ABSTRACT
The subcritical water extraction of Undaria pinnatifida (blade, sporophyll, and root) was evaluated to determine its chemical properties and biological activities. The extraction was conducted at 180 °C and 3 MPa. Root extracts exhibited the highest phenolic content (43.32 ± 0.19 mg phloroglucinol/g) and flavonoid content (31.54 ± 1.63 mg quercetin/g). Sporophyll extracts had the highest total sugar, reducing sugar, and protein content, with 97.35 ± 4.23 mg glucose/g, 56.44 ± 3.10 mg glucose/g, and 84.93 ± 2.82 mg bovine serum albumin (BSA)/g, respectively. The sporophyll contained the highest fucose (41.99%) and mannose (10.37%), whereas the blade had the highest galactose (48.57%) and glucose (17.27%) content. Sporophyll had the highest sulfate content (7.76%). Key compounds included sorbitol, glycerol, L-fucose, and palmitic acid. Root extracts contained the highest antioxidant activity, with IC50 values of 1.51 mg/mL (DPPH), 3.31 mg/mL (ABTS+), and 2.23 mg/mL (FRAP). The root extract exhibited significant α-glucosidase inhibitory activity with an IC50 of 5.07 mg/mL, indicating strong antidiabetic potential. The blade extract showed notable antihypertensive activity with an IC50 of 0.62 mg/mL. Hence, subcritical water extraction to obtain bioactive compounds from U. pinnatifida, supporting their use in functional foods, cosmetics, and pharmaceuticals is highlighted. This study uniquely demonstrates the variation in bioactive compound composition and bioactivities across different parts of U. pinnatifida, providing deeper insights. Significant correlations between chemical properties and biological activities emphasize the use of U. pinnatifida extracts for chronic conditions.
Subject(s)
Antioxidants , Plant Extracts , Undaria , Antioxidants/pharmacology , Antioxidants/isolation & purification , Antioxidants/chemistry , Undaria/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Water/chemistry , Plant Roots/chemistry , Flavonoids/isolation & purification , Flavonoids/pharmacology , Flavonoids/chemistry , Antihypertensive Agents/pharmacology , Antihypertensive Agents/isolation & purification , Antihypertensive Agents/chemistry , Phenols/isolation & purification , Phenols/pharmacology , Phenols/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors/isolation & purification , Glycoside Hydrolase Inhibitors/chemistry , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , Edible SeaweedsABSTRACT
Flavobacterium strains exert a substantial influence on roots and leaves of plants. However, there is still limited understanding of how the specific interactions between Flavobacterium and their plant hosts are and how these bacteria thrive in this competitive environment. A crucial step in understanding Flavobacterium - plant interactions is to unravel the structure of bacterial envelope components and the molecular features that facilitate initial contact with the host environment. Here, we have revealed structure and properties of the exopolysaccharides (EPS) produced by Flavobacterium sp. Root935. Chemical analyses revealed a complex and interesting branched heptasaccharidic repeating unit, containing a variety of sugar moieties, including Rha, Fuc, GlcN, Fuc4N, Gal, Man and QuiN and an important and extended substitution pattern, including acetyl and lactyl groups. Additionally, conformational analysis using molecular dynamics simulation showed an extended hydrophobic interface and a distinctly elongated, left-handed helicoidal arrangement. Furthermore, properties of the saccharide chain, and likely the huge substitution pattern prevented interaction and recognition by host lectins and possessed a low immunogenic potential, highlighting a potential role of Flavobacterium sp. Root935 in plant-microbial crosstalk.
Subject(s)
Flavobacterium , Polysaccharides, Bacterial , Flavobacterium/chemistry , Polysaccharides, Bacterial/chemistry , Polysaccharides, Bacterial/isolation & purification , Molecular Dynamics Simulation , Plant Roots/microbiology , Plant Roots/chemistryABSTRACT
Efficient delivery of nanoparticles (NPs) to plants is important for agricultural application. However, to date, we still lack knowledge about how NPs' charge matters for its translocation pathway, i.e., symplastic and apoplastic pathways, in plants. In this study, we synthesized and used negatively charged citrate sourced carbon dots (C-CDs, -37.97 ± 1.89 mV), Cy5 coated C-CDs (Cy5-C-CDs, -41.90 ± 2.55 mV), positively charged PEI coated carbon dots (P-CDs, +43.03 ± 1.71 mV), and Cy5 coated P-CDs (Cy5-P-CDs, +48.80 ± 1.21 mV) to investigate the role of surface charges and coatings on the employed translocation pathways (symplastic and apoplastic pathways) of charged NPs in plants. Our results showed that, different from the higher fluorescence intensity of P-CDs and Cy5-P-CDs in extracellular than intracellular space, the fluorescence intensity of C-CDs and Cy5-C-CDs was similar between intracellular and extracellular space in cucumber and cotton roots. It suggests that the negatively charged CDs were translocated via both symplastic and apoplastic pathways, but the positively charged CDs were mainly translocated via the apoplastic pathway. Furthermore, our results showed that root applied negatively charged C-CDs demonstrated higher leaf fluorescence than did positively charged P-CDs in both cucumber (8.09 ± 0.99 vs 3.75 ± 0.23) and cotton (7.27 ± 1.06 vs 3.23 ± 0.22), indicating that negatively charged CDs have a higher translocation efficiency from root to leaf than do positively charged CDs. It should be noted that CDs do not affect root cell activities, ROS level, and photosynthetic performance in cucumber and cotton, showing its good biocompatibility. Overall, this study not only figured out that root applied negatively charged CDs employed both symplastic and apoplastic pathways to do the transportation in roots compared with mainly the employment of apoplastic pathway for positively charge CDs, but also found that negatively charge CDs could be more efficiently translocated from root to leaf than positively charged CDs, indicating that imparting negative charge to NPs, at least CDs, matters for its efficient delivery in crops.
Subject(s)
Carbon , Plant Roots , Quantum Dots , Carbon/chemistry , Carbon/metabolism , Quantum Dots/chemistry , Quantum Dots/metabolism , Plant Roots/metabolism , Plant Roots/chemistry , Cucumis sativus/metabolism , Carbocyanines/chemistryABSTRACT
Zanthoxylum rhetsa (ZR) is used traditionally to manage a variety of ailments, including diabetes. Oxidative stress may accelerate the diabetic condition. The available antidiabetic and antioxidant drugs have many shortcomings including resistance, inefficiency, higher dose, side effects and costs. The goal of the current investigation was to assess the antioxidant capacity and antidiabetic activity of an ethanolic extract of Zanthoxylum rhetsa root bark (ZRRB) through in vitro, in vivo, and in silico methods. The antioxidant capacity of the ZRRB extract was measured using both the DPPH radical assay and the total antioxidant activity test. The oral glucose tolerance test (OGTT) and alloxan-induced diabetic mice model were also used to examine in vivo antidiabetic efficacy. Phytochemicals identification was done by GCMS analysis. Additionally, computational methods such as molecular docking, ADMET analysis, and molecular dynamics (MD) modeling were performed to determine the above pharmacological effects. The extract demonstrated significant DPPH scavenging activity (IC50 = 42.65 µg/mL). In the OGTT test and alloxan-induced diabetes mice model, the extract effectively lowered blood glucose levels. Furthermore, in vitro inhibition of pancreatic α-amylase studies demonstrated the ZRRB extract as a good antidiabetic crude drug (IC50 = 81.45 µg/mL). GCMS investigation confirmed that the crude extract contains 16 major phytoconstituents, which were docked with human peroxiredoxin-5, α-amylase, and sulfonylurea receptor 1. Docking and pharmacokinetic studies demonstrated that among 16 phytoconstituents, 6H-indolo[3,2,1-de] [1,5]naphthyridin-6-one (CID: 97176) showed the highest binding affinity to targeted enzymes, and imitated Lipinski's rule of five. Furthermore, MD simulation data confirmed that the aforementioned compound is very steady to the binding site of α-amylase and sulfonylurea receptor 1 receptors. Findings from in vitro, in vivo and in silico investigation suggest that ZRRB extract contains a lead compound that could be a potent source of antidiabetic drug candidate.
Subject(s)
Antioxidants , Diabetes Mellitus, Experimental , Hypoglycemic Agents , Molecular Docking Simulation , Plant Bark , Plant Extracts , Zanthoxylum , Zanthoxylum/chemistry , Animals , Plant Extracts/chemistry , Plant Extracts/pharmacology , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/therapeutic use , Mice , Diabetes Mellitus, Experimental/drug therapy , Antioxidants/pharmacology , Antioxidants/chemistry , Plant Bark/chemistry , Male , Plant Roots/chemistry , Gas Chromatography-Mass Spectrometry , Glucose Tolerance Test , Ethanol/chemistry , Molecular Dynamics SimulationABSTRACT
The uptake, translocation, and accumulation of mefentrifluconazole (MFZ), an innovative chiral triazole fungicide, in plants at the enantiomeric level are still unclear. Herein, we investigated the patterns and mechanisms of enantiomeric uptake, bioaccumulation, and translocation through several experiments. Rac-MFZ shows the strongest uptake and bioaccumulation capacity in wheat compared with its enantiomers, while S-(+)-MFZ has the highest translocation potential. Molecular docking provided evidence of the stronger translocation ability of S-(+)-MFZ than R-(-)-MFZ. Split-root experiments showed that MFZ and its enantiomers could undergo long-distance transport within the wheat. Active transport or facilitated and simple diffusion may be involved in the wheat uptake of MFZ. The limited acropetal translocation capability of MFZ may be attributed to the dominant uptake pathway of apoplastic. The concentrations of Rac-MFZ in different subcellular fractions varied greatly. In summary, this study provides novel insights for further understanding the behaviors of MFZ and its enantiomers in plants.
Subject(s)
Fungicides, Industrial , Triazoles , Triticum , Triticum/metabolism , Triticum/chemistry , Triazoles/chemistry , Triazoles/metabolism , Fungicides, Industrial/metabolism , Fungicides, Industrial/chemistry , Stereoisomerism , Biological Transport , Molecular Docking Simulation , Plant Roots/metabolism , Plant Roots/chemistryABSTRACT
Fusarium crown and root rot (FCRR) has emerged as a highly destructive soil-borne disease, posing a significant threat to the safe cultivation of tomatoes in recent years. The pathogen of tomato FCRR is Fusarium oxysporum f. sp. radicis-lycopersici (Forl). To explore potential phytotoxins from Forl, eight undescribed diterpenoids namely fusariumic acids A-H (1-8) were isolated. Their structures were elucidated by using spectroscopic data analyses, quantum chemical calculations, and X-ray crystallography. Fusariumic acids A (1) and C-H (3-8) were typical isocassadiene-type diterpenoids, while fusariumic acid B (2) contained a cage-like structure with an unusual 7,8-seco-isocassadiene skeleton. A biosynthetic pathway of 2 was proposed. Fusariumic acids A (1) and C-H (3-8) were further assessed for their phytotoxic effects on tomato seedlings at 200 µg/mL. Among them, fusariumic acid F (6) exhibited the strongest inhibition against the hypocotyl and root elongation of tomato seedlings, with inhibitory rates of 61.3 and 45.3%, respectively.
Subject(s)
Diterpenes , Fusarium , Plant Diseases , Plant Roots , Solanum lycopersicum , Fusarium/drug effects , Solanum lycopersicum/microbiology , Diterpenes/chemistry , Diterpenes/pharmacology , Plant Diseases/microbiology , Plant Roots/microbiology , Plant Roots/chemistry , Molecular StructureABSTRACT
CONTEXT: Derris reticulata Craib. and Glycyrrhiza glabra L., of the Fabaceae, have been used as active components in Thai herbal formulas for the treatment of fever and skin diseases. OBJECTIVE: To evaluate the physicochemical and pharmacological properties of the developed herbal gel formulation containing the combined extract from D. reticulata stem wood and G. glabra root (RGF). MATERIALS AND METHODS: The potential of the herbal gel formulation containing RGF (8% w/w) as the active ingredient was studied by evaluating the anti-inflammatory, antioxidant, and anti-Staphylococcus aureus activities using quantitative reverse transcription-polymerase chain reaction assay, spectrophotometric method, and broth microdilution technique, respectively. The reference standards for the biological testing included Nω-nitro-L-arginine (L-NA), ascorbic acid, catechin, and penicillin G. The stability study of the RGF herbal gel was performed by a heating-cooling test (at 45 °C for 24 h and at 4 °C for 24 h/1 cycle; for 6 cycles), and the bioactive marker compounds in the herbal gel were investigated by the HPLC technique. RESULTS: RGF showed promising pharmacological effects, particularly on its anti-inflammatory property (IC50 73.86 µg/mL), compared to L-NA (IC50 47.10 µg/mL). The RGF-containing gel demonstrated anti-inflammatory (IC50 3.59 mg/mL) and free radical scavenging effects (IC50 0.05-4.39 mg/mL), whereas it had no anti-S. aureus activity (MIC > 10 mg/mL). The active ingredient in the developed herbal gel significantly inhibited lipopolysaccharide-induced nitric oxide production by downregulating iNOS mRNA levels. The contents of the bioactive markers in the RGF gel (lupinifolin and glabridin) did not change significantly after stability testing. DISCUSSION AND CONCLUSIONS: The RGF-containing gel has potential to be further developed as an herbal product for the treatment of skin inflammation.
Subject(s)
Anti-Inflammatory Agents , Antioxidants , Derris , Gels , Glycyrrhiza , Plant Extracts , Staphylococcus aureus , Glycyrrhiza/chemistry , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/administration & dosage , Plant Extracts/pharmacology , Plant Extracts/administration & dosage , Staphylococcus aureus/drug effects , Animals , Derris/chemistry , Antioxidants/pharmacology , Antioxidants/administration & dosage , Antioxidants/isolation & purification , Mice , Plant Roots/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/administration & dosage , RAW 264.7 Cells , Drug StabilityABSTRACT
Physalis alkekengi L.var. franchetii (Mast.) Makino (PAF) is an important edible and medicinal plant resource in China. Historically, phytochemical studies have primarily examined the calyx and fruit due to their long-standing use in traditional Chinese medicine for their ability to clear heat and detoxify. Metabolites and bioactivities of other parts such as the leaves, stems and roots, are rarely studied. The study involved conducting metabolic profiling of five plant parts of PAF using UPLC-Q-Orbitrap-HRMS analysis, in conjunction with two bioactivity assays. A total of 95 compounds were identified, including physalins, flavonoids, sucrose esters, phenylpropanoids, nitrogenous compounds and fatty acids. Notably, 14 aliphatic sucrose esters, which are potentially novel compounds, were initially identified. Furthermore, one new aliphatic sucrose ester was purified and its structure was elucidated by 1D and 2D NMR analysis. The hierarchical clustering analysis and principal component analysis showed the close clustering of the root and stem, suggesting similarities in their chemical composition, whereas the leaf, calyx and fruit clustered more distantly. Orthogonal partial least-squares discriminant analysis results showed that 41 compounds potentially serve as marker compounds for distinguishing among plant parts. Variations in activity were observed among the plant parts during the comparative evaluation with biological assays. The calyx, leaf and fruit extracts showed stronger antibacterial and anti-inflammatory activities than the stem and root extracts, and 19 potential biomarkers were identified by S-plot analysis for the observed activities, including chlorogenic acid, luteolin, cynaroside, physalin A, physalin F, physalin J, apigetrin, quercetin-3ß-D-glucoside and five ASEs, which likely explain the observed potent bioactivity.
Subject(s)
Metabolomics , Physalis , Plant Extracts , Physalis/chemistry , Chromatography, High Pressure Liquid/methods , Metabolomics/methods , Plant Extracts/pharmacology , Plant Extracts/chemistry , Plant Leaves/chemistry , Fruit/chemistry , Animals , Mass Spectrometry/methods , Plant Roots/chemistry , Plant Stems/chemistry , Metabolome , Plants, Medicinal/chemistry , Mice , Phytochemicals/pharmacology , Phytochemicals/analysis , Phytochemicals/chemistryABSTRACT
BACKGROUND: cultivated and wild plants are used to treat different ailments. The Astragalus genus is found in temperate and dry climates; thus, it is found in Egypt and the arab world. Astragalus caprinus has a good amount of bioactive chemicals, which may help explain its therapeutic effects in reducing the risk of consequences from disease. METHOD: The phytochemical investigation of the herb and roots of Astragalus caprinus L. included the analytical characterization for the petroleum ether components by GC/MS, unsaponifiable matter (unsap. fraction), and fatty acids (FAME) investigation by GLC analysis. Main flavonoids were chromatographically isolated from ethyl acetate and n-butanol extracts. In vitro antimicrobial activity has been tested against the Gram-positive bacteria Staphylococcus aureus and Streptococcus mutans for different plant extracts, the Gram-negative bacteria Pseudomonas aeruginosa and Klebsiella pneumonia, the fungus Candida albicans and Aspergillus niger, and the Escherichia coli bacterium. Metabolite cytotoxicity was examined using the MTT assay against HepG-2 (human liver carcinoma) and MCF-7 (breast carcinoma). RESULTS: Identifying the important components of the herb and root petroleum ether extracts was achieved. Using column chromatography, luteolin, cosmosiin (apigenin-7-O-glucoside), and cynaroside (luteolin-7-O-glucoside) were separated and identified using UV, NMR, and Mass Spectroscopy. Root extracts displayed potential antimicrobial activity against most of the tested pathogens. Both extracts (herb and roots) were active against the MCF-7 cell line and HepG-2 cell line with IC50 62.5 ± 0.64 and 72.4 ± 2.3 µg/ml, and 75.9 ± 2.5 and 96.8 ± 4.2 µg/ml, respectively. CONCLUSION: Astragalus caprinus seems to be a promising source of bioactive compounds that could potentially aid in preventing disease complications and address common health issues in developing countries. Moreover, the various parts of this plant could be utilized as natural raw materials for producing health-boosting products that could address common health issues in developing countries.
Subject(s)
Astragalus Plant , Phytochemicals , Plant Extracts , Plant Extracts/pharmacology , Plant Extracts/chemistry , Humans , Astragalus Plant/chemistry , Phytochemicals/pharmacology , Phytochemicals/chemistry , Microbial Sensitivity Tests , MCF-7 Cells , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Plant Roots/chemistry , Egypt , Hep G2 Cells , Flavonoids/pharmacologyABSTRACT
Legume plants form symbiotic relationships with rhizobia, which allow plants to utilize atmospheric nitrogen as a nutrient. This symbiosis is initiated by secretion of specific signaling metabolites from the roots, which induce the expression of nod genes in rhizobia. These metabolites are called nod gene inducers (NGIs), and various flavonoids have been found to act as NGIs. However, NGIs of chickpea, the second major pulse crop, remain elusive. We conducted untargeted metabolome analysis of chickpea root exudates to explore metabolites with increased secretion under nitrogen deficiency. Principal component (PC) analysis showed a clear difference between nitrogen deficiency and control, with PC1 alone accounting for 37.5% of the variance. The intensity of two features with the highest PC1 loading values significantly increased under nitrogen deficiency; two prominent peaks were identified as O-methylated isoflavones, pratensein and biochanin A. RNA-seq analysis showed that they induce nodABC gene expression in the Mesorhizobium ciceri symbiont, suggesting that pratensein and biochanin A are chickpea NGIs. Pratensein applied concurrently with M. ciceri at sowing promoted chickpea nodulation. These results demonstrate that pratensein and biochanin A are chickpea NGIs, and pratensein can be useful for increasing nodulation efficiency in chickpea production.
Subject(s)
Cicer , Isoflavones , Mesorhizobium , Plant Root Nodulation , Symbiosis , Cicer/microbiology , Cicer/genetics , Cicer/metabolism , Isoflavones/metabolism , Isoflavones/pharmacology , Mesorhizobium/genetics , Mesorhizobium/metabolism , Mesorhizobium/physiology , Plant Root Nodulation/genetics , Plant Root Nodulation/drug effects , Bacterial Proteins/genetics , Bacterial Proteins/metabolism , Plant Roots/microbiology , Plant Roots/metabolism , Plant Roots/chemistry , Plant Roots/genetics , Methylation , Genistein/metabolism , Genistein/pharmacologyABSTRACT
Bisphenol A is a fluorophoric platform that is used to develop chemosensors for various species. Herein, we report a bisphenol A based Schiff-base molecule, 4,4'-(propane-2,2-diyl)bis(2-((E)-((2-hydroxy-5-methylphenyl)imino)methyl)phenol) (Me-H4L), as a selective chemosensor for Al3+. Among the several metal ions, it shows a significant increment in its fluorescence intensity (50 fold) at 535 nm in the presence of Al3+ ions. The enhanced fluorescence was attributed to the CHEFF mechanism and inhibition of CîN isomerization. The limit of detection value of Me-H4L for Al3+ was determined to be 9.65 µM. Its quantum yield and lifetime increased considerably in the presence of the cation. Some theoretical calculations were performed to explain the interaction between Al3+ and the probe. Furthermore, Me-H4L was applied in cell imaging studies using animal cells and plant roots.
Subject(s)
Aluminum , Benzhydryl Compounds , Fluorescent Dyes , Phenols , Plant Roots , Phenols/chemistry , Phenols/analysis , Benzhydryl Compounds/chemistry , Benzhydryl Compounds/analysis , Aluminum/analysis , Aluminum/chemistry , Plant Roots/chemistry , Fluorescent Dyes/chemistry , Animals , Schiff Bases/chemistry , Humans , Optical Imaging/methods , Spectrometry, Fluorescence/methods , Limit of DetectionABSTRACT
Plants produce an extraordinary array of natural products (specialized metabolites). Notably, these structurally complex molecules are not evenly distributed throughout plant tissues but are instead synthesized and stored in specific cell types. Elucidating both the biosynthesis and function of natural products would be greatly facilitated by tracking the location of these metabolites at the cell-level resolution. However, detection, identification, and quantification of metabolites in single cells, particularly from plants, have remained challenging. Here, we show that we can definitively identify and quantify the concentrations of 16 molecules from four classes of natural products in individual cells of leaf, root, and petal of the medicinal plant Catharanthus roseus using a plate-based single-cell mass spectrometry method. We show that identical natural products show substantially different patterns of cell-type localization in different tissues. Moreover, we show that natural products are often found in a wide range of concentrations across a population of cells, with some natural products at concentrations of over 100 mM per cell. This single-cell mass spectrometry method provides a highly resolved picture of plant natural product biosynthesis partitioning at a cell-specific resolution.
Subject(s)
Biological Products , Catharanthus , Mass Spectrometry , Single-Cell Analysis , Biological Products/metabolism , Biological Products/chemistry , Biological Products/analysis , Catharanthus/metabolism , Catharanthus/chemistry , Single-Cell Analysis/methods , Mass Spectrometry/methods , Plant Leaves/metabolism , Plant Leaves/chemistry , Plant Roots/metabolism , Plant Roots/chemistryABSTRACT
Rosa davurica Pall. is widely used in traditional oriental herbal therapy, but its components and molecular mechanisms of action remain unclear. This study investigates the antidiabetic potential of Rosa davurica Pall. root extract (RDR) and elucidates its underlying molecular mechanisms with in vitro and in vivo models. Data from the current study show that RDR exhibits strong antioxidant activity and glucose homeostasis regulatory effects. It significantly impacts glucose homeostasis in C2C12 skeletal muscle cells by inhibiting α-glucosidase activity. Further molecular mechanistic studies revealed that RDR promoted glucose uptake by phosphorylation of AMP-activated protein kinase (AMPK)/acetyl-CoA carboxylase (ACC), but not Phosphatidylinositol 3-kinase (PI 3-kinase)/Akt in C2C12 skeletal muscle cells. These actions increased the expression and translocation of glucose transporter type 4 (GLUT4) to the plasma membrane. In addition, RDR treatment in the STZ-induced diabetic rats remarkably improved the low body weight, polydipsia, polyphagia, hyperglycemia, and islet architecture and increased the insulin/glucose ratio. The liver (ALT and AST) and kidney marker enzyme (BUN and creatinine) levels were restored by RDR treatment as well. Phytochemical analysis identified eight major constituents in RDR, crucial for its antioxidant and antidiabetic activity. Through the molecular docking of representative glucose transporter GLUT4 with these compounds, it was confirmed that the components of RDR had a significantly high binding score in terms of structural binding. These findings from the current study highlight the antidiabetic effects of RDR. Collectively, our data suggest that RDR might be a potential pharmaceutical natural product for diabetic patients.
Subject(s)
Diabetes Mellitus, Experimental , Glucose Transporter Type 4 , Hypoglycemic Agents , Plant Extracts , Plant Roots , Rosa , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/therapeutic use , Plant Extracts/pharmacology , Plant Extracts/chemistry , Animals , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/metabolism , Plant Roots/chemistry , Rosa/chemistry , Rats , Glucose Transporter Type 4/metabolism , Male , Mice , Antioxidants/pharmacology , Antioxidants/chemistry , Blood Glucose/metabolism , Blood Glucose/drug effects , Cell Line , Glucose/metabolism , Molecular Docking Simulation , Muscle, Skeletal/drug effects , Muscle, Skeletal/metabolism , AMP-Activated Protein Kinases/metabolismABSTRACT
OBJECTIVE: Preparation and characterization of nano-emulsion formulations for Asparagus densiflorus aerial and root parts extracts. SIGNIFICANCE: Genus Asparagus is known for its antimicrobial and anticancer activities, however, freeze dried powder of aqueous - alcoholic extract prepared in this study, exhibited a limited water solubility, limiting its therapeutic application. Thus, encapsulation of its phytochemicals into nano-emulsion is proposed as a solution to improve water solubility, and facilitate its clinical translation. METHODS: the composition of extracts for both aerial and root parts of Asparagus densiflorus was identified by HPLC and LC-MS analysis. Nano-emulsion was prepared via homogenization where a mixture of Castor oil: phosphate buffered saline (10 mM, pH 7.4): Tween 80: PEG 600 in a ratio of 10: 5: 2.5: 2.5, respectively. Nano-emulsion formulations were characterized for particle size, polydispersity index (PDI), zeta potential, TEM, viscosity and pH. Then, the antibacterial and anticancer activities of nano-emulsion formulations versus their pure plant counterparts was assessed. RESULTS: The analysis of extracts identified several flavonoids, phenolics, and saponins which were reported to have antimicrobial and anticancer activities. Nano-emulsion formulations were monodispersed with droplet sizes ranging from 80.27 ± 2.05 to 111.16 ± 1.97 nm, and polydispersity index ≤0.3. Nano-emulsion formulations enhanced significantly the antibacterial (multidrug resistant bacteria causing skin and dental soft tissues infections) and anticancer (HuH7, HEPG2, H460 and HCT116) activities compared to their pure plant extract counterparts. CONCLUSION: Employing a nano-delivery system as a carrier for phytochemicals might be an effective strategy to enhance their pharmacological activity, overcome their limitations, and ultimately increase their potential for clinical applications.
Subject(s)
Anti-Bacterial Agents , Asparagus Plant , Emulsions , Plant Components, Aerial , Plant Extracts , Plant Roots , Plant Extracts/pharmacology , Plant Extracts/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Humans , Plant Components, Aerial/chemistry , Asparagus Plant/chemistry , Plant Roots/chemistry , Particle Size , Nanoparticles/chemistry , Microbial Sensitivity Tests , Antineoplastic Agents, Phytogenic/pharmacology , Antineoplastic Agents, Phytogenic/administration & dosage , Antineoplastic Agents, Phytogenic/chemistry , Solubility , Cell Line, Tumor , Drug Compounding/methods , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Antineoplastic Agents/administration & dosageABSTRACT
In this study, we present the synthesis of gold nanoparticles (AuNPs) using a completely green synthesis method without the use of any additional functionalizing agent, except dried turmeric root extract. The significant synthesis parameters were optimized, and the applicability of AuNPs was investigated in areas such as plasmonic and fluorescent sensing of aluminum (Al3âº) and chromium (Cr3âº) ions, reduction of 4-nitrophenol (4-NP), and degradation of methylene blue (MB) and methyl orange (MO) dyes. Characterization studies were performed using UV-Vis spectroscopy, TEM, FTIR, and XRD, revealing that the AuNPs predominantly had a spherical morphology and a very small particle size of 8.5 nm, with stability maintained up to 120 days. The developed AuNP-based plasmonic sensors relied on aggregation-induced decreases in absorption, along with a red shift in the spectra. Fluorescence sensing demonstrated a linear increase in intensity with increasing concentrations of Al3⺠and Cr3âº, with detection limits of 0.83 and 1.19 nM, respectively. The catalytic activities of AuNPs were tested in reducing 4-NP and degradations of MB and MO dyes (binary system) in tap water and wastewater, with the reactions following pseudo-first-order kinetics. This study highlights the potential of AuNPs synthesized from turmeric roots for various environmental and sensing applications.
Subject(s)
Curcuma , Gold , Metal Nanoparticles , Plant Extracts , Gold/chemistry , Metal Nanoparticles/chemistry , Curcuma/chemistry , Plant Extracts/chemistry , Green Chemistry Technology , Plant Roots/chemistry , Catalysis , Water Pollutants, Chemical/analysis , Water Pollutants, Chemical/chemistry , NitrophenolsABSTRACT
Siraitia grosvenorii Swingle is one of the first approved medicine food homology species in China, and it has been used as a natural sweetener in the food industry and as a traditional medicine to relieve cough and reduce phlegm. However, many S. grosvenorii roots are discarded yearly, which results in a great waste of resources. Twelve undescribed norcucurbitacin-type triterpenoid glycosides, siraitiaosides A-L (1-12), and six known analogs (13-18) were isolated from the roots of S. grosvenorii. The structures of isolated norcucurbitacin glycosides were elucidated by comprehensive data analyses, including HRESIMS, UV, IR, NMR, ECD calculations, and X-ray crystallography analysis. Siraitiaosides A-E (1-5) featured an unusual 19,29-norcucurbitacin framework while siraitiaosides F-L (6-12) featured a rare 29-norcucurbitacin framework. Notably, compound 4 displayed moderate anti-acetylcholinesterase (AChE) activity with an IC50 of 21.0 µM, meanwhile, compounds 16 and 18 exhibited pronounced cytotoxic activities against MCF-7, CNE-1, and HeLa cancer cell lines with IC50 values of 2.1-15.2 µM. In silico studies showed that compound 4 bound closely to AChE with a binding energy of -5.04 kcal/mol, and compound 18 could tightly bind to PI3K, AKT1, ERK2, and MMP9 proteins that related to autophagy, apoptosis, migration/invasion, and growth/proliferation. In summary, the roots of Siraitia grosvenorii have potential medicinal values due to the multiple bioactive components.
Subject(s)
Cell Proliferation , Cucurbitaceae , Glycosides , Plant Roots , Plant Roots/chemistry , Humans , Glycosides/chemistry , Glycosides/pharmacology , Glycosides/isolation & purification , Molecular Structure , Cell Proliferation/drug effects , Cucurbitaceae/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Drug Screening Assays, Antitumor , Structure-Activity Relationship , Apoptosis/drug effects , Cholinesterase Inhibitors/pharmacology , Cholinesterase Inhibitors/chemistry , Cholinesterase Inhibitors/isolation & purification , Dose-Response Relationship, Drug , Acetylcholinesterase/metabolism , Acetylcholinesterase/drug effects , Molecular ConformationABSTRACT
BACKGROUND: Depression is a serious and complex mental disease that has attracted worldwide attention because of its high incidence rate, high disability rate and high mortality. Excitotoxicity is one of the most important mechanisms involved in the pathophysiological process of depression. In our previous studies, n-butanol extract from maize roots was found to have good neuroprotective effects due to its antioxidative activity. However, the antidepressive effective constituents, efficacy in vivo and mechanism of action of maize root extracts have not been determined. PURPOSE: This study aimed to determine the main active neuroprotective compound in maize root extract and investigate its antidepressant effects and possible underlying mechanism in vitro and in vivo. METHODS: Sixteen extracts were isolated and purified from maize roots. The active components of the most active extracts of maize roots (hereafter referred to as EM 2) were identified using UF-HPLC-QTOF/MS. In vitro cell models of NMDA-induced excitotoxicity in SH-SY5Y cells were used to analyze the anti-excitatory activity of the extracts. The MTT assay and Annexin V-FITC/PI Apoptosis Detection were used to evaluate cell viability. Several network pharmacological strategies have been employed to investigate the potential mechanism of action of EM 2. The effects of EM 2 on depressive-like behaviors were evaluated in CUMS mice. Changes in the levels of related proteins were detected via western blotting. RESULTS: Among the 16 extracts extracted by n-butanol, EM 2 was determined to be the most active extract against NMDA-induced excitotoxicity by n-butanol extraction. Meanwhile, seventeen compounds were further identified as the main active components of EM 2. Mechanistically, EM 2 inhibited NMDA-induced excitatory injury in SH-SY5Y cells and alleviated the depressive-like behaviors of CUMS mice by suppressing NR2B and subsequently mediating the downstream CREB/TRKB/BDNF, PI3K/Akt and MAPK pathways, as well as the Nrf2/HO-1 antioxidant signaling pathway. CONCLUSION: The study indicated that EM 2 could potentially be developed as a potential therapeutic candidate to cure depression in NMDA-induced excitatory damage.
Subject(s)
Antidepressive Agents , Apoptosis , Depression , Neuroprotective Agents , Plant Extracts , Plant Roots , Zea mays , Animals , Antidepressive Agents/pharmacology , Zea mays/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Plant Roots/chemistry , Humans , Mice , Depression/drug therapy , Neuroprotective Agents/pharmacology , Cell Line, Tumor , Apoptosis/drug effects , Male , Brain-Derived Neurotrophic Factor/metabolism , Cell Survival/drug effects , Receptors, N-Methyl-D-Aspartate/metabolism , Signal Transduction/drug effectsABSTRACT
We have functionally characterized the high-affinity phosphate transporter (PiPT) from the root endophyte fungus Piriformospora indica. PiPT belongs to the major facilitator superfamily (MFS). PiPT protein was purified by affinity chromatography (Ni-NTA) and Size Exclusion Chromatography (SEC). The functionality of solubilized PiPT was determined in detergent-solubilized state by fluorescence quenching and in proteoliposomes. In the fluorescence quenching assay, PiPT exhibited a saturation concentration of approximately 2 µM, at a pH of 4.5. Proteoliposomes of size 121.6 nm radius, showed transportation of radioactive phosphate. Vmax was measured to be 232.2 ± 11 pmol/min/mg protein. We have found Km to be 45.8 ± 6.2 µM suggesting high affinity towards phosphate.
Subject(s)
Basidiomycota , Phosphate Transport Proteins , Basidiomycota/metabolism , Basidiomycota/chemistry , Phosphate Transport Proteins/metabolism , Phosphate Transport Proteins/genetics , Phosphate Transport Proteins/chemistry , Fungal Proteins/chemistry , Fungal Proteins/isolation & purification , Fungal Proteins/metabolism , Endophytes/metabolism , Endophytes/chemistry , Plant Roots/microbiology , Plant Roots/chemistry , Phosphates/metabolism , Phosphates/chemistryABSTRACT
The irrigation of soils with reclaimed contaminated wastewater or its amendment with sewage sludge contributes to the uptake of pharmaceuticals by vegetables growing in the soil. A multiresidue method has been devised to determine five pharmaceuticals and nine of their main metabolites in leafy and root vegetables. The method employs ultrasound-assisted extraction, clean-up via dispersive solid-phase extraction, and analysis through liquid chromatography-tandem mass spectrometry. Box-Behnken design was used to refine variables such as extraction solvent volume, time of extraction, number of extraction cycles, and the type and amount of d-SPE sorbent. The method achieved linearity (R2) greater than 0.994, precision (relative standard deviation) under 16% for most compounds, and detection limits ranging from 0.007 to 2.25 ng g-1 dry weight. This method was applied to a leafy vegetable (lettuce) and to a root vegetable (carrot) sourced from a local market. Parent compounds were detected at higher concentrations than their metabolites, with the exception of carbamazepine-10,11-epoxide.
Subject(s)
Plant Roots , Solid Phase Extraction , Tandem Mass Spectrometry , Vegetables , Vegetables/chemistry , Vegetables/metabolism , Plant Roots/chemistry , Plant Roots/metabolism , Pharmaceutical Preparations/analysis , Pharmaceutical Preparations/metabolism , Chromatography, Liquid/methods , Plant Leaves/chemistry , Plant Leaves/metabolism , Soil Pollutants/analysis , Soil Pollutants/metabolismABSTRACT
Eleutherococcus divaricatus (Siebold and Zucc.) S. Y. Hu. has been used in Traditional Chinese Medicine (TCM) due to its anticancer, immunostimulant, and anti-inflammatory activities. However, its mechanism of action and chemical composition are still insufficiently understood and require more advanced research, especially for cases in which anti-inflammatory properties are beneficial. The aim of this study was to evaluate the impact of E. divaricatus root extracts and fractions on proinflammatory serum hyaluronidase and tyrosinase in children diagnosed with acute lymphoblastic leukemia. Antioxidant and anti-melanoma activities were also examined and correlated with metabolomic data. For the first time, we discovered that the ethyl acetate fraction significantly inhibits hyaluronidase activity, with mean group values of 55.82% and 63.8% for aescin used as a control. However, interestingly, the fraction showed no activity against human tyrosinase, and in A375 melanoma cells treated with a doxorubicin fraction, doxorubicin activity decreased. This fraction exhibited the most potent antioxidant activity, which can be attributed to high contents of polyphenols, especially caffeic acid (24 mg/g). The findings suggest an important role of the ethyl acetate fraction in hyaluronidase inhibition, which may additionally indicate its anti-inflammatory property. The results suggest that this fraction can be used in inflammatory-related diseases, although with precautions in cases of patients undergoing chemotherapy.