Assessments of anticholinergic, antidiabetic, antioxidant activities and phenolic content of Stachys annua
TL;DR: In this article, the methanol extract of Stachys annua (MESA) and the water extract (WESA) were prepared and used for all biochemical analyses, and the results showed high inhibition effects against α-amylase and α-glycosidase enzymes, whereas they showed low inhibition effect against AChE and BChE enzymes.
Abstract: Some biochemical properties including phenolic content, anticholinergic, antidiabetic, and antioxidant activities of Stachys annua were determined in this study. The methanol extract of Stachys annua (MESA) and the water extract of Stachys annua (WESA) were prepared and used for all biochemical analyses. Antioxidant capacities of MESA and WESA were evaluated by six different in vitro bioanalytical methods including three reducing antioxidant methods and three radical scavenging antioxidant methods. Also, enzyme inhibition effect of Stachys annua against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-amylase, and α-glycosidase enzymes were determined separately. According to the results, both extracts showed high inhibition effects against α-amylase and α-glycosidase enzymes, whereas they showed low inhibition effects against AChE and BChE enzymes. The IC50 values of MESA and WESA against AChE (119.8 ± 2.4 μg/mL and 150.1 ± 3.0 μg/mL), BChE (192.1 ± 3.8 μg/mL and 186.7 ± 3.7 μg/mL), α-glycosidase (25.7 ± 0.5 μg/mL and 18.7 ± 0.4 μg/mL), and α-amylase (43.3 ± 0.9 μg/mL and 11.4 ± 0.2 μg/mL) were determined, respectively. Another goal of the study was to evaluate the phenolic compositions of Stachys annua by liquid chromatography and tandem mass spectrometry (LC-MS/MS). Quercetagetin-3,6-dimethylether (178.6 ± 33.5 μg/g), chlorogenic acid (118.2 ± 16.4 μg/g), and fumaric acid (102.5 ± 7.1 μg/g) were identified as major compounds in MESA. On the other hand, fumaric acid (309.5 ± 21.5 μg/g), apigenin (144.6 ± 11.7 μg/g), and chlorogenic acid (78.1 ± 10.8 μg/g) were identified as major compounds in WESA. This study will be a scientific base for further studies about Stachys annua for food or medicinal utilization.
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TL;DR: In this study, a general approach to the bonding and chelating properties of metals is described and basic principles and chemical principles of metal chelation methods, both in vivo and in vitro, are outlined and discussed.
Abstract: Heavy metals are essential for a wide range of biological processes, including the growth and reproduction of cells, synthesis of biomolecules, many enzymatic reactions, and the body’s immunity, but their excessive intake is harmful. Specifically, they cause oxidative stress (OS) and generate free radicals and reactive oxygen species (ROS) in metabolism. In addition, the accumulation of heavy metals in humans can cause serious damage to different organs, especially respiratory, nervous and reproductive and digestive systems. Biologically, metal chelation therapy is often used to treat metal toxicity. This process occurs through the interaction between the ligand and a central metal atom, forming a complex ring-like structure. After metals are chelated with appropriate chelating agents, their damage in metabolism can be prevented and efficiently removed from the body. On the other hand, heavy metals, including Zn, Fe and Cu, are necessary for the suitable functioning of different proteins including enzymes in metabolism. However, when the same metals accumulate at levels higher than the optimum level, they can easily become toxic and have harmful effects toward biomolecules. In this case, it induces the formation of ROS and nitrogen species (RNS) resulting in peroxidation of biological molecules such as lipids in the plasma membrane. Antioxidants have an increasing interest in many fields due to their protective effects, especially in food and pharmaceutical products. Screening of antioxidant properties of compounds needs appropriate methods including metal chelating assay. In this study, a general approach to the bonding and chelating properties of metals is described. For this purpose, the basic principles and chemical principles of metal chelation methods, both in vivo and in vitro, are outlined and discussed. Hence, in the main sections of this review, the descriptions related to metal ions, metal chelating, antioxidants, importance of metal chelating in biological system and definitions of metal chelating assays as widely used methods to determine antioxidant ability of compounds are provided. In addition, some chemical properties, technical and critical details of the used chelation methods are given.
71 citations
TL;DR: The benzoic acid derivatives in this series were the most promising derivatives, as they exhibited a good multifunctional inhibition at all experimental levels and in the in silico validation against hCA I, hCA II, and AChE, respectively, for the treatment of AD.
Abstract: Alzheimer's disease (AD) is a neurodegenerative disorder characterized by dementia, memory impairment, cognitive dysfunction, and speech impairment. The utility of cholinergic replacement by acetylcholinesterase (AChE) inhibitors in AD treatment has been well documented so far. Recently, studies have also evidenced that human carbonic anhydrases (hCAs) serve as an important target for AD treatment. In this direction, the improvement of new multitarget drugs, which can simultaneously modulate several mechanisms or targets included in the AD pathway, may be a potent strategy to treat AD. In light of these data for understanding and developing AD-related multitarget AChE and hCAs inhibitors, in this study, novel methylene-aminobenzoic acid and tetrahydroisoquinolynyl-benzoic acid derivatives (4a-g and 6a-g) were designed. The synthesized analogs were experimentally validated for their effects by in vitro and direct enzymatic tests. Also, the compounds were subjected to in silico monitoring with Schrodinger Suite software to assign binding affinities of potential derivatives based on Glide XP scoring, molecular mechanics-generalized Born surface area computing, and validation by molecular docking. The results revealed that 6c (1,3-dimethyldihydropyrimidine-2,4-(1H,3H)-dione-substituted, KI value of 33.00 ± 0.29 nM), 6e (cyclohexanone-substituted, KI value of 18.78 ± 0.09 nM), and 6f (2,2-dimethyl-1,3-dioxan-4-one-substituted, KI value of 13.62 ± 0.21 nM) from the benzoic acid derivatives in this series were the most promising derivatives, as they exhibited a good multifunctional inhibition at all experimental levels and in the in silico validation against hCA I, hCA II, and AChE, respectively, for the treatment of AD.
52 citations
TL;DR: In this article, the antioxidant activity of evaporated ethanolic extract (EESB) and lyophilized water extract (WESB), of Shaggy bindweed (Convulvulus betonicifolia mill), was evaluated.
35 citations
TL;DR: In this paper, the synthesis of N-phthalimidomethyl-substituted NHC precursors and their Ag(I)NHC coordination compounds were presented.
32 citations
TL;DR: The docking analysis results revealed that the interactions of the major compounds of the plant with AChE, B cholinesterase, GST, and α-Gly enzymes are responsible for the inhibitory activity.
Abstract: Medicinal plants have been used traditionally since ancient times as alternative medications to treat various human diseases. In this work, we examined the chemical constituent, antioxidant activity, and enzyme inhibition of an endemic plant Thymus migricus. The plant extracts showed remarkable inhibition effects against the acetylcholinesterase (AChE), butyrylcholinesterase (BChE), glutathione S-transferase (GST), and α-glycosidase (α-Gly) enzymes that are linked with some metabolic disorders. IC50 values (concentration of a sample to inhibit 50% of enzyme activity) for AChE, BChE, GST, and α-Gly were found as 18.23 mg/mL, 17.77 mg/mL, 31.5 mg/ml, and 16.5 mg/mL, respectively. Antioxidant activities of water extract of T. migricus (WET) and methanol extract of T. migricus (MET) were determined using four in vitro techniques. The extracts showed considerable antioxidant actions on all four techniques. In addition, quinic acid (18.30 mg/g), chlorogenic acid (0.94 mg/g), cynaroside (0.49 mg/g), luteolin (0.21 mg/g), and p-coumaric acid (0.19 mg/g) were characterized as major phenolic compounds using advanced LC–MS/MS technique. The interactions of some phenolic compounds with the enzymes have been investigated using molecular docking studies. The docking analysis results revealed that the interactions of the major compounds of the plant with AChE, BChE, GST, and α-Gly enzymes are responsible for the inhibitory activity.
28 citations
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TL;DR: Alpha-amylase (EC 3.1.2.1), which cleaves internal -1,4glycosidic linkages in starch to produce glucose, maltose, or dextrins, and glucoamylases (EC 4.2) are widely used in the industrial conversion of starch into sugars.
411 citations
TL;DR: The total antioxidant capacity of the aqueous extracts of some endemic herbs—prepared as infusions by steeping these herbs in hot water—was assayed with bis(neocuproine)copper(II) chloride, also known as the CUPRAC) reagent, which was easily accessible, rapid, stable and responsive to both hydrophilic and lipophilic antioxidants.
Abstract: The total antioxidant capacity of the aqueous extracts of some endemic herbs-prepared as infusions by steeping these herbs in hot water--was assayed with bis(neocuproine)copper(II) chloride, also known as the cupric ion reducing antioxidant capacity (CUPRAC) reagent, which was easily accessible, rapid, stable and responsive to both hydrophilic and lipophilic antioxidants. The highest antioxidant capacities of some herbal teas available in the Turkish market were observed for scarlet pimpernel (Anagallis arvensis), sweet basil (Ocimum basilicum), green tea (Camellia sinensis) and lemon balm (Melissa officinalis), in this order (1.63, 1.18, 1.07, and 0.99 mmol trolox equivalent (TR)/g, respectively). For infusions prepared from ready-to-use tea bags, the CUPRAC values were highest for Ceylon blended ordinary tea (4.41), green tea with lemon (1.61), English breakfast ordinary tea (1.26) and green tea (0.94), all of which were manufactured types of C. sinensis. Following the strongest antioxidant herbs with capacities close to or slightly exceeding 1.0 mmol TR/g, sage, thyme, coriander, coltsfoot, blackberry and immortelle (Helichrysum) exhibited capacities around 0.5 mmol TR/g. The correlation of the Folin total phenolic content of herbal teas with their CUPRAC and ABTS (2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) total antioxidant capacities gave linear curves with correlation coefficients of 0.966 and 0.936, respectively, showing that the CUPRAC assay results better correlated with total phenolic content of herbal teas. Absorbance versus concentration data at different dilutions and upon standard additions of model antioxidant compounds (trolox and quercetin) to herbal tea infusions showed that the absorbances (at 450 nm of the CUPRAC method) due to different antioxidant compounds in herbal tea infusions were additive; that is, the tested antioxidants did not chemically interact to cause apparent deviations from Beer's law.
395 citations
TL;DR: The information on the medicinal plants of the region for its availability to the researchers in different fields related to herbal drugs is presented.
331 citations
TL;DR: An approach to screening α-glucosidase inhibitors from medicinal plants using enzyme-coated magnetic bead suggested that enzyme- coated magnetic beads may be suitable for discovering active compounds from medicinal plant.
Abstract: α-Glucosidase plays important roles in the digestion and absorption of carbohydrates in the small intestine. The inhibition of α-glucosidase is regarded as a potential way to treat diabetes. We established an approach to screening α-glucosidase inhibitors from medicinal plants using enzyme-coated magnetic bead. Using 1-(3-dimethyl-aminopropyl)-3-ethylcarbodiimide and N-hydroxysuccinimide as reaction reagents, α-glucosidase was immobilized on the magnetic beads by covalent linkage. The conjugation of α-glucosidase to the magnetic beads was characterized using scanning electron microscope and X-ray diffractometer. The proposed approach was applied in fishing potential α-glucosidase inhibitors from extract of Morus alba, a Chinese medicinal plant. The structures of potential active compounds were identified via liquid chromatography–mass spectrometry and nuclear magnetic resonance. The results demonstrated that two flavonoids (isoquercitrin and astragalin) could bind to α-glucosidase, which was confirmed via conventional α-glucosidase inhibitory assay. Our findings suggested that enzyme-coated magnetic beads may be suitable for discovering active compounds from medicinal plants. Copyright © 2012 John Wiley & Sons, Ltd.
282 citations
TL;DR: In this paper, the authors investigated the antioxidant and anticholinergic properties of Galanga (Alpinia officinarum Hance) rhizome, which is a member of the ginger family (Zingiberaceae).
212 citations