HPLC-DAD-MS Characterization, Antioxidant Activity, α-amylase Inhibition, Molecular Docking, and ADMET of Flavonoids from Fenugreek Seeds.

Fenugreek (Trigonella foenum-graecum) has a great beneficial health effect; it has been used in traditional medicine by many cultures. Likewise, the α-amylase inhibitors are potential compounds in the development of drugs for the treatment of diabetes. The beneficial health effects of fenugreek lead us to explore the chemical composition of the seeds and their antioxidant and α-amylase inhibition activities. The flavonoid extraction from fenugreek seeds was achieved with methanol through a Soxhlet apparatus. Then, the flavonoid glycosides were characterized using HPLC-DAD-ESI-MS analysis. The antioxidant capacity of fenugreek seed was measured using DPPH, FRAP, ABTS, and CUPRAC assays. Finally, the α-amylase inhibition activity was carried out using in vitro and in silico methods. The methanolic extract was found to contain high amounts of total phenolics (154.68 ± 1.50 µg GAE/mg E), flavonoids (37.69 ± 0.73 µg QE/mg E). The highest radical-scavenging ability was recorded for the methanolic extract against DPPH (IC50 = 556.6 ± 9.87 µg/mL), ABTS (IC50 = 593.62 ± 9.35 µg/mL). The ME had the best reducing power according to the CUPRAC (A 0.5 = 451.90 ± 9.07 µg/mL). The results indicate that the methanolic extracts of fenugreek seed best α-amylase inhibition activities IC50 = 653.52 ± 3.24 µg/mL. Twenty-seven flavonoids were detected, and all studied flavonoids selected have good affinity and stabilize very well in the pocket of α-amylase. The interactions between the studied flavonoids with α-amylase were investigated. The flavonoids from fenugreek seed present a good inhibitory effect against α-amylase, which is beneficial for the prevention of diabetes and its complications.

assessment of antioxidant, neuroprotective, anti-urease and anti-tyrosinase capacities of leaves extracts.

OBJECTIVE: To characterize the chemical profile of methanolic crude extract and its fractions (Ethyl acetate, n-butanol and aqueous) using liquid chromatography-mass spectrometry (LC-MS) analysis, to evaluate their biological and pharmacological properties: antioxidant (1, 1-diphenyl-2-pycrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic) (ABTS), galvinoxyle free radical scavenging, reducing power, phenanthroline and ß carotene-linoleic acid bleaching assays), enzymes inhibitory ability against several enzymes [acetyl-cholinesterase (AChE), buthyrylcholinesterase (BChE), urease and tyrosinase]. METHODS: Secondary metabolites were extracted from Tamarix africana air-dried powdered leaves by maceration, the crude extract was fractionated using different solvents with different polarities (Ethyl acetate, n-butanol and aqueous). The amount of polyphenols, flavonoids and tannins (hydrolysable and condensed) were determined using colorimetric assays. A variety of biochemical tests were carried out to assess antioxidant and oxygen radical scavenging properties using DPPH, ABTS, galvinoxyle free radical scavenging, reducing power, phenanthroline and ß carotene-linoleic acid bleaching methods. Neuroprotective effect was examined against acetylcholinesterase and buthy-rylcholinesterase enzymes. The anti-urease and anti-tyrosinase activities were performed against urease and tyrosinase enzymes respectively. The extract's components were identified using LC-MS and compared to reference substances. RESULTS: The results indicated that Tamarix africana extracts presented a powerful antioxidant activity in all assays and exhibited a potent inhibitory effect against AChE and BChE as well as urease and tyrosinase enzymes. LC-MS analysis identified amount of eight phenolic compounds were revealed in this analysis; Apigenin, Diosmin, Quercetin, Quercetine-3-glycoside, Apigenin 7-O glycoside, Rutin, Neohesperidin and Wogonin in methanolic extract and its different fractions of Tamarix africana from leaves. CONCLUSIONS: Based on these findings, it is reasonable to assume that Tamarix africana could be considered as a potential candidate for pharmaceutical, cosmetics, and food industries to create innovative health-promoting drugs.

Phytochemicals, Antioxidant and Antimicrobial Potentials and LC-MS Analysis of Centaurea parviflora Desf. Extracts.

Centaurea parviflora (C. parviflora), belonging to the family Asteraceae, is an Algerian medicinal plant used in folk medicine to treat different diseases related to hyperglycemic and inflammatory disorders, as well as in food. The present study aimed to assess the total phenolic content, in vitro antioxidant and antimicrobial activity and phytochemical profile of the extracts of C. parviflora. The extraction of phenolic compounds from aerial parts was conducted using solvents of increasing polarity starting from methanol, resulting in crude extract (CE), to chloroform extract (CHE), ethyl acetate extract (EAE) and butanol extract (BUE). The total phenolic, flavonoid and flavonol contents of the extracts were determined using the Folin-Ciocalteu and AlCl3 methods, respectively. The antioxidant activity was measured with seven methods: 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, galvinoxyl free-radical-scavenging test, 2,2'-Azino-Bis(3-Ethylbenzothiazoline-6-Sulfonic Acid) (ABTS) assay, cupric reducing antioxidant capacity (CUPRAC), reducing power, Fe+2-phenanthroline reduction assay and superoxide-scavenging test. The disc-diffusion method aimed at testing the sensitivity of bacterial strains toward our extracts. A qualitative analysis with thin-layer chromatography of the methanolic extract was performed. Moreover, HPLC-DAD-MS was used to establish the phytochemical profile of the BUE. The BUE was found to contain high amounts of total phenolics (175.27 ± 2.79 µg GAE/mg E), flavonoids (59.89 ± 0.91 µg QE/mg E) and flavonols (47.30 ± 0.51 µg RE/mg E). Using TLC, different components such as flavonoids and polyphenols were noted. The highest radical-scavenging ability was recorded for the BUE against DPPH (IC50 = 59.38 ± 0.72 µg/mL), galvinoxyl (IC50 = 36.25 ± 0.42 µg/mL), ABTS (IC50 = 49.52 ± 1.54 µg/mL) and superoxide (IC50 = 13.61 ± 0.38 µg/mL). The BUE had the best reducing power according to the CUPRAC (A0.5 = 71.80 ± 1.22 µg/mL), phenanthroline test (A0.5 = 20.29 ± 1.16 µg/mL) and FRAP (A0.5 = 119.17 ± 0.29 µg/mL). The LC-MS analysis of BUE allowed us to identify eight compounds including six phenolic acids and two flavonoids: quinic acid, five chlorogenic acid derivatives, rutin and quercetin 3-o-glucoside. This preliminary investigation revealed that the extracts of C. parviflora have a good biopharmaceutical activity. The BUE possesses an interesting potential for pharmaceutical/nutraceutical applications.

LC-ESI/MS-phytochemical profiling with antioxidant and antiacetylcholinesterase activities of Algerian Senecio angulatus L.f. extracts.

Senecio angulatus L.f. is a flowering plant from the Asteraceae family that is native to South Africa and which was observed recently in the north and the east of Algeria. This study was aimed for the first time, to evaluate concomitantly phytochemical profiles, using LC-ESI/MS analysis, following by testing and assessing in vitro antioxidant and antiacetylcholinesterase activities of these specific species. The results indicated that the hydromethanolic and the acetate extracts have shown remarkable potent inhibitory effects on AChE with IC50 of (6.04 ± 0.05; 6.72 ± 0.10 µg/mL) respectively along with antioxidant potential of acetate for FRAP and phenanthroline methods with A0.5 of (11.15 ± 0.72; 5.72 ± 0.13 µg/mL) successively. Moreover, a high amount of cynarin and trans-ferulic acid was found in this extract whilst butanolic extract has recorded the highest amount of chlorogenic acid. Indeed phenolic compounds usually have a hydroxyl in their structure which may contribute significantly to the antioxidant activity.

Low concentrations of Ambrosia maritima L. phenolic extract protect endothelial cells from oxidative cell death induced by H2O2 and sera from Crohn's disease patients.

ETHNOPHARMACOLOGICAL RELEVANCE: A rising resort to herbal therapies in Crohn's disease (CD) alternative treatments has been recently observed due to their remarkable natural efficiency. In this context, the weed plant Ambrosia maritima L., traditionally known as Hachich el Aouinet in Algeria and as Damsissa in Egypt and Sudan, is widely used in North African folk medicine to treat infections, inflammatory diseases, gastrointestinal and urinary tract disturbances, rheumatic pain, respiratory problems, diabetes, hypertension and cancer. AIM OF THE STUDY: To assess an Ambrosia maritima L. phenolic extract for its phenolic profile composition, its potential antioxidant activity in vitro, and its cytoprotective effect on cultured primary human endothelial cells (ECs) stressed with H2O2 and sera from CD patients. MATERIALS AND METHODS: Phenolic compound extraction was performed with a low-temperature method. Extract chemical profile was attained by HPLC-DAD/ESI-MS. The extract in vitro antioxidant activity was assessed using several methods including cupric ion reducing power, DPPH radical scavenging assay, O-Phenanthroline free radical reducing activity, ABTS cation radical decolourisation assay, Galvinoxyl free radicals scavenging assay. Intracellular reactive oxygen species levels were evaluated in human endothelial cells by H2DCFDA, while cell viability was assessed by MTT. RESULTS: The phenolic compounds extraction showed a yield of 17.66% with three di-caffeoylquinic acid isomers detected for the first time in Ambrosia maritima L. Using different analytical methods, a significant in vitro antioxidant activity was reported for the Ambrosia maritima L. extract, with an IC50 value of 14.33 ± 3.86 µg/mL for the Galvinoxyl antioxidant activity method. Challenged with ECs the Ambrosia maritima L. extract showed a biphasic dose-dependent effect on H2O2-treated cells, cytoprotective and antioxidant at low doses, and cytotoxic and prooxidant at high doses, respectively. Viability and ROS levels data also demonstrated a prooxidant and cytotoxic effect of CD sera on cultured ECs. Interestingly, 10 µg/mL of Ambrosia maritima L. extract was able to counteract both CD sera-induced oxidative stress and ECs death. CONCLUSION: Our data indicated Ambrosia maritima L. as a source of bioactive phenolics potentially employable as a natural alternative for CD treatment.

Phenolic Characterization Using cLC-DAD Analysis and Evaluation of In Vitro and In Vivo Pharmacological Activities of Ruta tuberculata Forssk.

The perennial aromatic plant Ruta tuberculata Forssk (Rutaceae) has been traditionally used by Mediterranean peoples as folk medicine against several types of disease to treat diverse illness. The objective of this work is to evaluate the in vitro and in vivo pharmacological activities of the aqueous (RAE) and methanolic (MeOH) 80% (RME) extracts of Algerian R. tuberculata aerial parts. Antioxidant potential, neuro-protective and anti-arthritic activities were investigated in vitro using six antioxidant approaches and by determining acetyl-cholinesterase and bovine albumin denaturation inhibitory capacities, respectively. Furthermore, in vivo anti-ulcer and anti-inflammatory activities were evaluated on EtOH-induced gastric mucosal damage and carrageenan-induced paw edema models in mice. Moreover, bio-compounds' contents were also quantified using spectrophotometric and cLC-DAD methods. Both in vivo and in vitro investigations showed remarkable antioxidant activity of Ruta tuberculata Forssk, while methanolic extract (RME) of Ruta tuberculata Forssk exhibited more significant neuro-protective and anti-inflammatory effects. However, the antiulcer activity was more pronounced with RAE of R. tuberculata, which suggests that this plant can be considered as a natural resource of potent bioactive compounds that may act as antioxidant and anti-inflammatory agents, which underlines the importance of incorporating them in therapies in order to treat various diseases linked to oxidative stress, and they may also provide crucial data for the development of new anticholinesterase drugs to improve neurodegenerative diseases, such as Alzheimer's.

First report on phytochemical investigation, antioxidant and antidiabetic activities of Helianthemum getulum.

A new flavonoid, 5,7,2',4',5'-pentahydroxyflavone 3-O-ß-D-galactopyranoside (12) and twelve known derivatives: an aryltetralin-lignan (3), seven flavonoids (4-5, 7-10, 13) and four phenolic acids (1-2, 6, 11) have been isolated from the aerial parts of Helianthemum getulum Pomel. (Cistaceae family) an endemic species to the septentrional Sahara that is being studied for the first time. Structure elucidation of the isolated compounds was established by means of spectroscopic methods especially NMR and Mass Spectrometry. In vitro antioxidant (DPPH, ABTS, GOR and CUPRAC assays) and antidiabetic (micro-dilution method) activities of the crude extract, fractions and isolated compounds were performed. The new flavonol (12) and Compounds (2, 3, 7, 9) were found to be the most active, some of them exhibiting better activity than the antioxidant standards. Compounds 7, 9 and 3 showed higher α-glucosidase inhibitory activity compared to standard acarbose (IC50= 2.70 ± 0.03 µM, 3.09 ± 0.03 µM, 37.28 ± 1.20 µM and 275.43 ± 1.59 µM, respectively).

Chemical composition, antioxidant, and antimicrobial activities of two essential oils from Algerian propolis.

This study aims to investigate the chemical composition, antioxidant, and antimicrobial activity of two essential oils (EOs) from Algerian propolis. The volatile constituents were analyzed by gas chromatography-mass spectrometry. Fifty components were identified from the oils. The major components were found to be: cedrol (17.0%), ß-eudesmol (7.7%), and α-eudesmol (6.7%) in EO of propolis from Oum El Bouaghi (EOPO) whilst α-pinene (56.1%), cis-verbenol (6.0%), and cyclohexene,3-acetoxy-4-(1-hydroxy-1-methylethyl)-1-methyl (4.4%) in EO of propolis from Batna (EOPB). The antioxidant properties of EOPO and EOPB were determined using 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonate) (ABTS•+) and cupric reducing antioxidant capacity (CUPRAC assays), respectively. Both EOs had more cupric ion reducing ability than scavenging ABTS•+ radicals. The antimicrobial potential of the two EOs against eight pathogens was assayed by the agar diffusion method and the mode of action was determined by microdilution assay. The results revealed that EOPB was bactericidal for all tested pathogenic bacteria and fungicidal for Candida albicans ATCC 10231, whereas, EOPO showed bacteriostatic effect against Escherichia coli O157:H7 and Pseudomonas aeruginosa ATCC27853 and fungistatic effect against C. albicans ATCC 10231. Thus, the obtained results suggest the important use of propolis EOs as preservative agents.

Phytochemical Screening, In vitro Antioxidant and Enzyme Inhibitory Properties, and Acute Toxicity of Extracts from the Aerial Parts of Ephedra nebrodensis, a Source of Bioactive Compounds.

BACKGROUND: Due to the strong association between the chemistry of medicinal plants and their biological properties, it is important to determine their phytochemical composition to justify experimental tests. OBJECTIVE: The aim of this study was to evaluate the in vitro antioxidant and the enzyme inhibitory properties and to identify the bioactive compounds present in the extracts of Ephedra nebrodensis growing in Algeria. METHODS: Total phenolic and flavonoids content in these extracts were quantified by Folin- Ciocalteu and aluminum chloride methods. The antioxidant capacity was assessed using DPPH, ABTS, ß-carotene/linoleic acid, CUPRAC and FRAP assays, and in vitro cholinesterase activity against acetylcholinesterase and butyrylcholinesterase were evaluated. The chemical constituents of the extracts were analyzed by high-performance liquid chromatography coupled with mass spectrometric detection and gas chromatography. For the acute toxicity study, extracts were administered to mice at single dose of 2 g/kg and 5 g/kg by gavage. RESULTS: Plant extracts were rich in phenolic compounds. Ethyl acetate extract presented the highest phenolic (238.44 ± 1.50 µg GAE /mg of extract) and flavonoid (21.12 ± 0.00 µg QE /mg of extract) contents. Likewise, ethyl acetate extract showed potent radical scavenging and reducing properties. Ethanol-acetone extract showed inhibitory activity against acetylcholinesterase, and was a potent inhibitor of butyrylcholinesterase. In all extracts, flavonoids were the most abundant compounds. The phytochemical investigation showed the presence of alkaloids (ephedrine and pseudo-ephedrine). In the acute toxicity, the LD50 was superior to 5 g/kg body weight. There were no alterations in the histology of the liver and kidneys. CONCLUSION: This study demonstrated a good antioxidant potential and anticholinesterase activity of aerial parts of E. nebrodensis.

Chemical Composition and Antioxidant, Anti-Inflammatory, and Enzyme Inhibitory Activities of an Endemic Species from Southern Algeria: Warionia saharae.

Warionia saharae Benth. & Coss. (Asteraceae) is an endemic species of North Africa naturally grown in the southwest of the Algerian Sahara. In the present study, this species' hydromethanolic leaf extract was investigated for its phenolic profile characterized by ultra-high-performance liquid chromatography coupled with a diode array detector and an electrospray mass spectrometer (UHPLC-DAD-ESI/MS). Additionally, the chemical composition of W. saharae was analyzed by gas chromatography-mass spectrometry, and its antioxidant potential was assessed through five in vitro tests: DPPH● scavenging activity, ABTS●+ scavenging assay, galvinoxyl scavenging activity, ferric reducing power (FRP), and cupric reducing antioxidant capacity. The UHPLC-DAD-ESI/MS analysis allowed the detection and quantification of 22 compounds, with taxifolin as the dominant compound. The GC-MS analysis allowed the identification of 37 compounds, and the antioxidant activity data indicate that W. saharae extract has a very high capacity to capture radicals due to its richness in compounds with antioxidant capacity. The extract also showed potent α-glucosidase inhibition as well as a good anti-inflammatory activity. However, weak anti-α-amylase and anticholinesterase activities were recorded. Moreover, an in silico docking study was performed to highlight possible interactions between three significant compounds identified in W. saharae extract and α-glucosidase enzyme.

Chemical Composition, Acetylcholine Esterase and Anti-bacterial Activities of Essential Oils of Elaeosilenum thapsioides (Desf.) Maire from Algeria.

BACKGROUND: Traditionally, the Algerian medicinal plant Elaeosilenum thapsioides (Desf.) Maire has been used for many diseases. The present research work aims to explore the chemical and biological characterization of its essential oil. METHODS: The essential oils were obtained by hydrodistillation of different Elaeosilenum thapsioides (Apiaceae) aerial parts samples collected from two different regions (Mahouane and Megres) from Setif, Eastern Algeria. The chemical characterization of the obtained essential oils is reported here for the first time. Besides, they were evaluated for their in vitro Acetylcholinesterase (AChE) inhibitory activity involved in Alzheimer's disease using Ellman's spectrophotometric method. RESULTS: Additionally, their in vitro antimicrobial activity was assessed by the disc diffusion method. Both activities were performed at various oil concentrations. The GC/MS analysis of the essential oils from aerial parts (leaves, stems, flowers, and seeds) of E. thapsioides identified 47 constituents. Monoterpene hydrocarbons were the main components, ranging from 72.78 to 99.13%. Oxygenated monoterpenes and oxygenated sesquiterpenes ranged between 1.37 and 17.25% and 0.12 and 3.53% in essential oils from leaves and stems. Sesquiterpene hydrocarbons were present in small to large quantities in the essential oils of both populations, ranging from 0.69 to 13.44%. The presence of m-Methoxybenzyl isothiocyanate was recorded in stems essential oils from Mahouane and leaves essential oils from Merges, which was 9.73% and 3.72%, respectively. CONCLUSION: The stems essential oils obtained from plants collected in Mahouane showed the highest AChE inhibitory activity. The highest anti-bacterial activity was shown by the essential oil obtained from Megres leaves against Bacillus cereus ATCC 11778. The oils exhibited a moderate inhibitory activity in both tests.

Chemical Composition and Antioxidant, Antiparasitic, Cytotoxicity and Antimicrobial Potential of the Algerian Limonium Oleifolium Mill. Essential Oil and Organic Extracts.

This work aimed to investigate, for the first time, the chemical composition, antioxidant, antiparasitic, cytotoxicity, and antimicrobial activities of the aromatic plant Limonium oleifolium Mill. essential oil (EO) and organic extracts. L. oleifolium aerial parts essential oil was analyzed by GC-FID and GC-MS, and 46 constituents representing 98.25±1.12 % of the oil were identified. γ-Muurolene (10.81±0.07 %), cis-caryophyllene (7.71±0.06 %), o-cymene (7.07±0.01 %) and α-copaene (5.02±0.05 %) were the essential oil main compounds. The antioxidant activity of L. oleifolium EO and organic extracts (MeOH, CHCl3 , AcOEt, BuOH) was explored using 2,2-diphenyl-1-picrylhydrazyl (DPPH), ABTS, ß-carotene/linoleic acid, cupric reducing antioxidant capacity (CUPRAC), and ferric reducing power assays. The results showed that L. oleifolium EO exhibit antioxidant capacity (IC50 =17.40±1.32 µg/mL for DPPH assay, IC50 =29.82±1.08 µg/mL for ß-carotene assay, IC50 =25.23±1.01 µg/mL for ABTS assay, IC50 =9.11±0.08 µg/mL for CUPRAC assay and IC50 =19.41±2.06 mg/mL for reducing power assay). Additionally, the EO showed significant activity against trophozoite form of Acanthamoeba castellanii (IC50 =7.48±0.41 µg/mL) and promastigote form of Leishmania amazonensis (IC50 =19.36±1.06 µg/mL) and low cytotoxicity on murine macrophages (LC50  90.23±1.09 µg/mL), as well as good antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella oxytoca, and Pseudomonas aeruginosa. These results suggest that L. oleifolium essential oil is a valuable source of bioactive compounds presenting antioxidant, antiparasitic, and antimicrobial activities. Furthermore, it is considered nontoxic.

Antioxidant activity and characterization of flavonoids and phenolic acids of Ammoides atlantica by RP-UHPLC-ESI-QTOF-MSn.

In this study, phytochemical profiling of hydro-alcoholic extract of Ammoides atlantica aerial parts has been carried out using RP-UHPLC-ESI-QTOF-MS in negative ionization mode Chemical characterization was established according to the MS and MS/MS spectra. A total of 66 chemical compounds were detected. Among these, 45 compounds were identified: hydroxycinnamic acid and derivatives (26), hydroxybenzoic acids (4), flavones (11), flavonols (3), and a lignan. Total phenolics (371.57 mg/g) and total flavonoids (41.02 mg/g) contents were also determined. Moreover, the antioxidant activity of A. atlantica extract was also studied by six methods: DPPH (IC50: 23.31 µg/mL), ABTS+ (IC50: 11.31 µg/mL), O2- DMSO alkaline (IC50: 3.19 µg/mL), ferrous ions chelating assays (IC50: 102.35 µg/mL), reducing power (A0.50: 92.70 µg/mL) and CUPRAC (A0.50: 13.56 µg/mL) assays. These results suggest that the antioxidant activity of the hydroalcoholic extract was comparable to common antioxidant additives in most of the tests, representing a good alternative.

Chemical composition, in vitro antioxidant, anticholinesterase and antibacterial activities of Linaria scariosa Desf.

The study was performed on the dichloromethane (DCM), ethyl acetate (EAc) and n-butanol (Bu) fractions (F) obtained from the 80% ethanol extract of Linaria scariosa Desf. aerial parts, collected in the North Eastern region of Algeria. Remarkable total phenolic and flavonoid contents were obtained, mainly for EAcF. These results were in accordance with the antioxidant activity of EAcF against DPPH, ABTS, CUPRAC and reducing power tests. DCMF and BuF exhibited significant cholinesterase activity inhibition of BChE and AChE. Moreover, EAcF displayed only moderate antibacterial activities, especially against S. aureus. The biological results were correlated to the chemical components, deduced by both GC-MS analysis of the fractions and the isolation of hemipholin, pectolinarigenin, antirride, antirrinoside, pectolinarin and linariosise, some of which known to exhibit potent effects on the tested biological activities. The study provides the first biological and chemical investigation on Linaria scariosa Desf (unresolved name).

Pyrroloquinolone A, a new alkaloid and other phytochemicals from Atractylis cancellata L. with antioxidant and anticholinesterase activities.

A new alkaloid pyrroloquinolone A (1), along with fifteen known compounds 2-16 were isolated from the petroleum ether, EtOAc and n-BuOH extracts of the whole plant Atractylis cancellata L. Their structures were elucidated on the basis of extensive spectroscopic analysis including 1D- and 2D-NMR and HR-ESI-MS techniques. This is the first report of alkaloids in the genus Atractylis. Some of the isolated compounds and extracts were evaluated for their antioxidant potential (scavenging activity of DPPH and ABTS radicals, and reducing Fe+3 and Cu+2 power assays) and acetylcholinesterase and butyrylcholinesterase inhibitory activities. Compounds 8 and 11 showed good antioxidant capacity compared to ascorbic acid, BHA, and BHT used as standards, whereas compounds 1 and 2 exhibited good anticholinesterase activities compared to galantamine used as standard.

Nanocapsules containing Saussurea lappa essential oil: Formulation, characterization, antidiabetic, anti-cholinesterase and anti-inflammatory potentials.

Plant-based remedies have been widely used for the management of variable diseases due to their safety and less side effects. In the present study, we investigated Saussurea lappa CB. Clarke. (SL) given its largely reported medicinal effects. Specifically, our objective was to provide an insight into a new polymethyl methacrylate based nanocapsules as carriers of SL essential oil and characterize their biologic functions. The nanoparticles were prepared by nanoprecipitation technique, characterized and analyzed for their cytotoxicity, anti-inflammatory, anti-Alzheimer and antidiabetic effects. The results revealed that the developed nanoparticles had a diameter around 145 nm, a polydispersity index of 0.18 and a zeta potential equal to +45 mV and they did not show any cytotoxicity at 25 µg·mL-1. The results also showed an anti-inflammatory activity (reduction in metalloprotease MMP-9 enzyme activity and RNA expression of inflammatory cytokines: TNF-α, GM-CSF and IL1ß), a high anti-Alzheimer's effect (IC50 around 25.0 and 14.9 µg·mL-1 against acetylcholinesterase and butyrylcholinesterase, respectively), and a strong antidiabetic effect (IC50 were equal to 22.9 and 75.8 µg·mL-1 against α-amylase and α-glucosidase, respectively). Further studies are required including the in vivo studies (e.g., preclinical), the pharmacokinetic properties, the bioavailability and the underlying associated metabolic pathways.

Structural characterization, antioxidant, and antibiofilm activities of Coffea canephora green seeds.

OBJECTIVES: In order to explore Coffea canephora green seeds as natural extract for application in the functional-food industry, we focused this study to the evaluation of the antioxidant and the antiadhesion effect of C. canephora green seeds extracts. METHODS: The analysis of C. canephora green seeds extracts was carried out by RP-HPLC-PDA. These extracts were screened for antioxidant activities by ABTS and phenanthroline assays. The antibacterial activity was determined by microdilution method against three reference bacteria. The inhibition of bacterial adhesion at 1/8 MIC was carried out against three reference bacteria. RESULTS: The RP-HPLC-PDA revealed the presence of gallic acid, vanillin, quercetin, chlorogenic acid, and P-coumaric acid. The n-buatnol extract have the highest activity ABTS assays (3.96 ± 0.08 µg/mL). For this extract, the A0.5 was 1.90 ± 0.05 µg/mL for phenanthroline assay. The n-butanol extract and the methanolic extract have the higher antibacterial activity against Staphylococcus aureus ATCC 25923 (40 µg/mL).At MIC/8, the extracts of C. canephora showed 70% higher antidhesive activity against S. aureus ATCC 25923. CONCLUSIONS: Our finding provides an effective and specific new approach to the search of antioxidant and antiadhesive compounds for different uses.

Poly(ethyl acrylate-co-methyl Methacrylate-co-trimethylammoniethyl methacrylate chloride) (Eudragit RS100) Nanocapsules as Nanovector Carriers for Phoenix dactylifera L. Seeds Oil: a Versatile Antidiabetic Agent.

Food waste valorization practices have gained considerable attention focusing on the conversion of the waste into valuable products. In this context, the present study provides an insight into a new Eudragit RS100 based nanosystem as a carrier of date palm (Phoenix dactylifera L.) seeds oil known for its an antidiabetic activity. A priori systematic study was carried out in order to understand the individual impact of all contributing factors considered by the nanoprecipitation method. Then, date seeds oil nanoparticles were prepared, characterized and analyzed for their in vitro inhibition activity against: α-amylase and α-glucosidase. The results showed that the developed nanoparticles had an average diameter around 207 nm, a ζ-potential of +59 mV, and an encapsulation efficiency equal to 97 ± 1% with a loading capacity of 0.48 mg·mg-1. The α-amylase and α-glucosidase IC50 were found to be 87.6 and 155.3 µg·mL-1, respectively. Therefore, this study may surely open new perspectives for the development of novel health-promoting plant oils loaded-nanocarriers for several purposes.

Preliminary analysis of the chemical composition, antioxidant and anticholinesterase activities of Algerian propolis.

Many studies demonstrated that Algerian propolis possess a large spectrum of biological activity. However, few studies regarding its chemical composition are available on literature. We aimed in the present study to investigate the chemical composition of Algerian propolis. In addition, the antioxidants and anticholinesterase activities of propolis extracts are also reported. Chemical investigation of Algerian propolis allowed the isolation of 8 compounds. Their structures were identified on the basis of spectral data and comparison with literature. The isolated compounds are considered as markers of poplar and Citrus spp suggesting the use of both species as plant source of the tested propolis. The ethyl acetate extract of the tested propolis demonstrated the highest antioxidant activity. Among the tested extracts, only the petroleum ether and chloroform extracts exhibited an AChE inhibitory activity.

Phenolic constituents and antioxidant activity of Euphorbia retusa Forssk.

The aim of the present study was to evaluate the phenolic contents in capsule and root methanolic extracts of Euphorbia retusa followed by identification of phenolic on capsule extracts through high-performance liquid chromatography (HPLC- DAD) for the first time. Likewise, the antioxidant activity of both extracts was investigated by using Cupric reducing antioxidant capacity (CUPRAC). The result implies that E. retusa capsules have the highest phenolic and flavonoid contents with 105.33 ± 7.75 µg GAE.mg-1 extract 19.95 ± 0.96 µg QEs.mg-1 extract; respectively and the highest activity in CUPRAC assay with epigallocatechin 3-O-Gallate was the major flavonoid. Thus, our findings indicate that E. restusa capsules may be valorized in industrial fields.