Anti-acetylcholinesterase Activity Research Articles

LC-MS/MS Profiling, Biological Activities and Molecular Docking Studies of Simmondsia Chinensis Leaves.

This study aimed to assess the biological activities of Tunisian Simmondsia chinensis and characterize its potential bioactive compounds. Different extracts of S. chinensis were tested for their antioxidant, antibacterial, anti-α-amylase, and anti-acetylcholinesterase activities through in vitro assays. The methanolic extract exhibited the highest levels of antioxidant activity and total phenolic content (976.03 GAE/g extract) compared to the other extracts. Additionally, it demonstrated a substantial anti-acetylcholinesterase activity (PI=75 %) and potent antibacterial property, particularly against Enterococcus faecalis, Listeria monocytogenes, Bacillus cereus, Bacillus subtilis, and Salmonella enterica. The IC50 values of ethyl acetate and methanolic extracts against α-amylase were 42 μg/mL and 40 μg/mL, respectively, indicating potent anti-diabetic effects. HPLC-ESI-MS/MS analyses identified flavonoids and lignans as the major phenolic compounds in the methanolic extract. To better comprehend the mechanisms behind inhibitory effects on α-amylase and acetylcholinesterase enzymes, a molecular docking study was conducted. Consequently, these findings indicate that S. chinensis is a highly valuable natural resource with potential industrial applications.

Multiple NADPH-cytochrome P450 reductases from Lycoris radiata involved in Amaryllidaceae alkaloids biosynthesis.

Amaryllidaceae alkaloids (AAs), such as galanthamine and lycorine, are natural products of Lycoris radiata possessing various pharmacological activities including anti-acetylcholinesterase, anti-inflammatory, and antitumour activities. Elucidating the biosynthesis of these special AAs is crucial for understanding their production and potential modification for improved clinical application, of which cytochrome P450 enzymes catalyse the formation of key alkaloid skeletons and subsequent modification processes, with the NAPDH cytochrome P450 reductases (CPRs) serving as essential redox partners. This study identified three CPRs, LrCPR1, LrCPR2, and LrCPR3, encoding 700, 697 and 695 amino acids, respectively, which belong to Class II CPRs. The LrCPRs reduced cytochrome c and ferricyanide in an NADPH-dependent manner, and their activities all followed the typical Michaelis-Menten curve. In yeast, the co-expression of LrCPRs and CYP96T6 produced the galantamine-like alkaloid namely N-demethylnarwedine, suggesting that they support the catalytic activity of CYP96T6. Quantitative analysis of the transcriptional expression profiles showed that LrCPRs were expressed in all the examined tissues of L. radiata, and their gene expression patterns are consistent with other genes that may be involved in the biosynthetic pathway of AAs, including cinnamate 4-hydroxylase and phenylalanine ammonia-lyase. Our study firstly provides the functional characterization of LrCPRs in L. radiata, which will contribute to the discovery of biosynthetic pathways and heterologous production of AAs.

Investigation of the chemical composition and biological activities of Eremurus spectabilis M. Bieb through antioxidant, enzyme inhibition, COX-2 and iNOS assessment.

Eremurus spectabilis is widespread and used primarily for medicinal and culinary purposes. This study aimed to evaluate the chemical composition, antiradical and antioxidant activities, enzyme inhibitory activities, and anti-inflammatory properties of various extracts from the aerial parts of E. spectabilis. Various assays were used to investigate the antioxidant and enzyme inhibitory properties. The chemical composition of the tested extracts was analyzed using High-Performance Liquid Chromatography-Electrospray Ionization Tandem Mass Spectrometry (HPLC-ESI-MS/MS). Additionally, the extracts were tested on isolated mouse colon tissue challenged with E. coli lipopolysaccharide (LPS) to replicate the inflammation and oxidative stress burden characteristic of inflammatory bowel diseases. In the chemical composition, vanillic, ferulic, 4-hydroxybenzoic acids were the prominent compounds. The greatest antioxidant activity was observed in the methanol and water extracts from the aerial parts. Enzyme inhibition tests showed that the ethyl acetate extract had the highest anti-acetylcholinesterase activity. The gene expression of pro-inflammatory cyclooxygenase-2 (COX-2) and pro-oxidant inducible nitric oxide synthase (iNOS) biomarkers were assayed. Among the extracts, the methanol extract was the most effective in blunting LPS-induced gene expression of COX-2. E. spectabilis may serve as a valuable source of phytochemicals for combating oxidative stress and inflammation-driven diseases, with a particular emphasis on colon inflammatory condition.

Antimicrobial and anti-acetylcholinesterase activities of secondary metabolites isolated from Aspergillus fumigatus MNY-14

A systematic investigation of the secondary metabolites of Aspergillus fumigatus MNY-14, which was isolated from the ripe leaves of Achyranthes longifolia, led to the isolation of eighteen compounds, including twelve indole diketopiperazine alkaloids (1–12), an α-pyrone meroterpenoid (13), a nortriterpenoid (14), two benzophenones (15–16), and two quinoline alkaloids (17–18). Among them, compounds 8, 17 and 18 were isolated for the first time from A. fumigatus. The chemotaxonomic significance of the secondary metabolites was discussed. Some of the isolates (6, 10, 11, 10, 15 and 16) could be used as chemical markers for strain identification of this fungus. In addition, some of the isolates showed certain antimicrobial and acetylcholinesterase inhibitory activities.

Antioxidant, antiacetylcholinesterase and apoptotic effects of essential oil of Isodon wightii (Bentham) H. Hara

Isodon wightii (Bentham) H. Hara is well known for aromatic essential oil. This is the first study aimed to evaluate antioxidant, antiacetylcholinesterase and apoptotic potential of I. wightii oil. DPPH scavenging, metal ion chelation and antiacetylcholinesterase activities were carried out for the extracted essential oil from the leaves of I. wightii. Cytotoxic effect on HeLa cells was studied by MTT assay and its apoptotic potential was determined by Acridine Orange/Ethidium Bromide and Hoechst33258 stains. A significant free radical scavenging and metal ion chelation were determined for oil. Acetylcholinesterase inhibition was recorded with IC50 value of 7.864 µg/mL. The cytotoxic effect of oil on HeLa cells was calculated with IC50 value of 13.264 µg/mL. High level of apoptosed cells were observed at 100 µg/mL oil treated cells. The results of the study emphasise the medicinal importance of I. wightii essential oil which could be a prominent plant based cancer therapeutic agent.

Apocynaceae as a Potential Source for Acetylcholinesterase Inhibition in Symptomatic Regulation and Management of Alzheimer's Disease

: Memory loss or dementia is the key symptom of Alzheimer's disease (AD). In AD, significant interference in a progressive manner is observed in memory, behaviour, and cognitive abilities that affect the daily life of a person. At present, more than 50 million people are affected worldwide with Alzheimer's disease. Urgent attention is needed for the symptomatic regulation and management of this disease. The significant pharmacotherapy research in the last two decades gave only four drug compounds galanthamine, donepezil, rivastigmine, and memantine that inhibit the enzyme acetylcholinesterase (AChE) to elevate the availability of acetylcholine in the brain for symptomatic relief in AD patients. Plant-based AChE inhibitors from many plant families, mainly including Rutaceae, Papaveraceae, Apocynaceae, Rubiaceae, Amaryllidaceae, Liliaceae, Lycopodiaceae, Fabaceae, Lamiaceae, etc., have been characterized for the management of AD progression. AD progression is described by cholinergic, amyloid, Tau protein, oxidative stress, and neuroinflammatory hypothesis. To date, there is no comprehensive review in the literature that combined all plants of the Apocynaceae family showing anti-AChE activity. Therefore, the current review aims to present significant literature, especially on plant-derived compounds from the Apocynaceae family that inhibit AChE. The review compiled all plants showing potent anti-acetylcholinesterase activity. The anti-AChE activity of more than 30 plants is described, which may be potential targets to find new drug molecules by attracting the attention of researchers toward the Apocynaceae family. More than 8 species of genus Tabernaemontana of Apocynaceae have been investigated for indole alkaloids, demonstrating AChE inhibitory activity. The majority of anti-AChE compounds belong to the class of alkaloids.

Essential oil from Knema Elegans warb.: chemical composition, antioxidant and anti-acetylcholinesterase activities

Essential oil from Knema Elegans warb.: chemical composition, antioxidant and anti-acetylcholinesterase activities

Effectiveness of Tri-Kaysorn-Mas Extract in Ameliorating Cognitive-like Behavior Deficits in Ovariectomized Mice via Activation of Multiple Mechanisms.

Postmenopausal women have a higher probability of experiencing cognitive alterations compared to men, suggesting that the decline in female hormones may contribute to cognitive deterioration. Thailand traditionally uses Tri-Kaysorn-Mas (TKM), a blend of three medicinal herbs, as a tonic to stimulate appetite and relieve dyspepsia. Due to its antioxidant and anti-acetylcholinesterase activities, we investigated the effects of TKM (50 and 100 mg/kg/day, p.o., for 8 weeks) on cognitive deficits and their underlying causes in an ovariectomized (OVX) mouse model of menopause. OVX mice showed cognitive impairment in the Y-maze, novel object recognition task (NORT), and Morris water maze (MWM) behavioral tests, along with atrophic changes to the uterus, altered levels of serum 17β-estradiol, and down-regulated expression of estrogen receptors (ERα and ERβ). These behavioral effects were reversed by TKM. TKM decreased malondialdehyde (MDA) levels and mitigated oxidative stress in the brain by enhancing the activity of superoxide dismutase (SOD) and catalase (CAT) and by up-regulating the antioxidant-related gene Nrf2 while down-regulating Keap1. TKM also counteracted OVX-induced neurodegeneration by enhancing the expression of the neurogenesis-related genes BDNF and CREB. The results indicate that TKM extract alleviates oxidative brain damage and neurodegeneration while enhancing cognitive behavior in OVX mice, significantly improving cognitive deficiencies related to menopause/ovariectomy through multiple targets.

Combining chemical profiles and biological abilities of different extracts from Tanacetum nitens(Boiss. & Noë)Grierson using network pharmacology.

Tanacetum nitens(Boiss. & Noë)Grierson is an aromatic perennial herb used in Turkish traditional medicine to treat headache, fever, and skin diseases. This study aimed to investigate the chemical composition, antioxidant, enzyme inhibition, and cytotoxic properties of T. nitens aerial parts. Organic solvent extracts were prepared by sequential maceration in hexane, dichloromethane, ethyl acetate, and methanol while aqueous extracts were obtained by maceration or infusion. Nuclear magnetic resonance (NMR) and LC-DAD-MS analysis allowed the identification and quantification of different phytoconstituents including parthenolide, tanacetol B, tatridin B, quinic acid derivatives, β-sitosterol, and glycoside derivatives of quercetin and luteolin. The type and amount of these phytochemicals recovered by each solvent were variable and significant enough to impact the biological activities of the plant. Methanolic and aqueous extracts displayed the highest scavenging and ions-reducing properties while the dichloromethane and ethyl acetate extracts exerted the best total antioxidant activity and metal chelating power. Results of enzyme inhibition activity showed that the hexane, ethyl acetate, and dichloromethane extracts had comparable anti-acetylcholinesterase activity and the latter extract revealed the highest anti-butyrylcholinesterase activity. The best α-amylase and α-glucosidase inhibition activities were obtained from the hexane extract. The dichloromethane and ethyl acetate extracts exhibited the highest cytotoxic effect against the prostate carcinoma DU-145 cells. In conclusion, these findings indicated that T. nitens can be a promising source of biomolecules with potential therapeutic applications.

Chemical composition, antioxidant activity, enzyme inhibitory effects, and network pharmacology analysis of essential oil from Bulbophyllum kwangtungense Schltr.

The present study investigates the chemical composition of the essential oil (EO) from Bulbophyllum kwangtungense Schltr., evaluates its antioxidant, enzyme inhibitory activities, and analyzes its therapeutic mechanisms against oxidative damage through network pharmacology. The main components identified were n-hexadecanoic acid (9.95 %), linalool (9.17 %), 1-hexanol (5.16 %), pentadecanoic acid (4.66 %), (Z)-3-hexen-1-ol (3.39 %), phytol (2.67 %), linoleic acid (2.49 %), 1-hexadecanol (2.39 %), α-curcumene (2.28 %). The 2,2′-azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS), 1,1-diphenyl-2-picryl-hydrazyl radical (DPPH) free radical scavenging capacity was characterized by IC50 values of 0.43 ± 0.08 mg/mL and 3.87 ± 1.26 mg/mL. The ferric reducing antioxidant power (FRAP) antioxidant value (Trolox equivalent antioxidant concentration) was 116.49 ± 0.26 μM/g. The EO exhibited anti-β-lactamase activity with an IC50 of 229.4 ± 18.7 μg/mL. The anti-acetylcholinesterase activity was 18.10 ± 2.71% at the 500 μg/mL concentration. The network pharmacology analysis was conducted to reveal potential targets and pathways of oxidative damage involved in the therapeutic effects of our EO.

Unusual norcucurbitacin glycosides from the roots of Siraitia grosvenorii

Siraitia grosvenorii Swingle is one of the first approved medicine food homology species in China, and it has been used as a natural sweetener in the food industry and as a traditional medicine to relieve cough and reduce phlegm. However, many S. grosvenorii roots are discarded yearly, which results in a great waste of resources. Twelve undescribed norcucurbitacin-type triterpenoid glycosides, siraitiaosides A-L (1–12), and six known analogs (13–18) were isolated from the roots of S. grosvenorii. The structures of isolated norcucurbitacin glycosides were elucidated by comprehensive data analyses, including HRESIMS, UV, IR, NMR, ECD calculations, and X-ray crystallography analysis. Siraitiaosides A-E (1–5) featured an unusual 19,29-norcucurbitacin framework while siraitiaosides F-L (6–12) featured a rare 29-norcucurbitacin framework. Notably, compound 4 displayed moderate anti-acetylcholinesterase (AChE) activity with an IC50 of 21.0 μM, meanwhile, compounds 16 and 18 exhibited pronounced cytotoxic activities against MCF-7, CNE-1, and HeLa cancer cell lines with IC50 values of 2.1–15.2 μM. In silico studies showed that compound 4 bound closely to AChE with a binding energy of −5.04 kcal/mol, and compound 18 could tightly bind to PI3K, AKT1, ERK2, and MMP9 proteins that related to autophagy, apoptosis, migration/invasion, and growth/proliferation. In summary, the roots of Siraitia grosvenorii have potential medicinal values due to the multiple bioactive components.

Investigating flavonoids derived from Tribulus terrestris L. as prospective candidates for Alzheimer's disease treatment: Molecular docking modeling of their interactions with physiological system receptors

Alzheimer's disease (AD) stands as the primary cause of dementia, marked by its neurodegenerative essence, which results in cognitive impairment associated with memory and a decline in functionality. Currently there is no drug which can permanently cure the nervous lesions as well as completely eradicate this pathogenesis. The aim of this research is to examine the acetylcholinesterase activity of flavonoids identified in Tribulus terrestris L. (Tt) by predicting ligand-receptor binding. The research process begins with the preparation of protein and ligand structures. Subsequently, docking is performed, interaction between protein-ligands is then analyzed and visualized. Four phytoconstituents of Tt were chosen, and molecular docking simulations revealed that all four compounds exhibited good binding affinities. Based on the predicted ADMET values using the Lipinski rule, compounds with potentially good activity were identified. The results suggest that these compounds may exhibit anti-acetylcholinesterase activity.

Triterpenoid and trichothecenes from a rhizospheric soil-derived Paramyrothecium sp. KMU22107

A new phthalide derivative named paramlyktone (1) and a new arborinane-type triterpenoid named paramyrpenoid (2), together with ten previously described trichothecenes derivatives (3–12) were isolated and identified from a rhizospheric soil-derived Paramyrothecium sp. KMU22107 associated with Delphinium yunnanense. Their structural elucidation was achieved by the comprehensive analysis of spectroscopic data and comparison with literature values. Notably, paramyrpenoid (2) was the first example of an arborinane-type triterpenoid with a double bond at Δ12(13) and an additional methyl motif at C-8. This was the first report of arborinane-type triterpenoids from a fungus belonging to Paramyrothecium genus. In pharmacological studies, paramyrpenoid (2) demonstrated significant cytotoxic activity against the HL-60, SW480, A-549, MDA-MB-231 and SMMC-7721 cell lines, with IC50 values from 2.0 to 16.1 μM. Compounds 1 and 2 were also evaluated for anti-inflammatory, anti-acetylcholinesterase (AChE), and protein tyrosine phosphatase 1B (PTP1B) inhibitory activities in vitro.

Benzyloxychalcone Hybrids as Prospective Acetylcholinesterase Inhibitors against Alzheimer's Disease: Rational Design, Synthesis, In Silico ADMET Prediction, QSAR, Molecular Docking, DFT, and Molecular Dynamic Simulation Studies.

Acetylcholinesterase inhibitors (AChEIs) are crucial therapeutic targets for both the early and severe stages of Alzheimer's disease (AD). Chalcones and their chromone-based derivatives are well-known building blocks with anti-Alzheimer properties. This study synthesized 4-benzyloxychalcone derivatives and characterized their structures using IR, 1H NMR, 13C NMR, and HRMS. Additionally, the synthesized 4-benzyloxychalcone derivatives were tested for anti-acetylcholinesterase (AChE) activity. The synthesized compounds outperformed galantamine, which is used as a positive control against acetylcholinesterase. Utilizing an acetylcholinesterase (AChE) receptor (PDB ID: 4EY7)-chalcone derivative (12a-c), a molecular docking investigation was performed on the synthesized compounds. The goal was to predict the binding sites and energies of the derivatives with respect to the receptor amino acids. The dynamic behavior of the ligand-receptor complex resulting from the interaction of the best docking compounds 12a and 12c with the acetylcholinesterase receptor was used to analyze the stability via MD simulation. MM/GBSA and MM/PBSA were used to calculate free binding energies using snapshots from system trajectories. Advanced computational approaches incorporating long-range corrections were utilized to calculate the molecular characteristics of chalcone derivatives 12a-c at the DFT/wB97XD/6-311++G(d,p) level. We used the molecular electrostatic surface potential (MESP) with high-quality data and visualization to find the most active site in these molecules. Reactivity descriptors, including the condensed Fukui function, chemical hardness (η), dual descriptors, chemical potential (μ), and electrophilicity (ω), were calculated for the chalcone derivatives.

Changes in Anticholinesterase and Antioxidant Activities of Fruit Products during Storage

In this work, compotes, juices, and jams were produced using chokeberry, cherry, apricot, peach, apple (Idared and Champion), wild strawberry, or raspberry fruits. The anticholinesterase as well as antioxidant activities of fruits and preserves (freshly prepared and after 1, 5, and 10 months of storage) were compared. The loss (p < 0.05) of the anti-acetylcholinesterase (AChE) activity of freshly prepared products vs. corresponding fruits was observed (all preserves from raspberry, cherry juice and jam, apricot juice, and Idared and wild strawberry jams) while chokeberry juice and apricot compote increased the anti-AChE activity. In the case of the anti-BChE activity of freshly prepared products, no change (apricot juice and jam), the loss (chokeberry compote and jam, cherry juice and jam, Champion compote, p < 0.05), or the increase in the activity (peach and apple Idared, apricot compote, juice, apricot compote, raspberry juice, p < 0.05) were recorded. In most cases, the anticholinesterase activities of freshly prepared products vs. products stored for 10 months were retained, and no considerable losses of the biological activities were observed. Even after 10 months of storage, all of the preserves retained the anti-AChE activity (except apricot and Idared compotes, chokeberry, cherry and Idared juices, and chokeberry and apricot jams, p < 0.05). Similarly, the preserves retained the anti-BChE activity after 10 months of storage (at p < 0.05, except cherry, apricot, peach and Idared compotes, chokeberry juice and chokeberry, peach and raspberry jams, at p < 0.05).

Exploring the bioactive potential of Mentha longifolia from Northeast India: an inclusive study on phytochemical composition and biological activities

Mentha longifolia (Lamiaceae) is regarded as highly valuable aromatic medicinal species with wide range of pharmaceutical application. In the present work, leaf essential oil of M. longifolia was applied for the assessment of in vitro pharmacological potentials and compositional analysis. A sum of 15 compounds were detected by GC-FID and GC-MS analysis of M. longifolia essential oil with total area of 99.98% where major compounds were carvone (59.56%), D-limonene (20.81%), eucalyptol (10.08%). The anti-oxidant potency of M. longifolia was estimated using two methods viz., ABTS (2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid) and DPPH (2,2-diphenyl-1-picrylhydrazyl) assay where M. longifolia essential oil showed moderate anti-oxidant potency. M. longifolia essential oil revealed high anti-inflammatory and tyrosinase inhibitory activity with an IC50 value 3.68 μL/mL and 1.22 μL/mL respectively compared to standard sodium diclofenac (5.33 μL/mL) and kojic acid (2.28 μL/mL). The acetylcholinesterase (AchE) inhibitory and genotoxic assay was performed, where M. longifolia essential oil revealed strong anti-acetylcholinesterase and anti-genotoxic activity. Anti-microbial potential of M. longifolia essential oil was also where strong anti-bacterial activity was shown against Salmonella typhimurium, Bacillus cereus, Staphylococcus aureus, Micrococcus luteus. For anti-fungal activity, M. longifolia essential oil showed no zone of inhibition against any used strains except Aspergillus flavus. From the present research it was established that M. longifolia essential oil possesses pharmaceutical potential with strong AchE inhibitory, anti-inflammatory, anti-microbial, anti-tyrosinase, anti-genotoxic and anti-oxidant activity which can be used for plant-based drug development in future endeavor.

Enzyme inhibitory, antioxidant and anti-inflammatory activities of Anabasis articulata phenolic-rich extract; in vitro, in vivo, and in silico studies

The present study aimed at characterizing the phenolic composition of the aqueous extract from Anabasis articulata and its biological properties, in terms of in vitro antioxidant, enzyme inhibitory, and in vivo anti-inflammatory effects. The phytocomplex was investigated by HPLC-DAD analysis, whereas total phenolics, tannins and flavonoids using spectrophotometric methods. The antioxidant property of the extract was determined applying four assays (i.e. total antioxidant capacity, reducing power, DPPH, and β-carotene-linoleic acid bleaching). The enzymatic inhibitory function was evaluated against tyrosinase and acetylcholinesterase, whereas toxicological and anti-inflammatory aspects through in vivo evaluations. More in detail, twenty-one specific phenolic compounds were successfully detected, identified, and quantified in the plant extract, which showed considerable antioxidant potential. The aqueous preparation also revealed a high anti-tyrosinase and anti-acetylcholinesterase activity. In particular, an in-silico prediction analysis, by molecular docking approach, was performed to understand which plant metabolite from A. articulata could be potentially responsible for acetylcholinesterase inhibition, favoring the identification of putative new compounds useful for the treatment of neurodegenerative diseases. All the present evidence could partially explain and justify the therapeutic efficacy of the Algerian traditional medicine linked to the application of A. articulata aqueous extract.

Spermacoce alata Aubl. Essential Oil: Chemical Composition, In Vitro Antioxidant Activity, and Inhibitory Effects of Acetylcholinesterase, α-Glucosidase and β-Lactamase.

Spermacoce alata Aubl. is widely available in the market as traditional Chinese medicine and animal feed, due to its properties of clearing heat and treating malaria and its high-protein and crude fiber content. In this study, the essential oil of S. alata was obtained through hydrodistillation. GC-MS and GC-FID methods were used to identify the chemical components and their relative abundance. Furthermore, the antioxidant capacity was measured using DPPH, ABTS, and FRAP assays, and the inhibitory effects of acetylcholinesterase, α-glucosidase, and β-lactamase were also evaluated. A total of 67 compounds were identified, with the major constituents being palmitic acid (30.74%), linoleic acid (16.13%), and phenylheptatriyne (8.07%). The essential oil exhibited moderate antioxidant activity against DPPH (IC50 > 10 mg/mL), while the IC50 value for the ABTS assay was 3.84 ± 2.12 mg/mL and the FRAP assay value was 87.22 ± 12.22 µM/g. Additionally, the essential oil showed moderate anti-acetylcholinesterase activity (IC50 = 286.0 ± 79.04 μg/mL), significant anti-α-glucosidase activity (IC50 = 174.7 ± 13.12 μg/mL), and potent anti-β-lactamase activity (IC50 = 37.56 ± 3.48 μg/mL). The results suggest that S. alata has the potential for application in pharmacology, warranting further exploration and investigation.

Phytochemical Analysis, Acetylcholinesterase Inhibition, Antidiabetic and Antioxidant Activities of Atriplex halimus L. (Amaranthaceae Juss.).

Mediterranean saltbush Atriplex halimus L. (Amaranthaceae) from different bioclimatic arid zones (ten wild populations) were studied. Phenols contents, flavonoids, flavonols, tannins and anthocyanins were determined and then tested for their antioxidants, antidiabetic and anti-acetylcholinesterase (AChE) activities. Levels of total polyphenols including flavonoids and flavonols, tannins and anthocyanins were high and varied significantly among analyzed populations. Nine phenolic acids and four flavonoids were identified for the first time in the methanolic fraction and quantified by liquid high-performance chromatography system HPLC (DAD). All extracts showed a substantial antioxidant activity, as assessed by DPPH assay (1,1-diphenyl-2-picrylhydrazyl free radical) (IC50DPPH=147.3for population of Seliena), Ferric Reducing Antioxidant Power (FRAP; IC50FRAP=3.2 for populations of Sousse and Kairouan), and Chelation Fer test (IC50FerCh=1.5 μg/mL for populations of El-hamma and Mednine). Atriplex halimus possessed a high inhibitory effect against α-amylase activity (up to 2.6 mg ACE/gE), a moderate activity for α-glucosidase (up to 91.0 mg ACE/gE) and AChE (up to 147.2 μg/mL) compared to standard. The analyzed populations were isolated and subdivided into three distinct groups, without any bioclimatic structuration. Enzymatic activities seem to be associated with the presence, in plant extracts, of other classes of compounds then phenols such as terpenes, sterols, saponins, coumarins and carotenoids.

Furostanol glycosides, stilbenoids and nucleosides from the roots of Smilax perfoliata, and evaluation of their cytotoxic and anticholinesterase activities

Three undescribed compounds including two furosteroid glycosides (perfoloside and 22-O-methylperfoloside) and one stilbenedimer (perfolostilbene) together with 21 known compounds were isolated from the roots of Smilax perfoliata. The structural elucidation was established by extensive uses of HRMS, 1D and 2D spectroscopic techniques. The assignment of the stereocenters in perfolostilbene was based on NOESY data and ECD calculation. Among the isolates, two compounds showed marginal cytotoxic activity against KB and Hela cell lines while seven stilbenoids showed strong to weak antiacetylcholinesterase and antibutyrylcholinesterase activities with IC50 ranging between 2–197 µM.