ABSTRACT
The study presents antioxidant, phytochemical, anti-proliferative, and gene repression activities against Hypoxia-inducible factor (HIF-1) alpha and Vascular endothelial growth factor (VEGF) of Elaeocarpus sphaericus extract. Elaeocarpus sphaericus dried and crushed plant leaves were extracted using water and methanol by ASE (Accelerated Solvent Extraction) method. Total phenolic content (TPC) and total flavonoid content (TFC) were used to measure the extracts' phytochemical activity (TFC). Antioxidant potential of the extracts was measured through DPPH, ABTS, FRAP, and TRP. Methanolic extract of the leaves of E.â sphaericus has shown a higher amount of TPC (94.666±4.040â mg/gm GAE) and TFC value (172.33±3.21â mg/gm RE). The antioxidant properties of extracts in the yeast model (Drug Rescue assay) showed promising results. Ascorbic acid, gallic acid, hesperidin, and quercetin were found in the aqueous and methanolic extracts of E.â sphaericus at varying amounts, according to a densiometric chromatogram generated by HPTLC analysis. Methanolic extract of E.â sphaericus (10â mg/ml) has shown good antimicrobial potential against all bacterial strains used in the study except E.â coli. The anticancer activity of the extract in HeLa cell lines ranged from 77.94±1.03 % to 66.85±1.95 %, while it ranged from 52.83±2.57 % to 5.44 % in Vero cell lines at varying concentration (1000â µg/ml-31.2â µg/ml). A promising effect of extract was observed on the expression activity of HIF-1 and VEGF gene through RT-PCR assay.
Subject(s)
Antioxidants , Elaeocarpaceae , Humans , Antioxidants/chemistry , Vascular Endothelial Growth Factor A/genetics , Plant Extracts/pharmacology , Plant Extracts/chemistry , HeLa Cells , Escherichia coli , Flavonoids/analysis , Methanol , Phenols/pharmacology , Phenols/analysis , PhytochemicalsABSTRACT
Aristotelia chilensis or "maqui" is a tree native to Chile used in the folk medicine of the Mapuche people as an anti-inflammatory agent for the treatment of digestive ailments, fever, and skin lesions. Maqui fruits are black berries which are considered a "superfruit" with notable potential health benefits, promoted to be an antioxidant, cardioprotective, and anti-inflammatory. Maqui leaves contain non-iridoid monoterpene indole alkaloids which have previously been shown to act on nicotinic acetylcholine receptors, potassium channels, and calcium channels. Here, we isolated a new alkaloid from maqui leaves, now called makomakinol, together with the known alkaloids aristoteline, hobartine, and 3-formylindole. Moreover, the polyphenols quercetine, ethyl caffeate, and the terpenes, dihydro-ß-ionone and terpin hydrate, were also obtained. In light of the reported analgesic and anti-nociceptive properties of A. chilensis, in particular a crude mixture of alkaloids containing aristoteline and hobartinol (PMID 21585384), we therefore evaluated the activity of aristoteline and hobartine on NaV1.8, a key NaV isoform involved in nociception, using automated whole-cell patch-clamp electrophysiology. Aristoteline and hobartine both inhibited Nav1.8 with an IC50 of 68 ± 3 µM and 54 ± 1 µM, respectively. Hobartine caused a hyperpolarizing shift of the voltage-dependence of the activation, whereas aristoteline did not change the voltage-dependence of the activation or inactivation. The inhibitory activity of these alkaloids on NaV channels may contribute to the reported analgesic properties of Aristotelia chilensis used by the Mapuche people.
Subject(s)
Alkaloids , Elaeocarpaceae , Humans , Alkaloids/pharmacology , Indole Alkaloids , Plant Extracts/pharmacology , Analgesics/pharmacology , Anti-Inflammatory AgentsABSTRACT
Allelopathic compounds can play a vital role in protecting the environment from pollution by synthetic herbicides. Compounds isolated from plant species with allelopathic potential can be used as natural herbicides to control weeds and help reduce environmental pollution. Elaeocarpus floribundus has been reported to contain allelopathic compounds. Aqueous methanolic extracts of the leaves of this plant showed strong growth inhibitory potential against two test species (monocotyledonous Italian ryegrass and dicotyledonous alfalfa) in plants- and dose-dependent technique. Several extensive chromatographic separations of the E. floribundus leaf extracts yielded four active compounds 1, 2, 3, and 4 (novel compound). All the identified compounds showed strong growth inhibitory potential against cress. The concentrations caused for 50% growth limitation (I50 values) of the cress seedlings were in the range 500.4-1913.1 µM. The findings indicate that the identified compounds might play a pivotal function in the allelopathic potential of E. floribundus tree. This report is the first on elaeocarpunone and its allelopathic potential.
Subject(s)
Elaeocarpaceae , Herbicides , Plant Extracts/pharmacology , Plant Extracts/chemistry , Allelopathy , Plant Weeds , Herbicides/pharmacologyABSTRACT
Maqui berry (Aristotelia chilensis) is characterized by antioxidant and anti-inflammatory properties. The aim of this study was to evaluate the effect of maqui berry extracts on human skin fibroblasts (NHSFs) exposed to ultraviolet radiation (UVB). The photoprotective properties of the extracts were investigated via the determination of the total polyphenolic content (TPC) and antioxidant capacity (DPPH), and the chemical composition was assessed. The chemical purity of the extracts was studied via the evaluation of the toxic elements level. The water extract (MWE 57.75 ± 0.44 mg GAE/g) had the highest mean polyphenol content. The water (MWE) and ethanol (MEE70) extracts had the highest inhibitory activities against DPPH radical formation (283.63 ± 7.29 and 284.60 ± 4.31 mg Tx/L, respectively). The analyzed extracts were found to be safe in terms of toxic elements (arsenic, cadmium, lead). The tested extracts of maqui berry did not cause a cytotoxic effect on NHSF cells after 24, 48, and 72 h of incubation. When the NHSF cells were exposed to UVB radiation in the presence of maqui extracts, their viability was increased or maintained. The maqui berry extracts had a slightly protective effect against skin damage caused by UVB radiation. These were preliminary studies that require further research to determine which maqui compounds correspond with the photoprotective activity.
Subject(s)
Antioxidants , Elaeocarpaceae , Humans , Antioxidants/chemistry , Fruit/chemistry , Ultraviolet Rays/adverse effects , Elaeocarpaceae/chemistry , Fibroblasts , Water/analysis , Plant Extracts/chemistryABSTRACT
Some fruits and vegetables, rich in bioactive compounds such as polyphenols, flavonoids, and anthocyanins, may inhibit platelet activation pathways and therefore reduce the risk of suffering from CVD when consumed regularly. Aristotelia chilensis Stuntz (Maqui) is a shrub or tree native to Chile with outstanding antioxidant activity, associated with its high content in anthocyanins, polyphenols, and flavonoids. Previous studies reveal different pharmacological properties for this berry, but its cardioprotective potential has been little studied. Despite having an abundant composition, and being rich in bioactive products with an antiplatelet role, there are few studies linking this berry with antiplatelet activity. This review summarizes and discusses relevant information on the cardioprotective potential of Maqui, based on its composition of bioactive compounds, mainly as a nutraceutical antiplatelet agent. Articles published between 2000 and 2022 in the following bibliographic databases were selected: PubMed, ScienceDirect, and Google Scholar. Our search revealed that Maqui is a promising cardiovascular target since extracts from this berry have direct effects on the reduction in cardiovascular risk factors (glucose index, obesity, diabetes, among others). Although studies on antiplatelet activity in this fruit are recent, its rich chemical composition clearly shows that the presence of chemical compounds (anthocyanins, flavonoids, phenolic acids, among others) with high antiplatelet potential can provide this berry with antiplatelet properties. These bioactive compounds have antiplatelet effects with multiple targets in the platelet, particularly, they have been related to the inhibition of thromboxane, thrombin, ADP, and GPVI receptors, or through the pathways by which these receptors stimulate platelet aggregation. Detailed studies are needed to clarify this gap in the literature, as well as to specifically evaluate the mechanism of action of Maqui extracts, due to the presence of phenolic compounds.
Subject(s)
Elaeocarpaceae , Fruit , Adenosine Diphosphate/metabolism , Anthocyanins/analysis , Antioxidants/analysis , Elaeocarpaceae/chemistry , Flavonoids/analysis , Fruit/chemistry , Glucose/metabolism , Plant Extracts/chemistry , Platelet Aggregation Inhibitors/metabolism , Platelet Aggregation Inhibitors/pharmacology , Polyphenols/analysis , Thrombin/metabolism , Thromboxanes/analysis , Thromboxanes/metabolismABSTRACT
Cancer is one of the leading causes of death worldwide, accountable for a total of 10 million deaths in the year 2020, according to GLOBOCAN 2020. The advancements in the field of cancer research indicate the need for direction towards the development of new drug candidates that are instrumental in a tumour-specific action. The pool of natural compounds proves to be a promising avenue for the discovery of groundbreaking cancer therapeutics. Elaeocarpus ganitrus (Rudraksha) is known to possess antioxidant properties and after a thorough review of literature, it was speculated to possess significant biomedical potential. Green synthesis of nanoparticles is an environmentally friendly approach intended to eliminate toxic waste and reduce energy consumption. This approach was reported for the synthesis of silver nanoparticles from two different solvent extracts: aqueous and methanolic. These were characterized by biophysical and spectroscopic techniques, namely, UV-Visible Spectroscopy, FTIR, XRD, EDX, DLS, SEM, and GC-MS. The results showed that the nanoconjugates were spherical in geometry. Further, the assessment of antibacterial, antifungal, and antiproliferative activities was conducted which yielded results that were qualitatively positive at the nanoscale. The nanoconjugates were also evaluated for their anticancer properties using a standard MTT Assay. The interactions between the phytochemicals (ligands) and selected cancer receptors were also visualized in silico using the PyRx tool for molecular docking.
Subject(s)
Elaeocarpaceae , Metal Nanoparticles , Anti-Bacterial Agents/chemistry , Green Chemistry Technology , Metal Nanoparticles/chemistry , Molecular Docking Simulation , Nanoconjugates , Plant Extracts/chemistry , Plant Extracts/pharmacology , Silver/chemistry , Silver/pharmacology , Spectroscopy, Fourier Transform InfraredABSTRACT
Maqui-berry is characterised by presenting a high concentration of (poly)phenols, accounting anthocyanins (cyanidin and delphinidin) for over 85% of the total. These coloured flavonoids have demonstrated potential neurological activity, but the evidence of their antinociceptive properties is scarce. In order to cover this gap, different doses (suitable for human administration) of a maqui-berry powder (1.6% anthocyanin), using enteral and parenteral routes of administration, were compared at central and peripheral levels using a nociceptive pain model (formalin test) in mice. Gastric damage analysis as possible adverse effects of analgesic and anti-inflammatory drugs was also explored. Dose-antinociceptive response was confirmed using both routes of administration and in both neurogenic and inflammatory phases of the formalin test, without gastric damage. In conclusion, these preliminary data provide evidence of pharmacological properties of maqui-berry to alleviate nociceptive pain.
Subject(s)
Analgesics , Elaeocarpaceae , Nociceptive Pain , Plant Extracts , Analgesics/pharmacology , Animals , Anthocyanins , Elaeocarpaceae/chemistry , Fruit/chemistry , Mice , Plant Extracts/pharmacologyABSTRACT
Aristotelia chilensis is a plant rich in phenolics and other bioactive compounds. Their leaves are discarded as waste in the maqui berry industry. A new application of these wastes is intended by the recovery of bioactive compounds using pressurized hot water extraction with conventional or microwave heating. Both technologies have been selected for their green character regarding the type of solvent and the high efficiency in shorter operation times. Extractions were performed in the temperature range 140-200 °C with a solid/liquid ratio of 1:15 (w:w). The extracts' total phenolic content, antioxidant capacity, and saccharides content obtained with both heating methods were measured. Additionally, the thermo-rheological properties of the gelling matrix enriched with these extracts were analyzed. Optimum conditions for lyophilized extracts were found with conventional heating, at 140 °C and 20 min extraction; 250.0 mg GAE/g dry extract and 1321.5 mg Trolox/g dry extract. Close to optimum performance was achieved with microwave heating in a fraction of the time (5 min) at 160 °C (extraction), yielding extracts with 231.9 mg GAE/g dry extract of total phenolics and antiradical capacity equivalent to 1176.3 mg Trolox/g dry extract. Slightly higher antioxidant values were identified for spray-dried extracts (between 5% for phenolic content and 2.5% for antioxidant capacity). The extracts obtained with both heating methods at 200 °C contained more than 20% oligosaccharides, primarily glucose. All the formulated gelling matrices enriched with the obtained extracts displayed intermediate gel strength properties. The tested technologies efficiently recovered highly active antioxidant extracts, rich in polyphenolics, and valuable for formulating gelling matrices with potential applicability in foods and other products.
Subject(s)
Elaeocarpaceae/chemistry , Glucose/isolation & purification , Hydrogels/chemistry , Oligosaccharides/isolation & purification , Glucose/chemistry , Oligosaccharides/chemistry , Pressure , Temperature , Water/chemistryABSTRACT
Type 2 diabetes and obesity are major problems worldwide and dietary polyphenols have shown efficacy to ameliorate signs of these diseases. Anthocyanins from berries display potent antioxidants and protect against weight gain and insulin resistance in different models of diet-induced metabolic syndrome. Olanzapine is known to induce an accelerated form of metabolic syndrome. Due to the aforementioned, we evaluated whether delphinidin-3,5-O-diglucoside (DG) and delphinidin-3-O-sambubioside-5-O-glucoside (DS), two potent antidiabetic anthocyanins isolated from Aristotelia chilensis fruit, could prevent olanzapine-induced steatosis and insulin resistance in liver and skeletal muscle cells, respectively. HepG2 liver cells and L6 skeletal muscle cells were co-incubated with DG 50 µg/mL or DS 50 µg/mL plus olanzapine 50 µg/mL. Lipid accumulation was determined in HepG2 cells while the expression of p-Akt as a key regulator of the insulin-activated signaling pathways, mitochondrial function, and glucose uptake was assessed in L6 cells. DS and DG prevented olanzapine-induced lipid accumulation in liver cells. However, insulin signaling impairment induced by olanzapine in L6 cells was not rescued by DS and DG. Thus, anthocyanins modulate lipid metabolism, which is a relevant factor in hepatic tissue, but do not significantly influence skeletal muscle, where a potent antioxidant effect of olanzapine was found.
Subject(s)
Anthocyanins/pharmacology , Elaeocarpaceae/metabolism , Glucosides/pharmacology , Anthocyanins/chemistry , Anthocyanins/metabolism , Diabetes Mellitus, Type 2/metabolism , Fatty Liver/metabolism , Glucosides/chemistry , Hep G2 Cells , Hepatocytes/metabolism , Humans , Hypoglycemic Agents/pharmacology , Insulin/metabolism , Insulin Resistance/physiology , Lipid Metabolism , Lipids/pharmacology , Liver/drug effects , Liver/pathology , Muscle Fibers, Skeletal/metabolism , Muscle, Skeletal/metabolism , Obesity/metabolism , Olanzapine , Plant Extracts/pharmacology , Polyphenols/pharmacologyABSTRACT
Treatment options for pancreatic cancer (PC) are severely limited due to late diagnosis, early metastasis and the inadequacy of chemotherapy and radiotherapy to combat the aggressive biology of the disease. In recent years, plant-derived bioactive compounds have emerged as a source of novel, anti-cancer agents. Used in traditional medicine worldwide, Elaeocarpus species have reported anti-inflammatory, antioxidant and anti-cancer properties. This study aimed to isolate and identify potential anti-PC compounds in the fruit of Elaeocarpus reticulatus Sm. A 50% acetone crude extract significantly decreased the viability of four pancreatic cell lines (≥ 10 µg/mL for BxPC-3 cells) and induced apoptosis in BxPC-3 and HPDE cells. Analysis by HPLC identified the triterpenoid Cucurbitacin I as a likely component of the extract. Furthermore, treatment with Cucurbitacin I significantly reduced the viability of HPDE and BxPC-3 cells, with results comparable to the same concentration of gemcitabine. Interestingly, attempts to isolate bioactive compounds revealed that the crude extract was more effective at reducing PC-cell viability than the fractionated extracts. This study provides initial insight into the bioactive constituents of E. reticulatus fruits.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Cell Survival/drug effects , Elaeocarpaceae/chemistry , Fruit/chemistry , Plant Extracts/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Cell Cycle/drug effects , Cell Line, Tumor , Chromatography, High Pressure Liquid , Dose-Response Relationship, Drug , Humans , Pancreatic Neoplasms , Plant Extracts/chemistry , Triterpenes/chemistry , Triterpenes/pharmacologyABSTRACT
We previously reported that the ethyl acetate (EtOAc) fraction of a 70% ethanol extract of Elaeocarpus sylvestris (ESE) inhibits varicella-zoster virus (VZV) and human cytomegalovirus (HCMV) replication in vitro. PGG (1,2,3,4,6-penta-O-galloyl-ß-D-glucose) is a major chemical constituent of the EtOAc fraction of ESE that inhibits VZV but not HCMV replication. In this study, we comprehensively screened the chemical compounds identified in the EtOAc fraction of ESE for potential antiviral properties. Among the examined compounds, quercetin and isoquercitrin displayed potent antiviral activities against both VZV and HCMV with no significant cytotoxic effects. Both compounds strongly suppressed the expression of VZV and HCMV immediate-early (IE) genes. Our collective results indicated that, in addition to PGG, quercetin and isoquercitrin are bioactive compounds in the EtOAc fraction of ESE that effectively inhibit human herpesvirus replication.
Subject(s)
Elaeocarpaceae/chemistry , Herpesviridae/drug effects , Quercetin/analogs & derivatives , Quercetin/pharmacology , Antiviral Agents/chemistry , Antiviral Agents/isolation & purification , Antiviral Agents/pharmacology , Cells, Cultured , Herpesviridae/pathogenicity , Humans , Plant Extracts/chemistry , Plant Extracts/pharmacology , Quercetin/isolation & purification , Virus Diseases/drug therapy , Virus Diseases/virology , Virus Replication/drug effectsABSTRACT
BACKGROUND: Maqui berry (Aristotelia chilensis) has been reported to have anti-glycation, anti-inflammation, lipogenesis-inhibiting activities highly related to its anti-oxidation function, but practical efficacy studies on immunological mechanisms for atopic dermatitis, have not been reported yet. OBJECTIVE: This study investigated the immune regulation mechanism of Aristotelia chilensis water extract (ACWE) related to atopic-like dermatitis . METHODS: Antioxidant and anti-inflammatory effects of ACWE was assayed. Atopy inhibitory effect was evaluated using in vitro cell study and in vivo 2,4-dinitrochlorobenzene (DNCB)-induced mouse atopic-like dermatitis model. RESULTS: ACWE has good antioxidant activities, and atopic indications were improved in ACWE group in DNCB-induced atopic-like dermatitis model of BALB/c mice. In spleen cells from mice, ACWE increased interferon-gamma (IFN-γ) levels, and decreased interleukin-4 (IL-4) levels compared with the DNCB control. CONCLUSIONS: ACWE was efficacious for atopic dermatitis which indicates that ACWE might have potential as an agent for atopic dermatitis.
Subject(s)
Anti-Inflammatory Agents/therapeutic use , Dermatitis, Atopic/therapy , Plant Extracts/therapeutic use , Spleen/immunology , Animals , Dermatitis, Atopic/chemically induced , Dinitrochlorobenzene , Disease Models, Animal , Elaeocarpaceae/immunology , Humans , Interferon-gamma/metabolism , Interleukin-4/metabolism , Mice , Mice, Inbred BALB C , RAW 264.7 Cells , WaterABSTRACT
The increasing concentration of surface ozone (O3) was observed during recent decades in the world, which affects tree roots and forest soils. Meanwhile, the impact of ozone on tree roots is greatly affected by soil condition. However, there is a lack of knowledge about the possible effects of ozone on tree roots and soil processes. In this study, The influences of surface ozone (O3) stress on the root biomass, morphology, nutrients, soil properties, and soil enzyme activity of Elaeocarpus sylvestris and Michelia chapensis seedlings were examined at four O3 concentrations (charcoal-filtered air, 1 × O3 air, 2 × O3 air, and 4 × O3 air). Elevated O3 concentrations were found to significantly increase the root C content, N content, C/P ratio, and N/P ratio, and significantly decrease the root biomass, number of root tips, and root C/N ratio of both species. The soil organic matter content, pH, total N content, and urease and catalase activities of both species tended to increase. The limitation in root growth and responses in the root structure of E. sylvestris induced by elevated O3 concentrations led to increased bulk density and decreased soil porosity and void ratio. These profound effects of O3 concentrations on the roots and soil characteristics of these two species underscore the importance of research in O3 science.
Subject(s)
Air Pollutants/toxicity , Elaeocarpaceae/drug effects , Magnoliaceae/drug effects , Ozone/toxicity , Plant Roots/drug effects , Soil/chemistry , Air Pollutants/analysis , Biomass , China , Elaeocarpaceae/growth & development , Forests , Magnoliaceae/growth & development , Ozone/analysis , Plant Leaves/drug effects , Plant Leaves/growth & development , Plant Roots/growth & development , Seedlings/drug effects , Seedlings/growth & developmentABSTRACT
Abscisic acid (ABA) regulates the physiological and biochemical mechanisms required to tolerate drought stress, which is considered as an important abiotic stress. It has been postulated that ABA might be involved in regulation of plant phenolic compounds biosynthesis, especially anthocyanins that accumulate in plants subjected to drought stress; however, the evidence for this postulate remains elusive. Therefore, we studied whether ABA is involved in phenolic compounds accumulation, especially anthocyanin biosynthesis, using drought stressed Aristotelia chilensis plants, an endemic berry in Chile. Our approach was to use fluridone, an ABA biosynthesis inhibitor, and then subsequent ABA applications to young and fully-expanded leaves of drought stressed A. chilensis plants during 24, 48 and 72 h of the experiment. Plants were harvested and leaves were collected separately to determine the biochemical status. We observed that fluridone treatments significantly decreased ABA concentrations and total anthocyanin (TA) concentrations in stressed plants, including both young and fully-expanded leaves. TA concentrations following fluridone treatment were reduced around fivefold, reaching control plant levels. ABA application restored ABA levels as well as TA concentrations in stressed plant at 48 h of the experiment. We also observed that TA concentrations followed the same pattern as ABA concentrations in the ABA treated plants. Quantitative real-time PCR revealed that AcUFGT gene expression decreased in fully-expanded leaves of stressed plants treated with fluridone, while a subsequent ABA application increased AcUFGT expression. Taken together, our results suggest that ABA is involved in the regulation of anthocyanin biosynthesis under drought stress.
Subject(s)
Abscisic Acid/metabolism , Anthocyanins/metabolism , Elaeocarpaceae/metabolism , Plant Leaves/metabolism , Droughts , Gene Expression Regulation, PlantABSTRACT
Nine new alkaloids, (+)-1, (-)-1, 2, (+)-3, (-)-3, and 4-7, along with five known compounds (8-12), were obtained from the branches and leaves of Elaeocarpus angustifolius. The alkaloids were structurally characterized by NMR and MS data. The absolute configurations of (+)-1, (-)-1, (+)-3, and (-)-3 were determined by comparing their experimental and computed electronic circular dichroism spectra. (±)-8,9-Dehydroelaeocarpine (5), (±)-9-epielaeocarpine cis-N-oxide trifluoroacetate (6), and (±)-elaeocarpine trifluoroacetate (9) exerted weak inhibitory activities against butyrylcholinesterase with IC50 values of 39, 29, and 35 µM, respectively, while that of tacrine, the positive control, was 0.07 ± 0.01 µM. This is the first report of the cholinesterase inhibitory activities of Elaeocarpus alkaloids.
Subject(s)
Alkaloids/isolation & purification , Elaeocarpaceae/chemistry , Plant Leaves/chemistry , Alkaloids/chemistry , Alkaloids/pharmacology , Biological Assay , Cholinesterase Inhibitors/pharmacology , Chromatography, High Pressure Liquid , Crystallography, X-Ray , Molecular Structure , Spectrum Analysis/methodsABSTRACT
The alkaloids aristoteline (1), aristoquinoline (2), and aristone (3) were purified from the leaves of the Maqui tree Aristotelia chilensis and chemically characterized by NMR spectroscopy. The pharmacological activity of these natural compounds was evaluated on human (h) α3ß4, α4ß2, and α7 nicotinic acetylcholine receptors (AChRs) by Ca2+ influx measurements. The results suggest that these alkaloids do not have agonistic, but inhibitory, activity on each receptor subtype. The obtained IC50 values indicate the following receptor selectivity: hα3ß4 > hα4ß2 â« hα7. In the particular case of hα3ß4 AChRs, 1 (0.40 ± 0.20 µM) and 2 (0.96 ± 0.38 µM) show higher potencies compared with 3 (167 ± 3 µM). Molecular docking and structure-activity relationship results indicate that ligand lipophilicity is important for the interaction with the luminal site located close to the cytoplasmic side of the hα3ß4 ion channel between positions -2' and -4'. Compound 1 could be used as a molecular scaffold for the development of more potent noncompetitive inhibitors with higher selectivity for the hα3ß4 AChR that could serve for novel addiction and depression therapies.
Subject(s)
Alkaloids/pharmacology , Elaeocarpaceae/chemistry , Nicotinic Antagonists/pharmacology , Receptors, Nicotinic/drug effects , alpha7 Nicotinic Acetylcholine Receptor/antagonists & inhibitors , Alkaloids/chemistry , Alkaloids/isolation & purification , Humans , Molecular Docking Simulation , Nicotinic Antagonists/chemistry , Nicotinic Antagonists/isolation & purification , Structure-Activity RelationshipABSTRACT
Combined effects of cadmium (Cd) and acid rain on physiological characteristics in Eleocarpus glabripetalus seedlings were investigated under controlled conditions. The single Cd treatment and the combined Cd and acid rain treatment increased growth at low Cd concentrations, while decreased growth and photosynthesis at high Cd2+ concentrations. A low Cd2+ concentration (50â¯mgâ¯kg-1) combined with different acid rain treatments increased the seedling biomass. A high Cd2+ concentration (100â¯mgâ¯kg-1) under different acid rain treatments significantly decreased the biomass, the Fe content, chlorophyll fluorescence and photosynthetic parameters. Relative electric conductivity, malondialdehyde (MDA) content and peroxidase (POD) activity were increased while the reduced glutathione (GSH) content and catalase (CAT) activity were significantly lower at high Cd2+ concentration under acid rain. The results indicated that the combination of a high concentration of Cd2+ and acid rain aggravated the toxic effect of Cd2+ or acid rain alone on the growth and physiological parameters of E. glabripetalus due to serious damage to the chloroplast structure. These results provide novel insights into the combined effects of Cd2+and acid rain on woody plants and might also serve as a guide to evaluate forest restoration and biological safety in areas with Cd2+and acid rain pollution.
Subject(s)
Acid Rain/adverse effects , Cadmium/adverse effects , Elaeocarpaceae/physiology , Environmental Pollution/adverse effects , Seedlings/drug effects , Chlorophyll/metabolism , Chloroplasts/drug effects , Forests , Glutathione/metabolism , Malondialdehyde/metabolism , Oxidation-Reduction , Photosynthesis/drug effects , Seedlings/physiologyABSTRACT
Obesity is a major worldwide health threat. It is characterized by an abnormal adipose tissue overgrowth together with increased monocytes infiltration, causing inflammation and oxidative stress, events associated with several illnesses. Investigations have focused on the benefits of native fruit consumption, claiming these to be natural sources of bioactive compounds with antioxidant and anti-inflammatory characteristics. It has been widely stated that berries are a source of the most antioxidant compounds, and, thus, seem highly promising to endure research efforts on these vegetal matrices. The present article describes botanical, chemical and biomedical features of the Chilean native berries, Aristotelia chilensis, Ugni molinae, and Berberis microphylla. This work aims to potentiate incoming research focused on the search for novel treatments for first-order diseases with these particular plant sources.
Subject(s)
Berberis/chemistry , Elaeocarpaceae/chemistry , Fruit/chemistry , Myrtaceae/chemistry , Obesity/drug therapy , Phytochemicals/analysis , Anti-Inflammatory Agents/analysis , Anti-Inflammatory Agents/pharmacology , Antioxidants/analysis , Antioxidants/pharmacology , Chile , Humans , Inflammation/drug therapy , Inflammation/etiology , Obesity/complications , Oxidative Stress , Phytochemicals/pharmacologyABSTRACT
Often the mutualistic roles of extinct species are inferred based on plausible assumptions, but sometimes palaeoecological evidence can overturn such inferences. We present an example from New Zealand, where it has been widely assumed that some of the largest-seeded plants were dispersed by the giant extinct herbivorous moa (Dinornithiformes). The presence of large seeds in preserved moa gizzard contents supported this hypothesis, and five slow-germinating plant species (Elaeocarpus dentatus, E. hookerianus, Prumnopitys ferruginea, P. taxifolia, Vitex lucens) with thick seedcoats prompted speculation about whether these plants were adapted for moa dispersal. However, we demonstrate that all these assumptions are incorrect. While large seeds were present in 48% of moa gizzards analysed, analysis of 152 moa coprolites (subfossil faeces) revealed a very fine-grained consistency unparalleled in extant herbivores, with no intact seeds larger than 3.3 mm diameter. Secondly, prolonged experimental mechanical scarification of E. dentatus and P. ferruginea seeds did not reduce time to germination, providing no experimental support for the hypothesis that present-day slow germination results from the loss of scarification in moa guts. Paradoxically, although moa were New Zealand's largest native herbivores, the only seeds to survive moa gut passage intact were those of small-seeded herbs and shrubs.
Subject(s)
Extinction, Biological , Herbivory , Palaeognathae/physiology , Seed Dispersal , Trees/physiology , Animals , Elaeocarpaceae/physiology , Fossils , New Zealand , Seeds/physiology , Tracheophyta/physiology , Vitex/physiologyABSTRACT
The microencapsulation of maqui juice by spray-drying and freeze-drying was studied as a strategy to protect anthocyanins in new food formulations in order to improve the anthocyanin retention before consumption and the bioaccessibility. It is well known that the encapsulation method affects both the shape and size of powders, being assumed that undefined forms of freeze-drying powders might affect their stability due to the high permeability to oxygen. The objective of this study was to compare the microencapsulation of maqui juice by spray-drying and freeze-drying, evaluating the stability of specific anthocyanins in yogurt and after in vitro digestion. Results indicated that most relevant differences between spray-drying and freeze-drying powders were the morphology and particle size that affect their solubility (70.4â»59.5%) when they were reconstituted in water. Nevertheless these differences did not affect the stability of anthocyanins as other research have proposed. Both encapsulation methods generated powders with a high stability of 3-O-monoglycosylated anthocyanins in yogurt (half-life values of 75â»69 days for delphinidin-3-sambubioside). Furthermore, no significant differences in the bioaccessibility of anthocyanins between maqui juice powders (44.1â»43.8%) were found. In conclusion, the microencapsulation of maqui juice by freeze-drying is as effective as spray-drying to produce new value-added food formulations with stable anthocyanins.