Mechanism, kinetics, and antimicrobial activities of 2-hydroxy-1-naphthaldehyde semicarbazone as a new Jack bean urease inhibitor

2016 ◽  
Vol 40 (4) ◽  
pp. 3520-3527 ◽  
Author(s):  
Xue-Yue Jiang ◽  
Liang-Quan Sheng ◽  
Chong-Fu Song ◽  
Na-Na Du ◽  
Hua-Jie Xu ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Urease Inhibitor ◽  
Jack Bean Urease ◽  
Inhibitory Mechanism ◽  
Jack Bean ◽  
Fluorescence Titration ◽  
Titration Assay

A new inhibitor of jack bean urease, 2-hydroxy-1-naphthaldehyde semicarbazone, was synthesized and employed to investigate the inhibitory mechanism of HNDSC on jack bean urease by kinetic and fluorescence titration assay, and its antibacterial activities were also investigated.

scholarly journals Enzyme Inhibitory Kinetics and Molecular Docking Studies of Halo-Substituted Mixed Ester/Amide-Based Derivatives as Jack Bean Urease Inhibitors

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Muhammad Rashid ◽  
Hummera Rafique ◽  
Sadia Roshan ◽  
Shazia Shamas ◽  
Zafar Iqbal ◽  
...  
Keyword(s):  
Docking Studies ◽  
Binding Energies ◽  
Urease Inhibitor ◽  
Jack Bean Urease ◽  
Substituted Anilines ◽  
Jack Bean ◽  
Chemical Structures ◽  
Mixed Ester ◽  
Urease Enzyme ◽  
Better Than

A series of halo-substituted mixed ester/amide-based analogues 4a-l have been prepared as jack bean urease inhibitor, which showed good to excellent inhibition of enzyme activity. The role of halo-substituted benzoyl moieties and alkyl substituted anilines in urease inhibitory kinetics was also investigated. The alkyl-substituted anilines 1a–b reacted with chloroacetyl chloride to afford intermediates 2a-b, which were then reacted with different halo-substituted benzoic acids 3a–f to prepare the title compounds 4a-l. The chemical structures of final products 4a-l were ascertained by FTIR, 1H NMR, 13C NMR, and mass spectra. The compound 4b showed remarkable activity with IC50 1.6 ± 0.2  nM, better than the standard thiourea having IC50 472.1 ± 135.1  nM. The 2-chloro-substituted phenyl ring on one side of compound 4b and 4-isopropyl-substituted benzene on the other side play an essential role in inhibition of urease activity. Lineweaver–Burk plots (kinetics study) indicated about 4b derivative as a mixed type of inhibitor. The virtual screening performed against urease enzyme (PDBID 4H9M) showed that compounds 4b and 4e have binding energies of −7.8 and −7.9 Kcal/mol, respectively. Based upon our results, it was found that derivative 4b is a highly potent urease inhibitor, better than the standard thiourea.

Synthesis and Antimicrobial activities of Some Polyphenol compounds by Nano ZnO-TBAB as a Heterogeneous Catalytic Media

2020 ◽  
Vol 17 ◽  
Author(s):  
Rahele Bargebid ◽  
Ali Khalafi-Nezhad ◽  
Kamiar Zomorodian ◽  
Leila Zamani ◽  
Ali Ahmadinejad ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Reusable Catalyst ◽  
Nano Zno ◽  
Antifungal Activities ◽  
Chemical Structures ◽  
Heterogeneous Catalytic ◽  
Solvent Free Conditions ◽  
New Compounds ◽  
Derivatives Of

Introduction: Mannich reaction is a typical example of a three-component condensation reaction and the chemistry of Mannich bases has been the matter of search by researchers. Here an efficient procedure for the synthesis of some new Mannich derivatives of simple phenols is described. Methods: In this procedure a microwave-assisted and solvent less condensation were done between different phenols, secondary amines and paraformaldehyde. The reactions proceed in the presence of catalytic amount of nano ZnO and tetrabutylammonium bromide (TBAB) in excellent yields. 10 new compounds were synthesized (A1-A10). Chemical structures of all new compounds were confirmed by different spectroscopic methods. We optimized the chemical reactions in different conditions. Optimization reactions were done in the presence of different mineral oxides, different amount of TBAB and also different solvents. Nano ZnO and TBAB in catalytic amounts and solvent free conditions were the best conditions. All the synthesized compounds were screened for their antimicrobial activities. Antifungal and antibacterial activities of the synthesized compounds were evaluated against some Candida, filaments fungi, gram positive and gram negative bacteria by broth micro dilution method as recommended by CLSI. Results: The result showed that compounds A2, A3 and A4 against most of the tested Candida species and compounds A5 and A7 against C. parapsilosis and C. tropicalis, exhibited considerable antifungal activities. Also Compounds A8 and A10 showed desirable antifungal activities against C. neoformance and C. parapsilosis, respectively. The antibacterial activities of the synthesized compounds were also evaluated. Compounds A6 - A10 against E. Fecalis and compounds A5, A7, A9 and A10 against P. aeruginosa showed desirable antibacterial activities. Discussion: We have synthesized some new Mannich adducts of poly-hydroxyl phenols in the presence of nano-ZnO as a reusable catalyst, with the hope of discovering new lead compounds serving as potent antimicrobial agents. The advantages of this method are generality, high yields with short reaction times, simplicity, low cost and matching with green chemistry protocols. The antimicriobial studies of Mannich derivatives of phenols showed desirable results in vitro.

scholarly journals Inhibition of jack bean urease by amphiphilic peptides

2021 ◽  
Author(s):  
Zafar Ali Shah ◽  
Sadam Hussain ◽  
Serab Khan ◽  
Nawab Ali ◽  
Samiullah Burki ◽  
...  
Keyword(s):  
Jack Bean Urease ◽  
Jack Bean ◽  
Amphiphilic Peptides

Polyphenol Contents, Antioxidant and Antibacterial Activities of Aqueous Algerian Propolis Extracts

2021 ◽  
Author(s):  
E.K. Soltani ◽  
K. Zaim ◽  
K. Mokhnache ◽  
N. Haichour ◽  
S. Mezaache-Aichour ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Antibacterial Properties ◽  
Natural Antioxidants ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Aqueous Extracts

The propolis, an extremely complex resinous material, exhibits valuable pharmacological and biological properties, mainly attributed to the presence of polyphenols. The composition of propolis depends on time, vegetation, and the area of collection. Total flavonoid and polyphenol contents of aqueous extracts of propolis samples from different areas of Algeria, determined by using aluminum chloride and Folin–Ciocalteu colorimetric methods, were in the range of 3.047 ± 0.004–5.273 ± 0.013 mg/g and 96.833 ± 0.027–458.833 ± 0.0005 mg/g crude extract of propolis, respectively. This study examined the antioxidant and antimicrobial activities of propolis. Aqueous extracts of propolis were obtained in order to evaluate their antioxidant activities by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging, β-carotene and electrochemical assays. All tested propolis samples had relatively strong antioxidant activities, which were also correlated with the total polyphenol and flavonoid content present. The percentage of inhibition of lipid peroxidation of linoleic acid emulsion during 24 h varied between 86.04 ± 0.42 and 90.60 ± 3.77% among the tested samples. The highest DPPH radical scavenging activity was observed by ABAL (Ain Abassa Aqueous Extract) with IC50 = 8.49 ± 5.07 10−5 μg/ml, and the lowest was observed by SAL (Setif Aqueous Extract) with IC50 of 21.16 ± 0.0001 μg/ml. The most important antibacterial activity was obtained with Ain Abassa extract; the zones of inhibition obtained for this excerpt vary from 15.22 to 15.5 mm. Followed by the Setif extract with areas of 12.33 to 12.75 mm, the Tizi-Ouzou extract with areas of 10.11 to 11.11 mm. This study will bring an innovation for further studies with regard to the antioxidant and antibacterial properties of the aqueous extracts of propolis. This study corroborates that Algerian propolis is a rich source of natural antioxidants, properties which could be used in the prevention of different diseases, both in humans and in animals.

scholarly journals Isolation and antimicrobial effects of endophytic fungi from Edgeworthia chrysantha

2015 ◽  
Vol 10 (3) ◽  
pp. 529 ◽  
Author(s):  
Huawei Zhang ◽  
Chuanfeng Ruan ◽  
Xuelian Bai
Keyword(s):  
Ethyl Acetate ◽  
Endophytic Fungi ◽  
Fermentation Broth ◽  
Fungal Endophytes ◽  
Antimicrobial Effect ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Human Pathogens ◽  
Antimicrobial Effects ◽  
Staphyloccocus Aureus

<p>Ten fungal strains isolated from <em>Edgeworthia chrysantha</em>, one of traditional medicinal plants in China, were evaluated their antimicrobial activities against three human pathogens, <em>Escherichia coli, Staphyloccocus aureus and Candida albicans</em>, and two phytopathogens, <em>Rhizoctonia cerealis</em> and <em>Colletotrichum gloeosporioides</em>. The results indicated that most ethyl acetate extracts of fermentation broth of these fungal endophytes had stronger antimicrobial activities than their fermentation broth. Among these endophytic strains, both fermentation broth and the ethyl acetate extract of strain D showed the strongest inhibitory effects on all pathogens. Strains 5-19 and BZ also exhibited potent antibacterial activities. However, other strains had weak or no antimicrobial effect. This was the first report on the isolation and antimicrobial effects of endophytic fungi from <em>E. chrysantha</em>.   </p><p> </p>

scholarly journals Antifungal and Antibacterial Activities of Apple Vinegar of Different Cultivars

2021 ◽  
Vol 2021 ◽  
pp. 1-6
Author(s):  
Driss Ousaaid ◽  
Hassan Laaroussi ◽  
Meryem Bakour ◽  
Hayat Ennaji ◽  
Badiaa Lyoussi ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Total Phenolic Content ◽  
Phenolic Content ◽  
Antimicrobial Effect ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Total Phenolic ◽  
Plate Method ◽  
Golden Delicious ◽  
Pathogenic Microbes

This study was designed to assess the antimicrobial potencies of apple vinegar against pathogenic microbes. The acidity and total phenolic content were carried out by titration with NaOH 0.1 N and the Folin–Ciocalteu method, respectively, while the spread plate method, agar well diffusion, and MIC assays were used to determine the antimicrobial activities of different vinegar samples. Acidity and phenolic content were dependent on the variety, where the highest values were observed in S2 with 4.02 ± 0.04% and 1.98 ± 0.05 mg GAE/mL for acidity and total phenolic content, respectively. The spread plate method revealed that samples S1 and S2 obtained from the Red delicious variety and Golden delicious variety, respectively, inhibit the growth of all tested strains, while S3 obtained from different varieties and S4 obtained from the Gala royal variety inhibit only two microbes (Escherichia coli and Vibrio cholerae). Sample S1 presented moderate antimicrobial effect against all examined strains with a diameter of inhibition ranging from 11 ± 0.7 to 19 ± 0.5 mm and with MIC values ranging between 1/2 and 1/100. The findings of the current study confirm the usefulness of apple vinegar as a natural sanitizer that inhibits the growth of pathogenic microbes.

scholarly journals In-vitro Antimicrobial Activities and Phytochemical Screening of Selected Plant Extracts against Some Medically and Agriculturally Important Pathogens

2020 ◽  
pp. 167-189
Author(s):  
Yirgashewa Asfere ◽  
Ameha Kebede ◽  
Dejene Zinabu
Keyword(s):  
Stem Bark ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Plant Parts ◽  
Antibacterial And Antifungal Activities ◽  
Ruta Chalepensis ◽  
Crude Extracts ◽  
Growth Inhibitory ◽  
Scientific Justification

In Ethiopia, many plants are used for medicinal drive-by old-style naturopaths without any scientific justification for their therapeutic values. The principal aim of this study were to evaluate the in vitro antibacterial and antifungal activities of the leaf, root and stem bark extracts of Rhamnus prinioides (gesho), Justicia schimperiana (sensel) and Ruta chalepensis (Tena adam) against some common pathogenic species of bacteria and fungi. The results of this study shown that the crude extracts of ethanol, methanol, hexane and water crude extracts had antimicrobial activities on most bacterial and fungi species of some solvent extracts. Ethanol and methanol crude extracts had the highest growth inhibitory effects as compared with those of the aqueous and hexane crude extracts. But, the four solvent crude extracts had fewer antimicrobial activities than commercially available drug(chloramphenicol and clotrimazole). Campylobacter jejuni and Staphylococcus aureus were found to be the most vulnerable microbes to the crude ethanol (99.5%). The growth-inhibitory events of the crude extracts were found to be significantly dissimilar for both concentrations (30 and 60 mg/ml) in all plant parts (p < 0.05). In general, this study did not only indicate that the antibacterial activities of R. prinioides (gesho), J. schimperiana (sensel) and R. chalepensis (Tena adam). It also accesses a scientific justification for its old-style use against some diseases.

Single-step purification of urease by affinity chromatography

1974 ◽  
Vol 20 (4) ◽  
pp. 623-630 ◽  
Author(s):  
Bassanio L. Wong ◽  
Charles R. Shobe
Keyword(s):  
Enzyme Activity ◽  
Affinity Chromatography ◽  
Single Step ◽  
Jack Bean Urease ◽  
Jack Bean ◽  
Specific Activities ◽  
Single Step Purification

Single-step purification of urease (urea aminohydrolase; EC. 3.5.1.5) from cell-free extracts of Proteus morganii and from partially purified preparations of jack bean urease were achieved in less than 90 min by affinity chromatography on hydroxyurea-substituted beaded agarose columns. The specific activities of the purified enzymes were as high as, or higher than, those reported by other authors for urease preparations obtained by conventional techniques. In addition, yields of enzyme activity were routinely 6 to 100 times greater than recoveries previously reported for this enzyme.

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