scholarly journals Enhancing the antibacterial activity of antimicrobial peptide PMAP-37(F34-R) by cholesterol modification

2020 ◽  
Vol 16 (1) ◽  
Author(s):  
Liangliang Chen ◽  
Tengfei Shen ◽  
Yongqing Liu ◽  
Jiangfei Zhou ◽  
Shuaibing Shi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antimicrobial Peptide ◽  
Therapeutic Effect ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Therapeutic Effects ◽  
Microbial Infection ◽  
Cholesterol Modification

Abstract Background The problem of increasing resistance against conventional antibiotics has drawn people’s attention. Therefore, the development of novel antibacterial agents with effective and safe therapeutic effects is imminent. Antimicrobial peptides (AMPs) are considered a promising class of antibacterial agents due to their broad antibacterial spectrum. Results In this study, on the basis of our previously studied peptide PMAP-37(F34-R), a novel antimicrobial peptide Chol-37(F34-R) was developed by N-terminal cholesterol modification to increase hydrophobicity. We observed that the N-terminal cholesterol-modified Chol-37(F34-R) showed higher antimicrobial activity than PMAP-37(F34-R) in vitro. Chol-37(F34-R) also exhibited effective anti-biofilm activity and may kill bacteria by improving the permeability of their membranes. Chol-37(F34-R) exerted high stability in different pH, salt, serum, and boiling water environments. Chol-37(F34-R) also showed no hemolytic activity and substantially low toxicity. Furthermore, Chol-37(F34-R) exhibited good potency of bacteria eradication and promoted wound healing and abscess reduction in infected mice. Meanwhile, in S. aureus ATCC25923-infected peritonitis model, Chol-37(F34-R) exhibited an impressive therapeutic effect by reducing the decrease in systemic bacterial burden and alleviating organ damage. Conclusions Our findings suggested that the N-terminal cholesterol modification of PMAP-37(F34-R) could improve antibacterial activity. Chol-37(F34-R) displayed excellent bactericidal efficacy and impressive therapeutic effect in vivo. Thus, Chol-37(F34-R) may be a candidate for antimicrobial agents against microbial infection in the clinic.

scholarly journals In vitro antibacterial activity and in vivo therapeutic effect of Sesbania grandiflora in bacterial infected silkworms

2017 ◽  
Vol 55 (1) ◽  
pp. 1256-1262 ◽  
Author(s):  
Pimporn Anantaworasakul ◽  
Hiroshi Hamamoto ◽  
Kazuhisa Sekimizu ◽  
Siriporn Okonogi
Keyword(s):  
Antibacterial Activity ◽  
Therapeutic Effect ◽  
Sesbania Grandiflora ◽  
In Vitro Antibacterial Activity

scholarly journals Therapeutic Effects of Curcumin—From Traditional Past to Present and Future Clinical Applications

2019 ◽  
Vol 20 (15) ◽  
pp. 3757 ◽  
Author(s):  
Beatrice Bachmeier ◽  
Dieter Melchart
Keyword(s):  
Molecular Mechanisms ◽  
Malignant Tumors ◽  
Scientific Evidence ◽  
Treatment Strategies ◽  
Therapeutic Effects ◽  
Microbial Infection ◽  
Therapeutic Benefits ◽  
Novel Treatment Strategies

The efficacy of the plant-derived polyphenol curcumin, in various aspects of health and wellbeing, is matter of public interest. An internet search of the term “Curcumin” displays about 12 million hits. Among the multitudinous information presented on partly doubtful websites, there are reports attracting the reader with promises ranging from eternal youth to cures for incurable diseases. Unfortunately, many of these reports are not based on scientific evidence, but they feed the desideratum of the reader for a “miracle cure”. This circumstance makes it very difficult for researchers, who work in a scientifically sound and evidence-based manner on the therapeutic benefits (or side effects) of curcumin, to demarcate their results from sensational reports that circulate in the web and in other media. This is only one of many obstacles making it difficult to pave curcumin’s way into clinical application; others are its nonpatentability and low economic usability. A further impediment comes from scientists who never worked with curcumin or any other natural plant-derived compound in their own labs. They have never tested these compounds in any scientific assay, neither in vitro nor in vivo; however, they claim, in a sometimes polemic manner, that everything that has so far been published on curcumin’s molecular effects is based on artefacts. The here presented Special Issue comprises a collection of five scientifically sound articles and nine reviews reporting on the therapeutic benefits and the molecular mechanisms of curcumin or of chemically modified curcumin in various diseases ranging from malignant tumors to chronic diseases, microbial infection, and even neurodegenerative diseases. The excellent results of the scientific projects that underlie the five original papers give reason to hope that curcumin will be part of novel treatment strategies in the near future—either as monotherapy or in combination with other drugs or therapeutic applications.

scholarly journals Investigation of the Optimum Preparation of Peach Gum Polysaccharides and the In Vivo and In Vitro Therapeutic Effects on Acute Pyelonephritis

2019 ◽  
Vol 2019 ◽  
pp. 1-19
Author(s):  
Feifei Zhang ◽  
Jie Bai ◽  
Yao Zheng ◽  
Shuai Liang ◽  
Lei Lei ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Therapeutic Effect ◽  
Acute Pyelonephritis ◽  
Interleukin 2 ◽  
Urine Volume ◽  
Therapeutic Effects ◽  
Peach Gum

Background. Acute pyelonephritis (APN), known as stranguria in traditional Chinese medicine, is commonly treated with antibiotics. However, the rise in antibiotic resistance and the high rates of recurrence of APN make its treatment complicated, thus the development of alternative therapies is critical. Peach gum has long been recognized by traditional Chinese medicine as a food with medicinal value of relieving stranguria, but whether and how its primary constituent peach gum polysaccharides (PGPs) contribute to the diuretic function is still not clear. Purpose. The aim of this study was to investigate the optimum extraction process of PGPs and to evaluate its therapeutic effect on APN rats and to discover the underlying mechanism. Methods. In this study, surface design optimization was adopted to optimize the preparation of PGPs and HPLC and FT-IR spectra were used to evaluate the quality of PGPs; APN model rat was established by the Escherichia coli urinary tract infection method; the therapeutic effect and mechanism of PGPs on APN were determined by the visceral index, biochemical indicators, pathological section of the APN rat, and diuretic activity on mice and antibacterial activity in vitro. Results. Compared with an untreated APN group, the results showed that treatment with PGPs increased the APN-induced attenuation of secretory immunoglobulin A (sIgA) and creatinine clearance and decreased the APN-induced enhancement of the number of white blood cell (WBC), neutrophil counts (NC), bacteria load of the kidneys, kidney index, serum creatinine, urine volume, blood urea nitrogen (BUN), and interleukin-2 (IL-2) levels. The mechanism underlying these effects was further elucidated through in vitro experiments of the antibacterial and antiadhesion effects of PGPs. Conclusion. Due to the good therapeutic effects and advantages of PGPs, it could be considered as an alternative medicine to treat APN.

scholarly journals Shortened derivatives from native antimicrobial peptide LyeTx I: In vitro and in vivo biological activity assessment

2020 ◽  
pp. 153537022096696
Author(s):  
Leonardo Lima Fuscaldi ◽  
Joaquim Teixeira de Avelar Júnior ◽  
Daniel Moreira dos Santos ◽  
Daiane Boff ◽  
Vívian Louise Soares de Oliveira ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antimicrobial Peptide ◽  
Mammalian Cells ◽  
Antimicrobial Agents ◽  
Sodium Dodecyl ◽  
Alpha Helix ◽  
In Vitro Assays ◽  
Control Group

In the continuing search for novel antibiotics, antimicrobial peptides are promising molecules, due to different mechanisms of action compared to classic antibiotics and to their selectivity for interaction with microorganism cells rather than with mammalian cells. Previously, our research group has isolated the antimicrobial peptide LyeTx I from the venom of the spider Lycosa erythrognatha. Here, we proposed to synthesize three novel shortened derivatives from LyeTx I (LyeTx I mn; LyeTx I mnΔK; LyeTx I mnΔKAc) and to evaluate their toxicity and biological activity as potential antimicrobial agents. Peptides were synthetized by Fmoc strategy and circular dichroism analysis was performed, showing that the three novel shortened derivatives may present membranolytic activity, like the original LyeTx I, once they folded as an alpha helix in 2.2.2-trifluorethanol and sodium dodecyl sulfate. In vitro assays revealed that the shortened derivative LyeTx I mnΔK presents the best score between antimicrobial (↓ MIC) and hemolytic (↑ EC50) activities among the synthetized shortened derivatives, and LUHMES cell-based NeuriTox test showed that it is less neurotoxic than the original LyeTx I (EC50 [LyeTx I mnΔK] ⋙ EC50 [LyeTx I]). In vivo data, obtained in a mouse model of septic arthritis induced by Staphylococcus aureus, showed that LyeTx I mnΔK is able to reduce infection, as demonstrated by bacterial recovery assay (∼10-fold reduction) and scintigraphic imaging (less technetium-99m labeled-Ceftizoxime uptake by infectious site). Infection reduction led to inflammatory process and pain decreases, as shown by immune cells recruitment reduction and threshold nociception increment, when compared to positive control group. Therefore, among the three shortened peptide derivatives, LyeTx I mnΔK is the best candidate as antimicrobial agent, due to its smaller amino acid sequence and toxicity, and its greater biological activity.

scholarly journals Comparative Evaluation of Antibacterial Effects of Nanoparticle-Incorporated Orthodontic Primer: An In Vitro Study

2021 ◽  
pp. 030157422098818
Author(s):  
Cheepurupalli Meher Vineesha ◽  
D Praveen Kumar Varma ◽  
P Arun Bhupathi ◽  
CV Padma Priya ◽  
M Anoosha ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Antibacterial Effects ◽  
Disk Diffusion Method

Aim and Objectives: To compare and evaluate the antibacterial efficacy of various nanoparticles incorporated in orthodontic primer with that of conventional antimicrobial agents at different concentrations on Streptococcus mutans ( S. mutans) strain. Materials and Methods: Transbond XT Primer was mixed with 2.5% and 5% benzalkonium chloride (BAC), 0.2% and 2.5% chlorhexidine, 1% and 3% titanium dioxide (TiO2) nanoparticles, 0.2% and 0.5% nanohydroxyapatite, and 0.2% and 0.5% silica-doped nanohydroxyapatite powders. Antibacterial activity against S. mutans for all the materials was evaluated by the disk diffusion method for periods of 48 (T1) and 72 (T2) hours. Results: There was a significant increase in the antimicrobial activity of the orthodontic primer modified by the addition of antibacterial agents. The highest zone of inhibition against S. mutans was observed for silica-doped nanohydroxyapatite of 0.5% (11.03 mm) among all the nanoparticles, which was similar to the conventional antibacterial agents used in our study. Conclusions: • Among all the groups, BAC at 5% concentration showed the highest antimicrobial activity, and the least activity was exhibited by 1% TiO2 nanoparticles. • Silica-doped nanohydroxyapatite at 0.5% expressed the greatest antibacterial activity among all the nanoparticles. • All the materials showed sustained antibacterial activity even after 72 hours.

scholarly journals Nitric oxide for the prevention and treatment of viral, bacterial, protozoal and fungal infections

F1000Research ◽  
2021 ◽  
Vol 10 ◽  
pp. 536
Author(s):  
Philip M. Bath ◽  
Christopher M. Coleman ◽  
Adam L. Gordon ◽  
Wei Shen Lim ◽  
Andrew J. Webb
Keyword(s):  
Nitric Oxide ◽  
Fungal Infections ◽  
Post Exposure Prophylaxis ◽  
Therapeutic Effects ◽  
Microbial Infection ◽  
Phase Ii Trials ◽  
Inorganic Nitrate ◽  
Prevention And Treatment

Although the antimicrobial potential of nitric oxide (NO) is widely published, it is little used clinically. NO is a key signalling molecule modulating vascular, neuronal, inflammatory and immune responses. Endogenous antimicrobial activity is largely mediated by high local NO concentrations produced by cellular inducible nitric oxide synthase, and by derivative reactive nitrogen oxide species including peroxynitrite and S-nitrosothiols. NO may be taken as dietary substrate (inorganic nitrate, L-arginine), and therapeutically as gaseous NO, and transdermal, sublingual, oral, intranasal and intravenous nitrite or nitrate. Numerous preclinical studies have demonstrated that NO has generic static and cidal activities against viruses (including β-coronaviruses such as SARS-CoV-2), bacteria, protozoa and fungi/yeasts in vitro. Therapeutic effects have been seen in animal models in vivo, and phase II trials have demonstrated that NO donors can reduce microbial infection. Nevertheless, excess NO, as occurs in septic shock, is associated with increased morbidity and mortality. In view of the dose-dependent positive and negative effects of NO, safety and efficacy trials of NO and its donors are needed for assessing their role in the prevention and treatment of infections. Trials should test dietary inorganic nitrate for pre- or post-exposure prophylaxis and gaseous NO or oral, topical or intravenous nitrite and nitrate for treatment of mild-to-severe infections, including due to SARS-CoV-2 (COVID-19). This review summarises the evidence base from in vitro, in vivo and early phase clinical studies of NO activity in viral, bacterial, protozoal and fungal infections.

scholarly journals Nitric oxide for the prevention and treatment of viral, bacterial, protozoal and fungal infections

F1000Research ◽  
2021 ◽  
Vol 10 ◽  
pp. 536
Author(s):  
Philip M. Bath ◽  
Christopher M. Coleman ◽  
Adam L. Gordon ◽  
Wei Shen Lim ◽  
Andrew J. Webb
Keyword(s):  
Nitric Oxide ◽  
Fungal Infections ◽  
Post Exposure Prophylaxis ◽  
Therapeutic Effects ◽  
Microbial Infection ◽  
Phase Ii Trials ◽  
Inorganic Nitrate ◽  
Prevention And Treatment

Although the antimicrobial potential of nitric oxide (NO) is widely published, it is little used clinically. NO is a key signalling molecule modulating vascular, neuronal, inflammatory and immune responses. Endogenous antimicrobial activity is largely mediated by high local NO concentrations produced by cellular inducible nitric oxide synthase, and by derivative reactive nitrogen oxide species including peroxynitrite and S-nitrosothiols. NO may be taken as dietary substrate (inorganic nitrate, L-arginine), and therapeutically as gaseous NO, and transdermal, sublingual, oral, intranasal and intravenous nitrite or nitrate. Numerous preclinical studies have demonstrated that NO has generic static and cidal activities against viruses (including β-coronaviruses such as SARS-CoV-2), bacteria, protozoa and fungi/yeasts in vitro. Therapeutic effects have been seen in animal models in vivo, and phase II trials have demonstrated that NO donors can reduce microbial infection. Nevertheless, excess NO, as occurs in septic shock, is associated with increased morbidity and mortality. In view of the dose-dependent positive and negative effects of NO, safety and efficacy trials of NO and its donors are needed for assessing their role in the prevention and treatment of infections. Trials should test dietary inorganic nitrate for pre- or post-exposure prophylaxis and gaseous NO or oral, topical or intravenous nitrite and nitrate for treatment of mild-to-severe infections, including due to SARS-CoV-2 (COVID-19). This review summarises the evidence base from in vitro, in vivo and early phase clinical studies of NO activity in viral, bacterial, protozoal and fungal infections.

scholarly journals Syntheses and antibacterial activity of novel 6-fluoro-7-(gem-disubstituted piperazin-1-yl)-quinolines

1992 ◽  
Vol 70 (5) ◽  
pp. 1328-1337 ◽  
Author(s):  
Daniel T. W. Chu ◽  
Akiyo K. Claiborne ◽  
Jacob J. Clement ◽  
Jacob J. Plattner
Keyword(s):  
Antibacterial Activity ◽  
Chemical Synthesis ◽  
Antibacterial Agents ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Negative Organisms

A series of quinoline and naphthyridine antibacterial agents possessing an acyclic or cyclic gem-disubstituted piperazine substituent at the C-7 position have been prepared and evaluated in vitro and in vivo for antibacterial activity against a variety of Gram-positive and Gram-negative organisms. They are, however, not as active as quinolones or naphthyridines with a monosubstituted piperazine substituent at C-7. The chemical synthesis of these derivatives is also described.

scholarly journals Synthesis of copper sulfide nanoparticles and evaluation of in vitro antibacterial activity and in vivo therapeutic effect in bacteria-infected zebrafish

RSC Advances ◽  
2017 ◽  
Vol 7 (58) ◽  
pp. 36644-36652 ◽  
Author(s):  
Khan Behlol Ayaz Ahmed ◽  
Veerappan Anbazhagan
Keyword(s):  
Antibacterial Activity ◽  
Therapeutic Effect ◽  
Copper Sulfide ◽  
In Vitro Antibacterial Activity

Copper sulfide nanoparticles rescue bacteria infected zebrafish.

scholarly journals In Vitro and In Vivo Studies on the Antibacterial Activity and Safety of a New Antimicrobial Peptide Dermaseptin-AC

2021 ◽  
Author(s):  
Jiajia Chen ◽  
Doudou Hao ◽  
Kai Mei ◽  
Xin Li ◽  
Tingting Li ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Resistance ◽  
Antimicrobial Peptides ◽  
Antimicrobial Peptide ◽  
In Vivo Studies

In this study, we discovered a new antimicrobial peptide, Dermaseptin-AC, and studied its in vitro and in vivo antimicrobial activity. These studies provide some data for finding new antimicrobial peptides for overcoming antimicrobial resistance.

Sign in / Sign up

Export Citation Format

Share Document