scholarly journals Evaluation of 1,2-Benzothiazine 1,1-Dioxide Derivatives In Vitro Activity towards Clinical-Relevant Microorganisms and Fibroblasts

Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3503 ◽  
Author(s):  
Ruth K. Dudek-Wicher ◽  
Berenika M. Szczęśniak-Sięga ◽  
Rafał J. Wiglusz ◽  
Jan Janczak ◽  
Marzenna Bartoszewicz ◽  
...  

The global concern related with growing number of bacterial pathogens, resistant to numerous antibiotics, prone scientific environment to search for new antimicrobials. Antiseptics appear to be suitable candidates as adjunctive agents to antibiotics or alternative local treatment option aiming to prevent and treat infections. 1,2-benzothiazines are considered one the most promising of them. In this research twenty 1,2-benzothiazine 1,1-dioxide derivatives were scrutinized with regard to their biological activity. Three of them are new. For evaluation of compounds’ activity against microbial pathogens, disk diffusion method and serial microdilution method was applied. To establish the cytotoxicity profile of tested 1,2-benzothiazines 1,1-dioxides derivatives, the cytotoxicity assay using fibroblasts L292 was performed. Antimicrobial activity of all tested compounds against Gram-positive Staphylococcus aureus and Enterococcus faecalis strains was higher than antimicrobial activity of DMSO solvent, which possesses antimicrobial activity itself. Gram-negative P. aeruginosa, E. coli and K. pneumoniae have shown susceptibility only to compounds 3e, 7i and 7l. None of tested compounds was effective against C. albicans. Compound 6g has demonstrated the strongest antimicrobial potency (MIC = 0.00975 mg/mL) among compounds of series 6. Compounds of series 7, namely 7d, 7f, 7g had the lowest minimum inhibitory concentration (MIC). Compound 7f displayed also the lowest cytotoxic effect against fibroblast cell line among series 7 compounds. All tested derivatives displayed lower MIC against Gram-positive bacteria than commercially applied antiseptic, povidone iodine, which MIC value range for tested Gram-positive bacteria was 1.56–6.25 mg/mL.

2009 ◽  
Vol 4 (1) ◽  
pp. 93
Author(s):  
Tássia Campos de Lima Silva ◽  
Jorge Veras Filho ◽  
Janete Magali Araújo ◽  
Ulysses Paulino Albuquerque ◽  
Vânia Teixeira Lima ◽  
...  

ABSTRACT Objective: to determine the antimicrobial activity of three plant species of the genus Phyllanthus (P. amarus Schum. and Thom., P. tenellus Roxb. and Phyllanthus niruri L.) and its commercial dye (phytotherapic), opposite the bacteria and yeasts. Methods: we evaluated the antimicrobial activity against microorganisms by disk diffusion method, and then evaluated minimum inhibitory concentration of the best results from the microdilution method. Results: the medicinal species have antimicrobial activity to Gram-positive bacteria. The commercial dye showed significant antimicrobial activity. The extracts showed the best activity for S. aureus (P. amarus with MIC 0.16 mg / mL and P. tenellus with MIC 0.10 mg / mL), opposite to B. subtilis results were also satisfactory (P. amarus 0.25 mg / mL and P. tenellus 0.30 mg / mL). The commercial dye showed MIC greater than 1mg/ml only for S. aureus with MIC of 0.70 mg / mL, and for B. subtilis showed MIC 1.10 mg / mL. With respect to the yeast, all substances were less significant than for gram-positive bacteria, ranging from 0.70 to 1mg/ml for crude extracts and 1.10 to 1.20 mg / mL for the dyeing trade. Conclusion: this study showed the potential antibacterial and antifungal therapeutic value of these species can be better evaluated. Descriptors: Phyllanthus, MIC, antimicrobial, fungicide. RESUMOObjetivo: determinar a atividade antimicrobiana de três espécies de plantas do gênero Phyllanthus (P. amarus Schum e Thom.,  P. tenellus Roxb. e Phyllanthus niruri L.) e de sua tintura comercial (fitoterápico), frente a bactérias e leveduras. Métodos: foi avaliada a atividade antimicrobiana frente a microrganismos através do método de disco difusão, em seguida foram avaliadas as concentrações mínimas inibitórias dos melhores resultados a partir do método da microdiluição. Os extratos apresentaram melhor atividade para S. aureus (P. amarus com MIC 0,16 mg/mL e P. tenellus com MIC  0,10 mg/mL), frente a B. subtilis os resultados também foram satisfatórios (P. amarus 0,25mg/mL e P. tenellus 0,30mg/mL). A tintura comercial apresentou MIC maior que 1mg/mL apenas para S. aureus com MIC de 0,70mg/mL, já para B. subtilis apresentou MIC 1,10mg/mL. Com relação as leveduras, todas as substâncias resultaram ser menos expressivos  que para as bactérias gram-positivas, variando de 0,70 a 1mg/mL para os extratos brutos e 1,10 a 1,20 mg/mL para a tintura comercial. Conclusão: este estudo mostrou o potencial antibacteriano e antifúngicos destas espécies cujo valor terapêutico pode ser melhor avaliado. Descritores: Phyllanthus, CMI, antimicrobiana, fungicida. RESUMEN Objetivo: determinar la actividad antimicrobiana de tres especies de plantas del género Phyllanthus (P. amarus Schum y Thom., P. tenellus Roxb. y Phyllanthus niruri  L.) y su tinte comercial (phytotherapic), frente a las bacterias y levaduras. Métodos: se evaluó la actividad antimicrobiana contra microorganismos por el método de difusión en disco y, a continuación, detectado concentración mínima inhibitoria de los mejores resultados de la microdilución método. Resultados: los medicamentos especies actividad antimicrobiana de las bacterias Gram-positivas. El tinte comercial mostraron un importante actividad antimicrobiana. Los extractos mostraron la mejor actividad para S. aureus (P. amarus MIC con 0,16 mg / ml y P. tenellus MIC con 0,10 mg / ml), frente a B. subtilis resultados también fueron satisfactorios (P. amarus 0,25 mg / ml y P. tenellus 0,30 mg / ml). El tinte comercial mostró superior a 1mg/ml MIC sólo para S. aureus con CMI de 0,70 mg / ml, y para B. subtilis mostró MIC 1,10 mg / mL. Con respecto a la levadura, todas las sustancias eran menos importantes que para las bacterias gram-positivas, que van desde 0,70 a 1mg/ml de extractos crudos y de 1,10 a 1,20 mg / ml de tintura para el comercio. Conclusión: este estudio demostró el potencial antibacteriano y antimicótico valor terapéutico de estas especies pueden ser mejor evaluadas. Descriptores: Phyllanthus, CMI, los antibióticos, fungicidas. 


2014 ◽  
Vol 25 (3) ◽  
pp. 186-190 ◽  
Author(s):  
Andiara De Rossi ◽  
Danielly Cunha Araújo Ferreira ◽  
Raquel Assed Bezerra da Silva ◽  
Alexandra Mussolino de Queiroz ◽  
Léa Assed Bezerra da Silva ◽  
...  

Abstract: The objective of this in vitro study was to evaluate the antimicrobial effect of toothpastes containing natural extracts, chlorhexidine or triclosan. The effectiveness of toothpastes containing natural extracts (Parodontax(r)), 0.12% chlorhexidine (Cariax(r)), 0.3% triclosan (Sanogil(r)) or fluoride (Sorriso(r), control) was evaluated against yeasts, Gram-positive and Gram-negative bacteria using the disk diffusion method. Water was used as a control. Disks impregnated with the toothpastes were placed in Petri dishes containing culture media inoculated with 23 indicative microorganisms by the pour plate method. After incubation, the inhibition growth halos were measured and statistical analyses (α=0.05) were performed. The results indicated that all formulations, except for conventional toothpaste (Sorriso(r)), showed antimicrobial activity against Gram-positive bacteria and yeasts. The toothpaste containing natural extracts (Parodontax(r)) was the only product able to inhibit the growth of Pseudomonas aeruginosa. The toothpastes containing chlorhexidine, triclosan or natural extracts presented antimicrobial activity against Gram-positive bacteria and yeasts.


2021 ◽  
Vol 5 (3) ◽  

Objectives: This study aimed to examine the effect of ethanolic extract of local Basra henna leaves on Gram-positive bacteria species. Also, to assess the antibacterial properties of henna crude extract in vitro and compare them with antibiotics. Methods: In this study, Lawsonia inermis (henna) leaves were extracted with ethanol using the solvent extraction technique. The pathogens were isolated from wound samples obtained from hospitalized patients in two different hospitals in Duhok city. The culture of thirty isolates had been recognized by routine methods. Different concentrations of ethanol crude extract were acquired and bio-assayed in vitro to inhibit the growth of five human pathogenic Gram-positive bacteria. Agar well diffusion assay was used for achieving henna antibiotic activity. Moreover, an antibiotics susceptibility test was done by the disk diffusion method using the Muller-Hinton agar medium. Results: The growth of all tested bacteria was suppressed to various degrees by increasing the concentration of the extract. The data has revealed that Staphylococcus aureus was more sensitive than other examined isolates, where the diameter zone of inhibition was ranging from 16-27, 14-25, and 8-18 mm for Staphylococcus epidermidis, Lactobacillus spp. and Streptococcus pneumonia respectively. The antimicrobial activity of henna extract indicates that it is suitable for being used as significant certain medications. Consequently, henna is active to serve as an anti-bacterial agent against multi-drug resistant Gram-positive bacteria. Conclusion: The antimicrobial activity of henna extract indicates that it is suitable for being used as significant certain medications. Consequently, henna is active to serve as an anti-bacterial agent against multi-drug resistant Gram-positive bacteria.


2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Irina V. Galkina ◽  
Elena V. Tudriy ◽  
Yuliya V. Bakhtiyarova ◽  
Luiza M. Usupova ◽  
Marina P. Shulaeva ◽  
...  

A new series of bis-4,6-sulfonamidated 5,7-dinitrbenzofuroxans  7–11had been synthesized and tested for antimicrobial activity. The structures of new sulfanilamide derivatives were characterized by elemental analysis, IR spectroscopy, and mass spectrometry (MALDITOF). The synthesized compounds were tested for theirin vitroantimicrobial activity using the disk diffusion method against Gram-positive bacteriaStaphylococcus aureus; the Gram-negative bacteriaEscherichia coli, Pseudomonas aeruginosa, andProteus mirabilis; the fungal strainAspergillus niger; and the yeast-like pathogenic fungusCandida albicans. Our results indicate that the compounds7–11exhibit potent antimicrobial activity. The stability of the compounds was evaluated by TG and DSC methods.


2021 ◽  
Vol 2 (2) ◽  
Author(s):  
Eti Nurwening Sholikhah ◽  
Maulina Diah ◽  
Mustofa ◽  
Masriani ◽  
Susi Iravati ◽  
...  

Pycnarrhena cauliflora (Miers.) Diels., local name sengkubak, is one of indigenous plants from West Kalimantan that has been used as natural flavor. Pycnorrhena cauliflora is one of species of Menispermaceae family which is rich in bisbenzylisoquinoline alkaloids. This alkaloids are known to have various biological activities including antiprotozoal, antiplasmodial, antifungal and antibacterial activities. This study aimed to investigate antimicrobial activity of  the P. cauliflora (Miers.) Diels. methanolic extracts against gram-positive and gram-negative bacteria. The methanolic extract of P. cauliflora (Miers.) Diels., root, leaf and stem were prepared by maceration. The disk-diffusion method was then used to determine the antimicrobial activity of the extracts against Streptococcus pyogenes, S. mutants, Staphylococcus aureus, S. epidermidis, Salmonella typhi, Shigella flexneri, Pseudomonas aeruginosa and Escherichia coli after 18-24 h incubation at 37 oC. Amoxicillin was used as positive control for gram-positive bacteria and ciprofloxacin was used as gram-negative bacteria. The inhibition zones were then measured in mm. Analysis were conducted in duplicates. The results showed in general the methanolic extracts of P. cauliflora (Miers.) Diels. root (inhibition zone diameter= 10-23 mm) were more active than that leaf (0-15 mm) and stem (0-17 mm) extracts against gram-positive bacteria. The zone inhibition diameter of amoxicillin as positive control was 8-42 mm. In addition, the methanolic extracts of P. cauliflora (Miers.) Diels. root (12-17 mm) were also more active than that leaf (0-12 mm) and stem (0-12 mm) extracts against gram-negative bacteria. The zone inhibition diameter of ciprofloxacin as positive control was 33-36 mm. In conclusion, the methanolic extract of P. caulifloria (Miers.) Diels. root is the most extract active against both gram-positive and gram-negative bacteria. Further study will be focused to isolate active compounds in the methanolic extract of the root.


2013 ◽  
Vol 14 (5) ◽  
pp. 924-929 ◽  
Author(s):  
Reena Kulshrestha ◽  
J Kranthi ◽  
P Krishna Rao ◽  
Feroz Jenner ◽  
V Abdul Jaleel ◽  
...  

ABSTRACT Aim The present study was conducted to evaluate the efficacy of commercially available herbal toothpastes against the different periodontopathogens. Materials and methods Six herbal toothpastes that were commonly commercially available were included in the study. Colgate herbal, Babool, Meswak, Neem active, Dabur red toothpastes were tested for the study whereas sterile normal saline was used as control. Antimicrobial efficacies of dentifrices were evaluated against Streptococcus mutans and Actinobacillus actinomycetemcomitans. The antimicrobial properties of dentifrices were tested by measuring the maximum zone of inhibition at 24 hours on the Mueller Hinton Agar media inoculated with microbial strain using disk diffusion method. Each dentifrice was tested at 100% concentration (full strength). Results The study showed that all dentifrices selected for the study were effective against the entire test organism but to varying degree. Neem active tooth paste gave a reading of 25.4 mm as the zone of inhibition which was highest amongst all of the test dentifrices. Colgate Herbal and Meswak dentifrices recorded a larger maximum zone of inhibition, measuring 23 and 22.6 mm respectively, compared to other toothpastes. All other dentifrices showed the zone of inhibition to be between 17 and 19 mm respectively. Conclusion The antibacterial properties of six dentifrices were studied in vitro and concluded that almost all of the dentifrices available commercially had antibacterial properties to some extent to benefit dental health or antiplaque action. How to cite this article Jenner F, Jaleel VA, Kulshrestha R, Maheswar G, Rao PK, Kranthi J. Evaluating the Antimicrobial Activity of Commercially Available Herbal Toothpastes on Microorganisms Associated with Diabetes Mellitus. J Contemp Dent Pract 2013;14(5):924-929.


2019 ◽  
Vol 21 (2) ◽  
pp. 125
Author(s):  
U.B. Issayeva ◽  
G.S. Akhmetova ◽  
U.M. Datkhayev ◽  
M.T. Omyrzakov ◽  
K.D. Praliyev ◽  
...  

With the aim to introduce fragment of cyclopropane and fragments of p-, m-, o-fluorophenyls into the structures of N-ethoxyethylpiperidines, acylation of oxime and phenylacetylenic alcohol of 1-(2-ethoxyethyl)-4-ketopiperidine by cyclopropanecarbonylchloride was carried out; on the basis of 1-(2-ethoxyethyl)-4-ethynyl-4-hydroxypiperidine (cascaine alcohol), acylation by 4-fluoro-, 3-fluoro-, 2-fluorobenzoylchlorides was carried out with formation of the corresponding piperidine containing hydrochlorides of cyclopropanecarboxylic acid esters and para-, meta-, ortho-fluorobenzoic esters. Acylation reaction on the hydroxyl group of compounds is carried out in absolute dioxane, the acylating agents are cyclopropanecarbonylchloride, p-, m-, o-fluorobenzoyl chlorides taken in excess. The obtained esters of cyclopropanecarboxylic and para-, meta-, ortho-fluorobenzoic acids are crystalline substances with a clear melting point, well soluble in water, ethanol, acetone. P-fluorobenzoates are obtained with better yields, m-fluorobenzoates occupy an intermediate position, and o-fluorobenzoates are formed with the lowest yields. The best yields of fluorobenzoates are obtained using dioxane as a solvent. Para-, meta-, ortho-fluorobenzoic esters of 1-(2-ethoxyethyl)-4-ethynyl-4-hydroxypiperidine coded A-4 – A-6 were studied for the presence of antimicrobial activity, the actions of these preparations were evaluated in vitro in relation to strains of gram-positive bacteria Staphylococcus aureus, Bacillus subtilis, gram-negative strains of Escheriсhia coli, Pseudomonas aeruginosa and to yeast fungus Сandida albicans by the diffusion method into agar (holes). Introduction of fluorine atom into the structure of cascaine lead to manifestation of antimicrobial activity.


2020 ◽  
Vol 16 (2) ◽  
Author(s):  
P. M. Ridzuan ◽  
Hairul Aini Hamzah ◽  
Anis Shah ◽  
Norazian Mohd Hassan ◽  
Baharudin Roesnita

Antibacterial activity of different types of P. odorata leaf extracts was evaluated in combination with standard antibiotics. Persicaria. odorata leaves were extracted with n-hexane (n-hex), dichloromethane (DCM) and methanol (MeOH).  Each extract was applied on vancomycin (30µg), erythromycin (15µg) and gentamicin (10µg) discs, respectively. Disk diffusion method was used to evaluate the synergistic activity of each combination on Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae, Pseudomonas aeruginosa, Salmonella typhi, and Escherichia coli. Minimum inhibitory concentration (MIC) and gas chromatography mass spectrometry (GCMS) analysis was performed on the active extract. Synergistic effects seen were mainly from the n-hex+antibiotics combinations, mainly on the Gram-positive bacteria (7 additive, 5 antagonistic), with MIC range from 50 µg/ml to 100 µg/ml, as well as Gram-negative bacteria (2 additive, 2 indifferent, 5 antagonistic). In particular, synergism showed by the combination of n-hex+van were all additive against the susceptible bacteria. DCM extract combination showed synergistic effects on three Gram-positive species (S. aureus, S. epidermidis, S. pyogenes). Meanwhile, MeOH+antibiotics combination showed significant additive synergistic effects (p<0.05) on S. aureus and S. epidermidis.  The major compounds of leaves extract were decanal and β-citral. n-Hex extract superiorly inhibited Gram-positive bacteria growth as compared to DCM and MeOH extracts. The additive synergistic property of the n-hex P. odorata extract could be further studied for possible use as an antibacterial agent.


2012 ◽  
Vol 7 (5) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Alexis Peña ◽  
Luis Rojas ◽  
Rosa Aparicio ◽  
Libia Alarcón ◽  
José Gregorio Baptista ◽  
...  

The essential oil of the leaves of Espeletia nana Cuatrec, obtained by hydrodistillation, was analyzed by GC-MS, which allowed the identification of 24 components, which made up 99.9% of the oil. The most abundant compounds were α-pinene (38.1%), β-pinene (17.2%), myrcene (15.0%), spathulenol (4.2%), bicyclogermacrene (4.0%), α-zingiberene (4.0%), and γhimachalene (3.7%). Antibacterial activity was tested against Gram-positive and Gram-negative bacteria using the agar disk diffusion method. Activity was observed only against Gram-positive bacteria. MIC values were determined for Staphylococcus aureus ATCC 25923(200 μg/mL) and Enterococcus faecalis ATCC 29212 (600 μg/mL).


2018 ◽  
Vol 13 (8) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Mária Pl'uchtová ◽  
Teresa Gervasi ◽  
Qada Benameur ◽  
Vito Pellizzeri ◽  
Daniela Grul'ová ◽  
...  

Genus Mentha presents group of plants which are the most studied in family Lamiaceae. Aboveground parts are used for different purposes in pharmacy, food industry or confectionery. Most important is natural product extracted from leaves - essential oil (EO). The aim of presented experiment was to demonstrate different chemotype and compare antibacterial activity of two Mentha species EO. Plant samples were obtained from various environments – from Slovakia and from Italy. Dominant compounds were determined by GC/MS. The results showed high amount of menthol and menthone in tested Slovak peppermint EO. On the other hand, carvone and 1,8-cineole were determinate as dominant compounds in Italian spearmint EO. The antimicrobial activity of the EO was investigated by disc diffusion and broth micro dilution methods. EO was evaluated for their antibacterial activity against 7 microorganisms: Enterobacter cloacae, Salmonella spp., Klebsiella pneumoniae, Escherichia coli, Staphylococcus aureus, Streptococcus pyogenes. The determination results of antibacterial activity by agar disk diffusion method ranged from 7 to 14 mm of the growth inhibition zone. MIC of tested mint EO varied from 0.625 to 2.5 μg/mL. In addition, both EO showed relatively the same antibacterial activity against the selected Gram-negative bacteria. However, there is a variation in the antibacterial activity against Gram-positive bacteria.


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