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1.
Molecules ; 29(11)2024 May 30.
Article in English | MEDLINE | ID: mdl-38893452

ABSTRACT

This study investigates the chemical composition, nutritional, and biological properties of extracts obtained from A. melanocarpa berries using different extraction methods and solvents. Hydrodistillation and supercritical fluid extraction with CO2 allowed us to isolate fruit essential oil (HDEX) and fixed oil (SFEEX), respectively. A phenol-enriched extract was obtained using a mild ultrasound-assisted maceration with methanol (UAMM). The HDEX most abundant component, using gas chromatography-mass spectrometry (GC/MS), was italicene epoxide (17.2%), followed by hexadecanoic acid (12.4%), khusinol (10.5%), limonene (9.7%), dodecanoic acid (9.7%), and (E)-anethole (6.1%). Linoleic (348.9 mg/g of extract, 70.5%), oleic (88.9 mg/g, 17.9%), and palmitic (40.8 mg/g, 8.2%) acids, followed by α-linolenic and stearic acids, were the main fatty acids in SFEEX determined using high-performance liquid chromatography coupled with a photodiode array detector and an evaporative light scattering detector (HPLC-DAD/ELSD). HPLC-DAD analyses of SFEEX identified ß-carotene as the main carotenoid (1.7 mg/g), while HPLC with fluorescence detection (FLU) evidenced α-tocopherol (1.2 mg/g) as the most abundant tocopherol isoform in SFEEX. Liquid chromatography-electrospray ionization-MS (LC-ESI-MS) analysis of UAMM showed the presence of quercetin-sulfate (15.6%, major component), malvidin 3-O-(6-O-p-coumaroyl) glucoside-4-vinylphenol adduct (pigment B) (9.3%), di-caffeoyl coumaroyl spermidine (7.6%), methyl-epigallocatechin (5.68%), and phloretin (4.1%), while flavonoids (70.5%) and phenolic acids (23.9%) emerged as the most abundant polyphenol classes. UAMM exerted a complete inhibition of the cholesterol oxidative degradation at 140 °C from 75 µg of extract, showing 50% protection at 30.6 µg (IA50). Furthermore, UAMM significantly reduced viability (31-48%) in A375 melanoma cells in the range of 500-2000 µg/mL after 96 h of incubation (MTT assay), with a low toxic effect in normal HaCaT keratinocytes. The results of this research extend the knowledge of the nutritional and biological properties of A. melanocarpa berries, providing useful information on specific extracts for potential food, cosmetic, and pharmaceutical applications.


Subject(s)
Fruit , Photinia , Plant Extracts , Plant Extracts/chemistry , Plant Extracts/pharmacology , Fruit/chemistry , Photinia/chemistry , Humans , Antioxidants/chemistry , Antioxidants/pharmacology , Fatty Acids/analysis , Fatty Acids/chemistry , Oils, Volatile/chemistry , Oils, Volatile/pharmacology , Gas Chromatography-Mass Spectrometry , Chromatography, High Pressure Liquid/methods , Phytochemicals/chemistry , Phytochemicals/pharmacology , Phytochemicals/analysis
2.
Int J Mol Sci ; 24(6)2023 Mar 14.
Article in English | MEDLINE | ID: mdl-36982606

ABSTRACT

Citrus lumia Risso and Poit. 'Pyriformis' are horticultural varieties of Citrus lumia Risso. The fruit is very fragrant and pear-shaped, with a bitter juice, a floral flavor, and a very thick rind. The flavedo shows enlarged (0.74 × 1.16 mm), spherical and ellipsoidal secretory cavities containing the essential oil (EO), visible using light microscopy, and more evident using scanning electron microscopy. The GC-FID and GC-MS analyses of the EO showed a phytochemical profile characterized by the predominance of D-limonene (93.67%). The EO showed interesting antioxidant and anti-inflammatory activities (IC50 0.07-2.06 mg/mL), as evaluated by the in vitro cell-free enzymatic and non-enzymatic assays. To evaluate the effect on the neuronal functional activity, the embryonic cortical neuronal networks grown on multi-electrode array chips were exposed to non-cytotoxic concentrations of the EO (5-200 µg/mL). The spontaneous neuronal activity was recorded and the mean firing rate, mean burst rate, percentage of spikes in a burst, mean burst durations and inter-spike intervals within a burst parameter were calculated. The EO induced strong and concentration-dependent neuroinhibitory effects, with IC50 ranging between 11.4-31.1 µg/mL. Furthermore, it showed an acetylcholinesterase inhibitory activity (IC50 0.19 mg/mL), which is promising for controlling some of the key symptoms of neurodegenerative diseases such as memory and cognitive concerns.


Subject(s)
Citrus , Oils, Volatile , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Antioxidants/pharmacology , Antioxidants/chemistry , Citrus/chemistry , Acetylcholinesterase , Anti-Inflammatory Agents/pharmacology
3.
Int J Mol Sci ; 24(14)2023 Jul 20.
Article in English | MEDLINE | ID: mdl-37511452

ABSTRACT

Saponaria sicula Raf. grows in Sicily, Sardinia, and Algeria on limestone cliffs and volcanic sands 1300-2500 m above sea level. The aim of the present study was to investigate how the pedo-climatic conditions influence the micromorphological, phytochemical, and biological properties of Sicilian S. sicula leaves collected in the Madonie Mountains (SsM) and on Etna Mt (SsE). Micromorphological investigations revealed that leaves from SsM had a higher amount of calcium oxalate druses in the mesophyll and a more intense blue-green staining with Toluidine blue O, indicating a higher content of polyphenols. These data were confirmed by phytochemical analyses carried out on hydroalcoholic extracts, which showed a higher content of total phenols (8.56 ± 0.57 g GAE/100 g DE) and flavonoids (6.09 ± 0.17 g RE/100 g DE) in SsM. Sixty-four compounds were identified by LC-DAD-ESI-MS analysis with propelargonidin dimer as the most abundant compound (10.49% and 10.19% in SsM and SsE, respectively). The higher polyphenol content of SsM leaves matches also with their biological activity, identifying SsM extract as the strongest plant complex (IC50 2.75-477.30 µg/mL). In conclusion, the present study experimentally demonstrates that not only climatic differences but also soil characteristics affect the micromorphological, phytochemical, and biological features of this plant species.


Subject(s)
Saponaria , Antioxidants/analysis , Plant Extracts/chemistry , Polyphenols/analysis , Flavonoids/analysis , Phytochemicals/chemistry , Plant Leaves/chemistry , Sicily
4.
Molecules ; 28(10)2023 May 19.
Article in English | MEDLINE | ID: mdl-37241930

ABSTRACT

The nutritional and health properties of algae make them perfect functional ingredients for nutraceutical and cosmeceutical applications. In this study, the Phaeodactylum tricornutum Bohlin (Phaeodactylaceae), a pleiomorphic diatom commonly found in marine ecosystems, was investigated. The in vitro culture conditions used favoured the fusiform morphotype, characterized by a high accumulation of neutral lipids, as detected by fluorescence microscopy after BODIPY staining. These data were confirmed by HPLC-DAD-APCI-MS/MS analyses carried out on the ethanolic extract (PTE), which showed a high content of xanthophylls (98.99%), and in particular of fucoxanthin (Fx, 6.67 g/100 g PTE). The antioxidant activity (ORAC, FRAP, TEAC and ß-carotene bleaching) and photostability of PTE and Fx against UVA and UVB rays were firstly evaluated by in vitro cell-free assays. After this, phototoxicity and photoprotective studies were carried out on in vitro reconstructed human epidermidis models. Results demonstrated that PTE (0.1% Fx) and 0.1% Fx, both photostable, significantly (p < 0.05) reduce oxidative and inflammatory stress markers (ROS, NO and IL-1α), as well as cytotoxicity and sunburn cells induced by UVA and UVB doses simulating the solar radiation, with an excellent safety profile. However, PTE proved to be more effective than Fx, suggesting its effective and safe use in broad-spectrum sunscreens.


Subject(s)
Cosmeceuticals , Diatoms , Humans , Cosmeceuticals/pharmacology , Tandem Mass Spectrometry , Ecosystem , Xanthophylls/pharmacology , Lutein/pharmacology , Epidermis
5.
Int J Mol Sci ; 23(3)2022 Feb 01.
Article in English | MEDLINE | ID: mdl-35163632

ABSTRACT

Flavonols are a subclass of natural flavonoids characterized by a remarkable number of biotechnological applications and health-promoting properties. They attract researchers' attention due to many epidemiological studies supporting their usage. They are phytochemicals commonly present in our diet, being ubiquitous in the plant kingdom and, in particular, relatively very abundant in fruits and vegetables. All these aspects make flavonols candidates of choice for the valorization of products, based on the presence of a remarkable number of different chemical structures, each one characterized by specific chemical features capable of influencing biological targets inside the living organisms in very different manners. In this review, we analyzed the biochemical and physiological characteristics of flavonols focalizing our attention on the most promising compounds to shed some light on their increasing utilization in biotechnological applications in processing industries, as well as their suitable employment to improve the overall wellness of the humankind.


Subject(s)
Diet, Healthy , Flavonols/metabolism , Flavonols/pharmacology , Food Industry , Fruit/chemistry , Functional Food , Humans , Vegetables/chemistry
6.
Molecules ; 27(11)2022 May 26.
Article in English | MEDLINE | ID: mdl-35684369

ABSTRACT

Recently, there has been a growing interest in the recovery of agri-food waste within the circular economy perspective. In this study, the nutritional, phytochemical, and biological features of the cold-pressed hempseed oil (HSO) and hempseed meal (HSM) of two industrial hemp varieties (USO 31 and Futura 75, THC ≤ 0.2%) were evaluated. The HSOs showed a high total phenols and flavonoid content, which were confirmed by LC-DAD-ESI-MS analysis, with rutin as the most abundant compound (56.93-77.89 µg/100 FW). They also proved to be a rich source of tocopherols (81.69-101.45 mg/100 g FW) and of a well-balanced ω-6 to ω-3 fatty acid ratio (3:1) with USO 31, which showed the best phytochemical profile and consequently the best antioxidant activity (about two times higher than Futura 75). The HSMs still retained part of the phytochemicals identified in the HSOs (polyphenols, tocopherols, and the preserved ω-6/ω-3 fatty acids ratio) and a modest antioxidant activity. Furthermore, they showed a very interesting nutritional profile, which was very rich in proteins (29.88-31.44 g/100 g FW), crude fibers (18.39-19.67 g/100 g), and essential and non-essential amino acids. Finally, only a restrained amount of anti-nutritional factors (trypsin inhibitors, phytic acid, and condensed tannins) was found, suggesting a promising re-use of these byproducts in the nutraceutical field.


Subject(s)
Cannabis , Fatty Acids, Omega-3 , Refuse Disposal , Antioxidants/analysis , Antioxidants/pharmacology , Cannabis/chemistry , Fatty Acids, Omega-3/analysis , Nutrients/analysis , Phytochemicals/analysis , Phytochemicals/pharmacology , Plant Extracts , Plant Oils/chemistry , Seeds/chemistry , Tocopherols/analysis
7.
Molecules ; 27(13)2022 07 02.
Article in English | MEDLINE | ID: mdl-35807516

ABSTRACT

Peucedanum ostruthium (L.) W. D. J. Koch (Apiaceae) is a worldwide perennial herb native to the mountains of central Southern Europe. The rhizome has a long tradition in popular medicine, while ethnobotanical surveys have revealed local uses of leaves for superficial injuries. To experimentally validate these uses, plant material was collected in the Gran Paradiso National Park, Aosta Valley, Italy, and the rhizome and leaves were micromorphologically and phytochemically characterized. Polyphenol-enriched hydroalcoholic rhizome and leaf extracts, used in cell-free assays, showed strong and concentration-dependent antioxidant and anti-inflammatory activities. In vitro tests revealed cyclooxygenase and lipoxygenase inhibition by the leaf extract, while the rhizome extract induced only lipoxygenase inhibition. MTT assays on HaCaT keratinocytes and L929 fibroblasts showed low cytotoxicity of extracts. In vitro scratch wound test on HaCaT resulted in a strong induction of wound closure with the leaf extract, while the effect of the rhizome extract was lower. The same test on L929 cells showed similar wound closure induction with both extracts. The results confirmed the traditional medicinal uses of the rhizome as an anti-inflammatory and wound healing remedy for superficial injuries but also highlighted that the leaves can be exploited for these purposes with equal or superior effectiveness.


Subject(s)
Apiaceae , Plants, Medicinal , Anti-Inflammatory Agents/analysis , Anti-Inflammatory Agents/pharmacology , Lipoxygenases , Plant Extracts/analysis , Plant Extracts/pharmacology , Plant Leaves , Plants, Medicinal/chemistry , Rhizome/chemistry , Wound Healing
8.
Oncologist ; 26(1): 7-16, 2021 01.
Article in English | MEDLINE | ID: mdl-32852072

ABSTRACT

BACKGROUND: Neuregulin 1 (NRG1) fusions, which activate ErbB signaling, are rare oncogenic drivers in multiple tumor types. Afatinib is a pan-ErbB family inhibitor that may be an effective treatment for NRG1 fusion-driven tumors. PATIENTS AND METHODS: This report summarizes pertinent details, including best tumor response to treatment, for six patients with metastatic NRG1 fusion-positive tumors treated with afatinib. RESULTS: The six cases include four female and two male patients who ranged in age from 34 to 69 years. Five of the cases are patients with lung cancer, including two patients with invasive mucinous adenocarcinoma and three patients with nonmucinous adenocarcinoma. The sixth case is a patient with colorectal cancer. NRG1 fusion partners for the patients with lung cancer were either CD74 or SDC4. The patient with colorectal cancer harbored a novel POMK-NRG1 fusion and a KRAS mutation. Two patients received afatinib as first- or second-line therapy, three patients received the drug as third- to fifth-line therapy, and one patient received afatinib as fifteenth-line therapy. Best response with afatinib was stable disease in two patients (duration up to 16 months when combined with local therapies) and partial response (PR) of >18 months in three patients, including one with ongoing PR after 27 months. The remaining patient had a PR of 5 months with afatinib 40 mg/day, then another 6 months after an increase to 50 mg/day. CONCLUSION: This report reviews previously published metastatic NRG1 fusion-positive tumors treated with afatinib and summarizes six previously unpublished cases. The latter include several with a prolonged response to treatment (>18 months), as well as the first report of efficacy in NRG1 fusion-positive colorectal cancer. This adds to the growing body of evidence suggesting that afatinib can be effective in patients with NRG1 fusion-positive tumors. KEY POINTS: NRG1 fusions activate ErbB signaling and have been identified as oncogenic drivers in multiple solid tumor types. Afatinib is a pan-ErbB family inhibitor authorized for the treatment of advanced non-small cell lung cancer that may be effective in NRG1 fusion-driven tumors. This report summarizes six previously unpublished cases of NRG1 fusion-driven cancers treated with afatinib, including five with metastatic lung cancer and one with metastatic colorectal cancer. Several patients showed a prolonged response of >18 months with afatinib treatment. This case series adds to the evidence suggesting a potential role for afatinib in this area of unmet medical need.


Subject(s)
Carcinoma, Non-Small-Cell Lung , Lung Neoplasms , Adult , Afatinib/therapeutic use , Aged , Carcinoma, Non-Small-Cell Lung/drug therapy , Carcinoma, Non-Small-Cell Lung/genetics , Female , Humans , Lung Neoplasms/drug therapy , Lung Neoplasms/genetics , Male , Middle Aged , Mutation , Neuregulin-1/genetics , Oncogene Proteins, Fusion/genetics , Protein Kinase Inhibitors
9.
Phytother Res ; 35(9): 5269-5281, 2021 Sep.
Article in English | MEDLINE | ID: mdl-34173287

ABSTRACT

The aim of study was to evaluate and compare the phytochemical profile, the antioxidant and antimicrobial properties of two standardized extracts from non-psychotropic (Δ9 -tetrahydrocannabinol ≤0.2%) Cannabis sativa L. var. fibrante rich in cannabidiol (CBD). The two extracts, namely Cannabis Fibrante Hexane Extract 1 (CFHE1) and Cannabis Fibrante Hexane Extract 2 (CFHE2), were obtained by extraction with acidified hexane from dried flowering tops as such and after hydrodistillation of the essential oil, respectively. Gas chromatographic analysis showed that cannabinoids remained the predominant class of compounds in both extracts (82.56% and 86.38%, respectively), whereas a marked depletion of the terpenes occurred. Moreover, liquid chromatographic analysis highlighted a high titer of cannabidiol acid (CBDA) and CBD in CFHE1 and CFHE2, respectively. Both extracts showed a strong and concentration-dependent antioxidant activity and a potent antimicrobial activity against both Staphylococcus aureus ATCC 6538 (MIC and MBC of 4.88 µg/ml for CFHE1, and 4.88 and 19.53 µg/ml, respectively, for CFHE2) and methicillin resistant clinical strains (MIC values between 1.22 and 9.77 µg/ml and MBC values between 4.88 and 78.13 µg/ml). Considering this, the obtained results suggest that standardized extracts of C. sativa var. fibrante could find promising applications as novel antimicrobial agents.


Subject(s)
Cannabidiol , Cannabis , Plant Extracts , Anti-Infective Agents/pharmacology , Antioxidants/pharmacology , Cannabidiol/pharmacology , Dronabinol , Phytochemicals/pharmacology , Plant Extracts/pharmacology
10.
Phytother Res ; 35(2): 1099-1112, 2021 Feb.
Article in English | MEDLINE | ID: mdl-33034400

ABSTRACT

The purpose of this study was to evaluate the antioxidant and antimicrobial properties of two extracts from a new Chinese accession (G-309) of Cannabis sativa L. (Δ9 -tetrahydrocannabinol <0.2%) with high content of propyl side chain phytocannabinoids. Dried flowering tops, as such and after hydrodistillation of the essential oil, were extracted with acidic hexane to produce the Cannabis Chinese hexane extract 1 (CChHE1) and 2 (CChHE2), respectively. The phytochemical profile of CChHE1 and CChHE2 was investigated by gas chromatography-mass spectrometry (GC-MS) and liquid chromatography-diode array detector-electrospray ionization-tandem mass spectrometry (LC-DAD-ESI-MS/MS) analyses. The antioxidant properties were assessed by several in vitro cell-free assays. The antimicrobial activity was evaluated against Gram-positive and Gram-negative bacteria and the yeast Candida albicans. Phytochemical analyses highlighted a high content of cannabidivarinic acid (CBDVA) and tetraydrocannabivarinic acid (THCVA) in CChHE1, and cannabidivarin (CBDV) and tetraydrocannabivarin (THCV) in CChHE2. Both extracts showed remarkable antioxidant activity and strong antimicrobial properties (MIC 39.06 and MBC 39.06-78.13 µg/ml) against both ATCC and methicillin-resistant clinical strains of Staphylococcus aureus. In conclusion, standardized extracts of C. sativa Chinese accession could be promising for their possible use as novel antibacterial agents for the treatment of widespread S. aureus infections.


Subject(s)
Anti-Bacterial Agents/chemistry , Antioxidants/chemistry , Cannabis/chemistry , Plant Extracts/chemistry , China , Humans
11.
Molecules ; 26(21)2021 Nov 08.
Article in English | MEDLINE | ID: mdl-34771155

ABSTRACT

The phytotoxicity and eco-compatibility of essential oils (EOs) from Eucalyptus gunnii (EG) and E. pulverulenta 'Baby Blue' (EP), cultivated in Italy for their cut foliage, were investigated. Leaf micromorphology, EOs phytochemical characterization, and phytotoxicity were analysed. EP revealed a significantly higher oil gland density and a higher EO yield with respect to EG. In both EOs, 1,8-cineole was the major compound (~75%), followed by α-pinene in EG (13.1%) and eugenol in EP (7.5%). EO phytotoxicity was tested on both weeds (Lolium multiflorum, Portulaca oleracea) and crops (Raphanus sativus, Lactuca sativa, Lepidium sativum, Solanum lycopersicum, Pisum sativum, Cucumis sativus). EG EO inhibited germination of P. oleracea, R. sativus, and S. lycopersicum seeds (ranging from 61.5 to 94.6% for the higher dose used), while affecting only radical elongation in S. lycopersicum (ranging from 66.7 to 82.6%). EP EO inhibited germination of P. oleracea and R. sativus (ranging from 41.3 to 74.7%) and affected radical elongation of L. sativum and L. multiflorum (ranging from 57.4 to 76.0%). None of the EOs affected the germination and radical growing of L. sativa, P. sativum, and C. sativus. Moreover, EP EO was more active than EG EO in inhibiting α-amylase, a key enzyme for seed growth regulation. Brine shrimp lethality assay showed that both EOs are safe for aquatic organisms, suggesting their high eco-compatibility. The data collected provide useful information for future applications of these EOs in agriculture as safe and selective bioherbicides.


Subject(s)
Crops, Agricultural/drug effects , Eucalyptus/chemistry , Herbicides/pharmacology , Oils, Volatile/pharmacology , Phytochemicals/pharmacology , Plant Weeds/drug effects , Animals , Artemia , Germination/drug effects , Herbicides/chemistry , Herbicides/isolation & purification , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Phytochemicals/chemistry , Phytochemicals/isolation & purification
12.
Molecules ; 26(8)2021 Apr 08.
Article in English | MEDLINE | ID: mdl-33918091

ABSTRACT

The aim of the study was to investigate the micromorphology of Mentha pulegium leaves and flowers harvested in three different Sicilian (Italy) areas with peculiar pedo-climatic conditions, and to characterize the phytochemical profile, the phytotoxic activity, and the eco-compatibility of their essential oils (EOs) for potential use as safe bioherbicides. Light microscopy (LM) and scanning electron microscopy (SEM) highlighted that M. pulegium indumentum consists of non-glandular and glandular trichomes of different types. Peltate trichomes of plants from the different sites showed few significant differences in dimension and abundance, but they were characterized by a surprisingly high number of secretory cells both in leaves and flowers. Phytochemical analyses showed that oxygenated monoterpenes were the most abundant class in all the EOs investigated (92.2-97.7%), but two different chemotypes, pulegone/isomenthone and piperitone/isomenthone, were found. The complex of morphological and phytochemical data indicates that soil salinity strongly affects the expression of the toxic metabolite pulegone, rather than the EO yield. Phytotoxicity tests showed a moderate activity of EOs against the selected species as confirmed by α-amylase assay. Moreover, the low toxicity on brine shrimp provided a rationale for the possible use of investigated EOs as eco-friendly herbicides.


Subject(s)
Economics , Mentha pulegium/chemistry , Animals , Artemia , Flowers/anatomy & histology , Flowers/ultrastructure , Geography , Italy , Mentha pulegium/anatomy & histology , Mentha pulegium/ultrastructure , Oils, Volatile/analysis , Oils, Volatile/economics , Phytochemicals/toxicity , Plant Leaves/anatomy & histology , Plant Leaves/ultrastructure , Sus scrofa , Toxicity Tests , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism
13.
Plant Foods Hum Nutr ; 76(1): 111-117, 2021 Mar.
Article in English | MEDLINE | ID: mdl-33635514

ABSTRACT

In the present study an acidified methanol pistachio hull extract was investigated for antioxidant and inhibitory effects on melanin biosynthesis by in vitro and in vivo assays. The chromatographic analysis revealed that cyanidin-3-O-galactoside represents the main compound (98.37%). The pistachio hull extract efficiently inhibits the mono and diphenolase activity of mushroom tyrosinase (IC50= 141.07 and 116.08 µg/mL, respectively) and it was able, thanks to its strong antioxidant and free-radical scavenging activities, to hinder the L-DOPA auto-oxidation in a concentration-dependent manner (125-500 µg/mL). Results of in vivo assay showed that the treatment with pistachio hull extract (10 µg/mL) reduced pigmentation in zebrafish embryos at early stages of development (60.01% of inhibition vs control). In conclusion, these findings suggest that the ripe pistachio hull may be considered as a promising source of antioxidant and skin whitening agents for the development of new products useful in preventing the pigmentation disorders in humans and/or to improve the food quality.


Subject(s)
Pistacia , Animals , Antioxidants/pharmacology , Nuts , Plant Extracts/pharmacology , Zebrafish
14.
Phytother Res ; 34(9): 2287-2302, 2020 Sep.
Article in English | MEDLINE | ID: mdl-32309898

ABSTRACT

The aim of this study was to compare the micro-morphological features of two different non-drug Cannabis sativa L. biotypes (Chinese accession G-309 and one fibrante variety) and to evaluate the phytochemical profile as well as some biological properties of the essential oils (EOs) obtained by hydrodistillation of dried flowering tops. After a micro-morphological evaluation by scanning electron microscopy, the phytochemical composition was analysed by GC-FID and GC-MS analyses. Antioxidant and anti-acetylcholinesterase properties were investigated by several in vitro cell-free assays, while neuroactive effects were evaluated on mouse cortical neuronal as well as human iPS cell-derived central nervous system cells grown on MEA chips. Both EOs showed strong antioxidant properties mainly attributable to the high content of hydroxylated compounds as well as significant anti-acetylcholinesterase activities (IC50 74.64 and 57.31 µg/ml for Chinese accession and fibrante variety, respectively). Furthermore, they showed a concentration-dependent inhibition of spontaneous electrical activity of human and mouse neuronal networks, with the fibrante variety, which showed the best activity (MFR, IC50 0.71 and 10.60 µg/ml, respectively). The observed biological activities could be due to a synergic effect between terpenes and phytocannabinoids, although in vivo studies, which clarify the molecular mechanism, are still lacking.


Subject(s)
Acetylcholinesterase/therapeutic use , Antioxidants/therapeutic use , Cannabis/chemistry , Oils, Volatile/therapeutic use , Plant Extracts/therapeutic use , Acetylcholinesterase/pharmacology , Animals , Antioxidants/pharmacology , Humans , Mice , Oils, Volatile/pharmacology , Plant Extracts/pharmacology
15.
Phytother Res ; 34(4): 742-768, 2020 Apr.
Article in English | MEDLINE | ID: mdl-31858645

ABSTRACT

Viral infections represent one of the main causes of disease worldwide, especially today due to the increase of migration, global travel, and urbanization. The several side effects of the conventional drugs and the growing phenomenon of resistance have led researchers to turn to the plant kingdom as a source of potential new antiviral drugs. The aim of this work is to summarize the updated evidence for antiviral activity of different plants and their isolated bioactive compounds, evaluating also the potential interactions, which can occur in cotreatment with conventional antiviral drugs. The plant complexes have proved to be usually more active than their most abundant isolated compounds by hypothesizing synergistic mechanisms. In addition to cellular and molecular investigations, molecular docking studies have proved essential in highlighting the interaction mechanisms of bioactive compounds with target molecules. However, the use of nonstandardized extracts, or too high concentrations in vitro, which do not reproduce their bioavailability in vivo, are often limiting factors. Moreover, the lack of studies concerning the safety profile of plant extracts and their isolated compounds, alone or in combination with conventional antiviral drugs, is the most worrying aspect. In light of this, further studies are needed to validate their possible therapeutic use.


Subject(s)
Antiviral Agents/pharmacology , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Virus Diseases/drug therapy , Animals , Antiviral Agents/chemistry , Humans , Molecular Docking Simulation , Phytochemicals/chemistry , Phytochemicals/isolation & purification , Plant Extracts/chemistry
16.
Molecules ; 25(8)2020 Apr 19.
Article in English | MEDLINE | ID: mdl-32325864

ABSTRACT

BACKGROUND: Fruit peels are generally underutilized byproducts of the food industry, although they are valuable sources of bioactive compounds. The aim of this study is to evaluate a new application for three Citrus peel EOs as bio-herbicides. METHODS: After a micro-morphological evaluation of Citrus peels by SEM analysis, the phytochemical composition of the EOs of Citrus × bergamia Risso & Poit., Citrus × myrtifolia Raf., and Citrus limon (L.) Osbeck was characterized by GC/FID and GC/MS analyses. The in vitro phytotoxicity against germination and initial radical elongation of several crop and weed species was evaluated. Furthermore, the eco-compatibility of these EOs has been assessed by the brine shrimp (Artemia salina) lethality assay. RESULTS: SEM analysis highlighted the morphometric differences of the schizolysigenous pockets among the peels of the three Citrus species. Oxygenated monoterpenes are the main constituents in C. × bergamia (51.09%), whereas monoterpene hydrocarbons represent the most abundant compounds in C. × myrtifolia (82.15%) and C. limon (80.33%) EOs. They showed marked and selective phytotoxic activity in vitro, often at very low concentration (0.1 µg/mL) against all plant species investigated, without showing any toxicity on Artemia salina, opening the perspective of their use as safe bio-herbicides.


Subject(s)
Citrus/chemistry , Fruit/chemistry , Monoterpenes/analysis , Oils, Volatile/analysis , Plant Oils/analysis , Seeds/drug effects , Animals , Artemia/drug effects , Gas Chromatography-Mass Spectrometry , Microscopy, Electron, Scanning , Monoterpenes/chemistry , Monoterpenes/toxicity , Oils, Volatile/chemistry , Oils, Volatile/toxicity , Plant Oils/chemistry , Plant Oils/toxicity
17.
Wilderness Environ Med ; 31(3): 266-272, 2020 Sep.
Article in English | MEDLINE | ID: mdl-32682706

ABSTRACT

INTRODUCTION: The potential efficacy of selected plant extracts to counteract the dermal toxicity of jellyfish envenomation was investigated using an in vitro cell culture model. METHODS: We studied plant extracts from Carica papaya, Ananas comosus, and Bouvardia ternifolia, known for their antivenom properties, in pairwise combinations with tissue homogenates of the jellyfish Pelagia noctiluca, Phyllorhiza punctata, and Cassiopea andromeda, to evaluate modulations of jellyfish cytotoxic effects. L929 mouse fibroblasts were incubated with pairwise jellyfish/plant extract combinations and examined by MTT assay (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide). RESULTS: C papaya and A comosus significantly lowered the cytotoxicity of P noctiluca and P punctata but induced a slight worsening of C andromeda cytotoxicity. Conversely, B ternifolia was protective against P punctata, ineffective against P noctiluca, and worsened C andromeda cytotoxicity. CONCLUSIONS: Data showed species-specific and contrasting effects of plant extracts, suggesting that those containing protease activities, namely A comosus and C papaya, are more effective in lowering the cytotoxicity of jellyfish venom containing toxic peptidic factors such as phospholipase A. However, all examined plants require further investigation in vivo to evaluate their ability to counteract jellyfish injury to the skin.


Subject(s)
Antivenins/pharmacology , Cnidarian Venoms/adverse effects , Plant Extracts/pharmacology , Scyphozoa/drug effects , Ananas/chemistry , Animals , Antivenins/chemistry , Carica/chemistry , Mice , Plant Extracts/chemistry , Rubiaceae/chemistry , Tetrazolium Salts , Thiazoles
18.
BMC Complement Altern Med ; 19(1): 6, 2019 Jan 07.
Article in English | MEDLINE | ID: mdl-30612544

ABSTRACT

BACKGROUND: Candida sp. represent the most common cause of fungal infections worldwide. In the present work, we have evaluated the activity of an essential oil extracted from pistachio hulls against a number of standard and clinical strains of Candida sp. METHODS: C. albicans ATCC 64550, C. parapsilosis ATCC 22019, 4 clinical strains of C. albicans, 3 clinical strains of C. parapsilosis and 3 clinical strains of C. glabrata were used. All clinical isolates were identified by species-specific PCR-based methods. Susceptibility studies were performed using pistachio hull essential oil alone or in combination with antifungal compounds. The interactions between pistachio hull essential oil and selected antifungal compounds were also evaluated using the checkerboard method and the mechanisms of interaction investigated by droplet size distribution. RESULTS: Pistachio hull essential oil was fungicidal at the concentrations between 2.50 and 5.0 mg/ml. D-limonene and 3-Carene were the components with major activity. An antagonistic effect was observed with all combinations tested. CONCLUSION: The antifungal activity of pistachio hull essential oil could be used to help control resistance in Candida species. More studies need to be performed to elucidate the mechanisms responsible for the activity of pistachio hull essential oil.


Subject(s)
Antifungal Agents/pharmacology , Candida/drug effects , Oils, Volatile/pharmacology , Pistacia/chemistry , Plant Oils/pharmacology , Candidiasis/microbiology , Humans , Microbial Sensitivity Tests , Oils, Volatile/chemistry , Plant Oils/chemistry
19.
Phytother Res ; 33(5): 1526-1537, 2019 May.
Article in English | MEDLINE | ID: mdl-30907039

ABSTRACT

The aim of this work was to investigate the phytochemical profile and biological properties of different colours of betalain cactus pear extracts, evaluating their antioxidant, cytoprotective, and anti-angiogenic properties by cell-free, cell-based, and in vivo assays. A QuEChERS extraction method followed by RP-LC-DAD-MS/MS analysis showed that indicaxanthin and betanin were the main compounds (≥94.32% and ≥96.95%, respectively). Orange cactus pear extracts exert the best antioxidant activity in all assays carried out, in particular into ORAC (17,352.55 ± 987.407 mg trolox equivalents/100 g dry weight) and ß-carotene bleaching (60.35%) assays. The red ones, instead, showed the best cytoprotective activity decreasing the cell mortality, LDH, and Caspase-3 release ranging from 4.0 to 55%. According to antioxidant results, the orange cactus pear extracts showing also the highest anti-angiogenic activity (IC50 19.31 µg/ml), followed by the red (IC50 23.55 µg/ml) and the yellow ones (IC50 33.97 µg/ml). In light of the results and correlation analysis, the behaviour of these molecules varies a lot according to their structure and physicochemical features and synergistic activity between betalain classes may be postulated; so the plant complex could be of greater interest compared with the isolated molecules for potential nutraceutical and pharmaceutical uses.


Subject(s)
Antioxidants/chemistry , Betalains/chemistry , Fruit/chemistry , Opuntia/chemistry , Phytochemicals/therapeutic use , Plant Extracts/chemistry , Phytochemicals/pharmacology
20.
Chem Biodivers ; 16(9): e1900314, 2019 Sep.
Article in English | MEDLINE | ID: mdl-31397975

ABSTRACT

In this study, we investigated the phenolic composition of the crude extract (MeOH 80 %) of Alnus cordata (Loisel.) Duby stem bark (ACE) and its antioxidant and skin whitening properties. RP-LC-DAD analysis showed a high content of hydroxycinnamic acids (47.64 %), flavanones (26.74 %) and diarylheptanoids (17.69 %). Furthermore, ACE exhibited a dose-dependent antioxidant and free-radical scavenging activity, expressed as half-maximal inhibitory concentration (IC50 ): Oxygen radical absorbance capacity (ORAC, IC50 1.78 µg mL-1 )>Trolox equivalent antioxidant capacity (TEAC, IC50 3.47 µg mL-1 )>2,2-Diphenyl-1-picrylhydrazyl (DPPH, IC50 5.83 µg mL-1 )>ß-carotene bleaching (IC50 11.58 µg mL-1 )>Ferric reducing antioxidant power (FRAP, IC50 17.28 µg mL-1 ). Moreover, ACE was able to inhibit in vitro tyrosinase activity (IC50 77.44 µg mL-1 ), l-DOPA auto-oxidation (IC50 39.58 µg mL-1 ) and in an in vivo model it exhibited bleaching effects on the pigmentation of zebrafish embryos (72 h post fertilization) without affecting their development and survival. In conclusion, results show that A. cordata stem bark may be considered a potential source of agents for the treatment of skin disorders due to its bleaching properties and favorable safety profiles, associated to a good antioxidant power.


Subject(s)
Alnus/chemistry , Antioxidants/pharmacology , Enzyme Inhibitors/pharmacology , Polyphenols/pharmacology , Skin/drug effects , Animals , Antioxidants/chemistry , Antioxidants/isolation & purification , Biphenyl Compounds/antagonists & inhibitors , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/isolation & purification , Monophenol Monooxygenase/antagonists & inhibitors , Monophenol Monooxygenase/metabolism , Picrates/antagonists & inhibitors , Plant Bark/chemistry , Plant Extracts/chemistry , Polyphenols/chemistry , Polyphenols/isolation & purification , Zebrafish
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