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Keywords = phyto-inhibitory activity

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25 pages, 9717 KB  
Article
Phyto-Sesquiterpene Lactones Prevent the Development of Multidrug Resistance in TNBC via ABC Transporters Inhibition and STAT3/MYC Signaling
by Ying-Tzu Chang, I-Ting Wu, Chien-Hsing Lee and Chin-Chuan Hung
Cancers 2025, 17(8), 1321; https://doi.org/10.3390/cancers17081321 - 14 Apr 2025
Cited by 1 | Viewed by 845
Abstract
Background: Multidrug resistance (MDR) in triple-negative breast cancer (TNBC) leads to treatment failure and tumor recurrence. Dysregulation of the MYC oncogene is associated with the pathogenesis of TNBC and the development of chemoresistance via overexpression of ATP-binding cassette (ABC) transporters. Therefore, in the [...] Read more.
Background: Multidrug resistance (MDR) in triple-negative breast cancer (TNBC) leads to treatment failure and tumor recurrence. Dysregulation of the MYC oncogene is associated with the pathogenesis of TNBC and the development of chemoresistance via overexpression of ATP-binding cassette (ABC) transporters. Therefore, in the present study, we aimed to identify molecules from a natural product origin that prevent the development of MDR in TNBC by targeting the MYC signaling. Methods: The cell viability of TNBC was evaluated using sulforhodamine assay. Protein levels were detected by western blots or enzyme-linked immunosorbent assays. Intracellular calcein and hoechst33342 accumulation assay aimed to evaluate the inhibitory ability of phytocompounds on drug-efflux functions of ABCB1 and ABCG2 transporters. The Cancer Genome Atlas (TCGA) database was used to explore clinical genomic data. Furthermore, the zebrafish xenotransplantation model bearing Dil-labeled TNBC cells was applied to testify the in vivo effects of phyto-sesquiterpene lactones. Results: The results of the present study demonstrated that the phyto-sesquiterpene lactones exhibited an MDR prevention effect by repressing efflux activities of ABCB1 and ABCG2 transporters. Mechanistic studies showed that phyto-sesquiterpene lactones inducted TNBC cell apoptosis and cell cycle G2/M arrested by blocking the STAT3/MYC pathway. Clinical genomic data demonstrated that the percentages of MYC amplification and mRNA were upregulated approximately two-fold higher in the TNBC patients than the non-TNBC breast cancer patients. The survival of patients with an alteration in MYC was significantly lower in TNBC as compared to other subtypes. Moreover, the results of the zebrafish xenograft model confirmed that phyto-sesquiterpene lactones exerted stronger inhibitory effects on TNBC tumor growth in vivo. Conclusions: In conclusion, these three phyto-sesquiterpene lactones were promising candidates for TNBC treatment and shed light on the prevention of developing MDR TNBC. Full article
(This article belongs to the Section Cancer Drug Development)
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22 pages, 1497 KB  
Article
Investigations of In Vitro Anti-Acetylcholinesterase, Anti-Diabetic, Anti-Inflammatory, and Anti-Cancer Efficacy of Garden Cress (Lepidium sativum Linn.) Seed Extracts, as Well as In Vivo Biochemical and Hematological Assays
by Ahmed M. Naglah, Abdulrahman A. Almehizia, Mohamed A. Al-Omar, Asma S. Al-Wasidi, Mayada H. Mohamed, Sanad M. Alsobeai, Ashraf S. Hassan and Wael M. Aboulthana
Pharmaceutics 2025, 17(4), 446; https://doi.org/10.3390/pharmaceutics17040446 - 31 Mar 2025
Cited by 1 | Viewed by 1138
Abstract
Background/Objectives: The current research was designed to quantify the active phyto-constituents and investigate the in vitro biological efficiency of different garden cress (Lepidium sativum Linn.) seed extracts against chronic diseases as well as the in vivo toxicities that may be induced in [...] Read more.
Background/Objectives: The current research was designed to quantify the active phyto-constituents and investigate the in vitro biological efficiency of different garden cress (Lepidium sativum Linn.) seed extracts against chronic diseases as well as the in vivo toxicities that may be induced in mice upon the administration of each extract at both studied therapeutic doses. Methods: The in vitro biological efficiency of different L. sativum extracts, such as methanolic, aqueous, acetone, and ethyl acetate extracts, was assessed. The inhibition percentage (%) and the median inhibitory concentration (IC50) values of different L. sativum extracts were estimated against acetylcholinesterase enzyme, diabetes mellitus (α-amylase and α-glucosidase enzymes), and inflammation (cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), and 5-lipoxygenase (5-LOX) enzymes). Additionally, the median inhibitory concentration (IC50) values of different L. sativum extracts against HepG-2, Caco-2, and A549 cells were assessed using 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Moreover, the toxicities that might be induced in mice at hematological (using an automatic blood analyzer) and biochemical levels were evaluated. Results: It was found that the methanolic L. sativum extract possessed the highest in vitro biological activities compared to the other studied extracts. The inhibition percentage values of the methanolic extract were 51.34, 54.35, 44.10, 43.48, and 40.78% against acetylcholinesterase, α-amylase, α-glucosidase, protein denaturation, and proteinase enzymes, respectively. The methanolic extract also exhibited an inhibitory effect against the COX-1 (55.05%), COX-2 (57.30%), and 5-LOX (50.15%) enzymes. Additionally, the methanolic extract possesses the highest cytotoxic activity against HepG-2, Caco-2, and A549 cells, with IC50 values of 52.27, 40.73, and 37.95 μg/mL, respectively. The median lethal doses (LD50) showed that the methanolic extract was safer when administered orally, followed by aqueous and acetone, then ethyl acetate extract. It was found that methanolic, aqueous, and acetone extracts showed no alterations when administered orally at two studied doses (1/10 and 1/20 of LD50) compared to the control. Conclusions: This study concluded that the methanolic extract possessed the highest in vitro biological activities and was safer than the other studied extracts, followed by aqueous, acetone, and then ethyl acetate extract. In the future, the in vivo biological efficacy of the methanolic L. sativum extract will be evaluated, as well as an elucidation of its mechanism against chronic diseases. Full article
(This article belongs to the Section Drug Targeting and Design)
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22 pages, 11600 KB  
Article
Comprehensive GC-MS Characterization and Histochemical Assessment of Various Parts of Three Colchicum Species from Bulgarian Flora
by Ivayla Dincheva, Ilian Badjakov, Vasil Georgiev, Ivanka Semerdjieva, Radka Vrancheva, Ivan Ivanov and Atanas Pavlov
Plants 2025, 14(2), 270; https://doi.org/10.3390/plants14020270 - 18 Jan 2025
Cited by 5 | Viewed by 1396
Abstract
This study presents a comprehensive phyto- and histochemical analysis of three Colchicum species: Colchicum autumnale L., the Balkan endemic Colchicum bivonae Guss., and the Bulgarian endemic Colchicum diampolis Delip. et Česchm. Using gas chromatography-mass spectrometry (GC-MS), 66 metabolites were identified, encompassing free amino, [...] Read more.
This study presents a comprehensive phyto- and histochemical analysis of three Colchicum species: Colchicum autumnale L., the Balkan endemic Colchicum bivonae Guss., and the Bulgarian endemic Colchicum diampolis Delip. et Česchm. Using gas chromatography-mass spectrometry (GC-MS), 66 metabolites were identified, encompassing free amino, organic, phenolic, and fatty acids, sugars, and alkaloids, which were distributed among various plant parts. Organ-specific metabolic patterns revealed that corms and seeds are particularly rich in alkaloids, supporting their roles in chemical defense and survival during dormancy. Conversely, flowers, leaves, and capsules were enriched with energy-related and phenolic compounds, playing critical roles in reproduction and stress tolerance. Histochemical investigations localized alkaloids predominantly in the endosperm of seeds, parenchyma of corms, and vascular bundles of flowers. Notably, the endemic C. bivonae and C. diampolis displayed unique chemical profiles. Moderate acetylcholinesterase inhibitory activity (AChE) was observed across various plant organs. Statistical analyses demonstrated significant interspecies and organ-specific chemical differentiation, with certain metabolites serving as key markers. These findings enhance our understanding of the chemical composition, organ specialization, and potential as a source of new biomolecules in these Colchicum species. They underscore the ecological and pharmacological importance of endemic taxa and provide a framework for future research into their sustainable utilization and potential bioactivities. Full article
(This article belongs to the Section Phytochemistry)
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24 pages, 5777 KB  
Article
Inhibitory Effects and Composition Analysis of Romanian Propolis: Applications in Organic and Sustainable Agriculture
by Gabriel Heghedűş-Mîndru, Mirel Glevitzky, Ramona Cristina Heghedűş-Mîndru, Gabriela-Alina Dumitrel, Maria Popa, Ioana Glevitzky, Diana Obiștioiu, Ileana Cocan and Mihaela Laura Vică
Plants 2024, 13(23), 3355; https://doi.org/10.3390/plants13233355 - 29 Nov 2024
Cited by 2 | Viewed by 1645
Abstract
Propolis is a sustainable and environmentally friendly agrochemical of natural origin, a resinous mixture produced by honeybees. It is used as a natural remedy in multiple pathologies., but it is also a natural defense enhancer, a phytostimulator that helps to bind, bloom, and [...] Read more.
Propolis is a sustainable and environmentally friendly agrochemical of natural origin, a resinous mixture produced by honeybees. It is used as a natural remedy in multiple pathologies., but it is also a natural defense enhancer, a phytostimulator that helps to bind, bloom, and pollinate plants. Propolis is used in organic farming as a phytoprotector and phytostimulator. The present study investigates the main physical–chemical parameters of Romanian propolis, its antifungal activity against five fungal strains (Aspergillus niger, Aspergillus flavus, Penicillium chrysogenum, Fusarium oxysporum, and Rhizopus stolonifer) and its phyto-inhibitory activity when it is applied on the layer and under the layer for different grain crops (wheat, maize, oats, and barley). Different doses were used—1, 5, and 10 g of propolis powder—and the growth of the plume was monitored for 13 days. The physical–chemical parameters investigated are volatile oils, wax, oxidation index, melting point, dry matter, ash, and resin, and maximum values were obtained for phenols (189.4 mgGAE/g), flavonoids (84.31 mgQE/g), and IC50 (0.086 µg/mL). Propolis demonstrates high antifungal activity against all fungal strains. The results showed that propolis has the best phyto-inhibition potential among the studied grain crops when it is applied on the layer, with the lowest plume growth for maize (14 mm), followed by oats, barley, and lastly wheat (24 mm). Propolis can find increasing application in sustainable and environmentally friendly agriculture and the obtaining of organic food. Full article
(This article belongs to the Section Phytochemistry)
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17 pages, 1335 KB  
Article
The In Vitro Antibacterial Activity of Phytogenic and Acid-Based Eubiotics against Major Foodborne Zoonotic Poultry Pathogens
by Konstantinos Kiskinis, Tilemachos Mantzios, Vangelis Economou, Evanthia Petridou, Anestis Tsitsos, Apostolos Patsias, Ioanna Apostolou, Georgios A. Papadopoulos, Ilias Giannenas, Paschalis Fortomaris and Vasilios Tsiouris
Animals 2024, 14(11), 1611; https://doi.org/10.3390/ani14111611 - 29 May 2024
Cited by 1 | Viewed by 1816
Abstract
The aim of the study was to investigate in vitro the antibacterial activity of 8 commercial drinking water additives against major zoonotic poultry pathogens (Campylobacter spp., Escherichia coli, Salmonella Typhimurium, Staphylococcus aureus and Listeria spp.). We tested two essential oil-based phytogenics [...] Read more.
The aim of the study was to investigate in vitro the antibacterial activity of 8 commercial drinking water additives against major zoonotic poultry pathogens (Campylobacter spp., Escherichia coli, Salmonella Typhimurium, Staphylococcus aureus and Listeria spp.). We tested two essential oil-based phytogenics (Phyto CSC Liquide B, AEN 350 B Liquid), two acid-based eubiotics (Salgard® liquid, Intesti-Flora), and four blends of essential oils and organic acids (ProPhorceTM SA Exclusive, Herbal acid, Rigosol-N and Eubisan 3000). The antibacterial activity was determined by estimating the minimum inhibitory concentration (MIC) using a microdilution method. The MICs of the products against Campylobacter spp. ranged from 0.071% to 0.568% v/v, in which Herbal acid, a blend rich in lactic and phosphoric acids, also containing thyme and oregano oils, exhibited the highest efficacy (MIC: 0.071% v/v) against all the tested strains. The MICs of the tested products against Escherichia coli ranged between 0.071% and 1.894% v/v. Specifically, the MIC of Rigosol-N, a blend of high concentrations of lactic and acetic acid, was 0.142% v/v for both tested strains, whereas the MICs of Intesti-Flora, a mixture rich in lactic and propionic acid, ranged from 0.284% to 0.568% v/v. The MICs of the products against Salmonella Typhimurium were between 0.095% and 1.894% v/v. Specifically, the MIC of Eubisan 3000, a blend rich in oregano oil, was 0.284% v/v. The MICs against Staphylococcus aureus were between 0.142% and 9.090% v/v. The MICs of Phyto CSC Liquide B, which is rich in trans-cinnamaldehyde, were between 3.030% and 9.090% v/v, showing the highest MIC values of all tested products. Finally, the MIC values of the tested commercial products against Listeria spp. were 0.095% to 3.030% v/v. The MICs of ProPhorceTM SA Exclusive, a highly concentrated blend of formic acid and its salts, were 0.095–0.142% v/v against Listeria spp., while the MICs of AEN 350 B Liquid were between 0.284% and 1.894% exhibiting high Listeria spp. strain variability. In conclusion, all the selected commercial products exhibited more or less antibacterial activity against pathogenic bacteria and, thus, can be promising alternatives to antibiotics for the control of zoonotic poultry pathogens and the restriction of antimicrobial-resistant bacteria. Full article
(This article belongs to the Special Issue Recent Advance in Veterinary Microbiology)
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22 pages, 2943 KB  
Article
Biocomposite Materials Derived from Andropogon halepensis: Eco-Design and Biophysical Evaluation
by Marcela-Elisabeta Barbinta-Patrascu, Cornelia Nichita, Bogdan Bita and Stefan Antohe
Materials 2024, 17(5), 1225; https://doi.org/10.3390/ma17051225 - 6 Mar 2024
Cited by 6 | Viewed by 1796
Abstract
This research work presents a “green” strategy of weed valorization for developing silver nanoparticles (AgNPs) with promising interesting applications. Two types of AgNPs were phyto-synthesized using an aqueous leaf extract of the weed Andropogon halepensis L. Phyto-manufacturing of AgNPs was achieved by two [...] Read more.
This research work presents a “green” strategy of weed valorization for developing silver nanoparticles (AgNPs) with promising interesting applications. Two types of AgNPs were phyto-synthesized using an aqueous leaf extract of the weed Andropogon halepensis L. Phyto-manufacturing of AgNPs was achieved by two bio-reactions, in which the volume ratio of (phyto-extract)/(silver salt solution) was varied. The size and physical stability of Andropogon—AgNPs were evaluated by means of DLS and zeta potential measurements, respectively. The phyto-developed nanoparticles presented good free radicals-scavenging properties (investigated via a chemiluminescence technique) and also urease inhibitory activity (evaluated using the conductometric method). Andropogon—AgNPs could be promising candidates for various bio-applications, such as acting as an antioxidant coating for the development of multifunctional materials. Thus, the Andropogon-derived samples were used to treat spider silk from the spider Pholcus phalangioides, and then, the obtained “green” materials were characterized by spectral (UV-Vis absorption, FTIR ATR, and EDX) and morphological (SEM) analyses. These results could be exploited to design novel bioactive materials with applications in the biomedical field. Full article
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17 pages, 2498 KB  
Article
Applications of Romanian Propolis in Phyto-Inhibitory Activity and Antimicrobial Protection: A Comparative Study
by Ramona Cristina Heghedűş-Mîndru, Mirel Glevitzky, Gabriel Heghedűş-Mîndru, Gabriela-Alina Dumitrel, Maria Popa, Doriana Maria Popa, Isidora Radulov and Mihaela Laura Vică
Antibiotics 2023, 12(12), 1682; https://doi.org/10.3390/antibiotics12121682 - 30 Nov 2023
Cited by 1 | Viewed by 2137
Abstract
Propolis use in medicine, pharmaceutical, cosmetic, and food industries is well known. This study aimed to investigate propolis’ phyto-inhibitory and antimicrobial potential. Nine propolis samples obtained from distinct Romanian regions and characterized in terms of physical–chemical parameters, phenols and flavonoid contents, and antioxidant [...] Read more.
Propolis use in medicine, pharmaceutical, cosmetic, and food industries is well known. This study aimed to investigate propolis’ phyto-inhibitory and antimicrobial potential. Nine propolis samples obtained from distinct Romanian regions and characterized in terms of physical–chemical parameters, phenols and flavonoid contents, and antioxidant properties were prepared as dry propolis and aqueous extracts. The phyto-inhibitory effect was comparatively tested on different cereals: hexaploid bread wheat (Triticum aestivum), maize (Zea mays L.), oats (Avena sativa L.), and barley (Hordeum vulgare L.), while their in vitro antimicrobial activity was evaluated against bacterial and fungal strains specific to cereals: Bacillus subtilis, B. cereus, Proteus mirabilis, Fusarium oxysporum, Penicillium chrysogenum, and Aspergillus niger. All propolis samples showed a phyto-inhibitory effect on the cereals, the most pronounced being corn and oats. Propolis powder samples displayed a lower phyto-inhibitory activity than propolis extracts. Also, all tested products showed inhibitory efficacy against both bacteria and fungi. Furthermore, principal component analysis showed differences between the samples’ phyto-inhibitory and antimicrobial properties depending on the geographical origin. Positive correlations were found between the polyphenols, flavonoid content, and antioxidant activity, respectively. These data support propolis’ phyto-pharmaceutical potential related to its use in plant crop management as an alternative in ecological agriculture. Full article
(This article belongs to the Special Issue Antimicrobial Activity of Natural Products and Plants Extracts)
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29 pages, 7116 KB  
Article
Galactoside-Based Molecule Enhanced Antimicrobial Activity through Acyl Moiety Incorporation: Synthesis and In Silico Exploration for Therapeutic Target
by Faez Ahmmed, Samiah Hamad Al-Mijalli, Emad M. Abdallah, Ibrahim H. Eissa, Ferdausi Ali, Ajmal R. Bhat, Joazaizulfazli Jamalis, Taibi Ben Hadda and Sarkar M. A. Kawsar
Pharmaceuticals 2023, 16(7), 998; https://doi.org/10.3390/ph16070998 - 13 Jul 2023
Cited by 5 | Viewed by 2820
Abstract
In this study, a series of galactoside-based molecules, compounds of methyl β-d-galactopyranoside (MDGP, 1), were selectively acylated using 2-bromobenzoyl chloride to obtain 6-O-(2-bromobenzoyl) substitution products, which were then transformed into 2,3,4-tri-O-6-(2-bromobenzoyl) compounds (27 [...] Read more.
In this study, a series of galactoside-based molecules, compounds of methyl β-d-galactopyranoside (MDGP, 1), were selectively acylated using 2-bromobenzoyl chloride to obtain 6-O-(2-bromobenzoyl) substitution products, which were then transformed into 2,3,4-tri-O-6-(2-bromobenzoyl) compounds (27) with various nontraditional acyl substituents. The chemical structures of the synthesized analogs were characterized by spectroscopic methods and physicochemical and elemental data analyses. The antimicrobial activities of the compounds against five human pathogenic bacteria and two phyto-fungi were evaluated in vitro and it was found that the acyl moiety-induced synthesized analogs exhibited varying levels of antibacterial activity against different bacteria, with compounds 3 and 6 exhibiting broad-spectrum activity and compounds 2 and 5 exhibiting activity against specific bacteria. Compounds 3 and 6 were tested for MIC (minimum inhibitory concentration) and MBC (minimum bactericidal concentration) based on their activity. The synthesized analogs were also found to have potential as a source of new antibacterial agents, particularly against gram-positive bacteria. The antifungal results suggested that the synthesized analogs could be a potential source of novel antifungal agents. Moreover, cytotoxicity testing revealed that the compounds are less toxic. A structure-activity relationship (SAR) investigation revealed that the lauroyl chain [CH3(CH2)10CO-] and the halo-aromatic chain [3(/4)-Cl.C6H4CO-] in combination with sugar, had the most potent activity against bacterial and fungal pathogens. Density functional theory (DFT)-calculated thermodynamic and physicochemical parameters, and molecular docking, showed that the synthesized molecule may block dengue virus 1 NS2B/NS3 protease (3L6P). A 150 ns molecular dynamic simulation indicated stable conformation and binding patterns in a stimulating environment. In silico ADMET calculations suggested that the designed (MDGP, 1) had good drug-likeness values. In summary, the newly synthesized MDGP analogs exhibit potential antiviral activity and could serve as a therapeutic target for dengue virus 1 NS2B/NS3 protease. Full article
(This article belongs to the Special Issue Structural and Computational-Driven Molecule Design in Drug Discovery)
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11 pages, 299 KB  
Article
Antimicrobial Efficacy of Phyto-L, Thiosulfonate from Allium spp. Containing Supplement, against Escherichia Coli Strains from Rabbits
by Francesco D’Amico, Gaia Casalino, Francesca Rita Dinardo, Michele Schiavitto, Antonio Camarda, Diana Romito, Antonella Bove and Elena Circella
Vet. Sci. 2023, 10(7), 411; https://doi.org/10.3390/vetsci10070411 - 23 Jun 2023
Cited by 3 | Viewed by 1888
Abstract
Colibacillosis, caused by enteropathogenic Escherichia coli (EPEC), is one of the most common diseases in rabbit farms, resulting in economic losses due to mortality and decrease in production. Until recently, antimicrobials were used to both treat and prevent disease on livestock farms, leading [...] Read more.
Colibacillosis, caused by enteropathogenic Escherichia coli (EPEC), is one of the most common diseases in rabbit farms, resulting in economic losses due to mortality and decrease in production. Until recently, antimicrobials were used to both treat and prevent disease on livestock farms, leading to the possible risk of antimicrobial resistance (AMR) and the selection of multidrug-resistant (MDR) bacteria. Therefore, interest in alternative control methods, such as the use of natural substances, has increased in the scientific community. The aim of this study was to evaluate the antimicrobial efficacy of Phyto-L (Pro Tech s.r.l.), a product containing organosulfur compounds (OSCs) such as propyl propane thiosulfonate (PTSO) from Allium spp., against 108 strains of E. coli isolated from rabbits with colibacillosis from 19 farms. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of Phyto-L were assessed. Bacterial suspensions with a charge of 108 CFU/mL, corresponding to those found in the rabbit gut under pathologic conditions, were tested with different concentrations from 20 to 0.15 μL/mL of Phyto-L. For each strain, the MIC and concentrations above the MIC were plated on Tryptic Soy agar (TSA) without Phyto-L to assess the MBCs. MIC and MBC values ranged from 1.25 to 5 μL/mL and 1.25 to 20 μL/mL, respectively, depending on the strain tested. The data showed an interesting antibacterial activity of Phyto-L against EPEC strains. Therefore, this product could be effective in preventing colibacillosis in field application, especially considering that 104–105 CFU/g of feces is the amount of E. coli usually found in the gut contents of rabbits under physiological condition. Full article
17 pages, 4299 KB  
Article
Phyto-Inhibitory and Antimicrobial Activity of Brown Propolis from Romania
by Mihaela Laura Vică, Mirel Glevitzky, Ramona Cristina Heghedűş-Mîndru, Gabriela-Alina Dumitrel, Gabriel Heghedűş-Mîndru, Maria Popa, Doriana Maria Faur, Ștefana Bâlici and Cosmin Adrian Teodoru
Antibiotics 2023, 12(6), 1015; https://doi.org/10.3390/antibiotics12061015 - 5 Jun 2023
Cited by 6 | Viewed by 2669
Abstract
The objective of this paper was to study the phyto-inhibitory and antimicrobial activity of brown propolis collected from the counties of four regions in Romania. The main physico-chemical and functional properties of 16 samples of propolis from different landforms of geographical regions were [...] Read more.
The objective of this paper was to study the phyto-inhibitory and antimicrobial activity of brown propolis collected from the counties of four regions in Romania. The main physico-chemical and functional properties of 16 samples of propolis from different landforms of geographical regions were determined. Their antimicrobial activities were established against 5 bacterial strains (Pseudomonas fluorescens, Bacillus subtilis, Bacillus cereus, Escherichia coli, and Proteus mirabilis) and 5 fungal strains (Alternaria alternata, Cladosporium cladosporioides, Fusarium oxysporum, Mucor racemosus, and Aspergillus niger). Simultaneously, the phyto-inhibitory effect of propolis samples on different cereals was highlighted: hexaploid bread wheat (Triticum aestivum), maize (Zea mays L.), oats (Avena sativa L.), and barley (Hordeum vulgare L.). Correlations between the antioxidant activity and total flavonoid and phenol content of the propolis samples were identified, respectively, and the statistical analysis highlighted that the diameter of the inhibition zone was influenced by the strain type (bacterial and fungal) and the geographical regions of propolis. Principal component analysis (PCA) indicated that out of seven principal components, only two exhibited > 0.5. Pearson’s correlation coefficient showed a low and moderate positive linear relationship between the diameter of the inhibition zone and the flavonoid and phenol concentration of the propolis samples. Full article
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12 pages, 3818 KB  
Article
The Enhanced Affinity of WRKY Reinforces Drought Tolerance in Solanum lycopersicum L.: An Innovative Bioinformatics Study
by Sandip Debnath, Achal Kant, Pradipta Bhowmick, Ayushman Malakar, Shampa Purkaystha, Binod Kumar Jena, Gaurav Mudgal, Mehdi Rahimi, Md Mostofa Uddin Helal, Rakibul Hasan, Jen-Tsung Chen and Faizul Azam
Plants 2023, 12(4), 762; https://doi.org/10.3390/plants12040762 - 8 Feb 2023
Cited by 15 | Viewed by 3359
Abstract
In the scenario of global climate change, understanding how plants respond to drought is critical for developing future crops that face restricted water resources. This present study focuses on the role of WRKY transcription factors on drought tolerance in tomato, Solanum lycopersicum L., [...] Read more.
In the scenario of global climate change, understanding how plants respond to drought is critical for developing future crops that face restricted water resources. This present study focuses on the role of WRKY transcription factors on drought tolerance in tomato, Solanum lycopersicum L., which is a significant vegetable crop. WRKY transcription factors are a group of proteins that regulate a wild range of growth and developmental processes in plants such as seed germination and dormancy and the stress response. These transcription factors are defined by the presence of a DNA-binding domain, namely, the WRKY domain. It is well-known that WRKY transcription factors can interact with a variety of proteins and therefore control downstream activities. It aims to simulate the effect of curcumin, a bioactive compound with regulatory capacity, on the protein–protein interaction events by WRKY transcription factors with an emphasis on drought stress. It was found that curcumin binds to WRKY with an energy of −11.43 kcal/mol with inhibitory concentration (Ki) 0.12 mM and has the potential to improve fruit quality and reinforce drought tolerance of S. lycopersicum, according to the results based on bioinformatics tools. The root means square deviation (RMSD) of the C-α, the backbone of 2AYD with ligand coupled complex, displayed a very stable structure with just a little variation of 1.89 Å. MD simulation trajectory of Cα atoms of 2AYD bound to Curcumin revealed more un-ordered orientation in PC1 and PC10 modes and more toward negative correlation from the initial 400 frames during PCA. Establishing the binding energies of the ligand–target interaction is essential in order to characterize the compound’s binding affinity to the drought transcription factor. We think we have identified a phyto-agent called curcumin that has the potential to enhance the drought tolerance. Compared to the part of the mismatch repair-base technique that can be used to fix drought related genes, curcumin performed better in a drop-in crop yield over time, and it was suggested that curcumin is a potential candidate factor for improving drought tolerance in tomatoes, and it needs future validation by experiments in laboratory and field. Full article
(This article belongs to the Special Issue Bioinformatics Toolkit for Plant Studies)
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14 pages, 2371 KB  
Article
Combined Application of Tacrolimus with Cyproconazole, Hymexazol and Novel {2-(3-R-1H-1,2,4-triazol-5-yl)phenyl}amines as Antifungals: In Vitro Growth Inhibition and In Silico Molecular Docking Analysis to Fungal Chitin Deacetylase
by Lyudmyla Antypenko, Fatuma Meyer, Zhanar Sadyk, Konstyantyn Shabelnyk, Sergiy Kovalenko, Karl Gustav Steffens and Leif-Alexander Garbe
J. Fungi 2023, 9(1), 79; https://doi.org/10.3390/jof9010079 - 5 Jan 2023
Cited by 7 | Viewed by 2907
Abstract
Agents with antifungal activity play a vital role as therapeutics in health care, as do fungicides in agriculture. Effectiveness, toxicological profile, and eco-friendliness are among the properties used to select suitable substances. Furthermore, a steady supply of new agents with different modes of [...] Read more.
Agents with antifungal activity play a vital role as therapeutics in health care, as do fungicides in agriculture. Effectiveness, toxicological profile, and eco-friendliness are among the properties used to select suitable substances. Furthermore, a steady supply of new agents with different modes of action is required to counter the well-known potential of human and phyto-pathogenic fungi to develop resistance against established antifungals. Here, we use an in vitro growth assay to investigate the activity of the calcineurin inhibitor tacrolimus in combination with the commercial fungicides cyproconazole and hymexazol, as well as with two earlier reported novel {2-(3-R-1H-1,2,4-triazol-5-yl)phenyl}amines, against the fungi Aspergillus niger, Colletotrichum higginsianum, Fusarium oxysporum and the oomycete Phytophthora infestans, which are notoriously harmful in agriculture. When tacrolimus was added in a concentration range from 0.25 to 25 mg/L to the tested antifungals (at a fixed concentration of 25 or 50 mg/L), the inhibitory activities were distinctly enhanced. Molecular docking calculations revealed triazole derivative 5, (2-(3-adamantan-1-yl)-1H-1,2,4-triazol-5-yl)-4-chloroaniline), as a potent inhibitor of chitin deacetylases (CDA) of Aspergillus nidulans and A. niger (AnCDA and AngCDA, respectively), which was stronger than the previously reported polyoxorin D, J075-4187, and chitotriose. The results are discussed in the context of potential synergism and molecular mode of action. Full article
(This article belongs to the Special Issue Biological Activity of Fungi: Interaction with the Environment)
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24 pages, 1583 KB  
Article
Thymus musilii Velen. Methanolic Extract: In Vitro and In Silico Screening of Its Antimicrobial, Antioxidant, Anti-Quorum Sensing, Antibiofilm, and Anticancer Activities
by Emira Noumi, Iqrar Ahmad, Nouha Bouali, Harun Patel, Siwar Ghannay, Ayshah Aysh ALrashidi, Mohammad A. Abdulhakeem, Mitesh Patel, Ozgur Ceylan, Riadh Badraoui, Afnan Elayyan Mousa Elayyan, Mohd Adnan, Adel Kadri and Mejdi Snoussi
Life 2023, 13(1), 62; https://doi.org/10.3390/life13010062 - 25 Dec 2022
Cited by 25 | Viewed by 3590
Abstract
Thymus musilii Velen. is a rare plant species cultivated in the Ha’il region (Saudi Arabia) under greenhouse conditions. In this work, we described, for the first time, the phytochemical composition, antimicrobial, antioxidant, anti-quorum sensing, and anticancer activities of T. musilii methanolic extract using [...] Read more.
Thymus musilii Velen. is a rare plant species cultivated in the Ha’il region (Saudi Arabia) under greenhouse conditions. In this work, we described, for the first time, the phytochemical composition, antimicrobial, antioxidant, anti-quorum sensing, and anticancer activities of T. musilii methanolic extract using both experimental and computational approaches. The obtained results showed the identification of eight small-like peptides and eighteen phyto-compounds by using high-resolution liquid chromatography–mass spectrometry (HR-LCMS) dominated mainly by compounds belonging to isoprenoid, fatty acyl, flavonoid, and alkaloid classes. The tested extracts exhibited high antifungal and antibacterial activity with the mean diameter of growth inhibition zones ranging from 12.33 ± 0.57 mm (Pseudomonas aeruginosa ATCC 27853) to 29.33 ± 1.15 mm (Candida albicans ATCC 10231). Low minimal inhibitory concentrations were recorded for the tested micro-organisms ranging from 0.781 mg/mL to 12.5 mg/mL. While higher doses were necessary to completely kill all tested bacterial and fungal strains. Thyme extract was able to scavenge DPPH, ABTS•+, β-carotene, and FRAP free radicals, and the IC50 values were 0.077 ± 0.0015 mg/mL, 0.040 ± 0.011 mg/mL, 0.287 ± 0.012 mg/mL, and 0.106 ± 0.007 mg/mL, respectively. The highest percentage of swarming and swimming inhibition was recorded at 100 µg/mL with 39.73 ± 1.5% and 25.18 ± 1%, respectively. The highest percentage of biofilm inhibition was recorded at 10 mg/mL for S. typhimurium ATCC 14028 (53.96 ± 4.21%) and L. monocytogenes ATCC 7644 (49.54 ± 4.5 mg/mL). The in silico docking study revealed that the observed antimicrobial, antioxidant, and anticancer activities of the constituent compounds of T. musilii are thermodynamically feasible, notably, such as those of the tripeptides (Asn-Met-His, His-Cys-Asn, and Phe-His-Gln), isoprenoids (10-Hydroxyloganin), and diterpene glycosides (4-Ketoretinoic acid glucuronide). Full article
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12 pages, 1237 KB  
Article
Chemical Composition, Antimicrobial Activity, and Withdrawal Period of Essential Oil-Based Pharmaceutical Formulation in Bovine Mastitis Treatment
by Zorana Kovačević, Dragana Tomanić, Ivana Čabarkapa, Ljubiša Šarić, Jovan Stanojević, Katarina Bijelić, Ivan Galić, Zoran Ružić, Mihajlo Erdeljan and Nebojša Kladar
Int. J. Environ. Res. Public Health 2022, 19(24), 16643; https://doi.org/10.3390/ijerph192416643 - 11 Dec 2022
Cited by 14 | Viewed by 3232
Abstract
Due to the emergence of antibiotic-resistant bacteria, the risk it represents to public health, and the possible consequences for animal health and welfare, there is an increasing focus on reducing antimicrobial usage (AMU) in animal husbandry. Therefore, a great interest in developing alternatives [...] Read more.
Due to the emergence of antibiotic-resistant bacteria, the risk it represents to public health, and the possible consequences for animal health and welfare, there is an increasing focus on reducing antimicrobial usage (AMU) in animal husbandry. Therefore, a great interest in developing alternatives to AMU in livestock production is present worldwide. Recently, essential oils (EOs) have gained great attention as promising possibilities for the replacement of antibiotics. The current study aimed to test the potential of using a novel EO-based pharmaceutical formulation (Phyto-Bomat) in bovine mastitis treatment. The antibacterial activity was performed using the microdilution technique. Lactating dairy cows were treated with 15 mL of Phyto-Bomat in the inflamed quarter for 5 consecutive days in order to analyze blood and milk samples for thymol and carvacrol residues using gas chromatography and mass spectrometry (GC–MS). Antimicrobial activity expressed as the minimum inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) indicates that this formulation has the highest activity against Gram-positive strains. The dominant compounds in Phyto-Bomat were thymol and carvacrol, at 12.58 ± 1.23 mg/mL and 23.11 ± 2.31 mg/mL, respectively. The quantification of these two compounds in evaluated biological samples showed that 24 h after administration the concentration of thymol and carvacrol in milk samples was at the same level as before application. On the other hand, thymol and carvacrol were detectable in plasma samples even after 24 h post-treatment, with values ranging from 0.15–0.38 and 0.21–0.66 µg/mL, respectively. The tested formulation showed encouraging results of antibacterial activity against bovine mastitis pathogens, as well as the withdrawal period of dominant compounds, which implies that further testing regarding the bacteriological and clinical cure rates in clinical settings is needed. Full article
(This article belongs to the Special Issue Recent Advances in Food Safety and Food Microbiology)
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16 pages, 3966 KB  
Article
Green Chemistry Based Synthesis of Zinc Oxide Nanoparticles Using Plant Derivatives of Calotropis gigantea (Giant Milkweed) and Its Biological Applications against Various Bacterial and Fungal Pathogens
by Ammara Farooq, Umair A. Khan, Haider Ali, Manda Sathish, Syed Atif Hasan Naqvi, Shehzad Iqbal, Haider Ali, Iqra Mubeen, Muhammad Bilal Amir, Walid F. A. Mosa, Alaa Baazeem, Mahmoud Moustafa, Sulaiman Alrumman, Ali Shati and Sally Negm
Microorganisms 2022, 10(11), 2195; https://doi.org/10.3390/microorganisms10112195 - 4 Nov 2022
Cited by 25 | Viewed by 4995
Abstract
Nanotechnology is a burning field of scientific interest for researchers in current era. Diverse plant materials are considered as potential tool in green chemistry based technologies for the synthesis of metal nanoparticles (NPs) to cope with the hazardous effects of synthetic chemicals, leading [...] Read more.
Nanotechnology is a burning field of scientific interest for researchers in current era. Diverse plant materials are considered as potential tool in green chemistry based technologies for the synthesis of metal nanoparticles (NPs) to cope with the hazardous effects of synthetic chemicals, leading to severe abiotic climate change issues in today’s agriculture. This study aimed to determine the synthesis and characterization of metal-based nanoparticles using extracts of the selected plant Calotropis gigantea and to evaluate the enzyme-inhibition activities and antibacterial and antifungal activity of extracts of metal-based zinc nanoparticles using C. gigantea extracts. The crystal structure and surface morphology were characterized by X-ray diffraction (XRD) and scanning electron microscopy (SEM). C. gigantea was examined for antimicrobial activity against clinical isolates of bacteria and fungi. The water, ethanolic, and acetone extracts of C. gigantea were studied for their antagonistic action against bacterial strains (E. coli, S. aureus, P. multocida, and B. subtilis) and selected fungal strains (A. paracistic, F. solani, A. niger, S. ferrugenium, and R. nigricans). In vitro antimicrobial activity was determined by the disc diffusion method, where C. gigantea was tested for AChE and BChE inhibitory activity using Ellman’s methodology. The kinetic analysis was performed by the proverbial Berthelot reaction for urease inhibition. The results showed that out of all the extracts tested, ethanolic and water extracts possessed zinc nanoparticles. These extracts showed the maximum zone of inhibition against F. solani and P. multocida and the lowest against S. ferrugenium and B. subtilis. A potential source of AChE inhibitors is certainly provided by the abundance of plants in nature. Numerous phyto-constituents, such as AChE and BChE inhibitors, have been reported in this communication. Water extract was active and has the potential for in vitro AChE and BChE inhibitory activity. The urease inhibition with flower extracts of C. gigantea revealed zinc nanoparticles in water extracts that competitively inhibited urease enzymes. In the case of cholinesterase enzymes, it was inferred that the water extract and zinc nanoparticles have more potential for inhibition of BChE than AChE and urease inhibition. Furthermore, zinc nanoparticles with water extract are active inthe inhibition of the bacterial strains E. coli, S. aureus, and P. multocida and the fungal strains A. paracistic, F. solani, and A. niger. Full article
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