Broad-spectrum Bactericide Research Articles

Synthesis and Antibacterial Activity of PCMX Derivative

Abstract: Para Chloro Meta Xylenol (PCMX) is an exceptionally broad spectrum bactericide and preservative with a long established and proven use in controlling bacteria, mildew and fungal growth in a wide range of applications (medical, domestic and industrial). Chloroxylenol, also known as para chloro meta xylenol, is an antiseptic and disinfectant which is used for skin disinfection and cleaning surgical instruments. It is also used within a number of household disinfectants and wound cleaners. Their analogues viz. hybrid / ester molecules also possess various biological activities which prompted us to synthesize a novel analogue for their future application as bioactive molecule. The synthesized compound was characterized by IR, 1HNMR, mass spectral data, elemental analysis and screened for its potential antibacterial activity against Gram positive and Gram negative bacteria. It shows a promising antibacterial activity.

Immunotoxicity induced by triclocarban exposure in zebrafish triggering the risk of pancreatic cancer

Owing to frequent application as a broad-spectrum bactericide, triclocarban (TCC) exposure has raised great concern for aquatic organisms and human health. Herein, based on transcriptome sequencing data analysis of zebrafish, we confirmed that TCC induced oxidative stress and dysimmunity through transcriptional regulation of the related genes. With aid of the Cancer Genome Atlas (TCGA) assembler database, 52 common differentially expressed genes, whose functions were related to immunity, were screened out by virtue of the meta-analysis of pancreatic cancer sample data and differential transcription profiles from TCC-exposed larvae. Acute TCC exposure affected formation of the innate immune cells, delayed mature thymic T-cell development, reduced immunoglobulin M (IgM) levels and promoted excessive release of the pro-inflammatory factors (IL-6, IL-1β and tnfα). Under TCC exposure, the expressions of the genes associated with immune cell abundance in pancreatic cancer were significantly down-regulated, while the levels of ROS were prominently increased in concomitant with suppressed antioxidant activity. Moreover, a series of marker genes (pi3k, nrf2, keap1, ho-1 and nqo1) in the PI3K/Nrf2 antioxidant-stress pathway were abnormally expressed under TCC exposure. Interestingly, vitamin C decreased the malformation and increased the survival rate of 120-hpf larvae and effectively alleviated TCC-induced oxidative stress and immune responses. Overall, TCC exposure induced immunotoxicity and increased the risk of pancreatic cancer by inhibiting the antioxidant capacity of the PI3K/Nrf2 signal pathway. These observations enrich our in-depth understanding of the effects of TCC on early embryonic-larval development and immune damage in zebrafish.

A win-win scenario for antibacterial activity and skin mildness of cationic surfactants based on the modulation of host-guest supramolecular conformation

The commercial cationic surfactants (CSAa) with quaternary ammonium (QA) groups have proved to be broad-spectrum bactericide against bacteria, fungi, and viruses. Nevertheless, they inevitably exhibit potent irritation on the skin. In this work, we systematically investigated the regulatory mechanism of the host-guest supramolecular conformation with β-cyclodextrin (β-CD) on the bactericidal performance and skin irritation of CSAa with different head groups and chain lengths. When the ratio of incorporated β-CD is not greater than 1:1, the bactericidal efficiency of CSAa@β-CD (n > 12) remained above 90 % due to the free QA groups and hydrophobic fraction that can act on negatively charged bacterial membranes. And once the ratio of β-CD exceeded 1:1, the β-CD attracted to the bacterial surface by hydrogen bonding might prevent CSAa@β-CD from acting on bacteria, resulting in a decrement in antibacterial performance. Even so, the antibacterial activity of CSAa with long alkyl chains (n = 16, 18) was independent from the complexation of β-CD. Accordingly, both the zein solubilization assay and the neutrophil migration assay on zebrafish skin evidenced that β-CD attenuated the interaction of surfactant with skin model proteins and the inflammatory effect on zebrafish, thereby enhancing skin mildness. In this way, we hope to create a simple but effective brainpower using the host-guest approach to guarantee both bactericidal efficiency and skin mildness without modifying the chemical structure of these commercial biocides.

Ethylicin Inhibition of Xanthomonas oryzae pv. oryzicola In Vitro and In Vivo

Infestation of rice with the bacterium Xanthomonas oryzae pv. oryzicola (Xoc) causes the serious disease bacterial leaf streak (BLS). We studied the effect of ethylicin, a broad-spectrum bactericide, on Xoc both in vivo and in vitro. Ethylicin increases the defensive enzyme activities and defensive genes expression of rice. Ethylicin also significantly inhibited Xoc activity in vitro compared with other commercial bactericides. The half-maximal effective concentration (EC50) of ethylicin was 2.12 μg/mL. It has been shown that ethylicin can inhibit Xoc quorum sensing through the production of extracellular polysaccharides and enzymes, which disrupt the Xoc cell membrane. We used proteomic analysis to identify two oxidative phosphorylation pathway proteins (ACU12_RS13405 and ACU12_RS13355) which affected the virulence of Xoc and validated them using quantitative real-time polymerase chain reaction (qRT-PCR). The results indicate that ethylicin can increase the defense responses of rice and control Xoc proliferation.

Study on the toxic-mechanism of triclosan chronic exposure to zebrafish (Danio rerio) based on gut-brain axis

Triclosan (TCS), as a broad-spectrum bactericide, is extensively used in the fine chemical and textile industries. It is recognized as a new type of environmental endocrine disruptor with frequent detection and environmental pollution. However, the toxicity mechanism regarding neurodevelopment and neurobehavior remains unclear. This study is intended to explore the underlying toxic mechanism of TCS based on gut-brain axis. TCS-chronic exposure affected the development of zebrafish, induced feminization, obesity physical signs and abnormal organ index and caused neurobehavioral abnormalities by inhibiting both neurotransmitter acetylcholinesterase and dopamine activity, promoting brain neuron apoptosis and accelerating diencephalic lesions. Meanwhile, TCS-chronic exposure led to gut microbiota dysbiosis and decreased diversity, such as increased pathogenic bacteria and decreased probiotics in adult zebrafish gut, which caused many pathological damages, including partial shedding and ablation of intestinal villi, inflammatory infiltration, thinning of intestinal wall, and increased goblet cell in villus. Based on the communication between intestinal peripheral nerves and CNS, the above histopathological injuries and disorders were well underpinned and illustrated by the changes of biomarkers and the expression of related marker genes in the gut-brain axis. Additionally, short-chain fatty acids (SCFA), as the regulators of intestinal sympathetic nerve activation, are also secreting products of intestinal microflora and play a crucial role in regulating the balance of intestinal flora and protecting intestinal homeostasis. SCFA in low doses can effectively alleviate and rescue the toxic effects under TCS exposure, which evidenced that TCS exerted systemic toxic effects on the gut-brain axis by influencing the composition and diversity of gut flora in zebrafish, and fully demonstrated the interaction effect between intestine and brain. Hence, these findings contribute to the understanding, prevention, and diagnosis of endocrine disrupting diseases caused by environmental pollutants from the perspective of the gut-brain axis, and strengthening the early warning, management and control of TCS pollution.

Synthesis, Antibacterial and Insecticidal Activities of Novel Capsaicin Derivatives Containing a Sulfonic Acid Esters Moiety.

In order to develop an efficient and broad-spectrum bactericide, a series of novel capsaicin derivatives containing a sulfonic acid esters moiety was synthesized. The structure of these compounds were confirmed by nuclear magnetic resonance spectroscopy (NMR) and high-resolution mass spectrum (HRMS). The results of the bioactivities revealed that some target compounds exhibited remarkable antibacterial activity. Compound 3b exhibited the highest activities against Pseudomonas syringae pv. actinidiae (Psa), Xanthomonas oryzae pv. oryzae (Xoo), and Xanthomonas axonopodis pv. citri (Xac), and the values were 86, 54, and 92% at 50 μg/ml, respectively, which were higher than were for thiodiazole copper (87, 34, and 77%) and bismerthiazol (87, 37 and 75%). Although some compounds also showed certain activity against Spodoptera frugiperda, it was weaker than the positive controls monosultap and mulfoxaflor. Thus, the bioassay results recommend that these newly designed and synthesized scaffolds should be used as a bactericide lead compound rather than an insecticide lead compound.

The effect of acidic pH on the adsorption and lytic activity of the peptides Polybia-MP1 and its histidine-containing analog in anionic lipid membrane: a biophysical study by molecular dynamics and spectroscopy.

Antimicrobial peptides (AMPs) are part of the innate immune system of many species. AMPs are short sequences rich in charged and non-polar residues. They act on the lipid phase of the plasma membrane without requiring membrane receptors. Polybia-MP1 (MP1), extracted from a native wasp, is a broad-spectrum bactericide, an inhibitor of cancer cell proliferation being non-hemolytic and non-cytotoxic. MP1 mechanism of action and its adsorption mode is not yet completely known. Its adsorption to lipid bilayer and lytic activity is most likely dependent on the ionization state of its two acidic and three basic residues and consequently on the bulk pH. Here we investigated the effect of bulk acidic (pH 5.5) and neutral pH (7.4) solution on the adsorption, insertion, and lytic activity of MP1 and its analog H-MP1 to anionic (7POPC:3POPG) model membrane. H-MP1 is a synthetic analog of MP1 with lysines replaced by histidines. Bulk pH changes could modulate this peptide efficiency. The combination of different experimental techniques and molecular dynamics (MD) simulations showed that the adsorption, insertion, and lytic activity of H-MP1 are highly sensitive to bulk pH in opposition to MP1. The atomistic details, provided by MD simulations, showed peptides contact their N-termini to the bilayer before the insertion and then lay parallel to the bilayer. Their hydrophobic faces inserted into the acyl chain phase disturb the lipid-packing.

Bacteria-specific phototoxic reactions triggered by blue light and phytochemical carvacrol

Development of alternatives to antibiotics is one of the top priorities in the battle against multidrug-resistant (MDR) bacterial infections. Here, we report that two naturally occurring nonantibiotic modalities, blue light and phytochemical carvacrol, synergistically kill an array of bacteria including their planktonic forms, mature biofilms, and persisters, irrespective of their antibiotic susceptibility. Combination but not single treatment completely or substantially cured acute and established biofilm-associated Acinetobacter baumannii and methicillin-resistant Staphylococcus aureus infections of full thickness murine third-degree burn wounds and rescued mice from lethal Pseudomonas aeruginosa skin wound infections. The combined therapy diminished bacterial colony-forming units as high as 7.5 log10 within 30 min and introduced few adverse events in the survival of cocultured mammalian cells, wound healing, or host DNA. Mechanistic studies revealed that carvacrol was photocatalytically oxidized into a series of photoreactive substrates that underwent photolysis or additional photosensitization reactions in response to the same blue light, forming two autoxidation cycles that interacted with each other resulting in robust generation of cytotoxic reactive oxygen species. This phototoxic reaction took place exclusively in bacteria, initiated by blue light excitation of endogenous porphyrin-like molecules abundantly produced in bacteria compared with mammalian cells. Moreover, no bacterial resistance developed to the combined treatment after 20 successive passages. This highly selective phototoxic reaction confers a unique strategy to combat the growing threat of MDR bacteria.

Co-effects of C/Ag dual ion implantation on enhancing antibacterial ability and biocompatibility of silicone rubber

Although silicone implants are the most popular choice around the world for breast augmentation, reconstruction, and revision, due to the poor antibacterial properties and limited biocompatibility of silicone rubber (SR), one of the major complications, capsule contracture, is a lingering problem. To overcome the two main shortcomings, a dual ion implantation technique was applied to modify the surface of SR with the basic skeleton element of organic matter, carbon (C) and the broad-spectrum bactericide, silver (Ag). We present surface characterization, toxicological effects, and evaluation of the mechanical, antibacterial and biocompatible properties of C and Ag co-implanted SR (C/Ag−SRs). After ion implantation, surface roughness and tensile strength of these new materials increased. Biotoxicity was fully assessed by in vitro experiments on human fibroblasts and in vivo experiments on rats, showing that the low-Ag groups met safety standards. Both the anti-bacterial adhesion and bactericidal abilities of C/Ag−SRs were superior to those of SR, which had few antibacterial activities, especially against Staphylococcus epidermidis. With respect to biocompatibility, the adhesion of fibroblasts was promoted, while their proliferation was moderately inhibited on ion-implanted surfaces. After subcutaneous implantation in rats for 7, 30, 90 and 180 d, the capsular thickness around C/Ag−SRs was significantly lower than that around the SR. Additionally, there was no difference in the inflammatory reaction after 7 d of retention in vivo between C/Ag−SRs and SR. The results demonstrate that C/Ag−SRs are desirable shell materials for breast implants.

Rapid destruction of triclosan by Iron(III)-Tetraamidomacrocyclic ligand/hydrogen peroxide system

Iron(III)-tetraamidomacrocyclic ligand (Fe(III)-TAML) activators can activate hydrogen peroxide to oxidize many kinds of organic pollutants. In this study, we investigated the degradation of triclosan, a widely used broad-spectrum bactericide, under the treatment of Fe(III)-TAML/H2O2 system at different pH conditions. We also studied the influence of natural organic matter (NOM) on the degradation process. Our results showed that complete removal of triclosan could be obtained within several minutes under the optimal conditions. The degradation of triclosan by Fe(III)-TAML/H2O2 system exhibited strong pH-dependence and the degradation rate increased with the increase in pH level from 7.0 to 10.0. When adding fulvic acid (FA) or humic acid (HA) in the reaction system, the degradation of triclosan could be suppressed slightly, and HA exhibited stronger inhibition than FA. Based on the analysis of reaction intermediates, phenoxyl radical reaction and ring open reaction were involved in the decomposition of triclosan. Significant inhibition of overall toxicity to Photobacterium phosphoreum further confirmed the high efficiency of Fe(III)-TAML/H2O2 system for the removal of antibiotic activities resulting from the parent triclosan molecule and its degradation products.

A 2D-2D heterojunction Bi2WO6/WS2-x as a broad-spectrum bactericide: Sulfur vacancies mediate the interface interactions between biology and nanomaterials

We report a heterojunction Bi2WO6/WS2-x with sulfur vacancies as a broad-spectrum bactericide to efficiently kill Gram-positive and Gram-negative bacteria in vitro and in vivo under visible-light irradiation. Sulfur vacancies in single-layer WS2 make the surface electron-rich. Integration of Bi2WO6 with WS2 enhances the photoelectric activity under visible-light irradiation. Sulfur vacancies promote the generation of radicals and the extraction of membrane phospholipids from bacterial cells. Density functional theory verifies that S vacancies strengthen the interactions between the Bi2WO6/WS2-x surface and H2O, enhancing the generation of ·OH. Two-dimensional correlation spectroscopy analysis reveals that perturbation of β-sheet proteins and formation of outer-sphere surface complexes contribute to the high antibacterial capacity. Bi2WO6/WS2-x accelerates the re-epithelialization and healing of infected wounds in an animal model. Uncommonly, Bi2WO6/WS2-x does not exhibit drug resistance and is biocompatible with human cells. Our results indicate that vacancy-functionalized heterojunctions are potentially promising antibacterial agents by regulating the interface interaction between biology and nanomaterials.

Triclosan treatment to pregnant albino rats affects offspring numbers and the liver of both the pregnant rats and their offspring, and these effects are ameliorated by co-treatment with bee honey.

We have assessed the effects of the broad-spectrum bactericide triclosan on the liver of pregnant albino rats and their offspring, and evaluated the protective potential of bee honey, which has radical-scavenging properties. The study involved treatment of 72 pregnant rats followed by examination of the pregnant rats and their offspring. The pregnant rats were divided equally into six groups (I-VI), each of which was subdivided equally into two Subgroups (A and B). Rats in the A subgroups were gavaged with a daily dose of 1.26 ml distilled water (IA), 1 ml corn oil (IIA), 1.68 ml aqueous solution of Clover Blossom honey (IIIA), 0.3 mg triclosan (IVA), 13 mg triclosan (VA), or 1.68 ml aqueous solution of honey with 13 mg triclosan (VIA), throughout pregnancy. Rats in the B subgroups received the same treatments throughout pregnancy and for 14 days after delivery. At the end of the experiments, the offspring's numbers were recorded and blood samples were taken from the pregnant rats for analysis. The livers of the studied groups were subjected for; histological study, morphometric analysis, and biochemical estimation of markers of oxidative stress. The results showed that the acceptable daily intake of triclosan did not induce significant pathological changes in the liver while high dose of triclosan induced pathological changes in the livers and reduced the numbers of offspring. Co-administration of honey with triclosan ameliorated most pathological change. Therefore, decrease the exposure of the pregnant women to triclosan is encouraged or co-supplementation with bee honey if exposure could not be avoided.

Loading and Sustained Release of Benzyl Ammonium Chloride (BAC) in Nano-Clays.

Benzyl ammonium chloride (BAC) is a broad-spectrum bactericide, but vulnerable to leaching by water. In this paper, halloysite nanotubes (HNT) and montmorillonite (MMT) were used as drug carriers to load BAC, in order to achieve good anti-mildew activity and long-term sustained release properties. The HNT and MMT nano-composites were characterized by transmission electron microscope (TEM), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), thermogravimetric analysis (TGA), and nitrogen adsorption/desorption. XRD results showed that BAC intercalated the interlayer of MMT, and expanded the interlayer spacing from 1.15 nm to 1.75 nm. Pore analysis showed that BAC decreased the cavity of halloysite nanotubes to a certain extent, which indicated that BAC loaded inside the lumen of HNT successfully. TG analysis showed that the loading capacity of MMT to BAC was higher than HNT. The accelerated-release experiments revealed both two clays have significant sustained-release effects on BAC, and the releasing rate of HNT was relatively lower. Both HNT and MMT have promising application prospects as sustained-release carriers. The inhibition test showed that BAC in nano-clay has good anti-mildew resistance performance.

Neo-5,22E-Cholestadienol Derivatives from Buthus martensii Karsch and Targeted Bactericidal Action Mechanisms

The discovery and search for new antimicrobial molecules from insects and animals that live in polluted environments is a very important step in the scientific search for solutions to the current problem of antibiotic resistance. Previously, we have reported that the secondary metabolite with the antibacterial action discovered in scorpion. The current study further isolated three new compounds from Buthus martensii karsch, while compounds 1 and 2 possessed 5,22E-cholestadienol derivatives whose structure demonstrated broad spectrum bactericide activities. To explore the antibacterial properties of these new compounds, the result shows that compound 2 inhibited bacterial growth of both S. aureus and P. aeruginosa in a bactericidal rather than a bacteriostatic manner (MBC/MIC ratio ≤ 2). Similarly, with compound 1, a ratio of MBC/MIC ≤ 2 indicates bactericidal activity inhibited bacterial growth of P. aeruginosa. Remarkably, this suggests that two compounds can be classified as bactericidal agents against broad spectrum bactericide activities for 5,22E-cholestadienol derivatives from Buthus martensii karsch. The structures of compounds 1–3 were established by comprehensive spectra analysis including two-dimensional nuclear magnetic resonance (2D-NMR) and high-resolution electrospray ionization-mass spectrometry (HRESI-MS) spectra. The antibacterial mechanism is the specific binding (various of bonding forces between molecules) using compound 1 or 2 as a ligand based on the different receptor proteins’—2XRL or 1Q23—active sites from bacterial ribosome unit A, and thus prevent the synthesis of bacterial proteins. This unique mechanism avoids the cross-resistance issues of other antibacterial drugs.

Lactobacillus crispatus as biomarker of the healthy vaginal tract.

Decades of research have shown that the lactobacilli inhabiting the human vagina are the first line of defense in the female urogenital and reproductive tracts. In healthy cervicovaginal microbiota, Lactobacillus crispatus is prevalent and beneficial with production of copious amounts of lactic acid potent broad spectrum bactericide virucide and immunomodulator. Future and preventic approaches may need to include probiotics, prebiotics also have the potential to optimize and restore the vaginal ecosystem.

Detection of difenoconazole pesticides in pak choi by surface-enhanced Raman scattering spectroscopy coupled with gold nanoparticles

Difenoconazole is a highly effective and broad-spectrum triazole bactericide pesticide and was generally applied to protect and cure foods such as vegetables and fruits.

Structural hybridization of three aminoglycoside antibiotics yields a potent broad-spectrum bactericide that eludes bacterial resistance enzymes

Systematically blending structural features from obsolete aminoglycosides gleaned from X-ray co-crystal models rendered a promising antibiotic inert to enzymatic modification.

Disinfection efficacy and mechanism of slightly acidic electrolyzed water on Staphylococcus aureus in pure culture

Slightly acidic electrolyzed water (SAEW), considered as a broad-spectrum and high-performance bactericide are increasingly applied in the food industry. However, its disinfection mechanism has not been completely elucidated. This study aims to examine the disinfection efficacy and mechanism of SAEW on Staphylococcus aureus, compared with that of sodium hypochlorite (NaClO) and hydrochloric acid (HCl). SAEW treatment significantly reduced S. aureus by 5.8 log CFU/mL in 1 min, while 3.26 and 2.73 log reductions were obtained with NaClO and HCl treatments, respectively. A series of biological changes including intracellular potassium leakage, TTC-dehydrogenase relative activity and bacterial ultrastructure destruction were studied following disinfection treatment of S. aureus. The results showed that SAEW decreased the relative activity of TTC-dehydrogenase by 65.84%. Comparing intracellular potassium leakage, the SAEW treatment caused a greater percent of protein leakage (108.34%) than the NaClO (18.75%) or HCl (0.84%) treatments. These results demonstrated the potent impact SAEW had on the permeability of cell membranes. In addition, the ranking of partly agglutinated cellular inclusion formation was HCl > SAEW > NaClO. It appeared that HCl, along with its low pH value, are responsible for most of the cytoplasmic disruptions. Overall, this study demonstrated that the disinfection mechanism of SAEW was disrupting the permeability of cell membrane and the cytoplasmic ultrastructures in S. aureus cells.

Silver as a Bactericidal Coating for Biomedical Implants

Infection is a potentially serious complication of orthopedic implant surgery. While true for elective surgery, the risk of infection is significantly higher in trauma cases. Silver has been known as a broad-spectrum bactericide for centuries. In this work, we evaluate the use of silver films as bactericidal coatings on titanium-based orthopedic implants. Silver film structure and adhesion properties are presented. The silver films demonstrate bactericidal properties for bacteria that land on the surface of the film, but do little to kill bacteria in a nearby zone. This inability to create a zone of inhibition suggests that pure silver is an inadequate bactericide for orthopedic implants inserted in the medullary canal but may be useful as a coating to prevent bacterial adhesion or colonization.

Effect of Triclosan on the Renal Cortex of Adult Male Albino Rats and the Possible Protective Role of Ellagic Acid: Histological and Biochemical Study

Background: Triclosan (TCS) is widely used broad spectrum bactericide. Ellagic acid (EA) has radical scavenging properties. Aim of the work: to assess the structure of the renal cortex after TCS administration and to determine the possible protective role of EA. Materials and Methods: Thirty adult male albino rats were divided into three groups; control group, TCS treated group: TCS was administered 200 mg/kg, once daily for six week, by oral gavages. TCS-EA treated group: received in the same doses of TCS and EA (30 mg/kg) for six weeks. Blood urea nitrogen (BUN), serum creatinine (Sc) and uric acids (UA) were measured. Renal cortex samples were processed for light and electron microscope examination. Results: Examination of TCS treated group revealed increased glomerular cellularity in some corpuscles. Podocytes showed effacement of the foot processes and focal thickening of the glomerular basement membrane. Some tubules showed marked cellular disorganization. Disoriented basal mitochondria, areas of rarified cytoplasm and electron-dense bodies were noticed. Intense positive caspase-3 reaction was expressed in the tubular cells. TCS-EA showed improvement of morphological organization of renal cortex glomeruli, proximal and distal tubules with moderately expressed caspase-3 in renal tubules Statistical analysis showed significant increase of BUN, SC and BUN in TCS treated group in comparison with the control group.Their levels in TCS-EA treated group showed a significant decrease in comparison with TCS treated group Conclusion: In conclusion, TCS leads to alterations in the histological structure and functions of renal cortex of albino rats and EA supplementation could protect from these changes.