Antibacterial Effects of Derivatives of Porphyrin, Naphthalene diimide, Aminophenol and Benzodioxane on Methicillin Resistant Staphylococcus aureus and Neuropathogenic Escherichia coli K1

2020 ◽  
Vol 18 (3) ◽  
pp. 275-284
Author(s):  
Ruqaiyyah Siddiqui ◽  
Ayaz Anwar ◽  
Salwa Ali ◽  
Naveed Ahmed Khan

Background: Infectious diseases contribute to substantial mortality and morbidity worldwide despite advances in therapeutic intervention highlighting the need to identify drugs with antimicrobial properties. Methods: Here, we utilised several compounds from the following classes: porphyrin, naphthalene diimide, aminophenol derivatives, and benzodioxane, and evaluated their antibacterial activities. Bactericidal and bacteriostatic activity of these compounds were determined against methicillinresistant Staphylococcus aureus (MRSA) and Escherichia coli K1 with various concentrations of the drugs. Moreover, the ability of the bacteria to bind/associate to host cells was also ascertained in the absence and presence of aforementioned compounds. Results: The results revealed that porphyrin derivative (AYTHPP) had potent effects against MRSA, abolishing viability and blocking binding to the host cells. Importantly, novel AYTHPP exhibited powerful effects against MRSA even though it was not photoactivated. In contrast, other compounds, including naphthalene diimide, acetamol derivatives and benzodioxane, showed no inhibitory effects. Conclusion: The mechanism of action of porphyrin is likely through the production of reactive oxygen species causing oxidative stress, leading to apoptosis and/or necrosis via perturbations in the plasma membrane. Future studies will determine their in vivo efficacy together will associated molecular mode of action.

2021 ◽  
Vol 9 ◽  
Author(s):  
Thanh Chung Pham ◽  
Van-Nghia Nguyen ◽  
Yeonghwan Choi ◽  
Dongwon Kim ◽  
Ok-Sang Jung ◽  
...  

The ability to detect hypochlorite (HOCl/ClO−) in vivo is of great importance to identify and visualize infection. Here, we report the use of imidazoline-2-thione (R1SR2) probes, which act to both sense ClO− and kill bacteria. The N2C=S moieties can recognize ClO− among various typical reactive oxygen species (ROS) and turn into imidazolium moieties (R1IR2) via desulfurization. This was observed through UV–vis absorption and fluorescence emission spectroscopy, with a high fluorescence emission quantum yield (ՓF = 43–99%) and large Stokes shift (∆v∼115 nm). Furthermore, the DIM probe, which was prepared by treating the DSM probe with ClO−, also displayed antibacterial efficacy toward not only Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) but also methicillin-resistant Staphylococcus aureus (MRSA) and extended-spectrum ß-lactamase–producing Escherichia coli (ESBL-EC), that is, antibiotic-resistant bacteria. These results suggest that the DSM probe has great potential to carry out the dual roles of a fluorogenic probe and killer of bacteria.


1998 ◽  
Vol 42 (7) ◽  
pp. 1858-1861 ◽  
Author(s):  
Shinobu Tamura ◽  
Shuichi Miyazaki ◽  
Kazuhiro Tateda ◽  
Akira Ohno ◽  
Yoshikazu Ishii ◽  
...  

ABSTRACT The in vivo antibacterial activities of a new oral trinem, sanfetrinem cilexetil (a prodrug of sanfetrinem), were evaluated in comparison with those of cefdinir and amoxicillin. Sanfetrinem cilexetil showed potent efficacy against experimental murine septicemia caused by Staphylococcus aureus, Streptococcus pyogenes, and Escherichia coli and against murine respiratory infections caused by Streptococcus pneumoniae. Likewise, in murine models of respiratory infection by penicillin-susceptible and penicillin-resistant S. pneumoniae, sanfetrinem cilexetil was more effective than amoxicillin in reducing the number of bacteria in infected lungs. These results were reflected in its potent in vitro activity and high levels in plasma.


2020 ◽  
Vol 2 (2) ◽  
pp. 61-68
Author(s):  
Agnina Listya Anggraini ◽  
Ratih Dewi Dwiyanti ◽  
Anny Thuraidah

Infection is a disease caused by the presence of pathogenic microbes, including Staphylococcus aureus and Escherichia coli. Garlic (Allium sativum L.) has chemical contents such as allicin, alkaloids, flavonoids, saponins, tannins, and steroids, which can function as an antibacterial against Staphylococcus aureus and Escherichia coli. This study aims to determine the antibacterial properties of garlic extract powder against Staphylococcus aureus and Escherichia coli. This research is the initial stage of the development of herbal medicines to treat Staphylococcus aureus and Escherichia coli infections. The antibacterial activity test was carried out by the liquid dilution method. The concentrations used were 30 mg/mL, 40 mg/mL, 50 mg/mL, 60 mg/mL and 70 mg/mL. The results showed that the Minimum Inhibitory Concentration (MIC) against Staphylococcus aureus and Escherichia coli was 40 mg/mL and 50 mg / mL. Minimum Bactericidal Concentration (MBC) results for Staphylococcus aureus and Escherichia coli are 50 mg/mL and 70 mg/mL. Based on the Simple Linear Regression test, the R2 value of Staphylococcus aureus and Escherichia coli is 0.545 and 0.785, so it can be concluded that there is an effect of garlic extract powder on the growth of Staphylococcus aureus and Escherichia coli by 54.5% and 78.5%. Garlic (Allium sativum L.) extract powder has potential as herbal medicine against bacterial infections but requires further research to determine its effect in vivo.


2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Chunhui Miao ◽  
Mingyu Yu ◽  
Geng Pei ◽  
Zhenyi Ma ◽  
Lisong Zhang ◽  
...  

AbstractHost cells use several anti-bacterial pathways to defend against pathogens. Here, using a uropathogenic Escherichia coli (UPEC) infection model, we demonstrate that bacterial infection upregulates RhoB, which subsequently promotes intracellular bacteria clearance by inducing LC3 lipidation and autophagosome formation. RhoB binds with Beclin 1 through its residues at 118 to 140 and the Beclin 1 CCD domain, with RhoB Arg133 being the key binding residue. Binding of RhoB to Beclin 1 enhances the Hsp90-Beclin 1 interaction, preventing Beclin 1 degradation. RhoB also directly interacts with Hsp90, maintaining RhoB levels. UPEC infections increase RhoB, Beclin 1 and LC3 levels in bladder epithelium in vivo, whereas Beclin 1 and LC3 levels as well as UPEC clearance are substantially reduced in RhoB+/− and RhoB−/− mice upon infection. We conclude that when stimulated by UPEC infections, host cells promote UPEC clearance through the RhoB-Beclin 1-HSP90 complex, indicating RhoB may be a useful target when developing UPEC treatment strategies.


Author(s):  
Gouse Basha Sheik ◽  
Muazzam Sheriff Maqbul ◽  
Gokul Shankar S. ◽  
Ranjith M S

Objective: To isolate and characterize novel actinomycetes and to evaluate their antibacterial activity against drug-resistant pathogenic bacteriaMethods: In the present study, 19 soil samples were collected from different localities of Ad-Dawadmi, Saudi Arabia. Actinomycetes were isolated from these samples using serial dilution and plating method on Actinomycetes isolation agar supplemented with nalidixic acid and actidione to inhibit bacteria and fungi. Crude extracts of potential actinomycetes were produced by submerged fermentation. The antimicrobial activity of crude extracts of actinomycetes was tested against different bacteria using the agar well diffusion method. Characterization of the isolates was done by morphological, physiological and biochemical methods.Results: A total of 9 (47%) isolates of actinomycetes were isolated from 19 different soil samples tested. Among them, 4 (44%) isolates confirmed as Streptomyces sp. showed potential antimicrobial activity against one or more test organisms. Crude extracts were made from these 4 actinomycetes isolates(DOM1, DOM3, DP3, DP4)and tested for their antibacterial activities against 4 different clinical bacterial strains (Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Enterococcus). Crude extract from DP3 isolate showed highest antibacterial activity against all the four test organisms (28 mm, 21 mm, 20 mm and 18 mm) respectively and DP4 showed lowest antibacterial activity against all the four test organisms (14 mm, 12 mm, 0 mm, 6 mm) respectively. The highest zone of inhibition was shown by DP3 against Staphylococcus aureus (28 mm) and Escherichia coli was resistant for DP4. Most of the Inhibition zones produced by crude extracts showed significant differences when compared with control, tested against test organisms (P<0.05). Inhibition zones produced by DP3 and DOM1 against Staphylococcus aureus were 28 mm and 23 mm, respectively which were strong active when compared with control Ciprofloxacin (18 mm).Conclusion: Further studies for purification of bioactive metabolites and molecular characterization analysis of isolated Streptomyces sp. are in progress which would be helpful in discovering novel compounds of commercial value.


2020 ◽  
Vol 33 (02) ◽  
pp. 099-103
Author(s):  
Pritam Goswami ◽  
Sayak Ghosh ◽  
Sk Swaif Ali ◽  
Anamika Basu ◽  
Joydeep Khanra ◽  
...  

Abstract Background Panton-Valentine toxin (PVT) is an important pathological marker of staphylococcal infection mediated by functional as well as morphological damage of the phagocytic cells. Human body being an ecological niche for the bacteria shows higher affinity toward staphylococcal infection. A steady escalation in mortality and morbidity associated with antibiotic resistance in gram-positive infections is an emerging threat all over the globe; thus, it is important to find out an alternative strategy that can diminish the virulence and pathogenicity of the bacteria. Staphylococcin is a colicin-type chemical secreted by Staphylococcus aureus helps to prevent growth of organisms other than its progenitor. In this study, we evaluated the efficacy of homoeopathic medicine Staphylococcinum against staphylococcal PVT at different potencies (6CH, 12CH, 30CH and 200CH). Materials and Methods Different potencies of Staphylococcinum were administered in a leucocyte buffy coat preparation infected with staphylococcal suspension (0.5 McFarland's standard) along with control with alcohol. They were kept in incubator for 2 hours and then centrifuged at 1200 rpm for 5 minutes. Smears prepared on slides with centrifuged deposits stained by Preston and Morrell's modified Gram's method of staining and evaluated under the microscope. Results It was observed that there was extensive destruction of leukocytes in control and 6CH potency, while the degree of destruction decreased markedly from 12CH to 200CH. At 200CH potency, leukocytes were almost normal, which clearly indicate the preventive action of Staphylococcinum against PVT. The mean percentages of intact leucocytes were 0.73, 0.93, 10.00, 27.67 and 65.00 in control, 6CH, 12CH, 30CH and 200CH potencies, respectively. Conclusion The finding may help in the use of this medicine in moribund patients in cases of disseminated S. aureus infection as there is no known side effect of the medicine. However, in vivo study is necessary before such use in those cases.


2018 ◽  
Vol 7 (4) ◽  
pp. 392-398
Author(s):  
B.T Yunana ◽  
◽  
B. B Bukar ◽  
J. C Aguiyi ◽  
◽  
...  

The ethanol extracts of root, bark and leaf of Bridelia ferruginea was investigated for antibacterial activity against clinical isolate of Staphylococcus aureus and Escherichia coli. The extracts had significant antibacterial activity in vitro at concentration of 25 mg/ml, 50 mg/ml, 100 mg/ml and 200 mg/ml and in vivo at dose of 50 mg/kg and 100 mg/kg. The root extract in vitro had the highest zone of inhibition, followed by the bark extract for both Staphylococcus aureus and Escherichia coli. The concentration of 200 mg/ml had the highest zone of inhibition in vitro. The minimum inhibitory concentration (MIC) showed a decreasing inhibitory effect of the plant extracts for both Staphylococcus aureus and Escherichia coli as the concentration decreases with root having 3.125 mg/ml, bark having 6.25 mg/ml and leaf having 25 mg/ml for Staphylococcus aureus and Escherichia coli. Likewise, the minimum bactericidal concentration (MBC) showed decreasing bactericide effects with decrease concentration with root having 12.5 mg/ml, bark having 12.5 mg/ml and leaf having 25 mg/ml for Escherichia coli while root had 6.25mg/ml, bark had 12.5mg/ml and leaf had 25mg/ml for Staphylococcus aureus. The in vivo investigation showed that the root and bark extract exhibited antibacterial activity on both Staphylococcus aureus and Escherichia coli at doses of 100mg/kg and 50mg/kg; the root extract had higher activity than the bark and root/bark combined. The dose of 100 mg/kg had the highest colonies reduction for Staphylococcus aureus and Escherichia coli in vivo. Preliminary phytochemical screening of root, bark and leaves of Bridelia ferruginea revealed the presence of tannins, flavonoids, carbohydrates, cardiac glycoside (root, bark and leaves), saponins (root and bark). The presence of tannins, saponins, flavonoid, cardiac glycoside and carbohydrate in the bark and root extracts of the plant indicates that the bark and root extracts were pharmacological importance


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


2021 ◽  
Author(s):  
Fernando E. T. Cunha ◽  
Maria I. C. Ferreira ◽  
Rafael S. Cruz ◽  
Maria J. G. Ferreira ◽  
Clarissa M. Aquino ◽  
...  

Este trabalho reporta o potencial antibacteriano in vitro e toxicológico in vivo das folhas do jambo (Syzygium malaccense) frente a zebrafish (Danio rerio) adulto (ZFa). As folhas de jambo foram submetidas a desidratação (35 ± 2°C) por 24 horas, trituração e posterior extração de metabólitos por decocção, infusão e maceração com água destilada. Os extratos obtidos foram liofilizados e submetidos a análise de atividade antibacteriana in vitro frente a Gram-negativas (Escherichia coli ATCC 25922, Salmonella Enteritidis IAL 1132) e Gram-positivas (Listeria monocytogenes ATCC 19115 e Staphylococcus aureus ATCC 27664), bem como ao potencial toxicológico in vivo frente ao ZFa. O extrato obtido por infusão se mostrou mais promissor, pois apresentou concentração mínima bactericida (CMB) e concentração mínima inibitória (CMI) com maior potencial frente às gram- positivas (CMB - 6,25 e CMI - 6,25 mg/ml), bem como às gram-negativas (CMB - 25,0 e 3,125 e CMI - 3,125 mg/ml). Todos os extratos testados não se mostraram tóxicos frente ao zebrafish adulto e não alteraram o sistema locomotor dos mesmos. Desta forma, conclui-se que o extrato aquoso das folhas do jambo vermelho (Syzygium malaccense) obtido por infusão é seguro e pode ser utilizado como conservante natural com maior ação antibacteriana. Este trabalho nos conduz a novos estudos de isolamento e caracterização de princípios bioativos.


Sign in / Sign up

Export Citation Format

Share Document