. The activity of dihydromyricetin 3-O-rhamnoside (sin. dihydromyricitrin, ampelopsin 3-O-rhamnoside) (1) against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE); its absolute configuration using X-ray crystallography were determined for the first time. Inhibitory activity of 1 against AChE and BChE enzymes were determined using a slightly modified version of Ellman's method. Compound 1 was revealed to have a potent inhibition against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 0.070 ± 0.008 and 0.071 ± 0.004 mM, respectively, where IC50 values of the reference drug (galanthamine) were 0.023 ± 0.15 and 0.047 ± 0.91 mM. Compound 1 could be a promising molecule against Alzheimer's disease. [ABSTRACT FROM AUTHOR]

The use of Thymus species amongst the public and their importance in the scientific world is increasing day by day. In addition to being consumed as tea and spice, Thymus species are used as folk medicine for respiratory, digestive, skin, circulatory, genital, nervous, visual and urinary diseases. In this study, it was aimed to examine the essential oil and ethanol extract of the root and aerial parts of Thymus pubescens Boiss. et Kotschy ex Celak in the terms of their biological activity and chemical content. The phenolic content of the species was determined by LC-MS/MS, while triterpenoid content, the chemical composition of the essential oil as well as flavour was determined by GC–MS. In addition, their antioxidant and cytotoxic activities, as well as acetyl- (AChE) and butyrylcholinesterase (BChE), urease, tyrosinase, elastase, collagenase, HMG-CoA reductase and angiotensin-converting enzyme (ACE) inhibitory activities were studied. Thymol (53.33%) was determined as the major component in the essential oil, while β-fenchyl alcohol (43.87%) was determined as the major component of the flavour. According to the LC-MS/MS and GC–MS results, it was found that especially the aerial parts of the species have a high amount of rosmarinic acid (3875.76 µg analyte/g extract), quinic acid (2392.55), naringenin (970.39), oleanolic (92785.96) and ursolic (63373.32) acids. The essential oil of T. pubescens species was observed to show high activity in four antioxidant assays, e.g. inhibition of lipid peroxidation, DPPH and ABTS radical scavenging activity as well as CUPRAC, while the ethanol extracts showed moderate antioxidant activity. In enzyme inhibition assays, the aerial parts exerted marked BChE, elastase, and collagenase inhibitory activities (92.43±1.28%, 42.59±0.56, and 48.61±0.39 at 100 µg/mL, respectively). On the other hand, AChE, urease, tyrosinase, HMG-CoA reductase and ACE inhibitory activities of all extracts were from low to moderate levels. In particular, the aerial parts of the species displayed a high cytotoxic effect (vitality%: 6.82±0.01 at 200 µg/mL) in breast cancer (MCF-7) cell line. Due to its remarkable antioxidant capacity, high content of rosmarinic, oleanolic, and ursolic acids and especially BChE, elastase, and collagenase inhibitory activity, T. pubescens has the potential for using in food supplements, food preservatives, cosmetics, and pharmaceutical industries. [Display omitted] • The phenolic, triterpenoid and essential oil composition of Thymus pubescens determined by LC-MS/MS and GC–MS. • The high potential of butyryl-cholinesterase, elastase, and collagenase inhibitory activities. • High ursolic acid and thymol content of Thymus pubescens. [ABSTRACT FROM AUTHOR]

Medicinal and edible plants play a crucial role in the prevention and/or mitigation of different human diseases from ancient times to today. In folk medicine, there are different plants used for infectious disease treatment. During the past two decades, much attention has been paid to plants as novel alternative therapeutic agents for the treatment of infectious diseases due to their bioactive natural compounds such as phenol, flavonoids, tannins, etc. The genus Eryngium (Apiaceae) contains more than 250 flowering plant species, which are commonly used as edible and medicinal plants in different countries. In fact, some genus Eryngium species are used as spices and are cultivated throughout the world and others species are used for the treatment of hypertension, gastrointestinal problems, asthma, burns, fevers, diarrhea, malaria, etc. Phytochemical analysis has shown that genus Eryngium species are a rich source of flavonoids, tannins, saponins, and triterpenoids. Moreover, eryngial, one the most important and major compounds of genus Eryngium plant essential oil, possesses a significant antibacterial effect. Thus, the objective of this review is to critically review the scientific literature on the phytochemical composition and antibacterial effects of the genus Eryngium plants. In addition, we provide some information about traditional uses, cultivation, as well as phytochemistry. [ABSTRACT FROM AUTHOR]

Phenylethanoid glycosides are naturally occurring water-soluble compounds with remarkable biological properties that are widely distributed in the plant kingdom. Verbascoside is a phenylethanoid glycoside that was first isolated from mullein but is also found in several other plant species. It has also been produced by in vitro plant culture systems, including genetically transformed roots (so-called ‘hairy roots’). Verbascoside is hydrophilic in nature and possesses pharmacologically beneficial activities for human health, including antioxidant, anti-inflammatory and antineoplastic properties in addition to numerous wound-healing and neuroprotective properties. Recent advances with regard to the distribution, (bio)synthesis and bioproduction of verbascoside are summarised in this review. We also discuss its prominent pharmacological properties and outline future perspectives for its potential application. [ABSTRACT FROM AUTHOR]

Highlights: [•] Neurodegeneration-related enzyme inhibitory effects of Viburnum tinus was tested. [•] Antioxidant activity of the plant was tested in seven in vitro assays. [•] The branch–ethyl acetate and fruit–methanol extract had significant anticholinesterase effect. [•] Tyrosinase inhibitory activity of V. tinus was examined for the first time. [•] This is the first study on cholinesterase inhibition of V. tinus. [ABSTRACT FROM AUTHOR]