scholarly journals Novel Hybrid Chitosan Derivatives and Chalcones Moiety for Some Biological Applications: Synthesis, Characterization, Antimicrobial and Anti Cancer Activity

Author(s):  
E. Bagyaraj ◽  
E. Vakees ◽  
M. Aboobucker Sithique

Versatile hybrid organic polymers are prepared using two active intermediates such as cynuric chloride and chitosan derivatives. The prepared chalcones are characterized by using FT-IR, UV, and proton NMR, thermal analysis and Minimum inhibitory Concentration. Thermal stability of the synthesized hybrid polymer is found using TGA and the hybrid chitosan derivative chalcone is thermally stable up to 270 °C. The antimicrobial activity of the prepared chitosan containing chalcone moiety are find out using Minimum Inhibitory Concentration (MIC) method. The synthesized versatile chalcone shows excellent antimicrobial activity against gram-negative bacteria such as Pseudomonas aeruginosa; and Gram-positive bacteria Chalcone containing halogen moiety shows high activity (MIC 7.8 µg/mL) than the hydroxyl containing chalcone. Cytotoxicity activity of the synthesized composites shows high activity.

Author(s):  
Victor Hugo Alves do Nascimento ◽  
Alessandra Carla Guimarães Sobrinho ◽  
Cintya De Oliveira Souza ◽  
Jesus Nazareno Silva de Souza ◽  
Consuelo Lúcia Sousa

The aim of this work was to determine the compounds with antimicrobial capacity from crude extracts and leaf fractions of Byrsonima crassifolia and Inga edulis. A solid-liquid extraction was performed using three solvent systems (acetate, methanol and methanol: water). The extracts and fractions were submitted to antimicrobial susceptibility tests for Gram-negative and Gram-positive bacteria by disk diffusion and Minimum Inhibitory Concentration (MIC) methods. A solid phase extraction (SPE) was performed to identify phenolic compounds for pre-concentration and pre-purification of the extracts and fractions that presented antimicrobial potential. The methanolic fraction was able to extract the highest total phenolic content and also presented the largest halos in the disk diffusion test. The minimum inhibitory concentration ranged from 125 to 500 μg/ml mL-1 and from 12.5 to 200 μg/ml mL-1 for Gram-negative and Gram-positive bacteria, respectively. After SPE, the crude extracts and fractions showed inhibition halos against all themicroorganisms tested at a lower concentration when compared to the standardized antibiotics. Gallic acid, ferric acid, myricetin and quercetin showed antimicrobial activity when tested alone. Gallic acid, catechin, epicatechin, ferrulic acid, quercetin, and other 4 major compounds were identified and quantified for Byrsonima crassifolia and 3 compounds for Inga edulis.   Keywords: Vegetable Matrices. Antibiotics. Bioactive Compounds. Liquid Chromatography.   Resumo O objetivo do presente estudo foi determinar compostos com capacidade antimicrobiana de extratos brutos e frações de folhas de Byrsonima crassifolia e de Inga edulis. Foi realizado uma extração sólido-líquido utilizando três sistemas de solventes (acetato, metanol e metanol:água). Os extratos e frações foram submetidos aos testes de suscetibilidade antimicrobiana para bactérias Gram-negativas e Gram-positivas através dos métodos de disco-difusão e Concentração Inibitória Mínima-CIM. Para identificação dos compostos fenólicos foi realizada Extração em Fase Sólida (SPE), para pré- concentração e pré-purificação dos extratos e frações que apresentaram potencial antimicrobiano. A fração metanólica conseguiu extrair maior conteúdo de fenólicos totais, e apresentou os maiores halos no teste de disco-difusão. A concentração inibitória mínima variou de 125 a 500 µgES mL-1   e de 12,5 a 200 µgES mL-1 para bactérias Gram-negativas e Gram-positivas, respectivamente. Após SPE, os extratos brutos e frações apresentaram halos de inibição frente a todos os micro-organismos testados em uma concentração menor que a dos antibióticos padronizados. O ácido gálico, ácido ferrúlico, miricetina e quercetina apresentaram atividade antimicrobiana quando testados isoladamente. Foram identificados e quantificados nos extratos brutos e frações ácido gálico, catequina, epicatequina, ácido ferrúlico, quercetina, além de outros 4 compostos majoritários para Byrsonima crassifolia e 3 compostos para Inga edulis.   Palavras-chave: Matrizes Vegetais. Antibióticos. Compostos Bioativos. Cromatografia Líquida.


Author(s):  
V. N. Zorina ◽  
O. N. Vorobeva ◽  
N. A. Zorin

Aim. A comparative study of the effect ofbovine and human lactoferrin (LF) on Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Candida albicans strains. Materials and methods. The daily agar cultures of museum and clinical strains of microorganisms were standardized, diluted with physiological solution up (from 5000 microbial cells/ ml to 0.1 ml) was added to the stepwise dilution of LF (from 1000 pg /ml) and incubated 18 - 24 hours at 37°C. The amount of LF in the sample with the total apparent growth retardation of the microbes was the minimum inhibitory concentration (MIC) for the strain. Results. The MIC of human LF was 4 - 8 times less than MIC of bovine LF. The smallest dose was required for the suppression of C. albicans (11.3±1.5 and 43.8±9.5 pg/ml respectively), the largest when using human LF was needed to suppress S. aureus (38,2±4,6), and in a case of bovine LF - E. faecalis (206,3±51,1). Conclusion. Human LF is much more effective in suppressing bacterial infection, but in the course of evolution, there is an increase in the resistance of S. aureus to LF. The higher availability of bovine LF and the lack of a tendency to increase resistance, it is advisable to use high-doses of bovine LF in the treatment of resistant forms of bacteria and C. albicans.


2020 ◽  
Vol 21 (11) ◽  
pp. 1129-1137 ◽  
Author(s):  
Somayeh Mirsadeghi ◽  
Masoumeh F. Koudehi ◽  
Hamid R. Rajabi ◽  
Seied M. Pourmortazavi

Background: Herein, we report the biosynthesis procedure to prepare silver nanoparticles as reduction and capping agents with the aqueous plant extract of Perovskia abrotanoides. Methods: The therapeutic application of silver nanoparticles entirely depends on the size and shape of the nanoparticles therefore, their control during the synthesis procedure is so important. The effects of synthesis factors, for example, silver ion concentration, the mass of plant extract, reaction time and extraction temperature, on the size of silver particles were considered and optimized. Several analytical methods were used for the characterization of silver NPs including FT-IR and UV–Vis spectrophotometer, XRD and SEM. Results: The results showed that the mean size of the silver particles was about 51 nm. Moreover, the antibacterial properties of biosynthesized silver NPs were investigated by the minimum inhibitory concentration, minimum bactericidal concentration, and Well-diffusion tests. The minimum inhibitory concentration/ minimum bactericidal concentration values of silver NPs and aqueous plant extract versus Gram-positive bacteria (Staphylococcus aureus and Bacillus cereus) and Gram-negative bacteria (E. coli) were 3.03/0.00, 1.20/0.01, 3.06/0.00, 0.98/1.04, 1.00/0.05 and 1.30/0.03 (mg/mL), respectively. Conclusion: The antimicrobial activity study displayed that the synthesized silver nanoparticles by plant extract have better antimicrobial properties compared to aqueous plant extract of Perovskia abrotanoides.


Author(s):  
Devidas G. Anuse ◽  
Suraj N. Mali ◽  
Bapu R. Thorat ◽  
Ramesh S. Yamgar ◽  
Hemchandra K. Chaudhari

Background: Antimicrobial resistance is major global health problem, which is being rapidly deteriorating the quality of human health. Series of substituted N-(benzo[d]thiazol-2-yl)-2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)acetamide (3a-j) were synthesized from substituted N-(benzo[d]thiazol-2-yl)-2-chloroacetamide/bromopropanamide (2a-j) and 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole (2) and further evaluated for their docking properties and antimicrobial activity. Methods: All synthesized compounds were characterized by FT-IR, NMR and Mass spectral analysis. All compounds were allowed to dock against different antimicrobial targets having PDB ID: 1D7U and against common antifungal target having PDB ID: 1EA1. Results: The compounds 3d and 3h were showed good activity against Methicillin-resistant Staphylococcus aureus (MRSA, resistance Gram-positive bacteria). All synthesized compounds showed good to moderate activity against selected bacterial and fungal microbial strains. If we compared the actual in-vitro antimicrobial activity and in-silico molecular docking study, we found that molecules 3i and 3h were more potent than the others. Conclusion: Our current study would definitely pave the new way towards designing and synthesis of more potent 2-aminobenzothiazoles derivatives.


2017 ◽  
Vol 12 (01) ◽  
pp. 69-71
Author(s):  
Shamala T ◽  
A.M. Krupanidhi ◽  
Shanmukhappa S ◽  
B.E. Basavarajappa ◽  
Jayamma kulkarni

2020 ◽  
Vol 36 (2) ◽  
Author(s):  
Ana Flávia da Silva ◽  
Marisa de Oliveira Lopes ◽  
Cláudio Daniel Cerdeira ◽  
Ingridy Simone Ribeiro ◽  
Isael Aparecido Rosa ◽  
...  

The radish (Raphanus sativus L.) is a vegetable of the Brassicaceae family cultivated worldwide and has several medicinal properties. Its biological activities are related to various secondary metabolites present in the species, especially phenolics. Thus, the objectives of this study were the chemical analysis and evaluation of the antioxidant and antimicrobial activities of the dry extract and fractions of the fodder turnip leaves (R. sativus var. oleiferus Metzg.). Samples were analyzed by mass spectrometry and the antioxidant activity was evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical method and the reducing power method. Antimicrobial activity was determined by the agar diffusion and microdilution methods. The total phenols were concentrated in the butanol fraction (121.27 mg GAE/g) and the flavonoids were concentrated in the ethyl acetate fraction (98.02 mg EQ/g). The ethyl acetate fraction showed the best antioxidants results, with 83.45% of free radical scavenging and 11.34% of ferric ions reduction. The analysis of antimicrobial activity showed that the dry extract had the highest average zone of inhibition against Bacillus subtilis (18.67 mm). Smaller values of the minimum inhibitory concentration for Micrococcus luteus were, and the ethyl acetate fraction showed a lower minimum inhibitory concentration (0.1 mg/ml) for that microorganism. There was a strong correlation between the antioxidant activity and the content of phenols and flavonoids. The results showed the potential antioxidant and antimicrobial activities of this extract with the ethyl acetate fraction being most promising for further studies.


2014 ◽  
Vol 9 (9) ◽  
pp. 1934578X1400900
Author(s):  
Camila Hernandes ◽  
Silvia H. Taleb-Contini ◽  
Ana Carolina D. Bartolomeu ◽  
Bianca W. Bertoni ◽  
Suzelei C. França ◽  
...  

Reports on the chemical and pharmacological profile of the essential oil of Schinus weinmannifolius do not exist, although other Schinus species have been widely investigated for their biological activities. This work aimed to evaluate the chemical composition and antimicrobial activity of the essential oil of S. weinmannifolius collected in the spring and winter. The essential oils were extracted by hydrodistillation, analyzed by GC/MS and submitted to microdilution tests, to determine the minimum inhibitory concentration. The oils displayed different chemical composition and antimicrobial action. Bicyclogermacrene and limonene predominated in the oils extracted in the winter and spring, respectively, whereas only the latter oil exhibited antifungal activity.


2020 ◽  
Vol 12 (1) ◽  
pp. 71-75
Author(s):  
A.M. Aliyu ◽  
S.J. Oluwafemi ◽  
S. Kasim

All over the world, hundreds of plants have been identified based on researchers and experimental evidence as good sources of medicinal agents. The bioactive components (phytochemicals) of both the seeds and pulp of Cola milleni were extracted using ethanol as solvent. The bioactive components detected were alkaloids, tanins, saponins, cardiac glycosides, carbohydrates, sterols, resins and terpenes while Flavonoids, anthraquinones, anthracyanides and phenol were not detected for both the seed and pulps. Antimicrobial activity of the ethanol extract (Seed and pulp) against Staphylococcus aureus, Escherichia coli and Penicillium notatum was carried out using standard techniques. Staphylococcus aureus had the highest zone of inhibition for pulp having a range of 9.7mm±0.58mm - 19.7mm±2.52mm while Penicllium notatum had the least with 0.00mm. S.aureus also had the highest zone of inhibition range of 14.3mm±2.08mm - 21.3mm±1.53mm for the seed extract while penicillium had the least inhibition range of 5.0mm±1.00mm - 5.7mm±0.58. E.coli showed the highest minimum inhibitory concentration with ethanol extract of the pulp (160mg/ml) while penicillium notatum was not reactive. The minimum inhibitory concentration of seed against penillium notatum was the highest (160mg/ml) while staphylococcus aureus showed the lowest of 40mg/ml. The antimicrobial activity is as a result of the presence of phytochemicals detected, which suggest the use of the plant for the treatment of diseases caused by these organisms. Key words: Cola millenii, Phytochemical, Antimicrobial activity, Bacteria, Fungi


2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Ana Carolina Oliveira Silva ◽  
Elidiane Fonseca Santana ◽  
Antonio Marcos Saraiva ◽  
Felipe Neves Coutinho ◽  
Ricardo Henrique Acre Castro ◽  
...  

The development of the present study was based on selections using random, direct ethnopharmacological, and indirect ethnopharmacological approaches, aiming to evaluate which method is the best for bioprospecting new antimicrobial plant drugs. A crude extract of 53 species of herbaceous plants collected in the semiarid region of Northeast Brazil was tested against 11 microorganisms. Well-agar diffusion and minimum inhibitory concentration (MIC) techniques were used. Ten extracts from direct, six from random, and three from indirect ethnopharmacological selections exhibited activities that ranged from weak to very active against the organisms tested. The strain most susceptible to the evaluated extracts wasStaphylococcus aureus. The MIC analysis revealed the best result for the direct ethnopharmacological approach, considering that some species yielded extracts classified as active or moderately active (MICs between 250 and 1000 µg/mL). Furthermore, one species from this approach inhibited the growth of the threeCandidastrains. Thus, it was concluded that the direct ethnopharmacological approach is the most effective when selecting species for bioprospecting new plant drugs with antimicrobial activities.


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