scholarly journals Colloidal Iron Oxide Formulation for Equine Hoof Disinfection

Animals ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 766
Author(s):  
Maurizio Isola ◽  
Cristina Piccinotti ◽  
Massimiliano Magro ◽  
Luca Fasolato ◽  
Fabio Vianello ◽  
...  
Keyword(s):  
Iron Oxide ◽  
Colloidal Suspension ◽  
Bacterial Load ◽  
Inhibitory Effect ◽  
In Vitro Assays ◽  
Resistant Bacteria ◽  
Colloidal Iron ◽  
In Vivo Test

The presence of bacteria of various origins on horse hoofs enables the onset of infections following trauma or even post-surgical wounds. Thus, the analysis of new antibacterial substances is of fundamental importance. In this study, the antibacterial efficacy of Iron Animals (IA), a stable colloidal suspension of iron oxide, organic acids, and detergents, was tested in vitro and in vivo. In vitro assays were performed to test the unspecific inhibitory effect of IA on both gram-positive and gram-negative bacteria monitoring the microorganism growth by spectrophotometry (optical density OD600) at 37 °C for 24 h. In vivo test consists on the quantification of the bacterial load in colony forming units per gram (CFU/g) of specimens collected from the frog region of the anterior hooves of 11 horses. Sampling followed the application of four disinfectant protocols consisting of two consecutive 3 min scrubs with 50 mL of 10% Povidone-iodine (PI) or 4% Chlorhexidine (CHx), with or without an additional application for 15 min of 10 mL of Iron Animals (PI+IA and CHx+IA). In vitro, IA completely suppressed the bacterial growth of all the tested microorganisms, resulting in effectiveness also against CHx-resistant bacteria, such as Staphylococcus aureus. In vivo, PI emerged as an ineffective protocol; CHx was effective in 18% of cases, but with the addition of IA (CHx + IA) its use emerged as the best disinfectant protocol for horse hoof, achieving the lowest bacterial load in 55% of cases. The addition of IA, after PI or CHx, improves the effectiveness of both disinfectants leading to the highest bactericidal activity in 82% of cases.

scholarly journals Evaluation of cannabidiol’s inhibitory effect on alpha-glucosidase and its stability in simulated gastric and intestinal fluids

2021 ◽  
Vol 3 (1) ◽  
Author(s):  
Hang Ma ◽  
Huifang Li ◽  
Chang Liu ◽  
Navindra P. Seeram
Keyword(s):  
Molecular Docking ◽  
High Performance ◽  
Inhibitory Effect ◽  
In Vitro Assays ◽  
Inhibitory Effects ◽  
In Vivo Models ◽  
Glucosidase Activity ◽  
Intestinal Fluids

Abstract Objective Cannabidiol (CBD) has been reported to have anti-diabetic effects in pre-clinical and clinical studies but its inhibitory effects on α-glucosidase, a carbohydrate hydrolyzing enzyme, remain unknown. Herein, we evaluated CBD’s inhibitory effects on α-glucosidase using in vitro assays and computational studies. Methods CBD’s inhibitory effect on α-glucosidase activity was evaluated in a yeast enzymatic assay and by molecular docking. The stability of CBD in simulated gastric and intestinal fluids was evaluated by high-performance liquid chromatography analyses. Results CBD, at 10, 19, 38, 76, 152, 304, 608, and 1216 μM, inhibited α-glucosidase activity with inhibition of 17.1, 20.4, 48.1, 56.6, 59.1, 63.7, 74.1, and 95.4%, respectively. Acarbose, the positive control, showed a comparable inhibitory activity (with 85.1% inhibition at 608 μM). CBD’s inhibitory effect on α-glucosidase was supported by molecular docking showing binding energy (-6.39 kcal/mol) and interactions between CBD and the α-glucosidase protein. CBD was stable in simulated gastric and intestinal fluids for two hours (maintained ≥ 90.0%). Conclusions CBD showed moderate inhibitory effect against yeast α-glucosidase activity and was stable in gastric and intestinal fluids. However, further studies on CBD’s anti-α-glucosidase effects using cellular and in vivo models are warranted to support its potential application for the management of type II diabetes mellitus.

scholarly journals Effective antibacterial and anti-hemolysin activity of ellipticine hydrochloride against Streptococcus suis in mouse model

2021 ◽  
Author(s):  
Chenchen Wang ◽  
Hao Lu ◽  
Manli Liu ◽  
Gaoyan Wang ◽  
Xiaodan Li ◽  
...  
Keyword(s):  
Antimicrobial Resistance ◽  
Hemolytic Activity ◽  
Bacterial Resistance ◽  
Bacterial Load ◽  
Streptococcus Suis ◽  
Resistant Bacteria ◽  
Inappropriate Use ◽  
Important Virulence Factor

Streptococcal toxic shock-like syndrome (STSLS) caused by the epidemic strain of Streptococcus suis leads to severe inflammation and high mortality. The life and health of humans and animals are also threatened by the increasingly severe antimicrobial resistance in Streptococcus suis (S. suis). To discover novel strategies for the treatment of S. suis is an urgent need. Suilysin (SLY) is considered to be an important virulence factor in the pathogenesis of S. suis. In this study, ellipticine hydrochloride (EH) was firstly reported as a compound to antagonize the hemolytic activity of SLY. In vitro, EH was found to effectively inhibit SLY-mediated hemolytic activity. Furthermore, EH and SLY had a strong affinity, thereby directly binding to SLY to interfere the hemolytic activity. Meanwhile, it was worth noting that EH was also found to have a significant antibacterial activity. In vivo, compared with traditional ampicillin, EH could not only significantly improve the survival rate of mice infected with S. suis 2 strain Sc19, but also relieve lung pathological damage. Furthermore, EH effectively decreased the levels of inflammatory cytokines (IL-6, TNF-α) and blood biochemistry (ALT, AST, CK) in Sc19-infected mice. Additionally, EH markedly reduced the bacterial load of tissues in Sc19-infected mice. In conclusion, our findings suggest that EH can be a potential compound for treating S. suis infection in view of its antibacterial and anti-hemolysin activity. Importance In recent years, the inappropriate use of antibiotics unnecessarily causes the continuous emergence of resistant bacteria. The antimicrobial resistance of Streptococcus suis (S. suis) becomes also an increasingly serious problem. Targeting virulence can reduce the selective pressure of bacteria on antibiotics, thereby alleviating the development of bacterial resistance to a certain extent. Meanwhile, the excessive inflammatory response caused by S. suis infection is considered the primary cause of acute death. Here, we found that ellipticine hydrochloride (EH) exhibited effective antibacterial and anti-hemolysin activity against S. suis in vitro. In vivo, compared with ampicillin, EH had a significant protective effect on S. suis 2 strain Sc19-infected mice. Our results indicated that EH with dual antibacterial and antivirulence effects will contribute to medicating S. suis infections and alleviating the antimicrobial resistance of S. suis to a certain extent. More importantly, EH may develop into a promising drug for the treatment of acute death caused by excessive inflammation.

scholarly journals Triphenilphosphonium Analogs of Chloramphenicol as Dual-Acting Antimicrobial and Antiproliferating Agents

2021 ◽  
Author(s):  
Julia A. Pavlova ◽  
Zimfira Z. Khairullina ◽  
Andrey G. Tereshchenkov ◽  
Pavel A. Nazarov ◽  
Dmitrii A. Lukianov ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Resistant Bacteria ◽  
Inhibit Protein Synthesis ◽  
Translation Process ◽  
Gram Positive Bacteria ◽  
Biochemical Assays ◽  
Bacterial Ribosome ◽  
Derivatives Of

In the current work, in continuation of our recent research [1] we synthesized and studied new chimeric compounds comprising the ribosome-targeting antibiotic chloramphenicol (CHL) and the membrane-penetrating cation triphenylphosphonium (TPP) connected by alkyl linkers of different lengths. Using various biochemical assays, we showed that these CAM-Cn-TPP compounds bind to the bacterial ribosome, inhibit protein synthesis in vitro and in vivo in a way similar to that of the parent CHL, and significantly decrease membrane potential. Similar to CAM-C4-TPP, the mode of action of CAM-C10-TPP and CAM-C14-TPP on bacterial ribosomes differ from that of CHL. By simulating the dynamics of complexes of CAM-Cn-TPP with bacterial ribosomes, we have proposed a possible explanation for the specificity of the action of these analogs on the translation process. CAM-C10-TPP and CAM-C14-TPP stronger inhibit the growth of the Gram-positive bacteria in comparison to the CHL and suppress some strains of CHL-resistant bacteria. Thus, we have shown that TPP derivatives of CHL are dual-acting compounds that target the ribosomes and the cellular membranes of bacteria. The TPP fragment of CAM-Cn-TPP compounds contributes to the inhibitory effect on bacteria. Moreover, since the mitochondria of eukaryotic cells have qualities similar to those of their prokaryotic ancestors, we demonstrate the possibility of targeting chemoresistant cancer cells with these compounds.

scholarly journals Silver i-motifs and their antibacterial activity

2021 ◽  
Author(s):  
Jessica Bratt
Keyword(s):  
Antibacterial Activity ◽  
Therapeutic Potential ◽  
Bacterial Load ◽  
Therapeutic Benefit ◽  
In Vivo Studies ◽  
Resistant Bacteria ◽  
Drug Resistant Bacteria ◽  
Low Concentrations

<p>The spread of antibiotic resistance and the emergence of multi-drug resistant bacteria is a major threat to public health. This study investigated a unique cytosine rich DNA structure, the i-Motif to deliver soluble Ag+ as a novel antimicrobial agent (AgiMs). AgiMs were evaluated in vitro against P. aeruginosa and A. baumannii strains. AgiMs displayed significant antibacterial activity against both P. aeruginosa and A. baumannii (median MIC: 0.875 µM and 0.75 µM, respectively) by rapid, bactericidal and concentration-dependent effect. Low concentrations of AgiMs showed efficacy against PAO1 20-h biofilms, resulting in 57% reduction in biomass (5 x MIC). A single dose of AgiMs extended survival of G. Mellonella larvae, with the therapeutic benefit paralleled in the reduction of internal bacterial load. Synergistic interactions were observed with the combination of AgiMs and tobramycin, a common antibiotic used to treat P. aeruginosa infections; indicating the potential for AgiMs to reinstate the potency of current antibiotics. This silver-based agent might be an alternative to the failing antibiotic regimes for MDR resistant infections. Further in vitro and in vivo studies are warranted to confirm the therapeutic potential. </p>

scholarly journals A Short S-Equol Exposure Has a Long-Term Inhibitory Effect on Adipogenesis in Mouse 3T3-L1 Cells

2021 ◽  
Vol 11 (20) ◽  
pp. 9657
Author(s):  
Gilberto Mandujano-Lázaro ◽  
Carlos Galaviz-Hernández ◽  
César A. Reyes-López ◽  
Julio C. Almanza-Pérez ◽  
Abraham Giacoman-Martínez ◽  
...  
Keyword(s):  
Weight Control ◽  
Inhibitory Effect ◽  
New Drugs ◽  
Metabolic Effects ◽  
In Vitro Assays ◽  
Differentiation Protocol ◽  
Body Weight Control ◽  
The Impact

In the search for new drugs against obesity, the chronic disease that threatens human health worldwide, several works have focused on the study of estrogen homologs because of the role of estrogen receptors (ERs) in adipocyte growth. The isoflavone equol, an ERβ agonist, has shown beneficial metabolic effects in in vivo and in vitro assays; however, additional studies are required to better characterize its potential for body weight control. Here, we showed that the treatment of 3T3-L1 cells with 10 μM of S-equol for the first three days of the adipocyte differentiation protocol was able to prevent cells becoming semi-rounded and having a lipid droplet formation until the seventh day of culture; moreover, lipid accumulation was reduced by about 50%. Congruently, S-equol induced a reduction in mRNA expression of the adipogenic markers C/EBPα and PPARγ, and adipokines secretion, mainly Adiponectin, Leptin, Resistin, and MCP-1, while the release of PAI-1 was augmented. Moreover, it also reduced the expression of ERα and attenuated the subexpression of ERβ associated with adipogenesis. Altogether, our data suggested that S-equol binding to ERβ affects the transcriptional program that regulates adipogenesis and alters adipocyte functions. Future efforts will focus on studying the impact of S-equol on ER signaling pathways.

scholarly journals Silver i-motifs and their antibacterial activity

2021 ◽  
Author(s):  
Jessica Bratt
Keyword(s):  
Antibacterial Activity ◽  
Therapeutic Potential ◽  
Bacterial Load ◽  
Therapeutic Benefit ◽  
In Vivo Studies ◽  
Resistant Bacteria ◽  
Drug Resistant Bacteria ◽  
Low Concentrations

<p>The spread of antibiotic resistance and the emergence of multi-drug resistant bacteria is a major threat to public health. This study investigated a unique cytosine rich DNA structure, the i-Motif to deliver soluble Ag+ as a novel antimicrobial agent (AgiMs). AgiMs were evaluated in vitro against P. aeruginosa and A. baumannii strains. AgiMs displayed significant antibacterial activity against both P. aeruginosa and A. baumannii (median MIC: 0.875 µM and 0.75 µM, respectively) by rapid, bactericidal and concentration-dependent effect. Low concentrations of AgiMs showed efficacy against PAO1 20-h biofilms, resulting in 57% reduction in biomass (5 x MIC). A single dose of AgiMs extended survival of G. Mellonella larvae, with the therapeutic benefit paralleled in the reduction of internal bacterial load. Synergistic interactions were observed with the combination of AgiMs and tobramycin, a common antibiotic used to treat P. aeruginosa infections; indicating the potential for AgiMs to reinstate the potency of current antibiotics. This silver-based agent might be an alternative to the failing antibiotic regimes for MDR resistant infections. Further in vitro and in vivo studies are warranted to confirm the therapeutic potential. </p>

scholarly journals Antrodia cinnamomea Enhances Chemo-Sensitivity of 5-FU and Suppresses Colon Tumorigenesis and Cancer Stemness via Up-Regulation of Tumor Suppressor miR-142-3p

Biomolecules ◽  
2019 ◽  
Vol 9 (8) ◽  
pp. 306 ◽  
Author(s):  
Yan-Jiun Huang ◽  
Vijesh Kumar Yadav ◽  
Prateeti Srivastava ◽  
Alexander TH Wu ◽  
Thanh-Tuan Huynh ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Tumor Suppressor ◽  
Colony Formation ◽  
Inhibitory Effect ◽  
In Vitro Assays ◽  
Cancer Stemness ◽  
Antrodia Cinnamomea ◽  
Tumor Sphere

5-Fluorouracil (5-FU) regimen remains the backbone of the first-line agent to treat colon cancer, but often these patients develop resistance. Cancer stem cells (CSC’s) are considered as one of the key contributors in the development of drug resistance and tumor recurrence. We aimed to provide preclinical evidence for Antrodia cinnamomea (AC), as a potential in suppressing colon cancer CSC’s to overcome 5-FU drug-resistant. In-vitro assays including cell viability, colony formation, AC + 5-FU drug combination index and tumor sphere generation were applied to determine the inhibitory effect of AC. Mouse xenograft models also incorporated to evaluate in vivo effect of AC. AC treatment significantly inhibited the proliferation, colony formation and tumor sphere generation. AC also inhibited the expression of oncogenic markers (NF-κB, and C-myc), EMT/metastasis markers (vimentin and MMP3) and stemness associated markers (β-catenin, SOX-2 and Nanog). Sequential treatment of AC and 5-FU synergized and reduces colon cancer viability both in vivo and in vitro. Mechanistically, AC mediated anti-tumor effect was associated with an increased level of tumor suppressor microRNAs especially, miR142-3p. AC can be a potent synergistic adjuvant, down-regulates cancer stemness genes and enhances the antitumor ability of 5-FU by stimulating apoptosis-associated genes, suppressing inflammation and metastasis genes through miR142-3p in colon cancer.

scholarly journals Differential Selection of Multidrug Efflux Mutants by Trovafloxacin and Ciprofloxacin in an Experimental Model ofPseudomonas aeruginosa Acute Pneumonia in Rats

2001 ◽  
Vol 45 (2) ◽  
pp. 571-576 ◽  
Author(s):  
O. F. Join-Lambert ◽  
M. Michéa-Hamzehpour ◽  
T. Köhler ◽  
F. Chau ◽  
F. Faurisson ◽  
...  
Keyword(s):  
Bacterial Load ◽  
Resistant Bacteria ◽  
Multidrug Efflux ◽  
Time Curve ◽  
Treatment Regimens ◽  
Log Reduction ◽  
Dosing Regimens ◽  
Selection Of

ABSTRACT The ability of trovafloxacin and ciprofloxacin to select efflux mutants in vivo was studied in a model of acute Pseudomonas aeruginosa pneumonia in rats. Twelve hours after intratracheal inoculation of 106 CFU of P. aeruginosastrain PAO1 enmeshed in agar beads, two groups of 12 rats were treated by three intraperitoneal injections of each antibiotic given every 5 h. Dosing regimens were chosen to obtain a comparable area under the concentration-time curve from 0 to infinity/MIC ratio of 27.9 min for trovafloxacin (75 mg/kg of body weight) and of 32.6 min for ciprofloxacin (12.5 mg/kg). Twelve rats were left untreated and served as controls. Rats were sacrificed 12 h after the last injection (34 h after infection) for lung bacteriological studies. Selection of resistant bacteria was determined by plating lung homogenates on Trypticase soy agar plates containing antibiotic. In untreated animals, the frequency of resistant colonies was 10-fold higher than in agar beads. Compared to controls, both treatment regimens resulted in a 2-log reduction of lung bacterial load. The frequency of resistant colonies was 10-fold less with trovafloxacin than with ciprofloxacin at twice the MIC (7.4 × 10−5 versus 8.4 × 10−4, respectively) (P < 0.05) and at four times the MIC (6.2 × 10−4 versus 5.0 × 10−5, respectively) (P < 0.05). A multidrug resistance phenotype typical of efflux mutants was observed in all 41 randomly tested colonies obtained from treated and untreated rats. In agreement with in vitro results, trovafloxacin and ciprofloxacin preferentially selected MexCD-OprJ and MexEF-OprN overproducers, respectively. These results demonstrate the differential ability of trovafloxacin and ciprofloxacin to select efflux mutants in vivo and highlight the rapid emergence of those mutants, even without treatment.

scholarly journals Assessment of Three In Vitro Tests and an In Vivo Test for Chloroquine Resistance in Plasmodium falciparumClinical Isolates

1998 ◽  
Vol 36 (1) ◽  
pp. 243-247 ◽  
Author(s):  
Jean Bickii ◽  
Leonardo K. Basco ◽  
Pascal Ringwald
Keyword(s):  
Host Factors ◽  
Chloroquine Resistance ◽  
In Vitro Assays ◽  
In Vitro Tests ◽  
In Vitro Test ◽  
In Vivo Evaluation ◽  
In Vivo Test ◽  
Vitro Test

Three in vitro assays (the isotopic semimicrotest [700 μl per well; 24-well plates], the isotopic microtest [200 μl per well; 96-well plates], and the rapid in vitro test) and the standard in vivo test for chloroquine resistance were compared for 99 clinical isolates of Plasmodium falciparum obtained from symptomatic African patients. The 50% inhibitory concentrations determined by the two isotopic tests were similar and were highly correlated (r = 0.965; P < 0.05), showing a high concordance between the semimicrotest and the microtest. There was a moderate agreement between these two isotopic tests and the in vivo test. Most of the discordant results were probably due to host factors, including reinfections, pharmacokinetic variations, and immunologic response, which are eliminated in in vitro assays. The rapid in vitro test based on the inhibition of chloroquine efflux in the presence of verapamil was poorly concordant with the other tests. Despite some discordant results, isotopic in vitro assays are useful to characterize the phenotypes of individual isolates without the interference of host factors and are complementary to in vivo evaluation of drug efficacy. However, in vitro assays need to be standardized to allow direct comparison of results between different laboratories.

A in Vivo Assay for Standardizing Heparin Preparations

1979 ◽  
Vol 41 (03) ◽  
pp. 576-582
Author(s):  
A R Pomeroy
Keyword(s):  
In Vitro Assays ◽  
British Pharmacopoeia ◽  
In Vitro Method ◽  
Standard Preparation ◽  
Reliable Estimation ◽  
Assay Procedure ◽  
Accuracy And Precision ◽  
Heparin Preparation

SummaryThe limitations of currently used in vitro assays of heparin have demonstrated the need for an in vivo method suitable for routine use.The in vivo method which is described in this paper uses, for each heparin preparation, four groups of five mice which are injected intravenously with heparin according to a “2 and 2 dose assay” procedure. The method is relatively rapid, requiring 3 to 4 hours to test five heparin preparations against a standard preparation of heparin. Levels of accuracy and precision acceptable for the requirements of the British Pharmacopoeia are obtained by combining the results of 3 to 4 assays of a heparin preparation.The similarity of results obtained the in vivo method and the in vitro method of the British Pharmacopoeia for heparin preparations of lung and mucosal origin validates this in vivo method and, conversely, demonstrates that the in vitro method of the British Pharmacopoeia gives a reliable estimation of the in vivo activity of heparin.

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