Phenolic components, antioxidant activity, and mineral analysis of Capparis spinosa L

In addition to being consumed as food, caper (Capparis spinosa L.) fruits are also used in folk medicine to treat inflammatory disorders, such as rheumatism. C. spinosa L. is rich in phenolic compounds, making it increasingly popular because of its components’ potential benefits to human health. We analyzed a number of individual phenolic compounds and investigated in vitro biological activities of C. spinosa L. Sixteen phenolic constituents were identified using reverse phase-high performance liquid chromatography (RP-HPLC). Total phenolic compounds (TPCs), ferric reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity were used as determinants of antioxidant capacity. C. spinosa L. exhibited strong antioxidant activity and contained high levels of antioxidant compounds. Gentisic, sinapic and benzoic acid were detected in C. spinosa L. No gallic acid, proto-catechuic acid, proto-catechuic aldehyde, chlorogenic acid, p-OH benzoic acid, vanillic acid, caffeic acid, syringic acid, vanillin, syringaldehyde, p-coumaric acid, ferulic acid or rosmarinic acid were identified. Iron and zinc were present at high levels in samples. C. spinosa L. appears to be a good source of antioxidants and minerals that might serve to protect health and combat several diseases.Key words: Antioxidant, capers, Capparis spinosa L., phenolics

BRAZILIAN ARCHIVES OF BIOLOGY AND TECHNOLOGY A N I N T E R N A T I O N A L J O U R N A L Purification and characterization of extracellular α-amylase from a thermophilic Anoxybacillus thermarum A4 strain

ABSTRAC

Investigation of a wild pear species (Pyrus elaeagnifolia subsp Elaeagnifolia Pallas) from Antalya, Turkey: polyphenol oxidase properties and anti-xanthine oxidase, anti-urease, and antioxidant activity

WOS: 000395169000009Polyphenol oxidase properties and anti-xanthine oxidase, anti-urease, and antioxidant activity were investigated in Pyrus elaeagnifolia subsp. elaeagnifolia Pallas harvested from Antalya, Turkey. Optimum pH and temperature were 7.0 and 30 degrees C, respectively. Selected kinetic properties of polyphenol oxidase was evaluated.The K-m and V-max-values, using 4-methylcatechol as substrate, were calculated as 3.57 mM and 4781 U/mg protein, respectively. IC50-values ranged from 0.0036 to 4.0231 mM against sodium metabisulphite, ascorbic acid, sodium azide, and benzoic acid, while ascorbic acid was the strongest inhibitor. Aquatic extracts of the sample exhibited strong antioxidant capacity and substantial xanthine oxidase and urease inhibition, with IC50-values of 10.75 +/- 0.11 and 0.97 +/- 0.03 mg/mL, respectively

Polyphenol oxidase properties, anti-urease, and anti-acetylcholinesterase activity of Diospyros lotus L. (Plum Persimmon)

WOS: 000399642900020Diospyros lotus fruit polyphenol oxidase was purified using affinity chromatography, resulting in a 15-fold enrichment in specific activity. the purified enzyme, having 16.5 kDa molecular weight on sodium dodecyl sulfate-polyacrylamide gel electrophoresis, exhibited the highest activity toward 4-methylcatechol. Maximum diphenolase activity was reached at pH 7.0 and 60 degrees C in the presence of 4-methylcatechol. K-m and V-max values were calculated as 3.8 mM and 1250 U/mg protein, respectively. Ascorbic acid was a promising inhibitor with an IC50 value of 0.121 mu M. the activity of the purified enzyme was stimulated by Fe2+, Sr2+, Zn2+, and K+ and deeply inhibited by Hg2+, at 1 mM final concentration. Aqueous extract of Diospyros lotus L. fruit showed strong substantial urease and acetylcholinesterase inhibition, with IC50 values of 1.55 +/- 0.05 and 16.75 +/- 0.11 mg/mL, respectively

Synthesis, alpha-glucosidase inhibition and in silico studies of some 4-(5-fluoro-2-substituted-1H-benzimidazol-6-yl)morpholine derivatives

emirik, mustafa/0000-0001-9489-9093WOS: 000552631700004PubMed: 32563964In this study, a new series of 4-(5-fluoro-2-substituted-1H-benzimidazol-6-yl)morpholine derivatives has been synthesized and screened for their alpha-glucosidase inhibitory potential. All molecules showed a considerable alpha-glucosidase inhibitory potential with IC50 values ranging from 20.46 +/- 0.21 to 0.18 +/- 0.01 mu g/mL when compared with the acarbose (IC50 = 8.16 +/- 0.12 mu g/mL) as the standard. Compound 4 k having methoxy group on phenyl ring had the highest inhibitory effect with IC50 = 0.18 +/- 0.01 mu g/mL value among the examined compounds. Electron-donating groups such as methyl and methoxy on the phenyl ring played an important role in the inhibition. Also, the Lineweaver-Burk plots analysis displayed that the inhibition type of 4k was the competitive mode like acarbose as standard. in silico studies were also performed to explore the binding interaction of the most active compound

Synthesis and Biological Evaluation of Some Succinimide Hybrid Molecules

WOS: 000520225900015In this study, a new series of succinimide hybrid molecules containing isothiocyanate, coumarin, isatin, and furan moieties was synthesized and screened for alpha-glucosidase and antioxidant activities. Preliminary results revealed that all molecules showed good alpha-glucosidase inhibition effectiveness. Antioxidant activities of the hybrid molecules were determined using cupric reducing antioxidant capacity (CUPRAC) and ferric reducing antioxidant power (FRAP) assays. Also, the radical scavenging activities of the synthesized compounds were assayed by using the results showed that all compounds exhibited moderated to high scavenging activity

A simple and efficient synthesis of benzimidazoles containing piperazine or morpholine skeleton at C-6 position as glucosidase inhibitors with antioxidant activity

Ozil, Musa/0000-0002-1980-1364WOS: 000425897800049PubMed: 29287256A novel 2-(aryl)-6-morpholin-4-yl(or 4-methylpiperazin-1-yl)-1H-benzimidazole derivatives were designed and expeditiously synthesized starting from 5-morpholin-4-yl(or 4-methylpiperazin-1-yl)-2-nitroaniline with various aldehydes which were preliminarily screened for in vitro antioxidant activities and glucosidase inhibitors. the benzimidazoles were effectively synthesized by a rapid 'onepot' nitro reductive cyclization reaction using sodium hydrosulfite as a reagent. All reactions were conducted using both the microwave and conventional methods to compare yields and reaction times. Antioxidant activities of the synthesized compounds were clarified using various in vitro antioxidant assays including Cupric Reducing Antioxidant Capacity (CUPRAC, ranging from 5.511 to 19.703 mM Trolox/mg compound) and Ferric Reducing Antioxidant Power (FRAP) (1.141-12.943 mM FeSO4 center dot 7H(2)O/mg compound) assays. Also, the radical scavenging activities of these compounds were assayed using ABTS(center dot+) and DPPH center dot methods. the results showed that all compounds exhibited very high scavenging activity. These synthesized compounds were then evaluated for their a-glucosidase inhibitory potential and seven compounds demonstrated an inhibitory potential much better than the standard acarbose. Herein, we will provide details of the structure activity relationship of the benzimidazole analog for the potency. (C) 2017 Elsevier Inc. All rights reserved.Recep Tayyip Erdogan University, BAP, TurkeyRecep Tayyip Erdogan University [FBA-2017-700]The authors gratefully acknowledge financial support from Recep Tayyip Erdogan University, BAP, Turkey, through Project number FBA-2017-700

Synthesis and kinetics studies of N '-(2-(3,5-disubstituted-4H-1,2,4-triazol-4-yl)acetyl)-6/7/8-substituted-2-oxo-2H-chromen-3-carbohydrazide derivatives as potent antidiabetic agents

WOS: 000490073000001PubMed: 31609028A novel series of N '-(2-(3,5-disubstituted-4H-1,2,4-triazol-4-yl)acetyl)-6/7/8-substituted-2-oxo-2H-chromen-3-carbohydrazides were synthesized and studied for their alpha-glucosidase inhibition activity. Most of the synthesized compounds exhibited potential alpha-glucosidase inhibition activity with IC50 values ranging from 0.96 +/- 0.02 to 32.86 +/- 0.73 mu g/ml. Among them, compounds 3e and 4e, having a methoxy group on the coumarin ring, proved to be the most potent ones, showing an enzyme inhibition activity with IC50 = 0.96 +/- 0.02 and 1.44 +/- 0.06 mu g/ml, respectively. the kinetic study through Lineweaver-Burk plots revealed that the inhibition mechanism of the most active compounds 3d, 3e, 4d, and 4e, on the alpha-glucosidase activity, was found to be in the competitive mode

SYNTHESIS OF SOME NOVEL PYRAZOLINE AND PYRAZOLE DERIVATIVES AS POTENTIAL IN VITRO ANTI-XANTHINE OXIDASE AND ANTIOXIDANT ACTIVITIES

WOS: 0004618057000012-Pyrazolines and 2-pyrazole, electron-rich nitrogen containing heterocyclic systems, play an important role in several biological and pharmacological activities. in this paper, we report the synthesis of novel 3,5-disubtituted-2-pyrazoline and pyrazole derivatives (2a-b, 3a-b) starting from azachalcones (1a, 1b). the structure of the synthesised compounds were judged by H-1 NMR, C-13 NMR and IR. the synthesised 3,5-disubtituted- 2-pyrazoline and pyrazole derivatives were evaluated in vitro for their xanthine oxidase (XO) inhibitory activities, with most of the investigated compounds being shown to be potent inhibitors of bovine milk XO. Antioxidant activities of the synthesised compounds (1a, 1b, 2a-b, 3a-b) were determined with CUPric Reducing Antioxidant Capacity (CUPRAC), ABTS (2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)/Persulphate and DPPH (1,1-diphenyl-2-picrylhydrazyl) assays. Pyrazoline and pyrazol derivatives also revealed notable antioxidant activities in DPPH scavenging (SC50: 9.91-15.16 mu g/mL) and cupric reducing/antioxidant capacity (5.68-10.56 mM TEAC) tests. Also, compounds 3-(3-methylthiophen-2-yl)-5-(2-pyridinyl)-1H-pyrctzoline (2a) and 3-(4-methylthiophen-2-yl)-5-(2-pyridinyl)-1H-pyrazoline (2b) were found to be more potent radical scavenging activity than butylated hydroxy toluene (BHT) to ABTS(center dot+ )radical cation decolorisation assay.Recep Tayyip Erdogan UniversityRecep Tayyip Erdogan University [2013.102.02.6]This study was supported by grants from Recep Tayyip Erdogan University (project number: 2013.102.02.6) of Turkey

Synthesis and Antioxidant Evaluation of Some Novel Benzimidazole Derivatives Containing a Triazole Nucleus

WOS: 000395673500010Various benzimidazole compounds containing a triazole nucleus were synthesized and screened for their antioxidant activies. the structures of newly synthesized compounds were characterized by H-1 NMR, C-13 NMR and elemental analysis data. Antioxidant features of the synthesized compounds were investigated by different processes such as 2,2-diphenyl picryl hydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and CUPric reducing antioxidant capacity (CUPRAC) methods. Significant antioxidant activity was achieved by some of the synthesized compounds demonstrated as much activity as standards (AA and BHT). Correlation analysis between the CUPRAC antioxidant and ABTS radical scavenging assays revealed positive correlation (R-2=0.926), indicating differing antioxidant activities based on the reaction mechanism.Recep Tayyip Erdogan University Scientific Research Project UnitRecep Tayyip Erdogan University [2014.102.02.05]; Recep Tayyip Erdogan UniversityRecep Tayyip Erdogan UniversityThe authors report no conflicts of interest. This work was supported by Recep Tayyip Erdogan University Scientific Research Project Unit (BAP) under project number: 2014.102.02.05. Authors thank to Recep Tayyip Erdogan University for this support