scholarly journals The Biological Evaluation of Fusidic Acid and Its Hydrogenation Derivative as Antimicrobial and Anti-inflammatory Agents

2018 ◽  
Author(s):  
Pan-Pan Wu ◽  
Hao He ◽  
W. David Hong ◽  
Tong-Rong Wu ◽  
Su-Qing Zhao ◽  
...  
Keyword(s):  
Fusidic Acid ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Ear Edema ◽  
Gram Positive Bacteria ◽  
Mouse Ear ◽  
Anti Inflammatory

AbstractFusidic acid (WU-FA-00) is the only commercially available antimicrobial from the fusidane family that has a narrow spectrum of activity against Gram-positive bacteria. Herein, the hydrogenation derivative (WU-FA-01) of fusidic acid was prepared, and both compounds were examined against a panel of six bacterial strains. In addition, their anti-inflammation properties were evaluated using a 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema model. The results of the antimicrobial assay revealed that both WU-FA-00 and WU-FA-01 displayed a high level of antimicrobial activity against Gram-positive strains. Moreover, killing kinetic studies were performed, and the results were in accordance with the MIC and MBC results. We also demonstrated that the topical application of WU-FA-00 and WU-FA-01 effectively decreased TPA-induced ear edema in a dose-dependent manner. This inhibitory effect was associated with the inhibition of TPA-induced up-regulation of pro-inflammation cytokines IL-1β, TNF-α and COX-2. WU-FA-01 significantly suppressed the expression levels of p65, IκB-α, and p-IκB-α in the TPA-induced mouse ear model. Overall, our results showed that WU-FA-00 and WU-FA-01 not only had effective antimicrobial activitiesin vitro, especially to the Gram-positive bacteria, but also possessed strong anti-inflammatory effectsin vivo. These results provide a scientific basis for developing fusidic acid derivatives as antimicrobial and anti-inflammatory agents.

Contribution of Toll-like receptors to the innate immune response to Gram-negative and Gram-positive bacteria

Blood ◽  
2006 ◽  
Vol 109 (4) ◽  
pp. 1574-1583 ◽  
Author(s):  
Greg Elson ◽  
Irène Dunn-Siegrist ◽  
Bruno Daubeuf ◽  
Jérome Pugin
Keyword(s):  
Cell Activation ◽  
Dependent Manner ◽  
Toll Like Receptors ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Independent Manner ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Molecular Pattern ◽  
High Concentrations

Abstract Innate recognition of bacteria is a key step in the activation of inflammation and coagulation, and it is dependent on pathogen-associated molecular pattern (PAMP) ligation to Toll-like receptors (TLRs) and CD14. The dominant receptors activated when cells encounter a whole bacterium, which express several PAMPs, are poorly defined. Herein, we have stimulated various human cells with prototypic Gram-negative and Gram-positive bacteria. Receptor-dependent responses to whole bacteria were assessed using both TLR-transfected cells and specific monoclonal antibodies against TLRs, MD-2, and CD14. Enterobacteria-activated leukocytes and endothelial cells in a TLR4/MD-2–dependent manner, most likely via lipopolysaccharide (LPS). TLR2 activation was observed with a high bacterial inoculum, and in epithelial cells expressing TLR2 but not TLR4. Pseudomonas aeruginosa stimulated cells by both TLR2 and TLR4/MD-2. Gram-positive bacteria activated cells only at high concentrations, in a partially TLR2-dependent but TLR4/MD-2–independent manner. Either TLR or CD14 neutralization blocked activation to all bacterial strains tested with the exception of some Gram-positive strains in whole blood in which partial inhibition was noted. This study identifies dominant TLRs involved in responses to whole bacteria. It also validates the concept that host cell activation by bacterial pathogens can be therapeutically reduced by anti-TLR4, -TLR2, and -CD14 mAbs.

scholarly journals Topical Anti-Inflammatory Activity of Essential Oils of Alpinia calcarata Rosc., Its Main Constituents, and Possible Mechanism of Action

2020 ◽  
Vol 2020 ◽  
pp. 1-19
Author(s):  
Madhuvanthi Chandrakanthan ◽  
Shiroma M. Handunnetti ◽  
Galbada Sirimal Arachchige Premakumara ◽  
Selvaluxmy Kathirgamanathar
Keyword(s):  
Skin Inflammation ◽  
Inflammatory Activity ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Proinflammatory Mediators ◽  
Mouse Ear ◽  
Anti Inflammatory ◽  
Dose Dependent ◽  
Topical Analgesic

This study aimed at investigating the anti-inflammatory potential of essential oil from rhizome and leaf of Alpinia calcarata Rosc. (ACEO) with the focus of its topical anti-inflammatory activity along with its dominant compounds 1,8-cineole and α-terpineol using mouse ear edema model. ACEOs were analyzed by GC-MS. The anti-inflammatory activity was determined by studying the inhibition of overproduction of proinflammatory mediators—nitric oxide, reactive oxygen species, prostaglandins, cyclooxygenases, and cytokines induced by lipopolysaccharides in murine macrophages. Topical anti-inflammatory and antinociceptive activity was studied by 12-O-tetradecanoylphorbol-13-acetate (TPA) induced skin inflammation and formalin-induced pain model in mice, respectively. Rhizome oil has 1,8-cineole (31.08%), α-terpineol (10.31%), and fenchyl acetate (10.73%) as major compounds whereas the ACEO from leaves has 1,8-cineole (38.45%), a-terpineol (11.62%), and camphor (10%). ACEOs reduced the production of inflammatory mediators in vitro in a concentration-dependent manner. Further, ACEO and its major compounds reduced ear thickness, weight, myeloperoxidase, and cytokines significantly (p<0.01) in mouse ear. Dose-dependent reduction in flinching and licking in both the phases of pain sensation concludes the topical analgesic effect. Our findings suggest the potency of topical use of ACEOs for inflammatory disease conditions.

scholarly journals DhhP, a Cyclic di-AMP Phosphodiesterase of Borrelia burgdorferi, Is Essential for Cell Growth and Virulence

2014 ◽  
Vol 82 (5) ◽  
pp. 1840-1849 ◽  
Author(s):  
Meiping Ye ◽  
Jun-Jie Zhang ◽  
Xin Fang ◽  
Gavin B. Lawlis ◽  
Bryan Troxell ◽  
...  
Keyword(s):  
Borrelia Burgdorferi ◽  
Wild Type Strain ◽  
Wall Structure ◽  
Mammalian Host ◽  
Dependent Manner ◽  
Gram Positive ◽  
Content Type ◽  
Gram Positive Bacteria

ABSTRACTCyclic di-AMP (c-di-AMP) is a recently discovered second messenger in bacteria. Most of work on c-di-AMP signaling has been done in Gram-positive bacteria, firmicutes, and actinobacteria, where c-di-AMP signaling pathways affect potassium transport, cell wall structure, and antibiotic resistance. Little is known about c-di-AMP signaling in other bacteria.Borrelia burgdorferi, the causative agent of Lyme disease, is a spirochete that has a Gram-negative dual membrane. In this study, we demonstrated thatB. burgdorferiBB0619, aDHH-DHHA1 domainprotein (herein designated DhhP), functions as c-di-AMP phosphodiesterase. Recombinant DhhP hydrolyzed c-di-AMP to pApA in a Mn2+- or Mg2+-dependent manner. In contrast to c-di-AMP phosphodiesterases reported thus far, DhhP appears to be essential forB. burgdorferigrowth bothin vitroand in the mammalian host. Inactivation of the chromosomaldhhPgene could be achieved only in the presence of a plasmid-encoded inducibledhhPgene. The conditionaldhhPmutant had a dramatic increase in intracellular c-di-AMP level in comparison to the isogenic wild-type strain. Unlike what has been observed in Gram-positive bacteria, elevated cellular c-di-AMP inB. burgdorferidid not result in an increased resistance to β-lactamase antibiotics, suggesting that c-di-AMP's functions in spirochetes differ from those in Gram-positive bacteria. In addition, thedhhPmutant was defective in induction of the σSfactor, RpoS, and the RpoS-dependent outer membrane virulence factor OspC, which uncovers an important role of c-di-AMP inB. burgdorferivirulence.

scholarly journals Antibacterial and Anticancer Properties of New Fluoroquinolones

2019 ◽  
Vol 32 (2) ◽  
pp. 427-434
Author(s):  
Maha R. Al Rimawi ◽  
Yusuf M. Al-Hiari ◽  
Amal G. Al-Bakri ◽  
Sanaa K. Bardaweel
Keyword(s):  
Antibacterial Agents ◽  
Spectroscopic Techniques ◽  
Cell Culture System ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Anticancer Properties ◽  
Gram Positive Bacteria ◽  
Good Antibacterial Activity ◽  
Weak Activity

Fluoroquinolones are clinically successful antibacterial agents. In this work a series of novel 7-substituted anilino-8-nitrofluoroquinolone esters (3-9), acids (10-16) and 8-amino reduced derivatives (17-23) of the later compounds were successfully prepared and characterized using spectroscopic techniques. All the compounds tested (10-23) showed good antibacterial activity against both Gram-positive and Gram- negative standard bacterial strains. Interestingly, 8-amino reduced derivatives (17-22) were more active against both standard strains than their 8-nitro acid analogues (10-15). Moreover, some targeted compounds have shown reasonable activity mainly against resistant gram positive bacteria. In particular compounds 10, 12 and 16 displayed a potent activity against methicillin resistant S. aureus (MRSA) with MIC values of 4.7, 2.3 and 1.2 μg/mL, respectively. Lipophilicity could be a plausible explanation of such higher activity against the gram positive resistant strain (MRSA). Biological screening of cytotoxic activity against five cancer cell lines using an in vitro cell culture system was achieved for all tested compounds. These derivatives have shown weak activity for most of them. Interestingly, more lipophilic nitroacids (10-15) were more active than their analogous reduced acids (17-22).

scholarly journals Synthesis, characterization, and in vitro antimicrobial investigation of novel pyran derivatives based on 8-hydroxyquinoline

2019 ◽  
Vol 8 (1) ◽  
Author(s):  
Mohamed Rbaa ◽  
Abdelhadi Hichar ◽  
Omar Bazdi ◽  
Younes Lakhrissi ◽  
Khadija Ounine ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Magnetic Resonance ◽  
Penicillin G ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Wide Range

Abstract Background 8-Hydroxyquinoline derivatives are known for their extensive applications in the field of analytical chemistry and separation techniques; their complexes with transition metals also exhibit antibacterial and antifungal activity. Results In the present study, we synthesized a new series of pyranoquinoline derivatives and evaluated their antibacterial activities. The structures of the synthesized compounds were characterized by Fourier transform infrared (FT-IR), hydrogen-1 nuclear magnetic resonance, carbon-13 nuclear magnetic resonance, and elemental analysis. All the prepared compounds were evaluated in vitro as antimicrobial agents against Gram-positive and Gram-negative bacterial strains (Escherichia coli (ATCC35218), Staphylococcus aureus (ATCC29213), Vibrio parahaemolyticus (ATCC17802), and Pseudomonas aeruginosa (ATCC27853)). The screening test was determined by using the standard protocol of disc diffusion method (DDM). Conclusion We have synthesized new pyranic compounds bearing an 8-hydroxyquinoline moiety on their structure. The preliminary screening results showed that all the tested compounds have a remarkable inhibitory effect on the growth of the majority of the tested bacterial strains compared to the standard antibiotic (penicillin G), and the chlorinated compound (Q1) is more active against Gram-positive bacteria than Gram-negative bacteria such as the Staphylococcus aureus strain which is the most sensitive. Gram-positive bacteria are responsible for a wide range of infectious diseases, and rising resistance in this group is causing increasing concern. Thus, this study develops novel heterocyclic compound derivatives of 8-hydroxyquinoline that have demonstrated good antibacterial activity against Gram-positive bacteria. Graphical abstract

Biological evaluation of a Porphyrin-SPION nanoconjugate as an antimicrobial magnetic photosensitizer

2017 ◽  
Vol 21 (09) ◽  
pp. 581-588 ◽  
Author(s):  
Merlyn M. Thandu ◽  
Silvia Cavalli ◽  
Giada Rossi ◽  
Claudia B. Rizzardini ◽  
Daniele Goi ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pathogenic Bacteria ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Low Concentration ◽  
Gram Positive Bacteria

The present work describes the use of a magnetic porphyin (5-(4-carboxy-phenyl)-10,15,20-triphenyl-21H, 23H-porphyrin TPP) nanoconjugate (SPION-TPP) for destroying pathogenic bacteria followed by the recovery of the magnetic photosensitizer. SPION-TPP was tested for its activity against two different gram-positive bacterial strains (Staphylococcus aureus and Steptoccoccus mutans). It is observed that SPION-TPP at a very low concentration of 0.5 [Formula: see text]M is effective in destroying gram-positive bacteria (10[Formula: see text]–10[Formula: see text] CFU ml[Formula: see text] S. aureus with several orders reduction and few orders in S. mutans. The aim of this work is to combine photoactivity against microorganisms imparted by the photosensitizer with the possibility of recovering the nanoconstruct with magnets for disposal/reuse.

scholarly journals Anti-Inflammatory Comparison of Melatonin and Its Bromobenzoylamide Derivatives in Lipopolysaccharide (LPS)-Induced RAW 264.7 Cells and Croton Oil-Induced Mice Ear Edema

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4285
Author(s):  
Pimpichaya Sangchart ◽  
Panyada Panyatip ◽  
Teerasak Damrongrungruang ◽  
Aroonsri Priprem ◽  
Pramote Mahakunakorn ◽  
...  
Keyword(s):  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Dependent Manner ◽  
In Vivo Models ◽  
Raw 264.7 Macrophages ◽  
Ear Edema ◽  
Croton Oil ◽  
Anti Inflammatory

The pineal gland is a neuroendocrine organ that plays an important role in anti-inflammation through the hormone melatonin. The anti-inflammatory effects of melatonin and its derivatives have been reported in both in vitro and in vivo models. Our previous study reported the potent antioxidant and neuroprotective activities of bromobenzoylamide substituted melatonin. In silico analysis successfully predicted that melatonin bromobenzoylamid derivatives were protected from metabolism by CYP2A1, which is a key enzyme of the melatonin metabolism process. Therefore, the anti-inflammatory activities of melatonin and its bromobenzoylamide derivatives BBM and EBM were investigated in LPS-induced RAW 264.7 macrophages and croton oil-induced ear edema in mice. The experiments showed that BBM and EBM significantly reduced production of the inflammatory mediators interleukin-6 (IL-6), prostaglandin E2 (PGE2), and nitric oxide (NO) in a dose-dependent manner, but only slightly affected TNF-α in LPS-induced RAW 264.7 macrophages. This suggests that modifying melatonin at either the N1-position or the N-acetyl side chain affected production of NO, PGE2 and IL-6 in in vitro model. In the croton oil-induced mouse ear edema model, BBM, significantly decreased ear edema thickness at 2–4 h. It leads to conclude that bromobenzoylamide derivatives of melatonin may be one of the potential candidates for a new type of anti-inflammatory agent.

scholarly journals Anti-Inflammatory Property of the Ethanol Extract of the Root and Rhizome ofPogostemon cablin(Blanco) Benth

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Chu-Wen Li ◽  
Xiao-Li Wu ◽  
Xiao-Ning Zhao ◽  
Zu-Qing Su ◽  
Hai-Ming Chen ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Inflammatory Diseases ◽  
Ethanol Extract ◽  
Dependent Manner ◽  
Paw Edema ◽  
Ear Edema ◽  
Pogostemon Cablin ◽  
Mouse Ear ◽  
Anti Oxidant ◽  
Anti Inflammatory

The aim of this study was to investigate the anti-inflammatory property of the ethanol extract of the root and rhizome ofPogostemon cablin(ERP). The anti-inflammatory effect was evaluated using four animal models including xylene-induced mouse ear edema, acetic acid-induced mouse vascular permeability, carrageenan-induced mouse pleurisy, and carrageenan-induced mouse hind paw edema. Results indicated that oral administration of ERP (120, 240, and 480 mg/kg) significantly attenuated xylene-induced ear edema, decreased acetic acid-induced capillary permeability, inhibited carrageenan-induced neutrophils recruitment, and reduced carrageenan-induced paw edema, in a dose-dependent manner. Histopathologically, ERP (480 mg/kg) abated inflammatory response of the edema paw. Preliminary mechanism studies demonstrated that ERP decreased the level of MPO and MDA, increased the activities of anti-oxidant enzymes (SOD, GPx, and GRd), attenuated the productions of TNF-α, IL-1β, IL-6, PGE2and NO, and suppressed the activities of COX-2 and iNOS. This work demonstrates that ERP has considerable anti-inflammatory potential, which provided experimental evidences for the traditional application of the root and rhizome ofPogostemon cablinin inflammatory diseases.

scholarly journals Jasmine (Jasminum grandiflorum) Flower Extracts Ameliorate Tetradecanoylphorbol Acetate Induced Ear Edema in Mice

2020 ◽  
Vol 15 (4) ◽  
pp. 1934578X2091749
Author(s):  
Dongli Li ◽  
Xiaodan Tang ◽  
Chang Liu ◽  
Huifang Li ◽  
Shuzhen Li ◽  
...  
Keyword(s):  
Petroleum Ether Extract ◽  
Mouse Skin ◽  
Skin Inflammation ◽  
In Vitro Assays ◽  
Published Data ◽  
Ear Edema ◽  
Tetradecanoylphorbol Acetate ◽  
Mouse Ear ◽  
Anti Inflammatory

Published data from in vitro assays support the anti-inflammatory effects of jasmine ( Jasminum grandiflorum Linn.) but limited studies are reported in animal models. Herein, the anti-inflammatory effects of jasmine flower extracts (JFEs) including ethanol extract (JF-EE), petroleum ether extract (JF-PEE), ethyl acetate extract (JF-EAE), and n-butanol extract (JF-BE) were evaluated in a mouse ear edema model. Acute mouse ear skin inflammation was induced by tetradecanoylphorbol acetate (TPA; 125 µg/mL) and then treated with JFEs (100 mg/mL) or dexamethasone (DEX; 6.25 mg/mL; as a positive control). Jasmine flower extracts alleviated ear edema by reducing TPA-increased ear thickness and ear weight by 30.8% to 64.1% and 24.0% to 47.1%, respectively, whereas DEX showed comparable activity (by 71.8% and 49.1%, respectively). Their anti-inflammatory effects were supported by data from the immunohistochemical assays. Jasmine flower extracts reduced the inflammatory cells (from 5.5- to 9.5-fold) and the expressions of inflammation related enzymes including cyclooxygenase-2 and inhibitor of kappa-B kinase (from 1.9- to 2.8-fold and from 7.1- to 11.0-fold, respectively). Findings from this study showed that JFEs were able to ameliorate TPA-induced mouse skin inflammation. However, future studies on the underlying mechanisms of jasmine flower’s anti-inflammatory effects are warranted.

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