Variation in Phenolic Content, Antioxidant Activity and Alpha-amylase and Acetylcholinesterase Inhibitory Capacities of Different Extracts from Tunisian Satureja barceloi (Willk) L.

The antioxidant activity and the anti-α-amylase and anti-acetylcholinesterase capacities of secondary metabolites from different organs (roots, stems, leaves and flowers) of Tunisian Satureja barceloi were determined. The variation in the distribution of phenolic metabolites among roots, stems, leaves and flowers extracts of S. barceloi with various solvent systems (methanol, ethyl acetate, hexane and distilled water) has not been characterized before. Significant variation of phenolic compounds was observed according to organs rather than to extracting solvents. The analyzed organs show a high level of phenolic compounds although the stems contains the highest total polyphenols (132.53±0.48 mg AGE/g Ex), flavonoids (48.99±0.65 mg RE/g Ex) and flavonols (34.93±0.29 mg QE/g Ex) contents. The phenolic fraction was dominated by sagerinic acid, caffeic acid glucoside and epigallocatechin, detected using HPLC-PDA/ESI-MS. The antioxidant activity of all extracts, evaluated by four in vitro tests, was high and varied significantly according to the type of solvent used and the plant organ. The aqueous extracts of leaves exhibited the greatest inhibitory effect on alpha-amylase while the methanolic extract of leaves and stems revealed the most important acetylcholinesterase inhibitory effect. Hence, S. barceloi extracts could be used as a source of various bioactive molecules in pharmaceutical industry.

Deverra triradiata Hochst. ex Boiss. from the Northern Region of Saudi Arabia: Essential Oil Profiling, Plant Extracts and Biological Activities.

Devrra triradiata Hochst. ex Boiss is an occasional plant species in the Northern region of Saudi Arabia. The shrub is favored on sandy desert wadis, gypsaceous substrate, and sandy gravel desert. In folk medicine, the plant is used for many purposes; to relieve stomach pains, against intestinal parasites, and for the regulation of menstruation. The present study describes the chemical composition of the essential oils (EOs) of different plant parts of D. triradiata. In vivo and in vitro biological activities of plant extracts and essential oils were also studied. Phenylpropanoids, elemicin (flowers: 100%), dillapiole (Stems: 82.33%; and seeds: 82.61%), and apiol (roots: 72.16%) were identified as the major compounds. The highest antioxidant activity was recorded for the EOs of roots and stems (IC50 = 0.282 µg/mL and 0.706 µg/mL, respectively). For plant extracts, ethyl acetate showed the highest antioxidant activities (IC50 = 2.47 and 3.18 µg/mL). EOs showed high antifungal activity against yeasts with low azole susceptibilities (i.e., Malassezia spp. and Candida krusei). The MIC values of EOs ranged between 3.4 mg/mL and 56.4 mg/mL. The obtained results also showed phytotoxic potential of plant extracts both on the germination features of Triticum aestivum seeds and the vegetative growth of seedlings.

Chemical Composition, Antioxidant Potential and Enzymes Inhibitory Properties of Globe Artichoke By-Products.

In this study, chemical composition and in vitro biological activities of artichoke by-products (leaves, floral stems and bracts) issued from two Tunisian varieties were evaluated. Analysis was performed by means of high-performance liquid chromatography with diode array detection coupled to electrospray ionization mass spectrometric (LC/DAD/ESI-MS). Total phenolic (TPC) and flavonoid (TFC) contents as well as the antioxidant activity conducted by three complementary methods, DPPH, ABTS and FRAP tests, were performed for each sample. Enzyme inhibitory effects against acetylcholinesterase, butyrylcholinesterase and α-amylase were also studied. Results showed that TPC and TFC varied according to variety as well as the plant part. Bracts presented the highest TPC values (10-15 mg GAE/g DW), while leaves were distinguished by the highest TFC values (52-58 mg EQ/g DW). In vitro assays showed that Violet d'Hyères bracts and Blanc d'Oran leaves present the most antioxidant activities (30.040 and 20.428 mgET/gDW, respectively, by the DPPH method). Leaves demonstrated the highest acetylcholinesterase and butyrylcholinesterase inhibitory effects. Moreover, all organs displayed a noticeable inhibition towards α-amylase. LC/DAD/MS analysis revealed that artichoke by-products are a potential source of biopharmaceuticals such as luteolin derivatives from leaves and mono/dicaffeoylquinic acids in the other parts. This research demonstrates that globe artichoke by-products, unexploited in our country, are a promising source of natural health promoting compounds with potential applications in the food and pharmaceutical industries.

Polyphenolic extracts from the xerophyte Rhamnus lycioides as a radiation biodosimeter.

The majority of dosimeters currently in use are synthetic and very expensive. Therefore, the study of the dosimetric characteristics of polyphenolic extracts of xerophytes is useful because drought stress causes an increase in the production of these cheap and natural compounds containing benzene rings. Here, the polyphenolic compounds were extracted from Rhamnus lycioides which was collected from Bou-Hedma National Park in Tunisia and identified using liquid chromatography-mass spectrometry (LC-MS). We investigated the impact of cobalt-60 (60Co) irradiation (0-30 kilogray (kGy)) on the color parameters of polyphenolic extracts of R. lycioides using the Konica Minolta CR 300 portable colorimeter and UV-Visible spectroscopy. The structural and morphological characteristics of the irradiated extracts were assessed using Fourier transform infrared (FT-IR) spectroscopy, X-ray diffraction (XRD) technique and scanning electron microscopy (SEM). Overall, our results suggest that exposure to ionizing radiation (IR) of the polyphenolic components of the xerophyte R. lycioides has produced significant dose-dependent changes in their optical and morphological properties. Thus, these extracts can be valorized as biodosimeters in the dose range from 5 to 25 kGy.

Dittrichia viscosa L. Ethanolic Extract Based Ointment with Antiradical, Antioxidant, and Healing Wound Activities.

Dittrichia viscosa which belongs to the Asteraceae family is frequently used to treat hematomas and skin disorders in Mediterranean herbal medicine. This study aims to validate its antioxidant effects and its potential on healing wounds. The ethanolic extract of D. viscosa leaves was formulated as 2.5% and 5% (w/w) in ointment bases on the beeswax and sesame oil. During this study, the ethanolic D. viscosa extract, ointments containing 2.5% and 5% of D. viscosa extract, and the vehiculum were assessed for their total phenol content (TPC), caffeoylquinic acid content (CQC), and antioxidant activities using complementary methods (TAC, the DPPH, ABTS, FRAP, and the BCB). The effects on wound healing of obtained ointments were evaluated by excision of the wound in a mice model for 12 days. Subsequently, the excised wound areas were measured at the 3rd, 9th, and 12th days. The skin tissues were isolated for histological studies. The ointments containing D. viscosa extract (2.5%, 5%) possessed a considerable TPC, CQC, radical scavenging potential, and antioxidant activities compared to the vehiculum. Treated animals with ointments containing D. viscosa extract at 2.5% and 5% showed almost and totally healed wounds compared to the vehiculum and control groups, evidenced by good skin regeneration and reepithelialization. The present work showed the role of D. viscosa antioxidants exerted by its polyphenolic compounds, in particular, caffeoylquinic acids, in enhancing wound healing.

Chemical characterization and acaricidal activity of Drimia maritima (L) bulbs and Dittrichia viscosa leaves against Dermanyssus gallinae.

The emergence of resistance to chemical acaricides in Dermanyssus gallinae, together with their toxicity and high costs, has prompted investigations into the use of plant extracts as alternatives to chemical acaricidal treatments. Drimia maritima bulbs and Dittrichia viscosa (D. viscosa) leaf extracts were here characterized by HPLC-PDA-ESI-MS/MS, and their toxicity against D. gallinae was evaluated using contact methods. Twenty-nine compounds were identified in D. maritima extracts, with glucoscilliphaeoside derivatives (i.e., quercetin, kaempferol and bufadienolides) as the major components. Twenty-four phenolic compounds, mainly caffeic acid derivatives, were detected in D. viscosa extracts. D. maritima extracts displayed a significantly higher (p < 0.05) acaricidal activity than D. viscosa extracts, with 100% of D. gallinae mortality at a concentration of 100 mg/mL following 24 h exposure. The mortality rate of D. gallinae induced by D. viscosa extracts ranged from 25 to 45% following 48 h exposure at a concentration of 200 mg/mL. The acetonic extract of D. viscosa and D. maritima displayed the highest efficacy against D. gallinae. This study provides evidence of the diversity of bioactive compounds present in D. maritima bulbs and D. viscosa leaf extracts, which are both efficacious against D. gallinae. The higher efficacy of D. maritima bulb extracts might be linked to the presence of bufadienolides in its extracts.

Phytochemical profile and biological activities of Deverra tortuosa (Desf.)DC.: a desert aromatic shrub widespread in Northern Region of Saudi Arabia.

The present study describes the chemical composition of the essential oil of different plant parts of Devrra tortuosa; in vivo and in vitro biological activities of plant extract and essential oils. Apiol was found to be the major component of the oil (between 65.73% and 74.41%). The best antioxidant activities were observed for the oil of flowers (IC50 = 175 µg/ml). The samples of stems and roots exhibit lower antioxidant activity (IC50 = 201 µg/ml and 182 µg/ml, respectively). The values of IC50 showed that the extracts of methanol exhibit the highest antioxidants activities (IC50 = 64.8 102 µg/ml). EOs showed excellent antifungal activity against yeasts with low azole susceptibilities (i.e. Malassezia spp. and Candida krusei). The MIC values of oils varied between 2.85 mg/mL and 27 mg/mL. The obtained results also showed that the plant extracts inhibited the germination and the shoot and root growth of Triticum æstivum seedlings.

Chemical Composition, Antibacterial and Antifungal Activities of Crude Dittrichia viscosa (L.) Greuter Leaf Extracts.

The small amount of data regarding the antifungal activity of Dittrichia viscosa (L.) Greuter against dermatophytes, Malassezia spp. and Aspergillus spp., associated with the few comparative studies on the antimicrobial activity of methanolic, ethanolic, and butanolic extracts underpins the study herein presented. The total condensed tannin (TCT), phenol (TPC), flavonoid (TFC), and caffeoylquinic acid (CQC) content of methanol, butanol, and ethanol (80% and 100%) extracts of D. viscosa were assessed and their bactericidal and fungicidal activities were evaluated. The antibacterial, anti-Candida and anti-Malassezia activities were evaluated by using the disk diffusion method, whereas the anti-Microsporum canis and anti-Aspergillus fumigatus activities were assessed by studying the toxicity effect of the extracts on vegetative growth, sporulation and germination. The methanolic extract contained the highest TPC and CQC content. It contains several phytochemicals mainly caffeoylquinic acid derivatives as determined by liquid chromatography with photodiode array and electrospray ionisation mass spectrometric detection (LC/PDA/ESI-MS) analysis. All extracts showed an excellent inhibitory effect against bacteria and Candida spp., whereas methanolic extract exhibited the highest antifungal activities against Malassezia spp., M. canis and A. fumigatus strains. The results clearly showed that all extracts, in particular the methanolic extract, might be excellent antimicrobial drugs for treating infections that are life threatening (i.e., Malassezia) or infections that require mandatory treatments (i.e., M. canis or A. fumigatus).

Bioactive compounds from Hypericum humifusum and Hypericum perfoliatum: inhibition potential of polyphenols with acetylcholinesterase and key enzymes linked to type-2 diabetes.

CONTEXT: Natural products are reported to have a wide spectrum of pharmacological properties such as antimicrobial, anti-inflammatory and anti-cholinesterase. The genus Hypericum (Hypericaceae) is a source of a variety of molecules with different biological activities, notably hypericin and various phenolics. OBJECTIVES: The goals of the present work were the determination of total phenolic and flavonoid content, hypericin and hyperforin concentration as well as the evaluation of biological of Hypericum humifusum L. (Hhu) and Hypericum perfoliatum L. (Hper). MATERIALS AND METHODS: The various extracts of aerial parts were powdered, and then extracted with methanol. Antibacterial activity was performed according to minimum inhibitory concentration (MIC) and minimum bactericidal (MBC) methods against four Gram-positive bacteria, four Gram-negative bacteria and yeast. RESULTS: The results revealed that H. humifusum, bear the highest total phenolic and flavonoid content (48-113 mg GAE/g and 8-41 mg RE/g, respectively) as well as hypericin (60-90 mg/g) and hyperforin (8-30 mg/g) concentration. Both species showed significant antioxidant activity as revealed by DPPH, FRAP, ABTS, and metal chelating assays. H. humifusum exhibited a strong acetylcholinesterase (3.86-4.57 mg GALAEs/g), α-glucosidase (0.73-2.55 mmol ACEs/g) and α-amylase (3-8 mmol ACEs/g) inhibitory activity. The extract of H. humifusum exhibited strong antibacterial activity mainly against Staphylococcus epidermidis, Staphylococus aureus, and Enterococcus faecium (MIC values ranging from 200 to 250 µg/mL). The highest antifungal activity was showed for H. perfoliatum extract (MIC value = 250 µg/mL). CONCLUSION: The data suggest that H. humifusum could be used as valuable new natural agents with functional properties for pharmacology industries.

Targetting αvß3 and α5ß1 integrins with Ecballium elaterium (L.) A. Rich. seed oil.

In the present study, the effect of Ecbalium elaterium seed oil on adhesion, migration and proliferation of human brain cancer cell line (U87) was determined. Treatment of U87 cell line with the seed oil resulted in strong inhibition of their adhesion to fibrinogen (Fg), fibronectin (Fn). It also reduced their migration and proliferation in a dose-dependent manner without being cytotoxic. Concomitantly, by using Matrigel™ assays, the oil significantly inhibited angiogenesis. The anti- tumor effect of the oil is specifically mediated by αvß3 and α5ß1 integrins. The presence of integrin antagonists in seed oil from E. elaterium could be used for the development of anticancer drugs with targeted "multi-modal" therapies combining anti-adhesif, antiproliferative, antimetastasic and anti-angiogenic, approaches.

Lycium intricatum Boiss.: An unexploited and rich source of unsaturated fatty acids, 4-desmethylsterols and other valuable phytochemicals.

BACKGROUND: Lycium intricatum Boiss., a Solanaceous shrubbery is used in Tunisia as a windbreak and medicinal plant. However, it is considered as underexploited specie despite its high potential to serve as source with economic and nutritional value. To date only limited information about its phytochemistry, especially of its oil has been published. This work provides data on fatty acids, phytosterols and vitamin D composition of L. intricatum seed oil. It opens up new possibilities of developing L. intricatum as a new crop that contains phytochemicals with high added value little influenced by selection or commercial breeding. FINDINGS: The composition of fatty acids, phytosterols and vitamin D in L. intricatum seed oil was assessed by GC-FID. The main fatty acids of L. intricatum seed oil were linoleic acid (49.47%), palmitoleic acid (27.96%) and erucic acid (13.62%). Palimtic acid was present at low percentage (0.63%). The content of unsaturated fatty acids was high as 94.04%. The sterolic fraction was composed of stigmasterol (18.56 mg/100 g), ß-sitosterol (13.04 mg/100 g). L. intricatum oil is an oily matrix that contains hydrocarbons, mainly squalene (63.36 mg/100 g), and two triterpenic alcohol erythrodiol (80.36 mg/100 g) and uvaol (24.06 mg/100 g). provitamin D was present in high quantity (8.12 mg/100 g). CONCLUSIONS: From these results it has been shown that L. intricatum seeds have great potential as a source of fatty acids and phytosterols for natural health products.

Essential oil composition and antibacterial activity of Origanum vulgare subsp. glandulosum Desf. at different phenological stages.

Variation in the quantity and quality of the essential oil (EO) of wild population of Origanum vulgare at different phenological stages, including vegetative, late vegetative, and flowering set, is reported. The oils of air-dried samples were obtained by hydrodistillation. The yield of oils (w/w%) at different stages were in the order of late vegetative (2.0%), early vegetative (1.7%), and flowering (0.6%) set. The oils were analyzed by gas chromatography (GC) and GC-mass spectrometry (GC-MS). In total, 36, 33, and 16 components were identified and quantified in vegetative, late vegetative, and flowering set, representing 94.47%, 95.91%, and 99.62% of the oil, respectively. Carvacrol was the major compound in all samples. The ranges of major constituents were as follows: carvacrol (61.08-83.37%), p-cymene (3.02-9.87%), and γ-terpinene (4.13-6.34%). Antibacterial activity of the oils was tested against three Gram-positive and two Gram-negative bacteria by the disc diffusion method and determining their diameter of inhibition and the minimum inhibitory concentration (MIC) values. The inhibition zones and MIC values for bacterial strains, which were sensitive to the EO of O. vulgare subsp. glandulosum, were in the range of 9-36 mm and 125-600 µg/mL, respectively. The oils of various phenological stages showed high activity against all tested bacteria, of which Bacillus subtilis was the most sensitive and resistant strain, respectively. Thus, they represent an inexpensive source of natural antibacterial substances that exhibited potential for use in pathogenic systems.