UHPLC-MS/MS phenolic profiling and in vitro antioxidant activities of inula graveolens (L.) Desf

PubMed ID: 28697630Inula graveolens (L.) Desf. is an annual aromatic herb which has various uses on alternative medicine in many region of the world. In this study, antioxidant activities of ethanol and water extracts of the plant leaves were determined by in vitro DPPH method and phenolic composition of the plant sample was determined by LC-MS/MS analysis. The results showed that chlorogenic acid, quinic acid, hyperoside, protocatechuic acid and quercetin were the major phenolic compounds among the 27 standard compounds. The significant antioxidant capacity of the plant might be related with the high abundance of phenolic compounds. © 2017 Informa UK Limited, trading as Taylor & Francis Group

Polyphenol contents and antioxidant activity of lyophilized aqueous extract of propolis from Erzurum, Turkey

PubMed ID: 20685228Propolis, an extremely complex resinous material, exhibits valuable pharmacological and biological properties attributed to the presence of polyphenols. In this study, we determined the antioxidant properties of lyophilized aqueous extract of propolis (LAEP) from Erzurum province of Turkey and correlated the values with total levels of polyphenolic compounds. In order to estimate the capacity of LAEP to act as antioxidants, we studied its 1,1-diphenyl-2-picryl-hydrazyl radicals (DPPH), 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) radicals (ABTS+), N,N-dimethyl-p-phenylenediamine radicals (DMPD+), superoxide anion radicals (O2-) and hydrogen peroxide (H2O2) scavenging activity, total antioxidant activity, ferric ions (Fe3+) and cupric ions (Cu2+) reducing ability, ferrous ions (Fe2+) chelating activity. LAEP inhibited 93.2% lipid peroxidation of a linoleic acid emulsion at 30?g/mL concentration. On the other hand, BHA, BHT, ?-tocopherol and trolox displayed 83.3%, 82.1%, 68.1% and 81.3% inhibition of peroxidation at the same concentration, respectively. Quantitative amounts of caffeic acid, ferulic acid, syringic acid, ellagic acid, quercetin, ?-tocopherol, pyrogallol, p-hydroxybenzoic acid, vanillin, p-coumaric acid, gallic acid and ascorbic acid were detected by high performance liquid chromatography and tandem mass spectrometry (LC-MS/MS). This study will bring an innovation for further studies with regard to the antioxidant properties of LAEP. © 2010 Elsevier Ltd.BAP-2008/75The authors would like to express their gratitude to the Research Fund of the Atatürk University for the funding of Project (BAP-2008/75)

Characterization of Glycan İsomers Using Magnetic Carbon Nanoparticles as A MALDI Co-Matrix

Matrix-assisted laser desorption ionization-in source decay (MALDI-ISD) analysis is a useful technique in the structural analysis of glycans. Our recent publication demonstrated that magnetic carbon nanoparticles (MCNPs), used as a MALDI co-matrix, significantly enhanced ISD efficiency for glycomic analysis by MALDI-TOF. In this study, MCNPs were used for the structural study of isomeric glycans. Results from the standard glycans confirmed easy distinction of positional and linkage isomers without the need for further derivatization of glycan molecules. Extensive glycosidic and cross-ring fragmented ions provided different fragment patterns for various glycan isomers. Core- and branch-fucosylated isomers were distinguished by several unique ions, and pseudo-MS3 data were used to recognize the fucosylated branch. Although no diagnostic fragment ion was observed for 2,3- and 2,6-linked sialic acid isomers, their MALDI-ISD patterns were found to be significantly different (P < 0.05). Furthermore, the method introduced in this study could not only be used for the identification of glycan isomers but has also proved effective for the isomeric structural confirmation of gangliosides. GD1a and GD1b gangliosides were easily distinguished by the diagnostic ion originated from GD1a, produced by Z4?Z2? cleavages. Moreover, liquid chromatography coupled with MALDI-TOF was applied to analyze N-glycan isomers derived from a pooled human blood serum sample, providing an alternative method of isomeric glycomic analysis of biological specimens. © 2019 The Royal Society of Chemistry.National Institutes of Health National Institutes of Health: 1R01GM130091-01, 1R01GM112490-04, 1U01CA225753-01This work was supported by grants from National Institutes of Health, NIH (1R01GM112490-04, 1R01GM130091-01, and 1U01CA225753-01)

Herbal remedies against Huntington's disease: Preclinical evidences and future directions

Herbal medicines, or phytochemicals can treat various neurological disorders, and is actually preferred over synthetic drugs due to their lower cost, negligible side effects, easy availability and therapeutic efficiency. This article lists a total of 13 plant extracts, 27 plant derived natural compounds and 3 herbal formulations that were found to therapeutically cure Huntington's Disease, mainly by eliminating the toxic mHtt proteins(the product of the mutant gene responsible for HD). The various plant compounds, fractions, extracts and herbal formulations were summarized from popular scientific search engines and then analyzed on the basis of their source and bioactivity. To understand the behavioral, biochemical and morphological changes caused by HD, experimental models like 3-NP and transgenic animal models like rats, mice, Drosophila and Caenorhaditis elegans were used. Plants such as Bacopa monnieri, Celastrus paniculatus, Centella asiatica, Gastrodia elata, Panax ginseng, and Withania somnifera are some examples that possess anti-HD properties. Some examples of promising plant compounds possessing similar properties are fisetin, curcumin, hesperidin, trehalose, onjisaponin B, sesamol, resveratrol, kaempferol and melatonin. Herbal formulations discussed here are B307, CLMT and YGS. These are proved to be more beneficial than single herbs because they can regulate more targets. However, detailed study and further research should be conducted to determine the therapeutic efficacy of herbal extracts and compounds in HD models. © 2022 Elsevier Inc. All rights reserved

One-pot three-component synthesis of novel pyrazolo-acridine derivatives and assessment of their acetylcholinesterase inhibitory properties: An in vitro and in silico study

In this study, the synthesis and characterization of newly designed compounds containing pyrazole, acridine, and benzothiazole groups with their biological activity potentials were evaluated. For this purpose, the starting compound of our study, 1-(benzo[d]thiazol-2-yl)-3-(4-chlorophenyl)-1H-pyrazole-4-carbaldehyde (4), was synthesized according to the Vilsmeier-Haack method. Afterward, a series of new pyrazolo-acridine derivatives (7a-l) were obtained as a result of one-pot three-component reaction of compound 1 with 5,5-dimethyl cyclohexane-1,3?dione and various aromatic amines. The structures of the synthesized compounds were characterized using FT-IR, 1H NMR, 13C NMR, Mass spectroscopy techniques, and elemental analysis. Then, the enzyme inhibition effects of these compounds on acetylcholinesterase (AChE) were investigated. According to the in vitro AChE enzyme activity studies, the most effective inhibitions of the compounds 7f (0.76±0.19 µM), 7d (0.82±0.33 µM), and 7e (1.70±1.66 µM) were determined from their low Ki values. On the other hand, in silico molecular docking interactions of the respective compounds with AChE (pdb id: 4EY9) were carried out by using AutoDock Vina software. The molecular docking analyses showed the effective molecular interactions of all compounds (7a-7l) with the AChE enzyme from their low binding energy values. © 2022 Elsevier B.V.2016-87; Çankiri Karatekin ÜniversitesiThis research has been supported by Kütahya Dumlupınar University Scientific Research Projects Coordination Office under grant number 2016-87. Also, authors would like to thank Cankırı Karatekin University for providing spectroanalytical facilities and Kütahya Dumlupınar University, Faculty of Arts and Sciences, Department of Physics for FT-IR measurements.This research has been supported by Kütahya Dumlupınar University Scientific Research Projects Coordination Office under grant number 2016-87 . Also, authors would like to thank Cankırı Karatekin University for providing spectroanalytical facilities and Kütahya Dumlupınar University, Faculty of Arts and Sciences, Department of Physics for FT-IR measurements

Some metal chelates with Schiff base ligand: synthesis, structure elucidation, thermal behavior, XRD evaluation, antioxidant activity, enzyme inhibition, and molecular docking studies

Abstract: Schiff bases are well-known compounds for having significant biological properties. In this study, a new Schiff base ligand and its metal complexes were synthesized, and their antioxidant and enzyme inhibitory activities were evaluated. The new Schiff base ligand was synthesized with the condensation reaction of 6-tert-butyl 3-ethyl 2-amino-4,5-dihydrothieno[2,3-c]pyridine-3,6(7H)-dicarboxylate and 2-hydroxybenzaldehyde compounds. Fe(II), Co(II), and Ni(II) metal complexes of the novel Schiff base ligand were synthesized and characterized. The purity and molecular formula of the synthesized compounds were identified with elemental analysis, infrared, ultraviolet–visible, mass spectrophotometry, powder XRD, magnetic and thermal measurements. The Schiff base acted as a three dentate chelate. The analytical and spectroscopic data suggested an octahedral geometry for the complexes. The in vitro antioxidant method studies elucidated a more effective antioxidant character of the Schiff base ligand than its metal complexes but a less effective antioxidant potential than the standard antioxidant compounds. The enzyme inhibition potentials of the synthesized compounds for AChE, BChE, and GST enzymes were determined by in vitro enzyme activity methods. The Schiff base ligand was discovered to be the best inhibitor for the AChE and BChE with the values of 7.13 ± 0.84 µM and 5.75 ± 1.03 µM Ki, respectively. Moreover, the Fe(II) complex displayed the best Ki value as 9.37 ± 1.06 µM for the GST enzyme. Finally, molecular docking studies were carried out to see the structural interactions of the compounds. The metal complexes demonstrated better binding affinities with the AChE, BChE, and GST enzymes than the Schiff base ligand. This study identified a potential Schiff base molecule against both AChE and BChE targets to further investigate for in vivo and safety evaluation. Graphical abstract: [Figure not available: see fulltext.] © 2021, The Author(s), under exclusive licence to Springer Nature Switzerland AG