scholarly journals Synthesis and characterization of some new Schiff base derivatives of gabapentin, and assessment of their antibacterial, antioxidant and anticonvulsant activities

2021 ◽  
Vol 20 (1) ◽  
pp. 145-153
Author(s):  
Muhammad Farrukh Saleem ◽  
Mohsin Abbas Khan ◽  
Irshad Ahmad ◽  
Naveed Aslam ◽  
Umair Khurshid

Purpose: To synthesize and characterize some new gabapentin Schiff base derivatives, and to assess their antibacterial, antioxidant and antiepileptic activities.Methods: Four Schiff base derivatives of gabapentin, termed G1, G2, G3 and G4, were synthesized by condensation with benzoin, vanillin, acetophenone, and benzophenone, respectively. Their chemical identities were established by FTIR, 1 H NMR and 13C NMR techniques. The new compounds were screened for antibacterial activity using agar well method, antioxidant activity by DPPH assay, and anticonvulsant activity against pentylenetetrazole (PTZ) induced seizures in mice.Results: All the compounds showed antibacterial activity against the test strains to variable degrees, while the parent drug did not exhibit antibacterial activity. The zones of inhibition of compound G2 against Micrococcus luteus (36.2 ± 1.0 mm) and Serratia marcescens (28.2 ± 1.0 mm), and of compound G4 against Stenotrophomonas maltophilia (36.8 ± 1.0 mm) were larger compared to thestandard drug, doxycycline, exhibiting zones of inhibition 28.2 ± 1.3, 28.2 ± 0.9 and 20.0 ± 0.9 mm, respectively. In addition, compounds G1 and G2 possessed significantly greater (p < 0.05) radical scavenging activity (82.3 ± 1.8 and 92.3 ± 2.2 %, respectively) than the precursor drug, gabapentin (63.2± 2.6 %). The seizure scores for compounds G1 (0.7 ± 0.06) and G2 (0.9 ± 0.07) were comparable(p ˃ 0.05) with gabapentin (0.8 ± 0.06), while compounds G3 and G4 were less active (p < 0.05) than gabapentin.Conclusion: Compounds G1 and G2 exhibit good antibacterial and antioxidant activities while retaining the anticonvulsant activity of the parent drug, gabapentin, thus making them suitable candidates for further development for the treatment of neurodegenerative pathologies associated with bacterial infections. Keywords: Gabapentin, Antibacterial, Seizures, Antioxidant, Anticonvulsant

2018 ◽  
Vol 23 ◽  
pp. 2515690X1876273 ◽  
Author(s):  
Refilwe Given Kudumela ◽  
Peter Masoko

There is very little scientific information on indigenous plants used for medicinal purposes. Therefore, the aim of the study was to evaluate the antibacterial and antioxidant activities of the leaves of Commelina africana, Elephantorrhiza elephantina, Dombeya rotundifolia, and the whole plant excluding the roots of Schkuhria pinnata indigenous medicinal plants from the Limpopo Province, which may be used for the treatment in humans infected with bacterial pathogens. The screening of different phytoconstituents using standard methods revealed the presence of terpenoids, flavonoids, tannins, and saponins. The total phenolic, tannin, and flavonoid content were estimated using spectrophotometric methods. D rotundifolia had the highest amounts of phenol (259.00 ± 2.65 mg of gallic acid equivalent [GAE]/g), tannin (330.33 ± 15.63 mg of GAE/g), and flavonoid (19.90 ± 0.75 mg of quercetin equivalent [QE]/g) content, while S pinnata had the least. All the plants had antibacterial activity against Escherichia coli and Pseudomonas aeruginosa with the bioautography method. The microbroth dilution assay revealed antibacterial activity with minimum inhibitory concentration values raining from 0.02 to 2.50 mg/mL. D rotundifolia had the highest antioxidant activity in both the free radical scavenging and ferric reducing power methods. S pinnata and C africana extracts had high antibacterial activity, while D rotundifolia had high antioxidant activity, which made them potential plants for isolation of bioactive compounds and possible application in the pharmaceutical industry.


Molecules ◽  
2021 ◽  
Vol 26 (24) ◽  
pp. 7665
Author(s):  
Fabíola F. G. Rodrigues ◽  
Aline A. Boligon ◽  
Irwin R. A. Menezes ◽  
Fábio F. Galvão-Rodrigues ◽  
Gerson J. T. Salazas ◽  
...  

The increase in antibiotic resistance and the emergence of new bacterial infections have intensified the research for natural products from plants with associated therapy. This study aimed to verify the antibacterial and antioxidant activity of crude extracts of the genus Plectranthus species, being the first report on the modulation of aminoglycosides antibiotic activity by Plectranthus amboinicus extracts. The chemical composition was obtained by chemical prospecting and High-Performance Liquid Chromatography with diode arrangement detector (HPLC/DAD). The antibacterial activities of the extracts alone or in association with aminoglycosides were analyzed using the microdilution test. The antioxidant activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging. The phytochemical prospection allowed the flavonoids, saponins, tannins and triterpenoids to be identified. Quercetin, rutin, gallic acid, chlorogenic acid, caffeic acid, catechin, kaempferol, glycosylated kaempferol, quercitrin, and isoquercitrin were identified and quantified. The principal component analysis (PCA) observed the influence of flavonoids and phenolic acids from Plectranthus species on studied activities. Phytochemical tests with the extracts indicated, especially, the presence of flavonoids, confirmed by quantitative analysis by HPLC. The results revealed antibacterial activities, and synergistic effects combined with aminoglycosides, as well as antioxidant potential, especially for P. ornatus species, with IC50 of 32.21 µg/mL. Multivariate analyzes show that the inclusion of data from the antioxidant and antibacterial activity suggests that the antioxidant effect of these species presents a significant contribution to the synergistic effect of phytoconstituents, especially based on the flavonoid contents. The results of this study suggest the antibacterial activity of Plectranthus extracts, as well as their potential in modifying the resistance of the analyzed aminoglycosides.


2014 ◽  
Vol 74 ◽  
pp. 742-750 ◽  
Author(s):  
Chengyuan Liang ◽  
Juan Xia ◽  
Dong Lei ◽  
Xiang Li ◽  
Qizheng Yao ◽  
...  

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Kenza Ammor ◽  
Dalila Bousta ◽  
Sanae Jennan ◽  
Bahia Bennani ◽  
Abdellah Chaqroune ◽  
...  

The aim of this study is to investigate in vitro antioxidant and antibacterial activities of the aqueous and hydroethanolic extracts for aerial parts of Herniaria hirsuta. Extracts were screened for their possible antioxidant activities by three tests: DPPH free radical-scavenging, reducing power, and molybdenum systems. The screening of antibacterial activity of extracts was individually evaluated against sixteen bacteria species using a disc diffusion method. Flavonoids, total phenols, and tannins content were performed for both extracts. It shows higher content in the hydroethanolic extract. The hydroethanolic extract showed a significant antioxidant activity for the three methods studies to the aqueous extract, but nonsignificant results compared to the reference (BHT). However, both extracts have negative effect on the strains studies for the antibacterial activity.


2009 ◽  
Vol 2009 (23) ◽  
pp. 3467-3474 ◽  
Author(s):  
Oxana Kotova ◽  
Sergey Semenov ◽  
Svetlana Eliseeva ◽  
Sergey Troyanov ◽  
Konstantin Lyssenko ◽  
...  

2019 ◽  
Vol 31 (11) ◽  
pp. 2512-2516 ◽  
Author(s):  
Md. Zahidul Islam ◽  
Jannat Al Foisal ◽  
Mahbubur Rahman ◽  
Mst. Afsana Mimi ◽  
Faridul Islam ◽  
...  

The aim of the study was to characterize the chemical constituents and determine antibacterial and antioxidant activities of essential oils and three different extracts of Dryopteris marginalis. The root had essential oil yield of 0.36 % (w/w) in which 12 organic compounds representing 97.22% of the root oils were identified. Tyranton was found as the most abundant component with 77.571 % of the total concentration in the essential oil. The zones of inhibition of different organic extracts against the tested bacteria were found in the range of 6.5-15 mm. Pseudomonas was the most vulnerable with MICs of 15.62 μg/mL by both ethyl acetate and petroleum ether extract producing 3.8 mm zone of inhibition. The essential oils extracted from roots of Dryopteris marginalis showed maximum 85.29 % inhibition of radical scavenging at 2 mg/mL concentration. Among all root extracts, methanol extract exhibited 41.11 % inhibition at 2 mg/mL concentration.


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