Phytotoxic effects of commercial essential oils on selected vegetable crops: Cucumber and tomato

Essential oils of Origanum vulgare L., Rosmarinus officinalis L., Thymus mastichina L., Ocimum basilicum L., Melaleuca alternifolia Maiden & Betche ex Cheel, Eucalyptus globulus Labill., Gaultheria procumbens L. and Origanum majorana L., with herbicidal effects at different doses (0.125, 0.250, 0.50 and 1 μL/mL) were tested against Cucumis sativus L. and Solanum lycopersicum L., in order to ensure their harmlessness against these Mediterranean food crops. Oregano (carvacrol 60.42%) was the most damaging essential oil, exhibiting a dose-dependent phytotoxic activity against the seed germination and seedling growth of cucumber and tomato, whereas rosemary (1,8-cineole 24.95%, camphor 20.45% and α-pinene 16.70%) essential oil was the least injurious in cucumber and tomato seed germination. The cultivated vegetable crop cucumber was more resistant to tomato at all tested essential oils. Seedling growth studies showed that the radicle was more sensitive than the hypocotyl to the essential oils. In cucumber, only M. alternifolia essential oil significantly affected the hypocotyl growth of cucumber (34.61%) at the highest dose (1 μL/mL) assayed. Rosemary essential oil could be used as pre-emergent bioherbicide in the control of weeds affecting cucumber and tomato crops.     

Inhibitory effects of wild dietary plants on lipid peroxidation and on the proliferation of human cancer cells

Thirteen hydroalcoholic extracts of edible plants from Southern Italy were evaluated for their in vitro antioxidant and antiproliferative activity on three human cancer cell lines: breast cancer MCF-7, hepatic cancer HepG2 and colorectal cancer LoVo. After 48 h of incubation the most antiproliferative plant extract was rosemary (Rosmarinus officinalis L.) on LoVo cell line with IC₅₀ of 16.60 µg/ml. Oregano (Origanum vulgare L. subsp. viridulum) showed a selective antiproliferative activity on hepatic cancer with IC₅₀ of 32.59 µg/ml.All the extracts, with the exception of Diplotaxis tenuifolia (L.) DC., exerted antioxidant properties, the most active plants being dewberry (Rubus caesius L.) and “laprista” (Rumex conglomerates Murray) with IC₅₀ of 4.91 and 5.53 µg/ml, respectively. Rumex conglomeratus contained the highest amount of flavonoids (15.5 mg/g) followed by Portulaca oleracea L. (11.8 mg/g). Rosmarinus officinalis contained the highest number of terpenes. Among them ketoursene (14.7%) and aristolone (11.3%) were found to be the major constituents. P. oleracea and Raphanus raphanistrum L. subsp. landra contained the highest number of sterols.     

Antiproliferative effect of extracts from Aristolochia baetica and Origanum compactum on human breast cancer cell line MCF-7

Aristolochia baetica L. (Aristolochiaceae) and Origanum compactum Benth. (Lamiaceae) are native plants of Morocco used in traditional medicine. In order to systematically evaluate their potential activity on human breast cancer, four different polarity extracts from each plant were assessed in vitro for their antiproliferative effect on MCF-7 cells. As a result, several extracts of those plants showed potent cell proliferation inhibition on MCF-7 cells. Chloroform extract of A. baetica (IC50: 216.06?±?15 μg/mL) and ethyl acetate of O. compactum (IC50: 279.51?±?16 μg/mL) were the most active. Thin layer chromatography examination of the bioactive extracts of A. baetica and O. compactum showed the presence of aristolochic acid and betulinic acid, respectively. These results call for further studies of these extracts.     

Protective effect of dry olive leaf extract in adrenaline induced DNA damage evaluated using in vitro comet assay with human peripheral leukocytes

Excessive release of stress hormone adrenaline is accompanied by generation of reactive oxygen species which may cause disruption of DNA integrity leading to cancer and age-related disorders. Phenolic-rich plant product dry olive leaf extract (DOLE) is known to modulate effects of various oxidants in human cells. The aim was to evaluate the effect of commercial DOLE against adrenaline induced DNA damage in human leukocytes by using comet assay. Peripheral blood leukocytes from 6 healthy subjects were treated in vitro with three final concentrations of DOLE (0.125, 0.5, and 1 mg/mL) for 30 min at 37 °C under two different protocols, pretreatment and post-treatment. Protective effect of DOLE was assessed from its ability to attenuate formation of DNA lesions induced by adrenaline. Compared to cells exposed only to adrenaline, DOLE displayed significant reduction (P < 0.001) of DNA damage at all three concentrations and under both experimental protocols. Pearson correlation analysis revealed a significant positive association between DOLE concentration and leukocytes DNA damage (P < 0.05). Antigenotoxic effect of the extract was more pronounced at smaller concentrations. Post-treatment with 0.125 mg/mL DOLE was the most effective against adrenaline genotoxicity. Results indicate genoprotective and antioxidant properties in dry olive leaf extract, strongly supporting further explorations of its underlying mechanisms of action.     

Effects of Some Lamiaceae Species Methanol Extracts on Potential Mycotoxin Producer Fungi

In this study, antifungal effects of some Lamiaceae species (Thymbra spicata L.Satureja hortensis L., Origanum onites L., O. vulgare L. subsp. hirtum (Link) Iestswaart, O. vulgare L. subsp vulgare, O. minutiflorum O. Schwarz & P.H. Davis, Sideritis vuralii H. Duman & Baser and S. caesarea H. Duman, Aytaç & Baser) commonly used by people, were investigated. To determine the antifungal effects, the aerial parts of plant methanol extracts were tested against four fungal species, Aspergillus flavus Link., A. niger Raper, and Fennel, A. ochraceus K. Wilh., and Fusarium proliferatum (Matsushima) Nirenberg. Three plant species, O. vulgare subsp. hirtum, O. minutiflorum, and T. spicata, methanol extracts showed antifungicidal activity with a minimum inhibitory concentration (MIC) of 1.6 mg/ml against four potential mycotoxigenic fungi. The results were evaluated using statistical tests.     

Medicinal Lamiaceae with antioxidant properties, a potential source of rosmarinic acid]

Hydroalcholic extracts from four native medicinal Lamiaceae, Lycopus europaeus L., Melissa officinalis L., Origanum vulgare L. and Prunella vulgaris L. have shown significant antioxidative activities, by free radical scavenger effect on DPPH, compared with those of Rosmarinus officinalis L. and Salvia officinalis L. extracts. The antioxidative activity was partly in relation to the rosmarinic acid content. The major hydroxycinnamic compound, quantitatively determinated by HPLC, was present in large amount. The content in Prunella vulgaris L. spikes average 6.1%, based on dry weight.     

Anti-Helicobactor pylori activity of some Jordanian medicinal plants

Context: Natural flora are considered a major source of new agents for the treatment of Helicobactor pylori. The plants used in this study were selected based on previous traditional use.

Objective: In this study, we evaluated the effect of extracts of 16 medicinal plants grown in Jordan against clinical isolates of H. pylori.

Materials and methods: Tested plant extracts included Aloysia triphylla (L'Her.) Britton (Verbenaceae), Anethum graveolens L. (Apiaceae), Artemisia inculata Delile (Asteraceae), Capparis spinosa L. (Capparaceae), Crataegus aronia (L.) Bosc ex. DC. (Rosaceae), Inula viscose (L.) Ait (Asteraceae), Lavandula officinalis Chaix. (Lamiaceae), Lepidium sativum L. (Cruciferae), Origanum syriaca L. (Lamiaceae), Paronychia argentea Lam. (Caryophyllaceae), Passiflora incarnate L. (Passifloraceae), Psidium guajava L. (Myrtaceae), Sarcopoterium spinosum (L.) Spach (Rosaceae), Sesamum indicum L. (Pedaliaceae), Urtica urens L. (Urticaceae) and Varthemia iphionoids Boiss (Asteraceae). Clinical isolates of H. pylori were tested in vitro for susceptibility to each of the above plant crude extracts using disk diffusion method, and the MIC value was determined for each plant extract using the serial dilution method.

Results: Results showed that ethanol extracts of most medicinal plants exerted cytotoxiciy against H. pylori isolates. Among the tested plant extracts, A. triphylla (MIC: 90?µg/mL, MBC: 125?µg/mL) and I. viscosa (MIC: 83?µg/mL, MBC: 104?µg/mL) showed the strongest activity against both isolates of H. pylori.

Discussion and conclusion: Jordanian medicinal plants might be valuable sources of starting materials for the synthesis of new antibacterial agents against H. pylori.     

Melilotus albus and Dorycnium herbaceum extracts as source of phenolic compounds and their antimicrobial,antibiofilm, and antioxidant potentials

Melilotus albus Medic. and Dorycnium herbaceum Vill. (Fabaceae) acetone, ethyl acetate, and ethanol extracts were investigated for their in vitro antimicrobial, antibiofilm, and anti-oxidant activity with quantification of phenolic compound contents. In general, D. herbaceum extracts showed better antibacterial and antioxidant activity than M. albus extracts. Bacteria Bacillus subtilis, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa, and Proteus mirabilis were the most susceptible with the minimum inhibitory concentrations (MICs), determined by microdilution method, between 1.25–10 mg/mL. Antifungal activity was lower with the detectable MICs at 10 mg/mL and 20 mg/mL. The plant extracts, using the crystal violet assay, inhibit P. aeruginosa biofilm formation in concentration range from 5 mg/mL to 20 mg/mL whereas the effect on mature bacterial biofilm was lower. The antioxidant activity was evaluated using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radicals scavenging and reducing power model systems. The intensity of DPPH radicals scavenging activity, expressed as half maximal effective concentration (EC₅₀) values, was from 84.33 μg/mL to >1000 μg/mL. The extracts demonstrated reduced power in a concentration-dependent manner, with ethanol extract as the most active. The total phenols, flavonoids, and proanthocyanidins were determined spectrophotometrically while total extractable tannins were obtained by precipitation method. The phenolic compounds showed differences in their total contents depending on solvents polarities and plant species. Although the plants M. albus and D. herbaceum have not yet been fully explored, these results contribute better understanding of their biotic properties and potential application as antimicrobial and antioxidant agents.     

Antitumor activities of extracts from selected desert plants against HepG2 human hepatocellular carcinoma cells

Abstract

Context: Phytochemicals are produced by desert plants to protect themselves against stressful environments. They have been shown to be useful in preventing and fighting adverse pathophysiological conditions and complex diseases, including cancer. Although many desert plants have been investigated for their antitumor properties, a large number of them still remain to be explored for possible therapeutic applications in oncologic diseases.

Objective: To screen the antitumor effects of selected desert plants, namely Achillea fragrantissima (Forssk.) Sch. Bip. (Compositae), Ochradenus baccatus Delile (Resedaceae), Origanum dayi Post (Lamiaceae), Phlomis platystegia Post (Lamiaceae) and Varthemia iphionoides Boiss (Compositae), against an in vitro tumor model utilizing HepG2 human hepatocellular carcinoma cells.

Materials and methods: The aqueous extracts of aerial parts of the aforementioned plants were prepared and used for the in vitro experiments. The HepG2 cells were exposed to varying concentrations (0–4?mg/mL) of each plant extract for 24 or 48?h and the cytotoxicity was measured by the MTT assay.

Results: Following 24?h exposure, O. dayi extract exhibited a substantial antiproliferative effect in HepG2 cells (IC₅₀?=?1.0?mg/mL) followed by O. baccatus (IC₅₀?=?1.5?mg/mL). All plant extracts displayed cytotoxicity following 48?h exposure. Nevertheless, a substantial effect was observed with O. dayi (IC₅₀?=?0.35?mg/mL) or O. baccatus (IC₅₀?=?0.83?mg/mL).

Conclusion: The aqueous extracts from aerial parts of O. dayi and O. baccatus possess antitumor effects against human liver cancer cells. These desert plants represent valuable resources for the development of potential anticancer agents.     

Composition and anti-oxidant,anti-cancer and anti-inflammatory activities of Artemisia herba-alba,Ruta chalpensis L. and Peganum harmala L.

In this study, biological activities of methanolic extracts from Artemisia herba-alba, Ruta chalpensis L. and Peganum harmala L. plants, collected in Centre of Tunisia, were investigated. Results showed an important phenolic composition of Artemisia herba-alba (123.95 ± 4.3 g GAE/kg of dry mass). The extract of this plant showed, using different antioxidant assays (DPPH, ABTS and AAPH/linoleic acid methods) and an IFN-γ/LPS induced RAW 264.7 murine macrophages’ assay, the highest antioxidant (IC50 (DPPH assay) 20.64 ± 0.84 mg/L) and anti-inflammatory (72% inhibition at 150 mg/L) activities, respectively. Excepting Peganum harmala L. extract, the two other extracts showed a high anticancer activity against several cell lines (human bladder carcinoma RT112, human laryngeal carcinoma Hep2 and human myelogenous leukemia K562), for A. herba-laba IC50 = 81.59 ± 4.4, 59.05 ± 3.66 and 90.96 mg/L respectively, but not on normal peripheral blood mononuclear cells. All these biological activities are well correlated with the phenolic contents of these extracts. These findings demonstrate the remarkable potential of these plants as valuable source of antioxidants with exhibit original and interesting anti-inflammatory and anticancer capacities.     

Extraction of bioactive compounds from buriti (Mauritia flexuosa L.) fruit by eco-friendly solvents: Chemical and functional characterization

Buriti (Mauritia flexuosa L.) is a palm tree found in several regions of Latin America. Buriti fruit is a rich source of bioactive compounds such as carotenoids and phenolic compounds. Thus, the aim of this study was to extract bioactive compounds from buriti fruit by ethanol and a supramolecular solvent system (SUPRAS) formed by octanoic acid aggregates. The extracts were evaluated for total carotenoids, β-carotene, phenolic compounds and antioxidant capacity. Additionally, SUPRAS extracts were characterized for antibacterial activity and modulating effect. The extraction of β-carotene with SUPRAS showed a yield of 5.82 ± 0.05 mg/g for the peel and 26.7 ± 0.02 mg/g for the pulp. In relation to total phenolic compounds, the yields were 32.1 ± 1.2 μg GAE/g for the peel and 24.53 ± 4.9 μg GAE/g for the pulp. The presence of gallic acid, quercetin and catechin stand out regarding the phenolics identified. The extracts showed antioxidant activity, with an emphasis on the extracts obtained by SUPRAS, which presented EC₅₀ (concentration required to obtain a 50% antioxidant effect) for the ABTS radical sequestration of 3.00 μg/mL for the peel and 0.84 μg/mL for the pulp. When combined with norfloxacin and gentamicin antibiotics, the extracts also showed a synergistic action against multi-resistant strains of Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Thus, the extraction of bioactive compounds from buriti fruit using a safe, biocompatible, biodegradable and environmentally friendly solvent such as SUPRAS represents potential for developing new pharmaceuticals, cosmetics and functional foods.     

Evaluation of bronchodialatory and antimicrobial activities of Otostegia fruticosa: A multi-mechanistic approach

Otostegia fruticosa, a plant belonging to the family Lamiaceae, is endemic to Ethiopia. In Ethiopian traditional medicine, O. fruticosa has been used for the treatment of several respiratory-related disorders. The present study was designed to evaluate the bronchodilatory and antimicrobial activities of O. fruticosa leaves crude extract (Of.Cr). Ex-vivo experiments were conducted on guinea-pig trachea provided with physiological oxygenated buffer solution using emkaBath setup. The crude extract was analyzed by gas chromatography-mass spectrometry. Of.Cr, showed the presence of terpenes, fragrance components, saponins, and higher fatty acids. Of.Cr when tested on contracted tracheal chains with carbamylcholine (CCh, 1 µM) and high K⁺ (80 mM) produced relaxation by showing higher potency against CCh with incomplete inhibition of high K⁺. Dicyclomine, used as a positive control, also showed selectively higher potency to inhibit CCh when compared with its effect against K⁺. In the anticholinergic curves, Of.Cr at 1 mg/mL deflected CCh-induced concentration–response curves (CRCs) competitively to the right like dicyclomine (0.03 µM) and atropine whereas a higher dose of Of.Cr (3 mg/mL) produced a non-parallel shift in the CCh curves like a higher dose of dicyclomine (0.1 µM). In the calcium channel inhibitory assay, Of.Cr at 3 & 5 mg/mL, deflected CRCs of Ca⁺⁺ to the right like verapamil, used as positive control. Of.Cr, at concentrations (1–3 mg/mL) increases cAMP levels in isolated tracheal homogenates, similar to positive control phosphodiesterase inhibitor (papaverine). When tested for antibacterial activity against standard and clinical strains, Of.Cr was found more active (MIC 475 µg/ml) against S. aureus (NCTC 6571), while the maximum inhibition (MIC 625 µg/ml) was observed by the extract when tested against MRSA. These results determine the mechanistic pathways of the observed bronchodilatory effect of Otostegia fruticosa with a combination of anticholinergic and dual inhibition of phosphodiesterase and voltage-gated Ca⁺⁺ channels.     

Optimization of fermentation process of Cordyceps militaris and antitumor activities of polysaccharides in vitro

The influence of medium composition and cultural conditions on simultaneous yield of mycelia, intracellular polysaccharide, adenosine, and mannitol by Cordyceps militaris CGMCC 2909 was investigated with desirability functions in this study. An optimization strategy based on the desirability function approach, together with response surface methodology (RSM) has been used to optimize medium composition, and the optimal medium was obtained via the desirability as follows: yeast extract 10.33 g/L, sucrose 27.24 g/L, KH₂PO₄ 5.60 g/L and the optimal culture conditions are initial pH 6, 25°C, rotation speed 150 r/minute, inoculum size 4%(v/v), and medium capacity 40 mL/250 mL. Under these conditions, the yield of mycelia, intracellular polysaccharide, adenosine and mannitol reached 12.19 g/L, 0.6 g/L, 61.84 mg/L, and 1.38 g/L, respectively, and the D value was 0.77. Furthermore, the polysaccharides showed significant antitumor activities against HeLa and HepG2 in vitro in a dose-dependent manner in 72 hours. At a concentration of 1000 mg/mL, the inhibition rate of polysaccharides was 92.38% and 98.79%. The IC50 for HeLa and HepG2 were 70.91 μg/mL and 97.63 μg/mL, respectively.     

Analysis of Peganum harmala,Melia azedarach and Morus alba extracts against six lethal human cancer cells and oxidative stress along with chemical characterization through advance Fourier Transform and Nuclear Magnetic Resonance spectroscopic methods towards green chemotherapeutic agents

Traditional medicines implicate consumption of plant crude extracts, which may consist of extensive phytochemical diversity. Overall, the most biologically active extract of Peganum harmala (seeds) exhibited significant cytotoxic activity on Artemia salina with LC₅₀ value of 61.547 µg/mL, while P. harmala (roots) [LC₅₀ = 124.229 µg/mL] and M. azedarach (fruits) [LC₅₀ = 147.813 µg/mL] showed moderate cytotoxic potential. P. harmala (seeds) extract also showed the maximum antitumor potential with 52.278 µg/mL LC₅₀. Branches of P. harmala and Morus alba were not active in both bioassays. These outcomes were further reinforced by the levels of phenolics and flavonoids checked against gallic acid and quercetin equivalents, respectively, by standard curves. Current study aims to isolate, structurally characterize and analyze the bioactive compound from plant extracts by using chromatographic and spectrophotometric techniques. Bioactivity guided isolation of extracts led to the isolation of PH-HM-16 from ethyl acetate fraction P. harmala seeds. Chemical structure of PH-HM-16 was elucidated by ESI-MS, ¹H NMR, ¹³C NMR, HSQC and IR spectrum. The results demonstrated significant positive anticancer activities against six human cancer cell lines assessed through MTT cancer cell growth inhibition assay. PH-HM-16 was most effective against prostate cancer cell lines [IC₅₀ = 17.63 µg/mL] followed by breast cancer cell line MCF7 [IC₅₀ value of 41.81 µg/mL]. IC₅₀ value of PH-HM-16 against human myeloid leukemia cell line HL-60 and human colorectal tumor cells HCT-116 was observed as 68.77 µg/mL and 71.54 µg/mL respectively. The IC 50 value of PH-HM-16 compound was not significant against human gastric cancer SGC-7901 (111.89 µg/mL) and human lung adenocarcinoma epithelial cell line A549 (176.04 µg/mL). Isolated bioactive metabolite PH-HM-16 possesses significant antitumor potential so this could be the first step to develop an effective anticancer agent. Hence, this compound represents a promising potential to be chemically standardized or developed into pharmaceuticals for the chemoprevention and/or the treatment of certain types of cancer, especially as adjuvant phytotherapeutics in conventional chemotherapy.     

Effects of Essential Oils and Extracts from Certain Thymus. Species on Swimming Performance in Mice

Abstract

The effect of the methanol extracts and essential oils from the aerial parts of Thymus fallax. Fisch. & C.A. Mey. (Lamiaceae), T. kotschyanus. Boiss. et Hohen., and T. pubescens. Boiss. et Kotschy ex Celak on mouse swimming performance were studied using different doses. On the basis of our findings, the methanol extracts and oils shortened remarkably the immobility period during the forced swimming test in comparison with negative control and exhibited a dose-dependent antidepressant activity. The duration of immobility observed via the essential oils was less than that via the extracts in these experiments. The results of tests showed that the extracts and oils of T. fallax. had more antidepressant activity than T. kotschyanus. and T. pubescens..     

In vivo and in vitro antiviral activity of five Tibetan medicinal plant extracts against herpes simplex virus type 2 infection

Extracts from five Tibetan medicinal plants collected from the Tibetan Plateau were evaluated for antiviral activity against herpes simplex virus type 2 (HSV-2) in vitro and in vivo. Viral plaque reduction assays showed that extracts from four out of five plants inhibited HSV-2 infection significantly with 50% effective concentrations (EC₅₀) values ranging from 0.35?±?0.11 to 1.83?±?0.21?mg/mL. The other plant, Swertia mussotii Franch. (Gentianaceae), exhibited activity in inhibiting the viral biosynthesis. In the attachment assay, two plants, Dracocephalum heterophyllum Benth. (Lamiaceae) and Dracocephalum tanguticum Maxim. (Lamiaceae) reduced the attachment of HSV-2 to cell surface. Interestingly, all of the extracts showed virucidal activity. Analyzed by real-time PCR, three extracts showed strong inhibition of HSV DNA replication with Dracocephalum heterophyllum and Dracocephalum tanguticum at the concentration of 4?mg/mL and Lagotis brevituba Maxim. (Scrophulariaceae) at 1?mg/mL. BALB/c mice were used for determining in vivo efficacy. Mice encephalitis herpes models were established by infection with HSV-2. The extracts of Dracocephalum heterophyllum, Dracocephalum tanguticum, and Swertia mussotii at a dose of 1?g/kg per day significantly prolonged the mean survival times and reduced the mortality of HSV-2 infected mice compared with control group (P?<?0.05). Taken together, we conclude that the antiviral mechanisms of these plants involve various stages of virus replication. Extracts from three of these plants, Dracocephalum heterophyllum, Dracocephalum tanguticum, and Swertia mussotii, may be possible candidates in developing anti-HSV-2 medicine.     

Low temperature preservation: Influence of putative bioactive microalgae and hop extracts on sperm quality and bacterial load in porcine semen

The frequent use of antibiotics in artificial insemination promotes the development of antibiotic resistance. Therefore, alternatives must be considered. In this study, putative bioactive microalgae and hop extracts were examined to estimate their effect on quality and bacterial load of preserved porcine semen when used a low-temperature storage at 5 °C in Androstar® Premium (ASP) extender (Minitüb). Firstly, five algae extracts (Neochloris oleoabundans (NEO), Pseudococcomyxa simplex (PSEY), Phormidium ambiquum (PHA), Schizochlamydella minutissima (SCH), Cyanidioschyzon merolae (CYA)) and one hop extract (Humulus lupulus (HOP)) in four concentrations (0.2, 2, 20 and 200 μg/mL) were tested on their sperm-compatibility at 17 °C. All extracts in the concentrations 0.2 and 2 μg/mL appeared to be sperm compatible. After 72 h of storage at 5 °C, variants showed an increase of total bacterial subcultures from 103 (ASP w/o supplements) to 113/136/135/136/126/118 (ASP w/NEO/PSEY/PHA/HOP/SCH/CYA). Even though bacterial growth was not inhibited in general, all extracts showed an antimicrobial effect on specific bacteria, including Gram-positive (Trueperella pyogenes, Streptococcus porcinus) and Gram-negative bacterial species (Alcaligenes faecalis, Pseudomonas aeruginosa, Ralstonia sp., Pasteurella sp., Proteus sp., Providencia stuartii, and Escherichia coli). While the proportion of these species was 10% in the control (ASP w/o supplements), their proportion in the supplemented variants ranged from 8% (NEO, HOP) to as low as 3% (PSEY). Although the tested extracts are not suitable to replace conventional antibiotics due to their lack of broad-spectrum antimicrobial activity, they nevertheless present promising opportunities for bacteria-specific, customizable usage in boar semen extenders combined with antibiotics or other antimicrobial agents.     

Characterization of phenolic compounds in flowers of wild medicinal plants from Northeastern Portugal

Crataegus monogyna, Cytisus multiflorus, Malva sylvestris and Sambucus nigra have been used as important medicinal plants in the Iberian Peninsula since a long time ago, and are claimed to have various health benefits. This study aimed to determine the phenolic profile and composition of wild medicinal flowers of those species. The analysis was performed by HPLC–DAD–ESI/MS. Flavonoids, and particularly flavonols and flavones, were the main groups in almost all the studied samples. C. multiflorus sample gave the highest levels of total flavonoids (54.5 mg/g dw), being a chrysin derivative the most abundant flavone found (22.3 mg/g dw). C. monogyna revealed the highest concentration in phenolic acids (5.5 mg/g dw) that were not found in C. multiflorus sample; 5-O-caffeoylquinic acid was the most abundant phenolic acid found in the first species, being a procyanidin trimer also found (1.4 mg/g dw). Kaempferol-3-O-rutinoside (0.84 mg/g dw) and quercetin-3-O-rutinoside (14.9 mg/g dw) were the main flavonols present in M. sylvestris and S. nigra, respectively. Due to the well established antioxidant activity of phenolic compounds, the studied wild medicinal flowers could be selected for processing extracts with health-promoting properties or to be incorporate into functional beverages or products with bioactive properties related to oxidative stress.     

Cytotoxic effects of extracts obtained from plants of the Oleaceae family: bio-guided isolation and molecular docking of new secoiridoids from Jasminum humile

ContextTraditionally, Oleaceae plants are used to treat many diseases, such as rheumatism, hypercholesterolaemia, or ulcers.ObjectivesTo investigate the cytotoxic potential of Jasminum humile L., Jasminum grandiflorum L., and Olea europaea L. (Oleaceae) extracts against selected human cancer cells lines, followed by a phytochemical investigation of the most potent one.Materials and methodsThe 95% ethanol extracts of aerial parts of three oleaceous plants were examined for their cytotoxicity against HepG-2, MCF-7, and THP-1 cell lines using MTT assay and doxorubicin (positive control). J. humile was bio-selected and submitted to bio-guided fractionation. Chromatographic workup of ethyl acetate and n-butanol fractions afforded two new compounds; 1-methoxyjasmigenin (1) and 1-methyl-9-aldojasmigenin (2), along with five known ones (3–7). Structures were unambiguously elucidated using 1D/2D NMR and ESI-HRMS. Isolated compounds were assessed for their anti-proliferative potential, and both selectivity index and statistical significance were determined. Molecular docking was conducted against the Mcl-1 receptor using (AZD5991) as a standard.ResultsJasmoside (5) was the most potent anticancer compound showing IC₅₀ values of 66.47, 41.32, and 27.59 µg/mL against HepG-2, MCF-7, and THP-1 cell lines, respectively. Moreover, isojasminin (4) exhibited IC₅₀ values of 33.49, 43.12, and 51.07 µg/mL against the same cell lines, respectively. Interestingly, 5 exhibited the highest selectivity index towards MCF-7 and THP-1, even greater than doxorubicin. Molecular docking results were in full agreement with the MTT assay and the proposed SAR.ConclusionIn this study, two new compounds were purified. The biological activity highlighted jasmoside (5) as a lead anticancer drug for further future investigation.     

Cardiotonic effect of <Emphasis Type="Italic">Apocynum venetum</Emphasis> L. extracts on isolated guinea pig atrium

The effects on guinea-pig heart muscle of extracts of Apocynum venetum L. leaf, root, stem, old stem and Venetron—a polyphenol-rich extract of leaves—were studied by recording the mechanical activity and heart rate of isolated right atria. Cymarin—a cardiac glycoside—was also determined in A. venetum extracts by LC–MS/MS analysis. All extracts examined here showed a weak cardiotonic effect, i.e., induced a contractile response of the isolated atria and increased the pulse at a concentration of 1 mg/mL, which was not inhibited by propranolol (1 μM)—a β-adrenoceptor blocker. The cymarin content in extracts of A. venetum was ranked as follows: old stem >> stem > root > leaf >> Venetron. Since the cardiotonic effects of A. venetum extracts did not reflect the cymarin content, a possible mechanism other than that of cardiac glycosides was investigated. The inhibitory effects on phosphodiesterase 3 (PDE3) were studied in a cell-free enzyme assay; all extracts of various parts of A. venetum inhibited PDE purified from human platelets. These results suggest that PDE3 inhibition may contribute to the cardiotonic effects of A. venetum extracts.