scholarly journals Synthesis, Characterization, Antimicrobial Activity, and Genotoxicity Assessment of Two Heterocyclic Compounds Containing 1,2,3-Selena- or 1,2,3-Thiadiazole Rings

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4082 ◽  
Author(s):  
Mousa L. Al-Smadi ◽  
Reem Mansour ◽  
Amjad Mahasneh ◽  
Omar F. Khabour ◽  
Majed M. Masadeh ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Heterocyclic Compounds ◽  
Lethal Dose ◽  
Significant Inhibition ◽  
Gram Negative Bacteria ◽  
Highly Active ◽  
Pathogenic Microbes ◽  
Strong Antimicrobial Activity

New 1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives, (4-[4-((4-bromobenzyl)oxy)-phenyl]-1,2,3-thiadiazole (5a), 4-[4-((4-chlorobenzyl)oxy)-phenyl]-1,2,3-thiadiazole (5b)), (4-[4-((4-bromobenzyl)oxy)-phenyl]-1,2,3-selenadiazole (6a), and 4-[4-((4-chlorobenzyl)oxy)-phenyl]-1,2,3-selenadiazole (6b)), were prepared and screened in vitro for their antimicrobial activity against various pathogenic microbes. In addition, two compounds (5a and 6a) were examined for their in vivo genotoxicity using rats and an 8-hydroxy-2′-deoxyguanosine (8-OHdG) assay. Compounds 5a and 5b were found to be highly active against Gram-positive and Gram-negative bacteria. In addition, a significant inhibition of urinary 8-OHdG level (50.2%) was observed upon treatment of animals with 500 mg/kg body weight (b.w.) of compound 6a (p < 0.0001). However, compound 5a increased urinary 8-OHdG levels. The lethal dose (LD50) values for compounds 5a and 6a were determined by an up-and-down procedure (OECD 425; OECD 1998), which showed that these compounds are safe, since the LD50 was >5000 mg/kg b.w. Thus, the tested compounds might have the potential for use as antibiotics, since they have low genotoxicity and strong antimicrobial activity.

Antimicrobial Activity and Composition of the Essential Oil of Gontscharovia popovii from Iran

2006 ◽  
Vol 61 (9-10) ◽  
pp. 681-684 ◽  
Author(s):  
Ali Sonboli ◽  
Fatemeh Sefidkon ◽  
Morteza Yousefzadi
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Essential Oil ◽  
Staphylococcus Epidermidis ◽  
Gram Negative Bacteria ◽  
Capillary Gc ◽  
Aerial Parts ◽  
Full Flowering ◽  
Strong Antimicrobial Activity

AbstractThe aerial parts of Gontscharovia popovii (B. Fedtsch. and Gontsch.) Boriss. were collected at full flowering stage. The essential oil was isolated by hydrodistillation and analyzed by a combination of capillary GC and GC-MS. Thirty-one components were identified with the main constituent being carvacrol (71.9%), followed by linalool (5.5%), p-cymene (4.5%) and γ-terpinene (4.4%). The in vitro antimicrobial activity of the essential oil of G. popovii was studied against seven Gram-positive and Gram-negative bacteria (Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae) and three fungi (Candida albicans, Saccharomyces cerevisiae and Aspergillus niger). The results of the bioassays showed that the oil exhibited strong antimicrobial activity against all the tested fungi and bacteria except for the resistant bacterium Pseudomonas aeruginosa.

scholarly journals In vitro antibacterial effect of Euterpe oleracea Mart. and Theobroma grandiflorum hydroalcoholic extracts

2016 ◽  
Vol 21 (2) ◽  
Author(s):  
Lew Kan Sprenger ◽  
Elane Guerreiro Giese ◽  
Jeannie Nascimento Dos Santos ◽  
Marcelo Beltrão Molento
Keyword(s):  
Antimicrobial Activity ◽  
Inhibitory Concentration ◽  
Antimicrobial Treatment ◽  
Significant Inhibition ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Euterpe Oleracea ◽  
Agar Disc ◽  
Euterpe Oleracea Mart

This study evaluated the in vitro antimicrobial activity of these species against strains of Gram-positive and Gram-negative bacteria. The hydroalcoholic extracts were prepared from dried leaves, pulp and seeds of E. oleracea Mart. and T. grandiflorum by continuous percolation with 70% ethyl alcohol. The antimicrobial activity was evaluated against four microorganisms by the agar disc diffusion method and the minimal inhibitory concentration (MIC) assay. The antimicrobial activity showed that the açai pulp and seeds possessed significant inhibition in Clostridium perfringens (320 and 640 MIC), Staphylococcus aureus (80 and 320 MIC) and Pseudomonas aeruginosa (640 and 2560 MIC). Cupuassu extracts showed no effect on any bacteria. The use of açai extract products can be a sustainable, viable and an accessible alternative for antimicrobial treatment. New studies should be conducted to determine better results for acai herbals and new formulations of cupuassu extracts.

scholarly journals Immunomodulatory and Antimicrobial Activity of Babassu Mesocarp Improves the Survival in Lethal Sepsis

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Elizabeth S. B. Barroqueiro ◽  
Dayanna S. Prado ◽  
Priscila S. Barcellos ◽  
Tonicley A. Silva ◽  
Wanderson S. Pereira ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Phenolic Acids ◽  
Cecal Ligation ◽  
Significant Inhibition ◽  
Lymphoid Cells ◽  
Immunomodulatory Activity ◽  
Immunological Activity

Attalea speciosasynOrbignya phalerataMart. (babassu) has been used in the treatment of inflammatory and infectious diseases.Aim of the study. To investigate the antimicrobial and immunological activity of babassu mesocarp extract (EE).Material and Methods.Thein vitroantimicrobial activity was evaluated by disk diffusion assay and by determination of the minimum inhibitory concentration (MIC) toEscherichia coli,Pseudomonas aeruginosa,Enterococcus faecalis,Staphylococcus aureus,and methicillin-resistantStaphylococcus aureus(MRSA). The flavonoids and phenolic acids content were determined by chromatography. Thein vivoassays were performed in Swiss mice submitted to sepsis by cecal ligation and puncture (CLP). The mice received EE subcutaneously (125 or 250 mg/Kg), 6 hours after the CLP. The number of lymphoid cells was quantified and the cytokines production was determined by ELISA after 12 h.Results.EE was effective as antimicrobial toE. faecalis,S. aureus, and MRSA. EE is rich in phenolic acids, a class of compounds with antimicrobial and immunological activity. An increased survival can be observed in those groups, possibly due to a significant inhibition of TNF-αand IL-6.Conclusions.The EE showed specific antimicrobial activityin vitroand an important antiseptic effectin vivopossibly due to the antimicrobial and immunomodulatory activity.

scholarly journals EFFECTIVENESS OF THE FERMENTATIVE EXTRACT OF Lactobacillus acidophilus AS ANTIMICROBIALS AGAINST Aeromonas hydrophila

2019 ◽  
Vol 12 (4) ◽  
Author(s):  
Mst Nahid Akter ◽  
Roshada Hashim ◽  
Amalia Sutriana ◽  
Siti Azizah Mohd Nor
Keyword(s):  
Antimicrobial Activity ◽  
Survival Rate ◽  
Lactobacillus Acidophilus ◽  
Aeromonas Hydrophila ◽  
Significant Inhibition ◽  
Diffusion Method ◽  
Cell Free Extract ◽  
In Vivo Evaluation

The purpose of this study was to evaluate the in vitro and in vivo antimicrobial activity of the commercial Lactobacillus acidophilus (L. acidophilus) cells and cell free extract against Aeromonas hydrophila (A. hydrophila). The in vitro method was carried out using well diffusion method. For in vivo evaluation, the effect of L. acidophilus on the survival rate of Pangasianodon hypophthalmus (P. hypophthalmus) infected with A. hydrophila was evaluated. The well diffusion method showed a significant inhibition ability of L. acidophilus cells against A. hydrophila compared to the cell free extract. The inhibition diameters obtained with cells and cell free extract were 17.23 mm and 15.17 mm, respectively. P. hypophthalmus injected with L. acidophilus cells and cell free extract following challenged with A. hydrophila cells showed survival rate of 70% and 60% respectively, at 2-week post challenged. The gas chromatography-mass spectrophotometry (GC-MS) result revealed that a diverse of compounds was detected in both the L. acidophilus cells and cell free extract, among them the most abundant component was pyrrolo[1,2-a]pyrazine-1,4-dione, hexahydro-3-(2-methylpropyl), which showed a promising anticancerous activity and might be played a significant role in the recovery of the infectious P. hypophthalmus. The current study revealed that both cells and cell free extract of L. acidophilus have antimicrobial activity against A. hydrophila.

scholarly journals Saccharomicins, Novel Heptadecaglycoside Antibiotics Produced by Saccharothrix espanaensis: Antibacterial and Mechanistic Activities

2000 ◽  
Vol 44 (8) ◽  
pp. 2154-2159 ◽  
Author(s):  
M. P. Singh ◽  
P. J. Petersen ◽  
W. J. Weiss ◽  
F. Kong ◽  
M. Greenstein
Keyword(s):  
Fermentation Broth ◽  
Protein Biosynthesis ◽  
Dose Range ◽  
Lethal Dose ◽  
Antibacterial Activities ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Gram Positive Bacteria

ABSTRACT Saccharomicins A and B, two new heptadecaglycoside antibiotics, were isolated from the fermentation broth of the rare actinomyceteSaccharothrix espanaensis. They represent a novel class of bactericidal antibiotics that are active both in vitro and in vivo against bacteria and yeast (MICs: Staphylococcus aureus, <0.12 to 0.5; vancomycin-resistant enterococci, 0.25 to 16; gram-negative bacteria, 0.25 to >128; and yeast, >128 μg/ml), including multiply resistant strains. Saccharomicins protected mice from lethal challenges by staphylococci (subcutaneous 50% effective dose range of 0.06 to 2.6 mg/kg of body weight, depending on theS. aureus strain). The 50% lethal dose by the subcutaneous route was 16 mg/kg. Mechanistic studies with Escherichia coli imp and Bacillus subtilis suggested complete, nonspecific inhibition of DNA, RNA, and protein biosynthesis within 10 min of drug treatment. Microscopic examination of drug-treated cells also suggested cell lysis. These data are consistent with a strong membrane-disruptive activity. The antibacterial activities of the saccharomicins against gram-positive bacteria were unaffected by the presence of Ca2+ or Mg2+, but activity against gram-negative bacteria was substantially reduced.

scholarly journals In Vitro and In Vivo Activities of Novel 2-(Thiazol-2-ylthio)-1β-Methylcarbapenems with Potent Activities against Multiresistant Gram-Positive Bacteria

2003 ◽  
Vol 47 (8) ◽  
pp. 2471-2480 ◽  
Author(s):  
Yutaka Ueda ◽  
Makoto Sunagawa
Keyword(s):  
Bactericidal Activity ◽  
Bacterial Infections ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Log Reduction ◽  
Highly Active ◽  
Time Kill

ABSTRACT SM-197436, SM-232721, and SM-232724 are new 1β-methylcarbapenems with a unique 4-substituted thiazol-2-ylthio moiety at the C-2 side chain. In agar dilution susceptibility testing these novel carbapenems were active against methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE) with a MIC90 of ≤4 μg/ml. Furthermore, SM-232724 showed strong bactericidal activity against MRSA, in contrast to linezolid, which was bacteriostatic up to four times the MIC. SM-232724 showed good therapeutic efficacy comparable to those of vancomycin and linezolid against systemic infections of MRSA in cyclophosphamide-treated mice. The MICs of SM-197436, SM-232721, and SM-232724 for streptococci, including penicillin-intermediate and penicillin-resistant Streptococcus pneumoniae strains, ranged from ≤0.063 to 0.5 μg/ml. These drugs were the most active β-lactams tested against Enterococcus faecium, and the MIC90 s for ampicillin-resistant E. faecium ranged between 8 and 16 μg/ml, which were slightly higher than the value for linezolid. However, time-kill assays revealed the superior bactericidal activity of SM-232724 compared to those of quinupristin-dalfopristin and linezolid against an E. faecium strain with a 4-log reduction in CFU at four times the MIC after 24 h of exposure to antibiotics. In addition, SM-232724 significantly reduced the numbers of bacteria in a murine abscess model with the E. faecium strain: its efficacy was superior to that of linezolid, although the MICs (2 μg/ml) of these two agents are the same. Among gram-negative bacteria, these three carbapenems were highly active against Haemophilus influenzae (including ampicillin-resistant strains), Moraxella catarrhalis, and Bacteroides fragilis, and showed antibacterial activity equivalent to that of imipenem for Escherichia coli, Klebsiella pneumoniae, and Proteus spp. Thus, these new carbapenems are promising candidates for agents to treat nosocomial bacterial infections by gram-positive and gram-negative bacteria, especially multiresistant gram-positive cocci, including MRSA and vancomycin-resistant enterococci.

scholarly journals Comparative Antimicrobial Activity Study of Brassica oleceracea

Proceedings ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 64 ◽  
Author(s):  
Sandeep Waghulde ◽  
Nilofar Abid Khan ◽  
Nilesh Gorde ◽  
Mohan Kale ◽  
Pravin Naik ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Streptococcus Pyogenes ◽  
Antimicrobial Agents ◽  
Antimicrobial Effect ◽  
Significant Inhibition ◽  
Phytochemical Analysis ◽  
Gram Negative Bacteria ◽  
Gram Positive Bacteria ◽  
White Cabbage

Medicinal plants are in rich source of antimicrobial agents. The present study was carried out to evaluate the antimicrobial effect of plants from the same species as Brassica oleceracea namely, white cabbage and red cabbage. The preliminary phytochemical analysis was tested by using a different extract of these plants for the presence of various secondary metabolites like alkaloids, flavonoids, tannins, saponins, terpenoids, glycosides, steroids, carbohydrates, and amino acids. The in vitro antimicrobial activity was screened against clinical isolates viz gram positive bacteria Staphylococcus aureus, Streptococcus pyogenes, gram negative bacteria Escherichia coli, Pseudomonas aeruginosa. Extracts found significant inhibition against all the pathogens.

scholarly journals In Vitro and In Vivo Antibacterial Activities of S-4661, a New Carbapenem

1998 ◽  
Vol 42 (1) ◽  
pp. 94-99 ◽  
Author(s):  
Masakatsu Tsuji ◽  
Yoshikazu Ishii ◽  
Akira Ohno ◽  
Shuichi Miyazaki ◽  
Keizo Yamaguchi
Keyword(s):  
Antibacterial Activities ◽  
Gram Negative Bacteria ◽  
Drug Resistant ◽  
In Vitro Activity ◽  
Gram Positive ◽  
Highly Active ◽  
The Family ◽  
High Degree

ABSTRACT The in vitro and in vivo antibacterial activities of S-4661, a new 1β-methylcarbapenem, were compared with those of imipenem, meropenem, biapenem, cefpirome, and ceftazidime. The activity of S-4661 against methicillin-susceptible staphylococci and streptococci was comparable to that of imipenem, with an MIC at which 90% of the strains tested were inhibited (MIC90) equal to 0.5 μg/ml or less. S-4661 was highly active against members of the familyEnterobacteriaceae, Haemophilus influenzae, andMoraxella catarrhalis, with MIC90s ranging from 0.032 to 0.5 μg/ml. Against imipenem-resistant Pseudomonas aeruginosa, S-4661 was the most active among test agents (MIC90, 8 μg/ml). Furthermore, S-4661 displayed a high degree of activity against many ceftazidime-, ciprofloxacin-, and gentamicin-resistant isolates of P. aeruginosa. The in vivo efficacy of S-4661 against experimentally induced infections in mice caused by gram-positive and gram-negative bacteria, including penicillin-resistant Streptococcus pneumoniae and drug-resistant P. aeruginosa, reflected its potent in vitro activity and high levels in plasma in mice. We conclude that S-4661 is a promising new carbapenem for the treatment of infections caused by gram-positive and -negative bacteria, including penicillin-resistantS. pneumoniae and drug-resistant P. aeruginosa.

The Development of Homologous (Canine/Anti-Canine) Antibodies in Dogs with Haemophilia A (Factor VIII Deficiency): A Ten-Year Longitudinal Study

1993 ◽  
Vol 69 (01) ◽  
pp. 021-024 ◽  
Author(s):  
Shawn Tinlin ◽  
Sandra Webster ◽  
Alan R Giles
Keyword(s):  
Factor Viii ◽  
Canine Model ◽  
Significant Inhibition ◽  
Human Condition ◽  
Haemophilia A ◽  
Variable Expression ◽  
The Family ◽  
Over Time

SummaryThe development of inhibitors to factor VIII in patients with haemophilia A remains as a serious complication of replacement therapy. An apparently analogous condition has been described in a canine model of haemophilia A (Giles et al., Blood 1984; 63:451). These animals and their relatives have now been followed for 10 years. The observation that the propensity for inhibitor development was not related to the ancestral factor VIII gene has been confirmed by the demonstration of vertical transmission through three generations of the segment of the family related to a normal (non-carrier) female that was introduced for breeding purposes. Haemophilic animals unrelated to this animal have not developed functionally significant factor VIII inhibitors despite intensive factor VIII replacement. Two animals have shown occasional laboratory evidence of factor VIII inhibition but this has not been translated into clinical significant inhibition in vivo as assessed by clinical response and F.VIII recovery and survival characteristics. Substantial heterogeneity of inhibitor expression both in vitro and in vivo has been observed between animals and in individual animals over time. Spontaneous loss of inhibitors has been observed without any therapies designed to induce tolerance, etc., being instituted. There is also phenotypic evidence of polyclonality of the immune response with variable expression over time in a given animal. These observations may have relevance to the human condition both in determining the pathogenetic factors involved in this condition and in highlighting the heterogeneity of its expression which suggests the need for caution in the interpretation of the outcome of interventions designed to modulate inhibitor activity.

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