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1.
The current study was designed to evaluate the urease inhibitory profile of extract and fractions of Pistacia atlantica ssp. cabulica Stocks followed by bioactivity-guided isolated compounds. The crude extract was found significantly active with urease inhibitor (95.40% at 0.2 mg/mL) with IC50 values of 32.0 ± 0.28 μg/mL. Upon fractionation, ethyl acetate fraction displayed 100% urease inhibition with IC50 values of 19.9 ± 0.51 μg/mL at 0.2 mg/mL. However, n-hexane and chloroform fractions exhibited insignificant urease inhibition. Similarly, the isolated compound, transilitin (1) and dihydro luteolin (2) demonstrated marked urease attenuation with 95 and 98% respectively, at 0.15 mg/mL. Both the isolated compounds showed marked potency with IC50 values of 8.54 ± 0.54 and 9.58 ± 2.22 μg/mL, respectively. In short, both the extract and fractions and isolated compounds showed marked urease inhibition and thus a useful natural source of urease inhibition. 相似文献
2.
Muhammad Alamzeb M. Rafiullah Khan Mamoon-Ur-Rashid Saqib Ali Ashfaq Ahmad Khan 《Natural product research》2015,29(17):1664-1669
Bioassay-guided isolation and fractionation of Berberis jaeschkeana Schneid var. jaeschkeana stem resulted in the isolation and characterisation of a new long chain hydroxy ester named as berberinol (1) along with six known compounds (2–7). All the structures were established from 1D and 2D spectroscopic data. Crude extract, sub-fractions and all the isolated compounds were evaluated for their anti-fungal and urease enzyme inhibition properties. All of the sub-fractions and compounds showed good anti-fungal and urease enzyme inhibition properties. Minimum inhibitory concentrations (MICs) were calculated for all active samples in case of urease enzyme inhibition. MICs values were found to be in the range of 39.03–49.78 μg/mL for urease enzyme inhibition. 相似文献
3.
In the present study, the copolymeric hydrogels based on 2-hydroxyethyl methacrylate (HEMA) and itaconic acid (IA) were synthesized by gamma radiation induced radical polymerization, in order to examine the potential use of these hydrogels in immobilization of Citrullus vulgaris urease. Gelation and Swelling properties of PHEMA and copolymeric P (HEMA/IA) hydrogels with different IA contents (96.5/3.5, 94.4/5.6 and 92.5/7.5 mol) were studied in a wide pH range. Initial studies of so-prepared hydrogels show interesting pH sensitivity in swelling and immobilization. C. vulgaris urease was immobilized on HEMA/IA (92.5/7.5) at 6 kGy with 41.3% retention of activity. The properties of free and immobilized urease were compared. Immobilized urease maintained a higher relative activity than free urease at both lower and higher pH levels, indicating that the immobilized urease was less sensitive to pH changes than the free urease. The Km value of the immobilized urease was approximately 2 times higher than that of the free urease. Temperature stability was improved for immobilized enzyme. The free form exhibited a loss about 80% of activity upon incubation for 15 min at 80°C. The influence of various heavy metal ions at the concentration of l mM was improved after enzyme immobilization. The immobilization of C. vulgaris urease on HEMA/IA (92.5/7.5) at 6 kGy showed a residual activity of 47 % after 4 reuses. 相似文献
4.
Brussine Nadège Wakeu Kweka Jean-Bosco Jouda Gertrude Foudjo Melacheu Lazare Sidjui Sidjui Pierre Mkounga Mehreen Lateef 《Natural product research》2019,33(14):2011-2015
A new lactam, oligoamide (1), along with three known compounds (2–4), stigmasterol-3-O-β-D-glucopyranoside (2), formononetin (3) and (-)-pinitol (4) were isolated from the CH2Cl2/CH3OH (1:1) extract of the leaves of Angylocalyx oligophyllus by chromatographic separation. Their structures were elucidated on the basis of spectroscopic analysis (UV, IR, MS, 1D, and 2D NMR). Compound 1 was found to have weak antioxidant and urease inhibitory potential. 相似文献
5.
Anwar Sadat M. Alam Ashfaq Ahmad Bina Shaheen Siddiqui 《Natural product research》2015,29(24):2291-2294
Ethanol extract of the aerial parts of Bergenia ligulata was subjected to solvent–solvent separation followed by various chromatographic techniques that lead to isolation of bergenine (1), p-hydroxybenzoyl bergenin (2), 11-O-galloylbergenin (3) and methyl gallate (4) as major constituents. Ethyl acetate fraction showed a dose-dependent urease inhibitory pattern with IC50 value of 54μg/mL. Structures of compounds 1 and 3 were established by XRD and 2, 4 by NMR. All these compounds were subjected to DPPH scavenging activity, reducing power assay and urease inhibitory activity. The EC50 7.45 ± 0.2 μg/mL and 5.39 ± 0.28 μg/mL values in terms of antioxidant and reducing power, respectively, were less for 3. Compounds 1–3 showed moderate to significant urease inhibitory potential with IC50 57.1 ± 0.7, IC50 48.4 ± 0.3 and 38.6 ± 1.5. Antioxidant activities and urease inhibitory potential were investigated and compound 3 was found to be the most active. 相似文献
6.
Rasool Khan Abdullah Qasem Saif Mohammad Mansour Quradha Jawad Ali Abdur Rauf 《Natural product research》2015,29(5):466-468
In this paper we report the antimicrobial, antiradical and urease inhibitory potential along with photochemical investigation of the crude extracts of Cyphostemma digitatum Lam. Phytochemical screening of both the crude (hot/cold) alcoholic and aqueous extracts of C. digitatum showed the presence of alkaloids, flavonoids, saponins, coumarins, steroids, terpenoids and tannins. The crude methanolic extract (hot/cold) exhibited good antioxidant activity, while the aqueous extract was a weak antioxidant. The crude methanolic extract was found to be more active against Bacillus subtilis, while both the extracts showed moderate antifungal potential, the methanolic crude extract showed good urease inhibitory activity compared with the aqueous crude extract. 相似文献
7.
A new hydrazone 4-bromo-N′-(2-hydroxy-5-methoxybenzylidene)benzohydrazide (HL) was prepared and characterized by infrared and UV–vis spectra, as well as single-crystal X-ray diffraction. With the hydrazone as ligand, two new copper(II) complexes were prepared, [Cu2L2(NCS)2]·4H2O (1) and [CuBrL]·CH3OH (2). The complexes were characterized by infrared and UV–vis spectra, and single-crystal X-ray diffraction. The Cu in 1 is in a square pyramidal coordination geometry and that in 2 is in a square planar coordination geometry. The two complexes show effective Jack bean urease inhibitory activity, with IC50 values of 23.5 and 2.7 μM, respectively. A molecular docking study of 2 with the urease was performed. The relationship between the structure and urease inhibitory activity indicated that copper complex with square planar coordination is a better model for urease inhibition. 相似文献
8.
Nicholas E. Manicke Thomas Kistler Demian R. Ifa R. Graham Cooks Zheng Ouyang 《Journal of the American Society for Mass Spectrometry》2009,20(2):321-325
A newly developed high-throughput desorption electrospray ionization (DESI) source was characterized in terms of its performance
in quantitative analysis. A 96-sample array, containing pharmaceuticals in various matrices, was analyzed in a single run
with a total analysis time of 3 min. These solution-phase samples were examined from a hydrophobic PTFE ink printed on glass.
The quantitative accuracy, precision, and limit of detection (LOD) were characterized. Chemical background-free samples of
propranolol (PRN) with PRN-d7 as internal standard (IS) and carbamazepine (CBZ) with CBZ-d10 as IS were examined. So were two other sample sets consisting of PRN/PRN-d7 at varying concentration in a biological milieu of 10% urine or porcine brain total lipid extract, total lipid concentration
250 ng/μL. The background-free samples, examined in a total analysis time of 1. 5 s/sample, showed good quantitative accuracy
and precision, with a relative error (RE) and relative standard deviation (RSD) generally less than 3% and 5%, respectively.
The samples in urine and the lipid extract required a longer analysis time (2. 5 s/sample) and showed RSD values of around
10% for the samples in urine and 4% for the lipid extract samples and RE values of less than 3% for both sets. The LOD for
PRN and CBZ when analyzed without chemical background was 10 and 30 fmol, respectively. The LOD of PRN increased to 400 fmol
analyzed in 10% urine, and 200 fmol when analyzed in the brain lipid extract. 相似文献
9.
《Journal of Coordination Chemistry》2012,65(24):4164-4179
AbstractUrease catalyzes the decomposition of urea into ammonia, which has harmful effects on both human health and fertile soil. Aiming at exploring novel urease inhibitors, a series of hydrazone compounds and their CoIII, CuII, NiII, and ZnII complexes were prepared from 4-methoxy-N'-(pyridin-2-ylmethylene)benzohydrazide (HL). They are [CoClL(NCS)] (1), [CoL2]·Cl·CH3OH·H2O (2), [CuL(NCNCN)]n·nCH3OH (3), [NiL(HL)]·ClO4·CH3OH (4) and [ZnClL(OH2)]·CH3OH (5). The compounds were characterized by physico-chemical methods. Structures of the complexes were further confirmed by single crystal X-ray diffraction. The metal ions in 1, 3, and 5 display square pyramidal coordination and 2 and 4 display octahedral coordination. The inhibitory effects of the compounds on Jack bean urease were evaluated. The results showed that 3 has effective urease inhibitory activity, with IC50 value of (7.3?±?1.0) μmol L?1. 相似文献
10.
A highly sensitive, specific and simple LC‐MS/MS method was developed to investigate in vivo bio‐transformation of oleuropein in rat. Rat urine samples collected after the intravenous administrations were determined using liquid chromatography coupled to tandem mass spectrometry with electrospray ionization in the negative‐ion mode. The assay procedure involves a simple liquid–liquid extraction of parent oleuropein and the metabolite from rat urine with ethyl acetate. Chromatographic separation was operated with 0.1% formic acid aqueous and methanol in gradient program at a flow rate of 0.80 mL/min on an RP‐C18 column with a total run time of 30 min. This method has been successfully applied to simultaneous determination of oleuropein and its metabolite in rat urine. Oxygenation was found to be the major metabolic pathway of the oleuropein in rat after intravenous administration. Copyright © 2011 John Wiley & Sons, Ltd. 相似文献
11.
Luca Mazzei Michele Cianci Stefano Ciurli 《Chemistry (Weinheim an der Bergstrasse, Germany)》2022,28(64):e202201770
Hydroquinones are a class of organic compounds abundant in nature that result from the full reduction of the corresponding quinones. Quinones are known to efficiently inhibit urease, a NiII-containing enzyme that catalyzes the hydrolysis of urea to yield ammonia and carbonate and acts as a virulence factor of several human pathogens, in addition to decreasing the efficiency of soil organic nitrogen fertilization. Here, we report the molecular characterization of the inhibition of urease from Sporosarcina pasteurii (SPU) and Canavalia ensiformis (jack bean, JBU) by 1,4-hydroquinone (HQ) and its methyl and tert-butyl derivatives. The 1.63-Å resolution X-ray crystal structure of the SPU-HQ complex discloses that HQ covalently binds to the thiol group of αCys322, a key residue located on a mobile protein flap directly involved in the catalytic mechanism. Inhibition kinetic data obtained for the three compounds on JBU reveals the occurrence of an irreversible inactivation process that involves a radical-based autocatalytic mechanism. 相似文献
12.
In this study, the urease-dextran non-covalent complexes in various molar ratios were synthesized and compared to the free enzyme in terms of pH, temperature, thermal and storage stabilities. Especially, the complex with a molar ratio of nU/nDA = 40/1 showed highest thermal stability and had ca. 1.4-fold at 25°C and 2.5-fold at 80°C higher activity than the free enzyme. The complex showed a high catalytic activity in organic solvent. In addition, the thermal and storage stabilities of urease were improved greatly as dextran complex, which has advantages for usage in practice. 相似文献
13.
Salih Osman Mohammed El Sayed H. El Ashry Asaad Khalid Mohamed R. Amer Ahmed M. Metwaly Ibrahim H. Eissa Eslam B. Elkaeed Ahmed Elshobaky Elsayed E. Hafez 《Molecules (Basel, Switzerland)》2022,27(3)
The urease enzyme has been an important target for the discovery of effective pharmacological and agricultural products. Thirteen regio-selectively alkylated benzimidazole-2-thione derivatives have been designed to carry the essential features of urease inhibitors. The urease enzyme was isolated from Helicobacter pylori as a recombinant urease utilizing the His-tag method. The isolated enzyme was purified and characterized using chromatographic and FPLC techniques showing a maximal activity of 200 mg/mL. Additionally, the commercial Jack bean urease was purchased and included in this study for comparative and mechanistic investigations. The designed compounds were synthesized and screened for their inhibitory activity against the two ureases. Compound 2 inhibited H. pylori and Jack bean ureases with IC50 values of 0.11; and 0.26 mM; respectively. While compound 5 showed IC50 values of 0.01; and 0.29 mM; respectively. Compounds 2 and 5 were docked against Helicobacter pylori urease (PDB ID: 1E9Y; resolution: 3.00 Å) and exhibited correct binding modes with free energy (ΔG) values of −9.74 and −13.82 kcal mol−1; respectively. Further; the in silico ADMET and toxicity properties of 2 and 5 indicated their general safeties and likeness to be used as drugs. Finally, the compounds’ safety was authenticated by an in vitro cytotoxicity assay against fibroblast cells. 相似文献
14.
Gui-Hua Sheng Tian-Rui Wang Cun-Fang Wang Xiang-Fei Chen Zheng Ma Hai-Liang Zhu 《Journal of Coordination Chemistry》2017,70(20):3501-3512
[CuII(L)2.C12H10N2] with flufenamic acid (HL=C14H10F3NO2) and phenanthroline (C12H10N2O) was synthesized and characterized by C, H and N elemental analysis, single-crystal X-ray diffraction and, IR spectra. The urease inhibitory and antibacterial activities of the complex were tested. The complex showed strong inhibitory activity against jack bean urease with an IC50 value of 0.265 μM. Four bacteria, Bacillus subtilis, Escherichia coli, Staphylococcus aureus, and proteusbacillus vulgaris, were used in the antibacterial test. The complex showed strong inhibitory activity against the species with IC50 values of 2.016, 35.037, 10.680, and 3.820 μM. The interactions of the complex with human serum albumin (HSA) were studied through fluorescence spectroscopy. By analyzing the experimental data, we concluded that the fluorescence quenching mechanism of the complex with serum albumin was static quenching. The binding mode of the complex with DNA through UV spectroscopy was electrostatic binding or groove. 相似文献
15.
Sihan Guo Tianrui Wang Jiajin Xin Qiqige Hu Shanfa Ren Guihua Sheng 《Journal of Coordination Chemistry》2017,70(20):3449-3458
Two new copper(II) complexes, [CuL(HL)]·ClO4 (1) and [Cu2Br2L2]·0.85H2O (2), where L is the monoanionic form of 4-tert-butyl-N′-(1-(pyridin-2-yl)ethylidene)benzohydrazide (HL), have been prepared. The complexes were characterized by infrared and UV–vis spectra, and single crystal X-ray diffraction. Complex 1 is a mononuclear copper(II) species and 2 is a bromido-bridged dinuclear copper(II) species. The Cu ion in 1 is in an octahedral coordination mode and that in 2 is trigonal-bipyramidal. The Jack bean urease inhibitory assay indicated that 2 is active, with IC50 value of 20.6 ± 2.3 μmol L?1, while 1 is inactive. Molecular docking of 2 with Jack bean urease was studied. 相似文献
16.
《Arabian Journal of Chemistry》2022,15(5):103797
Tripleurospermum limosum (TL) has been used in folk medicine to treat gastritis. Toward the further development and use of TL, we report the phytochemical profiling, determination of active components, and antioxidant and enzyme inhibitory activities of TL. Nineteen compounds were identified by ultra-performance liquid chromatography-electrospray ionization-orbitrap-mass spectrometry for the first time in this plant. Phytochemical studies indicated that TL contained 11 types of phytochemicals. The active components [total carbohydrate content (TCC), total protein content (TProC), total triterpenoid content (TTC), total phenolic content (TPheC), total flavonoid content (TFC), total phenolic acid content (TPAC), condensed tannin content (CTC), and gallotannin content (GC)] of eight different solvent extracts were determined by ultraviolet–visible spectrophotometry. Aqueous extract had highest TProC, TPheC, and GC values. Methanol extract exhibited highest TCC and TFC values. Ethanol extract showed highest TPAC and CTC values and dichloromethane extract exhibited highest TTC value. Methanol extract showed strongest ability to scavenge 2,2-diphenyl-1-picrylhydrazyl radicals, 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt cation radicals, and hydroxyl radicals, and also exhibited highest antioxidant activity in ferric-reducing antioxidant power and cupric ion-reducing antioxidant capacity assays. Best iron and copper chelating activity and H2O2 scavenging ability were shown by aqueous extract. Ethanol extract showed strongest ability to scavenge superoxide radicals and effectively prevent β-carotene bleaching. Acetone extract had highest inhibitory activity toward α-glucosidase, α-amylase, and xanthine oxidase. Ethyl ether extract had highest inhibitory activity towards urease and angiotensin converting enzyme. Aqueous and ethanol extracts had strongest inhibitory activity toward acetylcholinesterase. Methanol extract showed highest inhibitory activity toward tyrosinase. Methanol extract showed good stability and antioxidant capacity during heating, at different pH values, and after in vitro digestion and had low toxicity. The efficacy of methanol extract in stabilizing olive and sunflower oils was studied, the results suggested that methanol extract had a protective effect on the primary oxidation of the two oils. TL may be useful as a source of active components for application in human nutrition and/or phytomedicine and methanol extract of TL could be used as a natural oil stabiliser. 相似文献
17.
Cun-Fang Wang Zhi-Jian Chen Ke-Dong Zhao Xiang-Fei Chen Chun-Yang Zhang 《Journal of Coordination Chemistry》2016,69(18):2656-2665
[CoIII(L1)2·H2O]NO3 (1), [MnII(L1)2·H2O] (2), and [ZnII(L1)2·H2O] (3) with a hydrazone derived from protocatechuic acid (HL1 = C15H13N3O3) were designed, synthesized, and characterized by C, H, N elemental analyses, single-crystal X-ray diffraction, and IR spectra, which revealed that the three complexes are similar structures. Docking study has been done. The urease inhibitory activities of the three complexes were tested. Complexes 1 and 3 showed strong inhibitory activity against jack bean urease with IC50 values of 45.9 and 11.64 μM. Complex 2 had no obvious inhibitory activity to urease; the IC50 was > 50 μM. 相似文献
18.
0IntroductionRareearthsarenowappliedwidelyinChina,whichcanimprovecropsyieldsandthetheirqualit-ies犤1犦.Thebeneficialeffectsmaybeduetothestimu-latoryeffectsoftheseelementsonthenutrientuptakebyplantsorontheincreasingofchlorophyllsynthesisintheplants犤2犦.Whilealotofresearcheshavebeendoneontheimprovednutritionofcropsafterapplica-tionofrareearths,muchlessattentionhasbeenpaidtothedeteriorationofsoilqualityduetotheapplicationofrareearthsforyears犤3犦.Scientistshavediscoveredthataccumula… 相似文献
19.
Tareq Abu-Izneid Abdur Rauf Muhammad Saleem Nashwa Mansour Mohamed I. S. Abdelhady Munjed M. Ibrahim 《Natural product research》2020,34(4):553-557
AbstractUrease inhibition potential of compound (1), guaiane-type sesquiterpene (2), confertin (3) and scopoletin (4) was carried out with high throughout mechanism-based assay. These compounds were isolated from Hypochaeris radicata L., an Asteraceae family member. The pure compounds were screened for their urease and carbonic anhydrase inhibitory activities. The ethyl acetate fractions were subjected to column chromatography, which resulted in the isolation and purification of four compounds (1–4). On evaluation, compounds (1–4) exhibited selective activity against urease enzyme with an IC50 value of 180.11 ± 2.00, 27.18 ± 0.80, 24.12 ± 0.2 and 30.12 ± 1.10 µM respectively. The compounds (1–4) were found to be inactive against carbonic anhydrase enzyme. Thiourea was used as standard inhibitor (21 ± 0.14 µM) of urease enzyme. 相似文献
20.
Ondansetron, a 5‐hydroxytryptamine type 3 (5‐HT3) receptor antagonist, is regarded as an excellent candidate to treat chemotherapy‐ and radiotherapy‐induced nausea and vomiting. To better understand the metabolic profiles of ondansetron in human urine, the metabolites were analyzed using liquid chromatography/mass spectrometry (LC/MSn). Urine samples were collected after oral administration of 8 mg ondansetron to healthy volunteers. Then samples were treated by solid‐phase extraction and detected with LC/MSn. Besides ondansetron, in human urine, a total of 19 metabolites including 13 new metabolites were detected and identified via comparing the retention time and product ion spectra with those of reference standards isolated and characterized. The results showed that ondansetron was metabolized via hydroxylation, glucuronidation, sulfation and minor N‐demethylation in human. LC/MSn was demonstrated to be useful and sensitive in the metabolic study of ondansetron. 相似文献