Synthesis and Antimicrobial Activities of 5-Arylidene-thiazolidine-2,4-dione Derivatives

Antibiotic resistance is considered one of the world's major public health concerns. The main cause of bacterial resistance is the improper and repeated use of antibiotics. To alleviate this problem, new chemical substances against microorganisms are being synthesized and tested. Thiazolidines are compounds having many pharmacological activities including antimicrobial activities. For this purpose some thiazolidine derivatives substituted at position 5 in the thiazolidine nucleus were synthesized and tested against several microorganisms. Using a disc diffusion method, antimicrobial activity was verified against Gram-positive, Gram-negative, and alcohol acid resistant bacteria and yeast. The minimum inhibition concentrations (MIC) and minimum bactericidal concentrations (MBC) were determined. All derivatives showed antimicrobial activity mainly against Gram-positive bacteria, with MIC values ranging from 2 to 16 µg/mL.

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Synthesis and Evaluation of Antimicrobial and Cytotoxic Activity of Oxathiine-Fused Quinone-Thioglucoside Conjugates of Substituted 1,4-Naphthoquinones

Molecules ◽

10.3390/molecules25163577 ◽

2020 ◽

Vol 25 (16) ◽

pp. 3577

Author(s):

Yuri E. Sabutski ◽

Ekaterina S. Menchinskaya ◽

Ludmila S. Shevchenko ◽

Ekaterina A. Chingizova ◽

Artur R. Chingizov ◽

...

Keyword(s):

Antimicrobial Activity ◽

Cytotoxic Activity ◽

Antimicrobial Activities ◽

Biologically Active ◽

Hydroxyl Group ◽

Diffusion Method ◽

Gram Positive ◽

Gram Positive Bacteria ◽

High Cytotoxic Activity ◽

Derivatives Of

A series of new tetracyclic oxathiine-fused quinone-thioglycoside conjugates based on biologically active 1,4-naphthoquinones and 1-mercapto derivatives of per-O-acetyl d-glucose, d-galactose, d-xylose, and l-arabinose have been synthesized, characterized, and evaluated for their cytotoxic and antimicrobial activities. Six tetracyclic conjugates bearing a hydroxyl group in naphthoquinone core showed high cytotoxic activity with EC50 values in the range of 0.3 to 0.9 μM for various types of cancer and normal cells and no hemolytic activity up to 25 μM. The antimicrobial activity of conjugates was screened against Gram-positive bacteria (Staphylococcus aureus, Bacillus cereus), Gram-negative bacteria (Pseudomonas aeruginosa and Escherichia coli), and fungus Candida albicans by the agar diffusion method. The most effective juglone conjugates with d-xylose or l-arabinose moiety and hydroxyl group at C-7 position of naphthoquinone core at concentration 10 µg/well showed antimicrobial activity comparable with antibiotics vancomicin and gentamicin against Gram-positive bacteria strains. In liquid media, juglone-arabinosidic tetracycles showed highest activity with MIC 6.25 µM. Thus, a positive effect of heterocyclization with mercaptosugars on cytotoxic and antimicrobial activity for group of 1,4-naphthoquinones was shown.

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Antimicrobial and antibiofilm activity of the essential oil from dried leaves of Eucalyptus staigeriana

Arquivos do Instituto Biológico ◽

10.1590/1808-1657000202018 ◽

2019 ◽

Vol 86 ◽

Cited By ~ 4

Author(s):

Marcos Saldanha Correa ◽

Joseli Schwambach ◽

Michele Bertoni Mann ◽

Jeverson Frazzon ◽

Ana Paula Guedes Frazzon

Keyword(s):

Antimicrobial Activity ◽

Essential Oils ◽

Antimicrobial Activities ◽

Diffusion Method ◽

Clinical Samples ◽

Resistant Bacteria ◽

Antibiofilm Activity ◽

Gram Positive ◽

Promising Alternative ◽

Gram Negative

ABSTRACT: In recent years, compounds with biological properties produced by plants have received attention as an alternative to control microorganisms. Essential oils extracted from green leaves of Eucalyptus sp. have been demonstrated to have antimicrobial activities, but so far there are no reports of antimicrobial activity of essential oils extracted from dried leaves of Eucalyptus staigeriana. So, the objectives of this study were to determine the chemical composition of the essential oils obtained from dried leaves of E. staigeriana (EOdlES) and to evaluate in vitro antimicrobial and antibiofilm activities of EOdlES against gram-positive and gram-negative, resistance and multiresistant Enterococcus faecalis isolated from food and clinical samples. The characterization of EOdlES was performed by gas chromatography-mass spectrometry (GC/MS). For this study, 26 bacterial strains were used, which included 11 reference strains and 15 antibiotic resistant and multiresistant E. faecalis strains. Antimicrobial activities of EOdlES against gram-positive and gram-negative were determined using the disc diffusion method. The minimum inhibitory concentration (MIC) value was evaluated by a microbroth dilution technique. The antibiofilm effects were assessed by microtiter plate method. As a result, 21 compounds were identified, being oxygenated monoterpenes (69.58%) the major chemical family. EOdlES showed only antimicrobial activity against gram-positive strains. E. faecalis resistant and multiresistant strains show the lowest MIC (3.12 to 6.25%), when compared with reference E. faecalis strain. EOdlES has the ability to inhibit the biofilm formation, but little or none ability to inhibit the preformed biofilm. This study demonstrates that EOdlES is a promising alternative to control important foodborne and clinic gram-positive resistant bacteria.

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Antimicrobial activity of Pycnarrhena cauliflora (Miers.) Diels. methanol extract

Indonesian Journal of Pharmacology and Therapy ◽

10.22146/ijpther.1656 ◽

2021 ◽

Vol 2 (2) ◽

Author(s):

Eti Nurwening Sholikhah ◽

Maulina Diah ◽

Mustofa ◽

Masriani ◽

Susi Iravati ◽

...

Keyword(s):

Antimicrobial Activity ◽

Methanolic Extract ◽

Biological Activities ◽

Positive Control ◽

Diffusion Method ◽

Gram Negative Bacteria ◽

Gram Positive ◽

Gram Negative ◽

Gram Positive Bacteria ◽

Methanolic Extracts

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.

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AKTIVITAS ANTIMIKROBA EKSTRAK DAUN JAMBU BIJI DARI BEBERAPA KULTIVAR TERHADAP Staphylococcus aureus ATCC 25923 DENGAN HOLE-PLATE DIFFUSION METHOD

Journal of Biological Researches ◽

10.23869/bphjbr.9.1.200310 ◽

2003 ◽

Vol 9 (1) ◽

pp. 49-51

Author(s):

Farida Lanawati Darsono ◽

Stephanie Devi Artemisia

Keyword(s):

Staphylococcus Aureus ◽

Antimicrobial Activity ◽

Traditional Medicine ◽

Tween 80 ◽

Antibacterial Activities ◽

Psidium Guajava ◽

Antimicrobial Activities ◽

Diffusion Method ◽

Gram Positive Bacteria ◽

Activity Test

A study has been performed on the antimicrobial activities of jambu biji (Psidium guajava Linn) leaves from several cultivars (red, white and yellow cultivar) against Staphylococcus aureus ATCC 25923 representing the Gram positive bacteria. The reason for conducting this research is that the leaves of jambu biji are frequently used in traditional medicine as a remedy against diarrhoea. The hole-plate diffusion method was used for conducting the antimicrobial activity test with antibiotics (Ampicilline trihidrat) as reference standards. The extracts of jambu biji for each cultivar were obtained by reflux with ethanol 96 percent. The concentrations of the extracts applied to the holes were 10 percent, 20 percent, and 30 percent w/v, the extracts were reconstituted with tween 80 and ethanol 96 percent. Based on the result of the study, it can be concluded that the extract of jambu biji from each cultivar with the concentration of 10 percent, 20 percent, and 30 percent w/v showed antibacterial activities against Staphylococcus aureus ATCC 25923. The result obtained statictically evaluated using Anava Factorial 3x3 and furthery tested for significancy (a = 0.05). Based on the results of study, it can be concluded that the extract of jambu biji leaves from red cultivar, white cultivar and yellow cultivar showed antibacterial activities against Staphylococcus aureus ATCC 25923.

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Antimicrobial Capacity of Plant Polyphenols against Gram-positive Bacteria: A Comprehensive Review

Current Medicinal Chemistry ◽

10.2174/0929867325666181008115650 ◽

2020 ◽

Vol 27 (15) ◽

pp. 2576-2606 ◽

Cited By ~ 17

Author(s):

Francisco Javier Álvarez-Martínez ◽

Enrique Barrajón-Catalán ◽

José Antonio Encinar ◽

Juan Carlos Rodríguez-Díaz ◽

Vicente Micol

Keyword(s):

Antimicrobial Activity ◽

Antibacterial Activity ◽

Mechanism Of Action ◽

Molecular Targets ◽

Membrane Receptors ◽

Resistant Bacteria ◽

Plant Polyphenols ◽

Gram Positive ◽

Gram Positive Bacteria ◽

Promising Source

Background: Multi-drug-resistant bacteria such as Methicillin-Resistant Staphylococcus aureus (MRSA) disseminate rapidly amongst patients in healthcare facilities and suppose an increasingly important cause of community-associated infections and associated mortality. The development of effective therapeutic options against resistant bacteria is a public health priority. Plant polyphenols are structurally diverse compounds that have been used for centuries for medicinal purposes, including infections treatment and possess, not only antimicrobial activity, but also antioxidant, anti-inflammatory and anticancer activities among others. Based on the existing evidence on the polyphenols’ antibacterial capacity, polyphenols may be postulated as an alternative or complementary therapy for infectious diseases. Objective: To review the antimicrobial activity of plant polyphenols against Gram-positive bacteria, especially against S. aureus and its resistant strains. Determine the main bacterial molecular targets of polyphenols and their potential mechanism of action. Methodology: The most relevant reports on plant polyphenols’ antibacterial activity and their putative molecular targets were studied. We also performed virtual screening of thousand different polyphenols against proteins involved in the peptidoglycan biosynthesis to find potential valuable bioactive compounds. The bibliographic information used in this review was obtained from MEDLINE via PubMed. Results: Several polyphenols: phenolic acids, flavonoids (especially flavonols), tannins, lignans, stilbenes and combinations of these in botanical mixtures, have exhibited significant antibacterial activity against resistant and non-resistant Gram-positive bacteria at low μg/mL range MIC values. Their mechanism of action is quite diverse, targeting cell wall, lipid membrane, membrane receptors and ion channels, bacteria metabolites and biofilm formation. Synergic effects were also demonstrated for some combinations of polyphenols and antibiotics. Conclusion: Plant polyphenols mean a promising source of antibacterial agents, either alone or in combination with existing antibiotics, for the development of new antibiotic therapies.

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Antimicrobial, Antioxidant and Cytotoxic Activities and Phytochemical Screening of Some Yemeni Medicinal Plants

Evidence-based Complementary and Alternative Medicine ◽

10.1093/ecam/nen004 ◽

2010 ◽

Vol 7 (3) ◽

pp. 323-330 ◽

Cited By ~ 49

Author(s):

Ramzi A. A. Mothana ◽

Salah A. A. Abdo ◽

Sidgi Hasson ◽

Faisal M. N. Althawab ◽

Sama A. Z. Alaghbari ◽

...

Keyword(s):

Antimicrobial Activity ◽

Cytotoxic Activity ◽

Hot Water ◽

Diffusion Method ◽

Scavenging Activity ◽

Phytochemical Screening ◽

Gram Positive ◽

Gram Positive Bacteria ◽

Methanolic Extracts ◽

Multiresistant Bacteria

The traditional medicine still plays an important role in the primary health care in Yemen. The current study represents the investigation of 16 selected plants, which were collected from different localities of Yemen. The plants were dried and extracted with two different solvents (methanol and hot water) to yield 34 crude extracts. The obtained extracts were tested for their antimicrobial activity against three Gram-positive bacteria, two Gram-negative bacteria, one yeast species and three multiresistantStaphylococcusstrains using agar diffusion method, for their antioxidant activity using scavenging activity of DPPH radical method and for their cytotoxic activity using the neutral red uptake assay. In addition, a phytochemical screening of the methanolic extracts was done. Antibacterial activity was shown only against Gram-positive bacteria, among them multiresistant bacteria. The highest antimicrobial activity was exhibited by the methanolic extracts ofAcalypha fruticosa,Centaurea pseudosinaica,Dodonaea viscosa,Jatropha variegata,Lippia citriodora,Plectranthus hadiensis,Tragia pungensandVerbascum bottae.Six methanolic extracts especially those ofA. fruticosa,Actiniopteris semiflabellata,D. viscosa,P. hadiensis,T. pungensandV. bottaeshowed high free radical scavenging activity. Moreover, remarkable cytotoxic activity against FL-cells was found for the methanolic extracts ofA. fruticosa,Iris albicans,L. citriodoraandT. pungens. The phytochemical screening demonstrated the presence of different types of compounds like flavonoids, terpenoids and others, which could be responsible for the obtained activities.

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Comparative Analysis of Antimicrobial Activities of Valinomycin and Cereulide, the Bacillus cereus Emetic Toxin

Applied and Environmental Microbiology ◽

10.1128/aem.02671-10 ◽

2011 ◽

Vol 77 (8) ◽

pp. 2755-2762 ◽

Cited By ~ 29

Author(s):

Marcel H. Tempelaars ◽

Susana Rodrigues ◽

Tjakko Abee

Keyword(s):

Antimicrobial Activity ◽

Comparative Analysis ◽

Membrane Potential ◽

Bacillus Cereus ◽

Antimicrobial Activities ◽

Gram Positive ◽

Content Type ◽

Gram Positive Bacteria ◽

Ph Range ◽

Main Component

ABSTRACTCereulide and valinomycin are highly similar cyclic dodecadepsipeptides with potassium ionophoric properties. Cereulide, produced by members of theBacillus cereusgroup, is known mostly as emetic toxin, and no ecological function has been assigned. A comparative analysis of the antimicrobial activity of valinomycin produced byStreptomycesspp. and cereulide was performed at a pH range of pH 5.5 to pH 9.5, under anaerobic and aerobic conditions. Both compounds display pH-dependent activity against selected Gram-positive bacteria, includingStaphylococcus aureus,Listeria innocua,Listeria monocytogenes,Bacillus subtilis, andBacillus cereusATCC 10987. Notably,B. cereusstrain ATCC 14579 and the emeticB. cereusstrains F4810/72 and A529 showed reduced sensitivity to both compounds, with the latter two strains displaying full resistance to cereulide. Both compounds showed no activity against the selected Gram-negative bacteria. Antimicrobial activity against Gram-positive bacteria was highest at alkaline pH values, where the membrane potential (ΔΨ) is the main component of the proton motive force (PMF). Furthermore, inhibition of growth was observed in both aerobic and anaerobic conditions. Determination of the ΔΨ, using the membrane potential probe DiOC2(3) (in the presence of 50 mM KCl) in combination with flow cytometry, demonstrated for the first time the ability of cereulide to dissipate the ΔΨ in sensitive Gram-positive bacteria. The putative role of cereulide production in the ecology of emeticB. cereusis discussed.

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Antimicrobial Activity of Some Egyptian Spice Essential Oils

Journal of Food Protection ◽

10.4315/0362-028x-52.9.665 ◽

1989 ◽

Vol 52 (9) ◽

pp. 665-667 ◽

Cited By ~ 288

Author(s):

R. S. FARAG ◽

Z. Y. DAW ◽

F. M. HEWEDI ◽

G. S. A. EL-BAROTY

Keyword(s):

Antimicrobial Activity ◽

Essential Oils ◽

Microbial Growth ◽

Inhibitory Effect ◽

Diffusion Method ◽

Gram Positive ◽

Filter Paper Disc ◽

Gram Negative ◽

Gram Positive Bacteria ◽

Chemical Structures

Six spice essential oils (sage, rosemary, caraway, cumin, clove, and thyme) and their basic ingredients were tested for their inhibitory effect against 3 strains of Gram-negative bacteria, 4 strains of Gram-positive bacteria, one acid fast bacterium, and one yeast. Preliminary screening of antimicrobial activity of the essential oils was done using the filter paper disc agar diffusion method. The minimum inhibitory concentration for each essential oil against various micro-organisms was also measured. Very low concentrations (0.25 – 12 mg/ml) of the various essential oils were sufficient to prevent microbial growth. The data show that Gram-positive bacteria were more sensitive to the antimicrobial compounds in spices than Gram-negative. The inhibition zones of different microbial growth produced by various essential oils were similar to those produced by their basic compounds. Thyme and cumin oils possessed very strong antimicrobial activity compared with the other essential oils. There was a relationship between the chemical structures of the most abundant compounds in the essential oils under investigation and the antimicrobial activity.

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PRELIMINARY PHYTOCHEMICAL SCREENING AND IN VITRO ANTI-MICROBIAL ACTIVITY OF ETHANOLIC EXTRACTS OF SEEDS OF PUNICA GRANATUM AGAINST STANDARD PATHOGENIC STRAINS

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2018v10i4.28464 ◽

2018 ◽

Vol 10 (4) ◽

pp. 55

Author(s):

Aditya Jyoti Bora ◽

Biswajit Dash ◽

Sujata Paul ◽

Bikash Gupta

Keyword(s):

Antimicrobial Activity ◽

Microbial Activity ◽

Sulfhydryl Group ◽

Ethanolic Extract ◽

Punica Granatum ◽

Diffusion Method ◽

Gram Positive ◽

Gram Negative ◽

Gram Positive Bacteria ◽

Anti Fungal

Objective: To estimate the anti-microbial activity of ethanolic extract of Punica granatum seeds (family-Punicaceae) in association with phytochemical analysis.Methods: The ethanolic extract of the seeds of Punica granatum was prepared and investigate for phytochemical constituents using standard methods. Antimicrobial activities of ethanolic extract were carried out against one Gram positive bacteria (Staphylococcus aureus) and one Gram negative bacteria (Escherichia coli). The anti-fungal activity of the plant extract was evaluated on Candida albicans. The testing was done by the disc diffusion method. A zone of inhibition of ethanolic extract was compared with that of standard Tetracycline for anti-bacterial activities and Fluconazole for anti-fungal activity.Results: The result of this study showed a good antibacterial effect of pomegranate juice against both Gram negative and Gram positive bacteria. The antimicrobial activity of the fruit may be due to its high content of polyphenols which causes phenolic toxicity by interfering with the sulfhydryl group of the bacterial proteins and high content of tannins which interferes with bacterial membrane stability.Conclusion: The present study concluded that ethanolic extract of the seeds of Punica granatum contains the high existence of phytochemicals. The ethanolic extract of the plant was found to possess promising antimicrobial activity when compared with the standards.

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Antimicrobial Activity of Plant Extracts againstBacillus Subtilis,Staphylococcus Aureusand Escherichia Coli

E-Journal of Chemistry ◽

10.1155/2011/824697 ◽

2011 ◽

Vol 8 (s1) ◽

pp. S282-S284 ◽

Cited By ~ 1

Author(s):

Liliwirianis N ◽

Wan Zuraida Wan Mohd Zain ◽

Jamaluddin Kassim ◽

Shaikh Abdul Karim

Keyword(s):

Escherichia Coli ◽

Antimicrobial Activity ◽

Inhibition Zone ◽

Diffusion Method ◽

Gram Negative Bacteria ◽

Gram Positive ◽

Gram Negative ◽

Gram Positive Bacteria ◽

Stemona Tuberosa ◽

Elephantopus Scaber

Local herbs have many potential that may be active with antimicrobial activity. A screening was conducted with 11 species of herbs collected in UiTM Pahang Forest Reserve.Epipremnumsp.,Zingibersp.Tetracera indica, Tectaria crenata, Piper stylosum, Homalomena propinque, Goniothalamus sp., Elephantopus scaber, Mapania patiolale, Melastomasp.,Stemona tuberosa, Phullagathis rotundifolia, Thotea grandifoliaandSmilaxsp. were extracted with methanol to obtain their crude. The agar diffusion method using blank disc of 6 mm diameter were loaded with 1000 µg/mL of methanol crude and applied to the inoculate plate was used to assess the antimicrobial activity against two gram positive bacteria (Bacillus subtilisandStaphylococcus aeureus) and one gram negative bacteria (Escherichia coli). The results evaluated as the diameter of the inhibition zone of microbial growth, showed that all the extracts were active against gram-positive bacteria and gram-negative bacteria. The extract ofStemona tuberosewas found to be the most active against theE. coliandS. aeureuswhilePiper stylosumactive againstB. subtilis.

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