scholarly journals In Vitro and In Vivo Activities of Fluoroquinolones against Aeromonas hydrophila

2003 ◽  
Vol 47 (7) ◽  
pp. 2217-2222 ◽  
Author(s):  
Wen-Chien Ko ◽  
Shyh-Ren Chiang ◽  
Hsin-Chun Lee ◽  
Hung-Jen Tang ◽  
Yin-Yi Wang ◽  
...  

ABSTRACT Aeromonas hydrophila, an uncommon human pathogen, can cause invasive infections in immunocompromised individuals. As the fluoroquinolones have been shown to be active in vitro against mesophilic aeromonads and clinical experience with the use of fluoroquinolones to treat aeromonads infections is limited, the antimicrobial activities of five selected drugs (ciprofloxacin, gatifloxacin, levofloxacin, lomefloxacin, and moxifloxacin) against A. hydrophila were studied in vitro and in mice. The MICs of the fluoroquinolones (except lomefloxacin), cefotaxime, and minocycline for 90% of 64 clinical isolates of A. hydrophila tested by the agar dilution method were ≤1 μg/ml. With a clinical cefotaxime-resistant strain, Ah 2743, in an in vitro time-kill study, at an inoculum of 7 × 105 CFU/ml incubated with fluoroquinolones, cefotaxime, or minocycline at concentrations equal to twice the MICs, the inhibitory effect lasted for less than 6 h and regrowth occurred thereafter. In an animal model with female BALB/c mice intraperitoneally infected with an inoculum of 1.1 × 107 CFU of Ah 2743, more mice in the ciprofloxacin-treated group survived (72.2%) than in the cefotaxime-, minocycline-, or cefotaxime-minocycline-treated group (P < 0.00001, log rank test). However, there were similar fatality rates, ranging from 71.4 to 87.5%, among mice treated with any of five fluoroquinolones. With a larger inoculum, 4.9 × 107 CFU, mice in the ciprofloxacin-treated group survived longer than those in the minocycline-, cefotaxime-, or cefotaxime-minocycline-treated group (30 h versus 18, 12, and 12 h, respectively [P < 0.002, log rank test]). However, in mice infected with cefotaxime-susceptible Ah 2556, ciprofloxacin was as effective as cefotaxime-minocycline. Thus, our results suggest that ciprofloxacin is at least as effective as cefotaxime-minocycline against murine A. hydrophila infections, which warrants clinical studies to delineate its role in human infections.

2002 ◽  
Vol 46 (11) ◽  
pp. 3580-3584 ◽  
Author(s):  
Hung-Jen Tang ◽  
Ming-Chung Chang ◽  
Wen-Chien Ko ◽  
Kun-Yen Huang ◽  
Chih-Lung Lee ◽  
...  

ABSTRACT The MICs of six fluoroquinolones as well as minocycline and cefotaxime for 46 clinical isolates of Vibrio vulnificus were determined by the agar dilution method. All the drugs tested had good activities against all isolates, with the MICs at which 90% of the isolates tested were inhibited (MIC90s) by five of the fluoroquinolones ranging between 0.03 and 0.06 μg/ml. The MIC90 of lomefloxacin, on the other hand, was 0.12 μg/ml. Time-kill studies were conducted with these agents and a clinical strain of V. vulnificus, VV5823. When approximately 5 × 105 CFU of V. vulnificus/ml was incubated with any one of the above-mentioned six fluoroquinolones at concentrations of two times the MIC, there was an inhibitory effect on V. vulnificus that persisted for more than 48 h with no noted regrowth. The efficacies of the fluoroquinolones were further evaluated in vivo in the mouse model of experimental V. vulnificus infection and compared to the efficacy of a combination therapy using cefotaxime plus minocycline. With an inoculum of 1.5 × 107 CFU, 28 (87.5%) of 32 mice in the cefotaxime-minocycline-treated group survived and 29 (91%) of the 32 mice in the moxifloxacin-treated group survived while none of the 32 mice in the control group did. With an inoculum of 3.5 × 107 CFU, the difference in survival rates among groups of 15 mice treated with levofloxacin (13 of 15), moxifloxacin (10 of 15), gatifloxacin (10 of 15), sparfloxacin (11 of 15), ciprofloxacin (12 of 15), or lomefloxacin (10 of 15) was not statistically significant while none of the 15 mice treated with saline survived. We concluded that the newer fluoroquinolones as single agents are as effective as the cefotaxime-minocycline combination in inhibiting V. vulnificus both in vitro and in vivo.


2014 ◽  
Vol 974 ◽  
pp. 394-397 ◽  
Author(s):  
Sroisiri Thaweboon ◽  
Boonyanit Thaweboon ◽  
Surachai Dechkunakorn ◽  
Passiri Nisalak ◽  
Rattiporn Kaypetch

Cratoxylumformosumis a plant widely distributed in mountainous area of various Asian countries. The extract prepared from the burnt bark has been used among the local people as a varnish to prevent tooth decay and other oral diseases. The aim of this study was to examine antifungal activity ofC. formosumgum againstCandidaalbicansand to evaluate its cytotoxicity. The gum prepared from the extract ofC.formosumwas investigated for antimicrobial activity against 3 strains ofC.albicans. Inhibition of microbial growth was primarily tested by agar diffusion method. A two-fold broth dilution method was then used to determine the minimum inhibitory concentration (MIC) of the gum. Based on the MIC value, cytotoxicity test was performed on mouse fibroblasts (ATCC clone 929) using agar overlay technique. Inhibitory effect of the gum was seen againstC. albicanswith zones of inhibition ranging from 8.0 to 9.3 mm. MIC values were between 0.50 and 1.25 mg/mL. In term of cytotoxicity,C. formosumgum at the concentration of 20 MIC (25 mg/mL) was classified as grade 3 (moderate cytotoxicity) whereas those of 10 MIC and 1 MIC were grade 1 (slight cytotoxicity). In conclusion, the gum prepared fromC. formosumextract exhibited antimicrobial activities against all the test strains ofC. albicans. From the present study, it can be suggested that this plant can be used as a novel antifungal agent, effective againstC.albicansinfections, due to its inhibitory effects onC. albicansand acceptable biocompatibility. Furtherin vitro/in vivostudies should be conducted to understand the mechanisms of action and to establish the safe profile of this gum for clinical usage.


Cancers ◽  
2018 ◽  
Vol 10 (12) ◽  
pp. 491 ◽  
Author(s):  
Heng-Wei Liu ◽  
Yu-Kai Su ◽  
Oluwaseun Bamodu ◽  
Dueng-Yuan Hueng ◽  
Wei-Hwa Lee ◽  
...  

Background: Glioblastoma (GBM), a malignant form of glioma, is characterized by resistance to therapy and poor prognosis. Accumulating evidence shows that the initiation, propagation, and recurrence of GBM is attributable to the presence of GBM stem cells (GBM-CSCs). Experimental approach: Herein, we investigated the effect of 4-Acetylantroquinonol B (4-AAQB), a bioactive isolate of Antrodia cinnamomea, on GBM cell viability, oncogenic, and CSCs-like activities. Results: We observed that aberrant expression of catenin is characteristic of GBM, compared to other glioma types (p = 0.0001, log-rank test = 475.2), and correlates with poor prognosis of GBM patients. Lower grade glioma and glioblastoma patients (n = 1152) with low catenin expression had 25% and 21.5% better overall survival than those with high catenin expression at the 5 and 10-year time-points, respectively (p = 3.57e-11, log-rank test = 43.8). Immunohistochemistry demonstrated that compared with adjacent non-tumor brain tissue, primary and recurrent GBM exhibited enhanced catenin expression (~10-fold, p < 0.001). Western blot analysis showed that 4-AAQB significantly downregulated β-catenin and dysregulated the catenin/LEF1/Stat3 signaling axis in U87MG and DBTRG-05MG cells, dose-dependently. 4-AAQB–induced downregulation of catenin positively correlated with reduced Sox2 and Oct4 nuclear expression in the cells. Furthermore, 4-AAQB markedly reduced the viability of U87MG and DBTRG-05MG cells with 48 h IC50 of 9.2 M and 12.5 M, respectively, effectively inhibited the nuclear catenin, limited the migration and invasion of GBM cells, with concurrent downregulation of catenin, vimentin, and slug; similarly, colony and tumorsphere formation was significantly attenuated with reduced expression of c-Myc and KLF4 proteins. Conclusions: Summarily, we show for the first time that 4-AAQB suppresses the tumor-promoting catenin/LEF1/Stat3 signaling, and inhibited CSCs-induced oncogenic activities in GBM in vitro, with in vivo validation; thus projecting 4-AAQB as a potent therapeutic agent for anti-GBM target therapy.


2011 ◽  
Vol 89 (6) ◽  
pp. 419-427 ◽  
Author(s):  
Misagh Alipour ◽  
Abdelwahab Omri ◽  
Zacharias E. Suntres

This study was carried out to examine the antimicrobial activity of the aqueous extract of Panax quinquefolius from North American ginseng (NAGE) root against Pseudomonas aeruginosa . The minimum inhibitory concentrations of reference and clinical isolates of Pseudomonas aeruginosa were measured by a standard agar-dilution method. At subinhibitory NAGE concentrations, the secretion of virulence factors, motility on agar, and adhesion to 96-well microplates were studied on the nonmucoid Pseudomonas aeruginosa O1 strain. At suprainhibitory concentrations, the activity of NAGE against mature biofilm complexes formed in the Calgary Biofilm Device and the Stovall flow cell were assessed. NAGE possessed an antibacterial activity against all the Pseudomonas aeruginosa strains at 1.25%–2.5% w/v. NAGE also significantly attenuated pyocyanin, pyoverdine, and lipase concentrations, stimulated twitching, and attenuated swarming and swimming motility. At 1.25% w/v, NAGE augmented adhesion, and at 5% w/v detached 1-day-old biofilms in microplates. The extract also eradicated 6-day-old mature biofilms (5% w/v), and fluorescence microscopy displayed a reduction of live cells and biofilm complexes compared with nontreated biofilms. These data suggest that the aqueous extract from North American ginseng possesses antimicrobial activities in vitro.


2003 ◽  
Vol 47 (11) ◽  
pp. 3667-3671 ◽  
Author(s):  
A. Liebetrau ◽  
A. C. Rodloff ◽  
J. Behra-Miellet ◽  
L. Dubreuil

ABSTRACT The antimicrobial activities of garenoxacin and eight other antibiotics against 641 anaerobic isolates were evaluated with the NCCLS agar dilution method. Overall, the MICs of garenoxacin for 50 and 90% of the strains tested (in micrograms per milliliter) were as follows: Bacteroides fragilis group, 0.5 and 2; Prevotella spp., 0.25 and 2; Fusobacterium spp., 0.25 and 0.5; Porphyromonas spp., 0.125 and 0.25; Bilophila wadsworthia, 0.5 and 1; Veillonella spp., 0.25 and 0.5; Clostridium spp., 0.25 and 1; Clostridium difficile, 2 and >64; Bifidobacterium spp., 1 and 2; Eggerthella lenta, 0.25 and 1; Propionibacterium spp., 0.5 and 0.5; gram-positive cocci, 0.125 and 0.25.


2019 ◽  
Vol 16 (9) ◽  
pp. 1020-1030
Author(s):  
Zhaochang Liang ◽  
Yuping Huang ◽  
Shiben Wang ◽  
Xianqing Deng

Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro antimicrobial activities were evaluated using a serial dilution method against several gram-positive strains, gram-negative strains and a fungi strain. Results: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF- α at the concentration of 20 µg/mL Compounds 5i, 6b, and 7b had comparable in vivo antiinflammatory activity to the reference drug dexamethasone at the dose of 50 mg/kg. In addition, several compounds showed antimicrobial activity against different strains, and compounds 5g and 5h exhibited potent inhibitory activities with the MIC value of 8 µg/mL against the Streptococcus pneumoniae CMCC 31968 and Staphylococcus aureus CMCC 25923, respectively. Compound 7b, which exhibited both anti-inflammatory and antimicrobial activities, should be studied as it is or after derivatization. Conclusion: It can be concluded that pyrazoles, with (thio)-semicarbazone moieties, have the potential to be developed into new anti-inflammatory agents.


2000 ◽  
Vol 44 (2) ◽  
pp. 283-286 ◽  
Author(s):  
Haruaki Tomioka ◽  
Katsumasa Sato ◽  
Hiroko Kajitani ◽  
Tatsuya Akaki ◽  
Shinji Shishido

ABSTRACT WQ-3034 is a newly synthesized acidic fluoroquinolone. We assessed its in vitro activity against Mycobacterium tuberculosisand M. avium complex using levofloxacin (LVFX), ciprofloxacin (CPFX), sparfloxacin (SPFX), and KRM-1648 (KRM) as reference drugs. The MICs of these agents were determined by the agar dilution method with 7H11 medium. The MICs at which 50 and 90% of the test strains were inhibited (MIC50s, and MIC90s, respectively) for the test quinolones for rifampin (RMP)-susceptible M. tuberculosis strains were in the order SPFX < LVFX ≦ WQ-3034 ≦ CPFX, while those for RMP-resistant M. tuberculosis strains were in the order SPFX ≦ WQ-3034 ≦ LVFX < CPFX. The MICs of KRM for RMP-susceptible M. tuberculosis were much lower than those of the test quinolones, while the MIC90 of KRM for RMP-resistant M. tuberculosis strains was higher than those of the quinolones. The MIC50s and MIC90s of the test drugs for M. avium were in the order KRM < SPFX < CPFX ≦ WQ-3034 ≦ LVFX, while those forM. intracellulare were in the order KRM < SPFX < WQ-3034 ≒ LVFX ≦ CPFX. Next, we compared the antimicrobial activities of the test drugs against M. tuberculosisorganisms residing in cells of the Mono Mac 6 macrophage (Mφ)-like cell line (MM6-Mφs) and of the A-549 type II alveolar cell line (A-549 cells). When drugs were added at the concentration that achieves the maximum concentration in blood, progressive killing or inhibition of the M. tuberculosis organisms residing in MM6-Mφs and A-549 cells was observed in the order KRM > SPFX ≧ LVFX > WQ-3034 > CPFX. The efficacies of all quinolones against intracellular M. tuberculosis organisms were significantly lower in A-549 cells than in MM6-Mφs. WQ-3034 at the MIC caused more marked growth inhibition of intramacrophage M. tuberculosis than did LVFX. These findings indicate that the in vitro anti-M. tuberculosis activity of WQ-3034 is greater than that of CPFX and is comparable to that of LVFX.


2013 ◽  
Vol 59 (4) ◽  
pp. 252-259 ◽  
Author(s):  
Lei Han ◽  
Jin'e Lei ◽  
Shaoshan Han ◽  
Li He ◽  
Chaofeng Ma ◽  
...  

Listeria monocytogenes is resistant to fosfomycin in vitro but is susceptible in vivo due to increased expression of positive regulator factor A (PrfA) and its dependent factor, hexose phosphate transporter (Hpt), upon infection of host cells. Amberlite, a polymeric adsorbent resin, could induce PrfA-dependent gene expression and thus, in theory, improve the sensitivity of L. monocytogenes to fosfomycin in vitro. In the current study, an improved susceptibility test based on Amberlite was developed using reference strains. Thirty-five clinical isolates were further examined to verify those preliminary results. Briefly, Amberlite increased in vitro fosfomycin sensitivity of all strains. Optimal Amberlite concentrations, as evaluated through the expression of phospholipase B (PlcB) and Hpt, were 10% and 15% (w/v) in agar media and 3% (w/v) in broth media. Mueller–Hinton (MH) medium, tryptone soya (TS) medium, and brain heart infusion (BHI) medium were used to verify the results in the control strains using agar dilution and broth micro- and macro-dilution methods. Better listerial growth was shown in TS and BHI than in MH. Both broth dilution methods yielded lower minimal inhibitory concentration (MIC) of fosfomycin than the agar dilution method. The MIC of fosfomycin for 35 clinical isolates was 2–32 μg/mL, suggesting improved susceptibility. In conclusion, in vitro sensitivity of L. monocytogenes to fosfomycin was substantially improved in the presence of 3% Amberlite-supplemented TSB or BHIB and the broth microdilution method. This improved method revealed the potential antilisterial activity of fosfomycin in vitro and could facilitate the therapy of listeriosis using fosfomycin.


Foods ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 1281
Author(s):  
Emanuel Vamanu ◽  
Florentina Gatea ◽  
Diana Roxana Pelinescu

Coffee grounds are a valuable source of bioactive compounds. In Romania, most of the amount obtained is lost through non-recovery; the rest is occasionally used as organic fertilizer. The coffee grounds were selected according to the roasting degree: blonde roasted (BR), medium roasted (MR), and dark roasted (DR). The study aimed to evaluate three extracts, obtained with a mixture of ethanol/water/acetic acid (50/49.5/0.5), depending on the roasting degree. The majority phenolic component, the antioxidant, and anti-inflammatory effect, as well as the role that gastrointestinal transit had on the bioavailability of bioactive compounds were determined. Chlorogenic acid was inversely proportional to the roasting degree. BR showed the best correlation between antioxidant and anti-inflammatory activities in vitro/in vivo. The antiproliferative capacity of the extracts determined an inhibitory effect on the tumor cells. Antimicrobial activities, relevant in the control of type 2 diabetes, were exerted through the inhibition of microbial strains (Escherichia coli). Following gastric digestion, BR demonstrated a maximum loss of 20% in the stomach. The recovery of coffee grounds depended on the pattern of functional compounds and the bioavailability of the main component, chlorogenic acid.


2017 ◽  
Vol 61 (11) ◽  
Author(s):  
Yuk-Yam Cheung ◽  
Mamie Hui

ABSTRACT We evaluated the in vitro and in vivo effects of nikkomycin Z combined with an echinocandin (anidulafungin or micafungin) against two Candida albicans isolates and their lab-derived echinocandin-resistant fks mutants with FKS1 S645Y and FKS1 S645P. Synergistic effects were observed in all tested strains (fractional inhibitory concentration index, <0.5). Enhanced survival was observed in an immunocompromised murine model (log-rank test, P < 0.02). Our study demonstrated the therapeutic potential of nikkomycin Z-echinocandin combinations in managing echinocandin resistance.


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