scholarly journals New chalcone derivatives as potential antimicrobial and antioxidant agent

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Emelda N. Okolo ◽  
David I. Ugwu ◽  
Benjamin E. Ezema ◽  
Joseph C. Ndefo ◽  
Florence U. Eze ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Antioxidant Activities ◽  
Salmonella Typhi ◽  
Moderate Activity ◽  
Chalcone Derivatives ◽  
No Inhibition ◽  
Standard Compound ◽  
Antioxidant Agent ◽  
Better Than

AbstractSeven chalcone derivatives were synthesized by the Claisen-Schmidt condensation. The structures of the compounds were confirmed by spectral data (Ultraviolet/visible, infrared, nuclear magnetic resonance and mass spectroscopy). The compounds were tested for their in silico and in vitro antimicrobial and antioxidant activities. The molecular docking assessments showed that all the compounds exhibited good binding affinity with the target microorganism proteins but, compounds 6e and 6g showed better binding affinity compared with the standards. The antimicrobial test revealed that all the compounds screened were active against Staphylococcus aureus and Bacillus subtilis and had minimum inhibitory concentrations (MIC) between 0.4 and 0.6 mg/mL. Compounds 6a, 6c and 6d had moderate activities on Salmonella typhi. Compounds 6b and 6c had moderate activity on Escherichia coli. Compound 6c had moderate activity on Aspergillus niger while compounds 6a and 6e had poor activity. All the compounds except compound 6e had no inhibition against Pseudomonas aeruginosa. The in-vitro antioxidant activity was assessed using ethylenediaminetetraacetate (EDTA) as the standard. Compounds 6c, 6e and 6g gave excellent inhibitory activity better than the standard. Compound 6a gave good activity at 500 μg/mL and 1000 μg/mL concentrations but, below the standard at 250 μg/mL and no inhibition at 125 μg/mL. Compound 6d had good inhibition at 500 μg/mL and 1000 μg/mL but, no inhibition at 125 μg/mL and 250 μg/mL. Compound 6b was found to be inactive in all the concentrations. Absorption, distribution, metabolism and excretion properties of the compounds were assessed using SwissADME. The results of lead likeness showed that compound 6e is a lead-like molecule.

scholarly journals Ducrosia ismaelis Asch. essential oil: chemical composition profile and anticancer, antimicrobial and antioxidant potential assessment

2020 ◽  
Vol 18 (1) ◽  
pp. 175-184 ◽  
Author(s):  
Ramzi A. Mothana ◽  
Fahd A. Nasr ◽  
Jamal M. Khaled ◽  
Omar M. Noman ◽  
Nael Abutaha ◽  
...  
Keyword(s):  
Gas Chromatography ◽  
Essential Oil ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Gas Chromatography Mass Spectrometry ◽  
Moderate Activity ◽  
Antioxidant Agent ◽  
Total Oil ◽  
Β Carotene ◽  
Mcf 7

AbstractThe essential oil of Ducrosia ismaelis Asch. (Apiaceae) that grows wild in Saudi Arabia was investigated utilizing gas chromatography (GC), and gas chromatography-mass spectrometry. Fifty constituents were characterized, representing 96.1% of the total oil. The D. ismaelis essential oil (DIEO) was distinguished by a high composition of oxygenated monoterpenes (51.6%). Decanal (40.6%), α-pinene (15.1%) and dodecanal (13.7%) were the fundamental components. Additionally, DIEO was evaluated for its cytotoxic, antibacterial, antifungal and antioxidant activities. DIEO revealed a great cytotoxic effectiveness against the tested cancer cell lines with IC50 values between 66.2 and 137.3 μg/mL particularly against MCF-7 cancer cells. Furthermore, the induction of apoptosis against MCF-7 cells has been asserted using staining assay (annexin VFITC and/or propidium iodide (PI) dyes) and flow cytometry technique. The DIEO possessed a strong antimicrobial activity against Gram-positive bacterial and fungal strains with MIC-values between 0.07 and 0.31 mg/ml. The values of MBC or MFC were almost once higher than those of MIC’s. Moreover, the β-carotene-bleaching and DPPH free radical-scavenging tests showed that DIEO had a moderate activity (68%) as an antioxidant agent in decolouring of the β-carotene at 1.0 mg/mL and a moderate radical scavenging for DPPH (66 and 72%) at 0.50 and 1.0 mg/mL.

scholarly journals Synthesis, Neuroprotection, and Antioxidant Activity of 1,1′-Biphenylnitrones as α-Phenyl-N-tert-butylnitrone Analogues in In Vitro Ischemia Models

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1127 ◽  
Author(s):  
Beatriz Chamorro ◽  
David García-Vieira ◽  
Daniel Diez-Iriepa ◽  
Estíbaliz Garagarza ◽  
Mourad Chioua ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Antioxidant Properties ◽  
Glucose Deprivation ◽  
Oxygen Glucose Deprivation ◽  
Human Neuroblastoma ◽  
In Vitro Ischemia ◽  
Lipoxygenase Inhibition ◽  
Antioxidant Agent

Herein, we report the neuroprotective and antioxidant activity of 1,1′-biphenyl nitrones (BPNs) 1–5 as α-phenyl-N-tert-butylnitrone analogues prepared from commercially available [1,1′-biphenyl]-4-carbaldehyde and [1,1′-biphenyl]-4,4′-dicarbaldehyde. The neuroprotection of BPNs1-5 has been measured against oligomycin A/rotenone and in an oxygen–glucose deprivation in vitro ischemia model in human neuroblastoma SH-SY5Y cells. Our results indicate that BPNs 1–5 have better neuroprotective and antioxidant properties than α-phenyl-N-tert-butylnitrone (PBN), and they are quite similar to N-acetyl-L-cysteine (NAC), which is a well-known antioxidant agent. Among the nitrones studied, homo-bis-nitrone BPHBN5, bearing two N-tert-Bu radicals at the nitrone motif, has the best neuroprotective capacity (EC50 = 13.16 ± 1.65 and 25.5 ± 3.93 μM, against the reduction in metabolic activity induced by respiratory chain blockers and oxygen–glucose deprivation in an in vitro ischemia model, respectively) as well as anti-necrotic, anti-apoptotic, and antioxidant activities (EC50 = 11.2 ± 3.94 μM), which were measured by its capacity to reduce superoxide production in human neuroblastoma SH-SY5Y cell cultures, followed by mononitrone BPMN3, with one N-Bn radical, and BPMN2, with only one N-tert-Bu substituent. The antioxidant activity of BPNs1-5 has also been analyzed for their capacity to scavenge hydroxyl free radicals (82% at 100 μM), lipoxygenase inhibition, and the inhibition of lipid peroxidation (68% at 100 μM). Results showed that although the number of nitrone groups improves the neuroprotection profile of these BPNs, the final effect is also dependent on the substitutent that is being incorporated. Thus, BPNs bearing N-tert-Bu and N-Bn groups show better neuroprotective and antioxidant properties than those substituted with Me. All these results led us to propose homo-bis-nitrone BPHBN5 as the most balanced and interesting nitrone based on its neuroprotective capacity in different neuronal models of oxidative stress and in vitro ischemia as well as its antioxidant activity.

scholarly journals ANTIMICROBIAL AND ANTIOXIDANT ACTIVITIES OF SELECTED PLANTS USED BY POPULATIONS FROM JURUENA VALLEY, LEGAL AMAZON, BRAZIL

2017 ◽  
Vol 9 (5) ◽  
pp. 179
Author(s):  
Larissa Irene Da Silva ◽  
Arunachalam Karuppusamy ◽  
Fabio Miyajima ◽  
Ivana Maria Povoa Violante ◽  
Isanete Geraldini Costa Bieski ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Shigella Flexneri ◽  
Antibacterial Activities ◽  
Total Phenolic ◽  
Moderate Activity ◽  
Cedrela Odorata ◽  
Frap Assay ◽  
Antioxidant Power ◽  
Mato Grosso

Objective: The purpose of this study was to evaluate selected Brazilian plants from Juruena valley region of Mato Grosso, for their in vitro antimicrobial and antioxidant activities.Methods: The powder obtained from different parts of the twenty-six (26) plants were macerated in hydroethanolic solution to obtain the extracts. The hydroethanolic extracts were tested for their in vitro antimicrobial activity by determining the MIC using broth microdilution. The 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical, ferric reducing antioxidant power (FRAP) and nitric oxide (NO) methods were used for the determination of antioxidant activities. Correlation between classes of secondary metabolites and antioxidant activity was assessed.Results: Phanera glabra extract (HEPg) showed broad antibacterial spectrum, presenting the best activity against Klebsiella pneumoniae. Hevea microphylla extract (HEHm) presented a narrow spectrum of antibacterial activity with strong effect against Shigella flexneri. The only plant with broad spectrum antifungal activity was Bertholletia excelsa (HEBe), with moderate activity against strains of Aspergillus and Candida. The following extracts were prominent regarding their activities in the DPPH and FRAP assays-HEBe, Cariniana rubra (HECr) and in the FRAP assay alone, Cedrela odorata (HECo) and HEPg. None of the extracts was active in the NO assay. A significant association was observed between DPPH activity and the total phenolic contents.Conclusion: Our results justified the use of some of the investigated plants in the Brazilian ethnomedicine. The antibacterial activities of these plants are bacteriostatic in nature. These findings support that a number of investigated plants could be a valuable source of new antioxidant and antimicrobial compounds that can potentially deliver novel mechanisms of actions.However, further studies are required.

scholarly journals Antimicrobial, antioxidant activities and toxicity on Cavia porcellus of Dialium angolense Welw. Ex Oliv, a traditional medicinal plant from Bagira in Eastern of DR Congo

2020 ◽  
Vol 13 (2) ◽  
pp. 166-180
Author(s):  
Bashige Chiribagula V ◽  
Bakari Amuri S ◽  
Okusa Ndjolo Philippe ◽  
Kahumba Byanga J ◽  
Duez P ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Acute Toxicity ◽  
Antioxidant Activities ◽  
Antimicrobial Properties ◽  
Salmonella Typhi ◽  
Antimicrobial Activities ◽  
Cavia Porcellus ◽  
E Coli

Dialium angolense is used in Bagira for its various medicinal properties particularly in the management of infectious diseases. In this study, the methanol and aqueous extracts of leaves and fruits were evaluated for their in vitro antioxidant and antimicrobial properties and their in vivo toxicity on Cavia porcellus. The major phytochemical classes of extracts were screened using standard in-tube reactions. The antimicrobial study was tested on Candida albicans, Escherichia coli, Salmonella typhi, Staphylococcus aureus and Streptococcus pneumoniae using agar well diffusion and dilution methods, while the antioxidant activity was evaluated by a DPPH assay. For the acute toxicity study, animals (6/group) were orally given in a single dose 5000, 1000 or 15000 mg of extract/kg body weight (BW) then observed for 14 days. In sub-acute toxicity assays, 150 or 300 mg/kg BW/day were orally given, and animals observed for 28 days. Total phenolics and total flavonoids contents ranged 1.19 to 1.61 mg GAE.g-1 and 0.45 to 1.01 mg QEg-1, respectively. The extracts presented antioxidant activity with IC50 ranging 4.9 to 6.9 µg/mL. The minimal inhibitory concentration (MIC) on tested strains ranged from 1.9 to 500 µg/mL with the aqueous extract of fruits as a most active extract: MIC=1.9 µg/mL on E. coli and C. albicans. No signs of toxicity were noted during the acute and sub-acute toxicity assessments, suggesting a maximal tolerate doses (MDT) and LD50 > 15000 mg/kg BW. This study highlights the antioxidant and antimicrobial activities of Dialium angolense and suggests that further studies be directed towards the isolation of active compounds.

In Vitro α-glucosidase Inhibition and Computational Studies of Kaempferol Derivatives from Dryopteris cycanida

2020 ◽  
Vol 20 (9) ◽  
pp. 731-737 ◽  
Author(s):  
Surriya Amin ◽  
Barkat Ullah ◽  
Mumtaz Ali ◽  
Haroon Khan ◽  
Abdur Rauf ◽  
...  
Keyword(s):  
Computational Studies ◽  
Vitro Assay ◽  
Pharmacological Studies ◽  
Standard Compound ◽  
Dependent Inhibition ◽  
Human Disorders ◽  
Ic50 Values ◽  
Phytochemical Studies ◽  
Better Than

Background: Dryopteris cycadina has diverse traditional uses in the treatment of various human disorders which are supported by pharmacological studies. Similarly, the phytochemical studies of this plant led to the isolation of numerous compounds. Methodology: The present study deals with α-glucosidase inhibition of various kaempferol derivates including kaempferol-3, 4/-di-O-α- L-rhamnopyranoside 1, kaempferol-3, 5-di-O-α-L-rhamnoside 2 and kaempferol-3,7-di-O-α- L-rhamnopyranoside 3. Results: The results showed marked concentration-dependent inhibition of the enzyme when assayed at different concentrations and the IC50 values of compounds 1-3 were 137±9.01, 110±7.33, and 136±1.10 mM, respectively far better than standard compound, acarbose 290±0.54 mM. The computational studies revealed strong docking scores of these compounds and augmented the in vitro assay. Conclusion: In conclusion, the isolated kaempferol derivatives 1-3 from D. cycadina exhibited potent α- glucosidase inhibition.

scholarly journals Phenolic compounds and antioxidant, antimicrobial and antimycobacterial activities of Serjania erecta Radlk. (Sapindaceae)

2013 ◽  
Vol 49 (4) ◽  
pp. 775-782 ◽  
Author(s):  
Claudia Andréa Lima Cardoso ◽  
Roberta Gomes Coelho ◽  
Neli Kika Honda ◽  
Arnildo Pott ◽  
Fernando Rogério Pavan ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Ethanolic Extract ◽  
Chemical Study ◽  
The Other ◽  
Moderate Activity ◽  
E Coli ◽  
Ethanolic Extracts ◽  
Leaves And Roots ◽  
Microtiter Assay

Serjania erecta Radlk.(Sapindaceae) is a medicinal plant traditionally used in Brazil. We assayed the ethanolic extract of leaves and roots against seven microorganisms. The REMA (Resazurin Microtiter Assay) assay was used to measure the biological activity in vitro against Mycobacterium tuberculosis and our results showed moderate activity of the ethanolic extract. On the other hand S. aureus, P. aeruginosa, S. setubal, C. albicans, S. cerevisiae and E. coli revealed that the leaves and roots of S. erecta inhibited the growth of all microorganisms. The ethanolic extracts of leaves and roots showed low values of antioxidant activities. The ethanolic extracts of leaves and roots were analyzed by chromatographic and spectrometric methods. (-)-Epicatechin, kaempferol aglycone and five glycoside derivates were isolated: kaempferol-3-O-α-L-rhamnopyranoside, kaempferol-3-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside from the roots and kaempferol, kaempferol 3,7-di-O-α-L-rhamnopyranoside, vitexin, isovitexin and (-)-epicatechin in the leaves. This is the first chemical study reported in the literature about this specie.

scholarly journals Potential In Vitro and In Vivo Antioxidant Activities from Piper Crocatum and Persea Americana Leaf Extracts

2019 ◽  
Vol 12 (2) ◽  
pp. 661-667
Author(s):  
Fatmawaty Fatmawaty ◽  
Ni G. M. Anggreni ◽  
Naufal Fadhil ◽  
Vivitri D. Prasasty
Keyword(s):  
Antioxidant Activities ◽  
Antioxidant Properties ◽  
Persea Americana ◽  
Health Claims ◽  
In Vitro Assays ◽  
Moderate Activity ◽  
Leaf Extracts ◽  
Water Fraction

Piper crocatum and Persea americana Mill leaves are commonly used in traditional medicinal remedies, such as antidiabetes, antitumors and Alzheimer treatment. However, the extensive use of plant extracts over worldwide becomes significant concerns including its safety, efficacy, and quality. Therefore, the accurate scientific evaluation has become a precondition for acceptance of herbal health claims. The aim of this study was to determine the antioxidant activities of Piper crocatum Ruiz & Pav and Persea americana Mill leaf extracts. Isolation of antioxidant fractions were conducted using organic solvent extraction techniques. Antioxidant assays were conducted by using in vitro and in vivo methods involving DPPH and MDA methods. In this study, in vitro assays of Persea americana Mill and Piper crocatum Ruiz & Pav leaf extracts showed the best activity in water fraction. Moreover, in vivo assays of both plant leaf extracts showed the best dose at 8 mg. Persea americana Mill and Piper crocatum Ruiz & Pav leaf extracts have been successfully determined in antioxidant actions in vitro and in vivo. Persea americana Mill in water and ethanol solvents exhibit strong antioxidant properties. Meanwile, Piper crocatum Ruiz & Pav exhibit moderate activity in water and weak antioxidant activity in ethanol. Both plant leaves showed that 8 mg dose was better than the dose of 4 mg and 16 mg in vivo.

scholarly journals Dihydrochalcone Derivatives from Populus balsamifera L. Buds for the Treatment of Psoriasis

2019 ◽  
Vol 21 (1) ◽  
pp. 256 ◽  
Author(s):  
Audrey Bélanger ◽  
Alexe Grenier ◽  
François Simard ◽  
Isabelle Gendreau ◽  
André Pichette ◽  
...  
Keyword(s):  
Native Americans ◽  
Antioxidant Activities ◽  
Skin Substitute ◽  
Psoriatic Skin ◽  
Populus Balsamifera ◽  
Slowing Down ◽  
Anti Inflammatory ◽  
Better Than

Psoriasis is a skin disorder characterized by epidermal hyperplasia, hyperkeratosis, and inflammation. The treatments currently available on the market only improve patients’ quality of life and are associated with undesirable side effects. Thus, research leading to the development of new, effective, and safer therapeutic agents is still relevant. Populus balsamifera L. buds were used traditionally by Native Americans to treat various skin pathologies such as eczema and psoriasis. In this study, the antipsoriatic activities of dihydrochalcone derivatives from Populus balsamifera L. buds, known as balsacones, were investigated. The experiments were performed in vitro using a psoriatic skin substitute model. Also, anti-inflammatory and antioxidant activities were investigated. The tested balsacones showed promising antipsoriatic properties by slowing down cell growth and by regulating the expression of involucrin, loricrin, and Ki67 better than methotrexate in psoriatic substitutes. All five tested compounds could be an effective topical treatment for psoriasis, with promising anti-inflammatory and antioxidant actions that may contribute to clinical improvement in patients with psoriasis.

scholarly journals IN VITRO ANTIBACTERIAL ACTIVITY OF CHALCONE DERIVATIVES FROM Kaempferia pandurata RHIZOMES AGAINST CLINICAL ISOLATE BACTERIA

2017 ◽  
Vol 13 (1) ◽  
pp. 41 ◽  
Author(s):  
Soerya Dewi Marliyana ◽  
Yana Maolana Syah ◽  
Didin - Mujahidin
Keyword(s):  
Antibacterial Activity ◽  
Clinical Isolate ◽  
Enterobacter Aerogenes ◽  
Salmonella Typhi ◽  
Chemical Components ◽  
Chalcone Derivatives ◽  
Microdilution Method ◽  
In Vitro Antibacterial Activity ◽  
Vacuum Liquid Chromatography

<p>In vitro antibacterial activity of chalcone derivatives from “temu kunci” (<em>K. pandurta</em>) rhizomes against clinical isolate bacteria has been done. Two chalcone derivatives, panduratin A (<strong>1</strong>) and 4-hydroxypanduratin A (<strong>2</strong>) were isolated from <em>Kaempferia pandurata</em> rhizomes. Isolation of the chemical components were done with extraction (maceration), vacuum liquid chromatography and radial chromatography methods. The structures were determined by NMR spectroscopy (<sup>1</sup>H-NMR, <sup>13</sup>C-NMR, 1D and 2D), then compare with data from literatures. Antibacterial activity was carried out with reference to the CLSI microdilution method, against eight clinical isolate bacteria such as <em>Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Enterobacter aerogenes, Pseudomonas aeruginosa, Salmonella typhi, Shigella dysentriae </em>and<em> Vibrio cholerae.</em> Compounds <strong>1</strong> and <strong>2</strong> showed significant antibacterial activity with highest activity against <em>S. aureus</em> and <em>B. subtilis</em> with MIC values of 2.4 to 18.8 µg/mL and MBC values of 4.8 to 37.5 µg/mL. These results showed these compounds as potential antibacterial agent for clinical isolate bacteria.</p>

scholarly journals Antibacterial activity of endosymbiotic bacterial compound from Pheretima sp. earthworms inhibit the growth of Salmonella Typhi and Staphylococcus aureus: in vitro and in silico approach

2021 ◽  
Author(s):  
Dirayah Rauf Husain ◽  
Riuh Wardhani
Keyword(s):  
Antibacterial Activity ◽  
Binding Affinity ◽  
In Silico ◽  
Pathogenic Bacteria ◽  
Salmonella Typhi ◽  
Inhibition Test ◽  
Diffusion Method ◽  
Agar Diffusion ◽  
Potent Inhibition

Background and Objectives: Earthworms coexist with various pathogenic microorganisms; thus, their immunity mecha- nisms have developed through a long process of adaptation, including through endogenous bacterial symbionts. This study aims to identify earthworm endosymbiont bacteria compounds and their antibacterial activity through an in vitro approach supported by an in silico approach. Materials and Methods: This research was conducted using the in vitro inhibition test through agar diffusion and the in silico test using molecular docking applications, namely, PyRx and Way2Drugs Prediction of Activity Spectra for Substances (PASS). Results: The in vitro results showed a potent inhibition activity with a clear zone diameter of 21.75 and 15.5 mm for Staph- ylococcus aureus and Salmonella Typhi, respectively. These results are supported by chromatography and in silico tests, which showed that several compounds in endosymbiotic bacteria, cyclo (phenylalanyl-prolyl) and sedanolide, have high binding affinity values with several antibiotic-related target proteins in both pathogenic bacteria. Cyclo (phenylalanyl-prolyl) has the highest binding affinity of -6.0 to dihydropteroate synthase, -8.2 to topoisomerase, and -8.2 to the outer membrane, whereas sedanolide has the highest binding affinity to DNA gyrase with approximately -7.3. This antibiotic activity was also clarified through the Way2Drugs PASS application. Conclusion: Ten active compounds of endosymbiont bacteria, Cyclo (phenylalanyl-prolyl) and sedanolide were potential candidates for antibacterial compounds based on the inhibition test of the agar diffusion method and the results of reverse docking and Way2Drugs PASS.

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