Antimicrobial and antioxidant evaluation of new quinolone based aurone analogs

Jardosh, Hardik H.; Patel, Manish P.

doi:10.1016/j.arabjc.2014.05.014

Cited by 29 publications

(13 citation statements)

References 33 publications

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“…evaluated the antibacterial effects of synthetic aurones and reported significant antibacterial effects against S. aureus , B. subtilis , C. tetani , E coli , P. aeruginosa , and Vibrio cholera as well as antifungal effects against C. albicans and A. clavatus . [ 12 ] In addition, Riaz et al . approved the antibacterial and antifungal effect of Snapdragon extract against Pasteurella multocida , Escherichia coli , B. subtilis , Aspergillus flavus , Aspergillus niger , Alternaria alternata , and Rhizopus solani .…”

Section: Discussionmentioning

confidence: 99%

“…Interestingly, most of the aurone analogs have shown excellent antibacterial and antifungal activities when compared with standard antibiotics and their minimum inhibitory concentrations (MICs) against Gram-positive bacteria such as Staphylococcus aureus , Bacillus subtilis , and Clostridium tetani and Gram-negative bacteria such as Escherichia coli and Pseudomonas aeruginosa and even against fungi such as Candia albicans , and Aspergillus clavatus has been determined. [ 11 12 ]…”

Section: Introductionmentioning

confidence: 99%

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Formulation of Herbal Gel of Antirrhinum majus Extract and Evaluation of its Anti- Propionibacterium acne Effects

et al. 2018

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Background:Antirrhinum majus contains aurone with excellent antibacterial and antifungal activities. In addition, visible light activates the endogenous porphyrins of Propionibacterium acne, which results in bacterial death. Therefore, considering the above-mentioned facts, the aim of the present study was to prepare a topical herbal gel of A. majus hydroalcoholic extract and to evaluate its antiacne effects with or without blue light combination as an activator of the porphyrins.Materials and Methods:Antibacterial activity of the shoot or petal extracts was evaluated by disc diffusion method and the minimum inhibitory concentration (MIC) was calculated. Various gel formulations were developed by the Experimental Design software. The obtained gel formulations were prepared and tested for pharmaceutical parameters including organoleptic features, pH, viscosity, drug content, and release studies. Finally, the antibacterial activity was evaluated against (P. acnes) with or without blue light.Results:The MIC of the extracts showed to be 0.25 μg/ml. Evaluation of the gel formulation showed acceptable properties of the best formulation in comparison to a gel in the market. Pharmaceutical parameters were also in accordance with the standard parameters of the marketed gel. Furthermore, statistical analyses showed significant antibacterial effect for gel when compared to negative control. However, combination of blue light with gel did not show any significant difference on the observed antibacterial effect.Conclusion:Because of the statistically significant in vitro antiacne effects of the formulated gel, further clinical studies for evaluation of the healing effects of the prepared gel formulation on acne lesions must be performed.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Formulation of Herbal Gel of Antirrhinum majus Extract and Evaluation of its Anti- Propionibacterium acne Effects

et al. 2018

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“…They are also considered phytoalexins produced by plants in response to pathogen attack [ 33 ]. Aurone derivatives have been reported to possess different bio-activities [ 34 ], such as anti-inflammatory [ 35 ], antibacterial [ 36 ], anti-malarial [ 37 , 38 ], anti-hepatitis [ 39 , 40 ], antioxidant [ 41 , 42 , 43 , 44 ], anticancer [ 45 , 46 , 47 , 48 , 49 ], and others. However, their ability to inhibit HPL has not been studied.…”

Section: Introductionmentioning

confidence: 99%

Exploring Aurone Derivatives as Potential Human Pancreatic Lipase Inhibitors through Molecular Docking and Molecular Dynamics Simulations

et al. 2020

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Inhibition of human pancreatic lipase, a crucial enzyme in dietary fat digestion and absorption, is a potent therapeutic approach for obesity treatment. In this study, human pancreatic lipase inhibitory activity of aurone derivatives was explored by molecular modeling approaches. The target protein was human pancreatic lipase (PDB ID: 1LPB). The 3D structures of 82 published bioactive aurone derivatives were docked successfully into the protein catalytic active site, using AutoDock Vina 1.5.7.rc1. Of them, 62 compounds interacted with the key residues of catalytic trial Ser152-Asp176-His263. The top hit compound (A14), with a docking score of −10.6 kcal⋅mol−1, was subsequently submitted to molecular dynamics simulations, using GROMACS 2018.01. Molecular dynamics simulation results showed that A14 formed a stable complex with 1LPB protein via hydrogen bonds with important residues in regulating enzyme activity (Ser152 and Phe77). Compound A14 showed high potency for further studies, such as the synthesis, in vitro and in vivo tests for pancreatic lipase inhibitory activity.

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“…Aurones, (Z)-2-benzylidenebenzofuran-3-(2H)-ones ( Figure 1c), constitute a less studied subclass of flavonoids although they are isosteres of flavones 5,6 . However, they have attracted attention with promising biological potential such as anti-microbial 7 , anti-cancer 8 , anti-leishmanial [9][10][11] , anti-histaminic 12 , antiinflammatory 13 , antioxidant 14 , insect anti-feedant 15 , herbicidal 16 , anti-HIV 17,18 , anti-HCV (hepatis C virus) 19,20 , anti-malarial 21,22 , ChE inhibitory 23,24 , MAO inhibitory 25 activities in the specified studies. The observed biological potential is thought to be due to the similarity of adenine of ATP and the flavonoids, consequently inhibition of the activity of ATP-dependent enzymes and proteins, which is essential for the function of enzymes and receptors.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and anti-cancer activity evaluation of new aurone derivatives

Demirayak

Yurttaş

Gündoğdu-Karaburun

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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In this study, we have synthesized 2-[3-or 4-(2-aryl-2-oxoethoxy)arylidene]benzofuran-3-one derivatives (D1-D38) and evaluated their anti-cancer activities. The final compounds were obtained in multistep synthesis reactions using benzofuranon-3-one derivatives (A1-A4, B) as starting materials which were gained in various synthetic ways. Aurone derivatives (C1-C10) were acquired with the condensation reaction of these starting materials and 3-/4-hydroxybenzaldehyde which were then reacted with a-bromoacetophenones to get final compounds. The anti-cancer activity of the selected compounds was performed by National Cancer Institute (NCI), USA against 60 human tumor cell lines derived from nine neoplastic diseases. Compounds exhibited anti-cancer activity in varying ratios.

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Antimicrobial and antioxidant evaluation of new quinolone based aurone analogs

Cited by 29 publications

References 33 publications

Formulation of Herbal Gel of Antirrhinum majus Extract and Evaluation of its Anti- Propionibacterium acne Effects

Formulation of Herbal Gel of Antirrhinum majus Extract and Evaluation of its Anti- Propionibacterium acne Effects

Exploring Aurone Derivatives as Potential Human Pancreatic Lipase Inhibitors through Molecular Docking and Molecular Dynamics Simulations

Synthesis and anti-cancer activity evaluation of new aurone derivatives

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