Synthesis and Biological Activities of Chalcones Derived from Nitroacetophenone

2012 ◽  
Vol 518-523 ◽  
pp. 255-260 ◽  
Author(s):  
Xiao Yang Qiu ◽  
Su Zhi Li ◽  
An Ran Shi

A series of nitrochalcones (compounds 1-10) were synthesized by reacting appropriate nitroacetophenones and suitable benzaldehydes. The synthesized products were evaluated for their cytotoxic, antibacterial (Bacillus subtilis, Escherichia coli, Pseudomonas fluorescence and Staphylococcus aureus) and antifungal (Aspergillus niger, Candida albicans and Trichophyton rubrum) activities in vitro. Among the compounds tested, (E)-3-(4-fluorophenyl)-1-(3-nitrophenyl)- prop-2-en-1-one (10) showed the favorable in vitro cytotoxic activity against human nasopharyngeal epidermoid tumor cell line KB, and (E)-3-(2-methoxyphenyl)-1-(3-nitrophenyl)prop-2-en-1-one (8) showed the strongest antimicrobial activity with MIC of 20 μg/mL against P. fluorescence.

2011 ◽  
Vol 396-398 ◽  
pp. 1875-1878 ◽  
Author(s):  
Yu Ting Liu ◽  
Hai Long Guo ◽  
Da Wei Yin

Three bis-acetylferrocene schiff bases have been synthesized and characterized by IR, 1H NMR, and elemental analysis, the results conformed well with expected structures. The synthesized compounds were screened in vitro for their antimicrobial activity against three Gram-negative (Escherichia coli, Pseudomonas aeruginosa, and Salmonella typhi) and two Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacterial strains. The results showed that these compounds are show excellent antimicrobia activities against Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi ,Bacillus subtilis,Staphylococcus aureus.


2018 ◽  
Vol 42 (6) ◽  
pp. 332-336 ◽  
Author(s):  
Sayed K. Ramadan ◽  
Eman A. E. El-Helw

6-Chloro-3-((2-oxo-5-phenylfuran-3(2 H)-ylidene)methyl)-4 H-chromen-4-one was utilised for the construction of N-heterocycles. The proclivity of this furanone towards some nitrogen nucleophiles, i.e. glycine, thiosemicarbazide, thiocarbohydrazide, phenylhydrazine and o-phenylenediamine, was studied. The structures of all products obtained were established on the basis of their analytical and spectral data. All synthesised compounds were screened for their in vitro antibacterial (two strains of bacteria; Escherichia coli and Staphylococcus aureus) and antifungal (two fungus strains; Aspergillus flavus and Candida albicans) activities. Some products exhibited promising antimicrobial activities.


2020 ◽  
Vol 151 ◽  
pp. 15550-15558
Author(s):  
Amégninou Agban ◽  
Yao Hoekou ◽  
Passimna Pissang ◽  
Tchadjobo Tchacondo ◽  
Komlan Batawila

Objectif : L’objectif de ce travail était d’évaluer in vitro l’activité antimicrobienne des extraits de feuilles et tige de Jatropha multifida sur la croissance de Candida albicans, Escherichia coli et Staphylococcus aureus, puis d’évaluer in vivo la toxicité de cette plante. Méthodologie et résultats : Les méthodes de diffusion en milieu gélosé et de microdilution en milieu liquide ont été utilisées pour évaluer l’effet antimicrobien. Une étude en subaigüe était réalisée afin d’explorer les effets toxiques de l’extrait aqueux des feuilles. Les résultats des tests antimicrobiens montrent une activité des extraits de feuilles et tige de J. multifida sur la croissance des souches utilisées avec des diamètres de zones d’inhibition allant de 8 à 25 mm et des concentrations minimales inhibitrices (CMI) variant de 0,039 mg/mL à 1,25 mg/mL à l’exception des souches de E. coli qui sont résistantes aux extraits de la tige. L’administration en subaigüe de l’extrait aqueux des feuilles de J. multifida à la dose de 600 mg/kg entraîne une perte significative de poids chez les souris. Conclusion et applications des résultats : Les extraits aqueux, éthanolique et hydroéthanolique des feuilles et tige de J. multifida possèdent d’activité antimicrobienne et pourraient être utilisés dans le traitement des Candidoses à C. albicans et des infections à S. aureus. Mais l’essai de toxicité subaigüe montre que l’extrait aqueux de la plante serait toxique. Des études toxicologiques approfondies restent donc nécessaires sur ces extraits afin de mieux élucider leur inocuité. Mots-clés : Jatropha multifida, extraits de feuilles et de tige, activités antifongique et antibactérienne, toxicité. Agban et al., J. Appl. Biosci. 2020 Evaluation du potentiel antimicrobien et de la toxicité des extraits de Jatropha multifida Linn, (Euphorbiaceae) 15551 Evaluation of antimicrobial potential and toxicity of Jatropha multifida Linn, (Euphorbiaceae) extracts ABSTRACT Objective: The objective of this study was to evaluate in vitro the antimicrobial activity of leaves and stem of Jatropha multifida extracts against Candida albicans, Escherichia coli and Staphylococcus aureus, and then to evaluate in vivo the toxicity of this plant. Methodology and Results: The agar well-diffusion and the NCCLS broth microdilution methods were used to assess the antimicrobial effect. A subacute study was carried out to explore the toxic effects of the aqueous extract of the leaves. The results of the antimicrobial tests show an activity of the extracts of leaves and stems of J. multifida on the growth of the strains used with diameters of inhibitory zones ranging from 8 to 25 mm and minimum inhibitory concentrations (MIC) varying from 0.039 mg/mL to 1.25 mg/mL exception E. coli strains which are resistant to extracts from the stem. Subacute administration of the aqueous extract of the leaves of J. multifida at a dose of 600 mg/kg leads to a significant loss of weight in the mice. Conclusion and application of findings : The aqueous, ethanolic and hydroethanolic extracts of the leaves and stem of J. multifida have antimicrobial activity and could be used in the treatment of Candidiasis and bacterial infections due respectively to C. albicans and S. aureus. But the subacute toxicity test shows that the aqueous extract of the plant would be toxic. Extensive toxicological studies therefore remain necessary on these extracts in order to better elucidate their safety. Keywords: Jatropha multifida extracts of leaves and stem, antifungal and antibacterial activities, toxicity


2015 ◽  
Vol 10 (6) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Corina Danciu ◽  
Florin Borcan ◽  
Codruta Soica ◽  
Istvan Zupko ◽  
Erzsébet Csányi ◽  
...  

In recent years polyurethane microstructures (PM) have gained increasing attention in the pharmaceutical field due to the importance of their practical application. Since finding that such a formulation with genistein could improve its applications, we have conducted a preliminary study regarding the in vitro antiproliferative (MCF7, MDA-MB-231 and T47D) and antimicrobial ( Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis (D), Bacillus subtilis, B. cereus, and Candida albicans) activity in order to test whether polyurethane micro structuresre present a good option for further modulation of genistein's bioavailability. It was concluded that the polyurethane micro structures are a bad in vitro partner for the isoflavone genistein.


Medicina ◽  
2008 ◽  
Vol 44 (12) ◽  
pp. 977 ◽  
Author(s):  
Alvydas Pavilonis ◽  
Algirdas Baranauskas ◽  
Ligita Puidokaitė ◽  
Žaneta Maželienė ◽  
Arūnas Savickas ◽  
...  

Objective. To evaluate the antimicrobial activity of soft and purified propolis extracts. Study object and methods. Antimicrobial activity of soft and purified propolis extracts was determined with reference cultures of Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 33499, Pseudomonas aeruginosa ATCC 27853, Proteus mirabilis ATCC 12459, Bacillus subtilis ATCC 6633, Bacillus cereus ATCC 8035, and fungus Candida albicans ATCC 60193. Microbiological tests were performed under aseptic conditions. Minimum inhibitory concentration (MIC) – the highest dilution of preparation (the lowest concentration of preparation) that suppresses growth of reference microorganisms – was determined. Results. Concentration of phenolic compounds in soft propolis extract that possesses antimicrobial activity against gram-positive (Staphylococcus aureus, Enterococcus faecalis) and gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Proteus mirabilis) is 0.587±0.054 mg and 0.587±0.054–0.394±0.022 mg (P>0.05) and in purified propolis extract – 0.427±0.044 mg and 0.256±0.02 mg (P>0.05). Klebsiella pneumoniae is most resistant to soft propolis extract when the concentration of phenolic compounds is 1.119± 0.152 mg and to purified propolis extract when the concentration of phenolic compounds is 1.013±0.189 mg (P>0.05). Spore-forming Bacillus subtilis bacteria are more sensitive to soft and purified propolis extracts when the concentration of phenolic compounds is 0.134±0.002 mg and 0.075±0.025 mg, respectively, and Bacillus cereus – when the concentration is 0.394±0.022 mg and 0.256±0.02 mg (P>0.05). Sensitivity of fungus Candida albicans to soft and purified propolis extracts is the same as Bacillus subtilis. Encapsulated bacterium Klebsiella pneumoniae is most resistant to antimicrobial action of soft and purified propolis extracts as compared with gram-positive Staphylococcus aureus and Enterococcus faecalis bacteria (P<0.05), gram-negative Escherichia coli, Pseudomonas aeruginosa, and Proteus mirabilis (P<0.05), sporeforming Bacillus subtilis and Bacillus cereus bacteria (P<0.05), and fungus Candida albicans (P<0.05). There is no statistically significant difference between antimicrobial effect of soft propolis extract and purified propolis extract on gram-positive bacteria, gram-negative bacteria, spore-forming bacteria, encapsulated bacteria, and Candida fungus. Conclusions. Soft and purified propolis extracts possess antimicrobial activity. They could be recommended as natural preservatives in the manufacture of pharmaceutical products.


2000 ◽  
Vol 55 (9-10) ◽  
pp. 778-784 ◽  
Author(s):  
Josep Serra Bonvehí ◽  
Francesc Ventura Coll

Abstract The composition, bacteriostatic and ROO• -scavenging potential activities of fifteen propolis samples from various botanic and geographic origins were determined to obtain objective information related to propolis quality. Variance analysis showed significant differences (p ≤ 0.05) in the contents of polyphenols, flavonoids and active components between fresh and aged propolis. The state of the product (fresh or aged) could be differentiate by using flavonoid pattern and biological activities. A minimum propolis concentration of 80 μg/ml was required inhibit Bacillus subtilis and Staphylococcus aureus while 800 μg/ml was required to inhibit Escherichia coli using fresh propolis. Aged propolis inhibit B. subtilis and S. aureus at concentration of 100 μg/ml and E. coli at 1000 μg/ml. A minimum flavonoids percentage of 18 g/100 g and a maximum ROO• -scavenging potential activity of 4.3 μg/ml were determined in fresh propolis. Flavonoids levels in aged propolis were approximately 20% lower than in fresh propolis. A maximum flavonoids percentage of 19.8 g/100 g and a ROO•-scavenging potential activity between 5.7 to 6.4 μg/ml in aged propolis were quantified. Another objective was to assess the use of ROO•-scavenging potential activity in propolis quality.


Author(s):  
E. A. Parashchuk ◽  
N. I. Tkachuk ◽  
S. M. Marchyshyn ◽  
H. R. Kozyr

Мета роботи. Визначення антимікробної активності бедринцю ломикаменевого підземних органів екстракту густого. Матеріали і методи.  Oб’єктoм для дoслідження обрано бедринцю ломикаменевого підземних органів екстракт густий (БЕГ-1, одержаний екстрагуванням 75 % етанолом і БЕГ-2, екстрагент 85 % етанол). В якості тест-культур використовували 5 музейних штамів: грампозитивні мікроорганізми Staphylococcus aureus АТСС 6538, спорову культуру Bacillus subtilis АТСС 6633, грамнегативну культуру Escherichia coli АТСС 25922 та Pseudomonas aeruginosa АТСС 9027. Антифунгальну дію з’ясовували відносно Candida albicans АТСС 885-653. Бактеріостатичні властивoсті дoсліджуваних oб’єктів встанoвлювали за результатами росту еталонних штамів мікроорганізмів у нативному водному розчині бедринцю та в розведені 1:2 та 1:4 в м'ясо-пептонному бульйоні; бактерицидні – за відсутністю росту вмісту пробірок із розведенням екстракту на щільних пoживних середoвищах (м’ясо-пептонний агар – МПА) для грампозитивних мікроорганізмів S. aureus, B. subtilis, для грамнегативної культури E. coli, P. аeruginosa. Агар Сабуро використовували для дріжджеподібних грибів роду Candida (C. аlbicans). Результати й обговорення. Бедринцю ломикаменевого підземних органів екстракт густий має широкий спектр антибактеріальної активності. Нативний екстракт БЕГ-1 по відношенню до тест-штамів S. aureus, B. subtilis, C. аlbicans проявляв бактерицидну дію. Бактеріостатичну дію він проявляв до P. aeruginosa, а по відношенню до E. coli антимікробного ефекту не виявлено. Екстракти в розведені 1:2 та 1:4 проявили бактерицидну дію відносно B. subtilis, бактеріостатичну – до S. aureus, C. albicans і не виявлено протимікробної дії до E. coli та P. aeruginosa. Нативний зразок БЕГ-2 по відношенню до усіх досліджуваних 5 тест–штамів проявив бактерицидну активність; у розведені 1:2 та 1:4 проявляв бактерицидну та бактеріостатичну дію відносно S. aureus, B. subtilis, C. albicans. Антимікробна дія по відношенню до E. coli та P. aeruginosa не виявлена. Антимікрoбну активність нативного бедринцю ломикаменевого екстракту густого також вивчали у дoслідах in vitro методом дифузії в агар –  метод “колодязів”. Штами S. aureus, C. albicans, B. subtilis, P. aeruginosa, E. coli проявили чутливість до нативного бедринцю ломикаменевого підземних органів екстракту густого. Грампозитивні бактеріальні штами S. aureus,а також гриби C. albicans, B. subtilis є найбільш чутливими до  БЕГ-2, а БЕГ-1 проявляв порівняно меншу чутливість. Грамнегативні культури P. aeruginosa та E. coli також проявили помірну чутливість до  БЕГ-1, але значно більшу чутливість до БЕГ-2. Висновки. 1. Експериментально встановлено, що обидва досліджувані зразки бедринцю ломикаменевого підземних органів екстракту густого проявляють антибактеріальну активність. 2. Бедринцю ломикаменевого підземних органів екстракт густий проявляв більш виражену антимікробну активність по відношенню до грампозитивної мікрофлори, тому є перспективним для створення лікарського засобу з антимікробними властивостями.


2020 ◽  
Vol 1 (2) ◽  
pp. 41-45
Author(s):  
A.Suparlan Isya Syamsu

Preliminary research has been conducted on the antimicrobial activity of n-Butanol extract of forest honey (Apis nigrocincta). This study aims to determine the antimicrobial activity of forest honey from Selayar Regency on the growth of test microbes, using the method of solid dilution with the test microbial Bacillus subtilis, Staphylococcus aureus, Streptococcus mutans, Pseudomonas aeruginosa, Salmonella typhi, Escherichia coli, Vibrio sp, Staphylococcus epidermidis, and Candida albicans against n-butanol extract from forest honey (Apis nigrocincta) at 1 mg/ml. The results obtained showed that n-butanol extract inhibited the growth of bacteria Bacillus subtilis, Escherichia coli, Staphylococcus aureus, Staphylococcus epidermidis, and Staphylococcus aureus. To estimate the compounds that provide antimicrobial activity, the TLC-Bioautography test is performed. Obtained the best results from the separation of compounds by TLC using Chlorophorom eluate: Acetone (3: 1). The TLC-Bioautographic test results showed that the spots with an Rf value of 0.29 gave activity to Bacillus subtilis, Escherichia coli, and Staphylococcus epidermidis, and gave positive results on the appearance of flavonoid compounds.


2021 ◽  
Vol 10 (9) ◽  
pp. e22610918051
Author(s):  
Soraya Castro Trindade ◽  
Jurandi Nery Pereira-Filho ◽  
Laerte Oliveira Barreto Neto ◽  
Thais Brito de Oliveira Moura ◽  
Antonio Pedro Fróes de Farias ◽  
...  

As espécies do gênero Lippia (Verbenaceae) possuem diversas moléculas bioativas, oriundas do seu metabolismo secundário, que apresentam atividade antimicrobiana, analgésica, antifúngica e imunomoduladora. Este estudo teve como objetivo avaliar a atividade antimicrobiana in vitro do extrato metanólico das folhas de L. alnifolia, L. origanoides, L. insignis e L. thymoides frente a microrganismos de importância clínica.  Foi realizada uma triagem fitoquímica dos extratos das plantas e a avaliação da atividade antimicrobiana pelo método de difusão em disco, além da determinação da concentração inibitória mínima (MIC) frente às bactérias Bacillus subtilis, Escherichia coli, Micrococcus luteus, Pseudomonas aeruginosa, Staphylococcus aureus e Salmonella choleraesuis, e os fungos Candida albicans e Candida glabrata. A presença de saponinas, terpenos, esteroides, cumarinas, ácidos fenólicos e flavonoides foi observada na análise fitoquímica. Os extratos metanólicos das folhas de L. alnifolia, L. origanoides e L. insignis apresentaram atividade antimicrobiana contra todas os microrganismos testados. O extrato metanólico da L. thymoides apresentou atividade antimicrobiana frente aos microrganismos M. luteus, P. aeruginosa, S. aureus, C. albicans e C. glabrata. A maioria dos extratos apresentou atividade bacteriostática e todos os extratos apresentaram atividade fungistática para C. albicans e fungicida para C. glabrata. A utilização dos extratos de Lippia pode ser uma alternativa viável no tratamento de doenças infecciosas de origem bacteriana e fúngica.


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