• Title/Summary/Keyword: inhibitory spectrum

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Sustained release of alginate hydrogel containing antimicrobial peptide Chol-37(F34-R) in vitro and its effect on wound healing in murine model of Pseudomonas aeruginosa infection

  • Shuaibing Shi;Hefan Dong;Xiaoyou Chen;Siqi Xu;Yue Song;Meiting Li;Zhiling Yan ;Xiaoli Wang ;Mingfu Niu ;Min Zhang;Chengshui Liao
    • Journal of Veterinary Science
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    • v.24 no.3
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    • pp.44.1-44.17
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    • 2023
  • Background: Antibiotic resistance is a significant public health concern around the globe. Antimicrobial peptides exhibit broad-spectrum and efficient antibacterial activity with an added advantage of low drug resistance. The higher water content and 3D network structure of the hydrogels are beneficial for maintaining antimicrobial peptide activity and help to prevent degradation. The antimicrobial peptide released from hydrogels also hasten the local wound healing by promoting epithelial tissue regeneration and granulation tissue formation. Objective: This study aimed at developing sodium alginate based hydrogel loaded with a novel antimicrobial peptide Chol-37(F34-R) and to investigate the characteristics in vitro and in vivo as an alternative antibacterial wound dressing to treat infectious wounds. Methods: Hydrogels were developed and optimized by varying the concentrations of crosslinkers and subjected to various characterization tests like cross-sectional morphology, swelling index, percent water contents, water retention ratio, drug release and antibacterial activity in vitro, and Pseudomonas aeruginosa infected wound mice model in vivo. Results: The results indicated that the hydrogel C proved superior in terms of cross-sectional morphology having uniformly sized interconnected pores, a good swelling index, with the capacity to retain a higher quantity of water. Furthermore, the optimized hydrogel has been found to exert a significant antimicrobial activity against bacteria and was also found to prevent bacterial infiltration into the wound site due to forming an impermeable barrier between the wound bed and external environment. The optimized hydrogel was found to significantly hasten skin regeneration in animal models when compared to other treatments in addition to strong inhibitory effect on the release of pro-inflammatory cytokines (interleukin-1β and tumor necrosis factor-α). Conclusions: Our results suggest that sodium alginate -based hydrogels loaded with Chol-37(F34-R) hold the potential to be used as an alternative to conventional antibiotics in treating infectious skin wounds.

Anti-inflammatory Effect of Myricetin from Rhododendron mucronulatum Turcz. Flowers in Lipopolysaccharide-stimulated Raw 264.7 Cells (Lipopolysaccharide로 유도된 Raw264.7 cell에서 Rhododendron mucronulatum Turcz. Flower으로부터 분리한 myricetin에 의한 염증 억제효과)

  • Choi, Moo-Young;Hong, Shin-Hyup;Cho, Jun-Hyo;Park, Hye-Jin;Jo, Jae-Bum;Lee, Jae-Eun;Kim, Dong-Hee;Kim, Byung-Oh;Cho, Young-Je
    • Journal of Life Science
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    • v.26 no.11
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    • pp.1245-1252
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    • 2016
  • As a research of inflammation inhibitory activity using natural resource, the inflammation inhibitory activity by purified active compound from Rhododendron mucronulatum flower was experimented. Rhododendron mucronulatum flower components were purified and separated with Sephadex LH-20 and MCI gel CHP-20 column chromatography, Purified compound was confirmed as myricetin by $^1H-NMR$, $^{13}C-NMR$ and Fast atom bombardment (FAB)-Mass spectrum to have inhibition activity on inflammatory factors secreted by Raw 264.7 cells in response to lipopolysaccharide stimulation. Myricetin inhibited nitric oxide (NO) expression in a concentration dependent manner, approximately 40% inhibition was observed at a concentration of $50{\mu}M$. The inhibition effect of myricetin on inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 protein expression was 20% and 80%, respectively, at a concentration of $25{\mu}M$. Myricetin also inhibited expression of the inflammatory cytokines, tumor necrosis factor $(TNF)-{\alpha}$, interleukin $(IL)-1{\beta}$, IL-6 and prostaglandin $E_2(PGE_2)$ in a concentration dependent manner; a concentration of $50{\mu}M$, 70%, 80%, 80% and 95% inhibition was observed, respectively. Therefore myricetin isolated from Rhododendron mucronulatum flowers is expected to have an anti-inflammatory effect in Raw 264.7 cell induced by lipopolysaccharides. The results can be expected myricetin from Rhododendron mucronulatum flower to use as functional resource for anti-inflammatory activity.

Inhibitory Effects of Dropwort (Oenanthe javanica) Extracts on Memory Impairment and Oxidative Stress and the Qualitative Analysis of Isorhamnetin in the Extracts (미나리 추출물의 기억력 손상 억제와 산화스트레스 억제 효과 및 Isorhamnetin 분석)

  • Won, Beom Young;Shin, Ki Young;Ha, Hyun Jee;Wee, Ji-Hyang;Yun, Yeo Sang;Kim, Ye Ri;Park, Yong Jin;Jung, Kyoung Ok;Sung, Hea Mi;Lee, Hyung Gun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.1
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    • pp.1-11
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    • 2016
  • This study was conducted to investigate effect of the acetylcholinesterase inhibitor activity, the protective effect of the extract on SH-SY5Y cell death by $H_2O_2$, the memory improvement from scopolamine-induced rat. Moreover, the antioxidant activity of isorhamnetin from the dropwort (Oenanthe javanica) was investigated. Acetylcholinesterase inhibitor activity was highest (28.59%) in Hwasun O. javanica extract (H-OJE). H-OJE and Naju O. javanica extract (N-OJE) were not significantly different. SH-SY5Y cell death deceased to 37.23% and 36.68% for H-OJE and N-OJE, respectively, following treatment with the extracts. O. javanica extracts showed a protective effect against $H_2O_2$-induced neurotoxicity. Treatment with O. javanica extracts slightly improved scopolamine-induced (1 mg/kg, i.p.) memory impairment in rats. H-OJE contained the highest total phenolic and flavonoid contents of 117 mg/g and 30 mg gallic acid equivalents/g, respectively, and had a DPPH radical scavenging activity ($SC_{50}$) of $113.8{\mu}g/mL$ and ABTS radical scavenging activity of $48.2{\mu}g/mL$, which was higher than the other extracts. The thiobarbituric acid reactive substances value was highest (50.2%) in H-OJE. Antioxidant activity differed significantly among dropwort extracts. Isorhamnetin was known as one of the flavonoid and for having neuroprotective effect. So we analyzed acid-hydrolyzed O. javanica extract HPLC. The results were that peak at 14 min and spectrum of the extracts was consistent with standard solution. The results of LC/MS/MS analysis were that the extract and standard solution were confirmed total ion chromatogram at identical time, precursor ion was 317 $[M-H]^+$ m/z, product ion was 302 $[M-H]^+$ m/z. Overall, the results showed that the dropwort extract led to memory improvement and had antioxidant activity. Based on these finding, further research to investigate the production of ethanol extract of dropwort as a processed food is warranted.

Transfer of Genes for Antimicrobial Resistance and Toxin of Hemolytic Escherichia coli Isolated from Feces of Pig Suffering Diarrhea to Human Isolates (설사 증상의 돼지 분변에서 분리된 용혈성 대장균의 항생제 내성과 독소의 인체로부터 분리된 균주로의 전이)

  • Lee Kyenam;Jung Byeong Yeal;Lee Yeonhee
    • Korean Journal of Microbiology
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    • v.40 no.4
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    • pp.286-294
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    • 2004
  • Between 1997 and 1998 in Korea, 56 isolates of Escherichia coli were obtained from pig suffering diarrhea. Among those, 38 isolates that showed the hemolytic activity, antimicrobial resistance, and toxin production were studied. Among 38 isolates, thirty-six isolates $(94.7\%)$ were resistant to tetracycline, 27 isolates $(71.0\%)$ were resistant to ampicillin, 26 isolates $(68.4\%)$ were resistant to chloramphenicol, and 21 isolates $(55.2\%)$ were resistant to trimethoprim, while none was resistant to aztreonam, amikacin, and norfloxacin. Among these iso­lates, 21 isolates $(55.3\%)$ were multiple drug resistant to at least four different class antimicrobial agents. Extended spectrum $\beta-lactamase$ producing isolates were not detected in the double disk synergy test. In these hemolytic Escherichia coli, heat-stable enterotoxin $(89.5\%)$ was the most prevalent toxin, followed by vero­toxins $(47.4\%),$ and then heat-labile enterotoxin $(31.6\%).$ Except 8 isolates $(21.0\%)$ which produced ST only, 12 isolates $(31.6\%)$ produced ST and LT, 13 isolates $(34.2\%)$ produced ST, VT, and VTe, and 5 isolates $(13.2\%)$ produced VT and VTe. However, none produced all 4 types of toxin, simultaneously. The predominant serotype could not be determined by the agglutination method. Sixteen isolates $(42.1\%)$ were strongly adhered to T-24 bladder cell and 17 isolates $(44.7\%)$ were to Caco-2 intestinal cell. Especially, 11 strains $(28.9\%)$ were evaluated as strongly adhesive to both T-24 cells and Caco-2 cells. Genes for toxin and the antimicrobial resistance were transferred to clinical isolates of Escherichia coli from human urine by the filter mating method. Results suggest the possibility that antimicrobial resistance and toxin can be transferred from animals to humans by direct con­tact of resistant bacteria as well as gene transfer, although there was no correlation between toxin production, adherent activity, and antimicrobial resistance among hemolytic E. coli isolated from pig suffering diarrhea.

Synthesis, Spectroscopic, and Biological Studies of Chromium(III), Manganese(II), Iron(III), Cobalt(II), Nickel(II), Copper(II), Ruthenium(III), and Zirconyl(II) Complexes of N1,N2-Bis(3-((3-hydroxynaphthalen-2-yl)methylene-amino)propyl)phthalamide (N1,N2-bis(3-((3-hydroxynaphthalen-2-yl)methylene-amino)propyl)phthalamide의 크롬(III), 망간(II), 철(III), 코발트(II), 니켈(II), 구리(II), 루테늄(III) 및 산화 지르코늄(II) 착물에 대한 합성과 분광학 및 생물학적 연구)

  • Al-Hakimi, Ahmed N.;Shakdofa, Mohamad M.E.;El-Seidy, Ahemd M.A.;El-Tabl, Abdou S.
    • Journal of the Korean Chemical Society
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    • v.55 no.3
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    • pp.418-429
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    • 2011
  • Novel chromium(III), manganese(II), iron(III), cobalt(II), nickel(II), copper(II), ruthenium(III), and zirconyl(II) complexes of $N^1,N^2$-bis(3-((3-hydroxynaphthalen-2-yl)methylene-amino)propyl)phthalamide ($H_4L$, 1) have been synthesized and characterized by elemental, physical, and spectral analyses. The spectral data showed that the ligand behaves as either neutral tridentate ligand as in complexes 2-5 with the general formula $[H_4LMX_2(H_2O)]{\cdot}nH_2O$ (M=Cu(II), Ni(II), Co(II), X = Cl or $NO_3$), neutral hexadentate ligand as in complexes 10-12 with the general formula $[H_4LM_2Cl_6]{\cdot}nH_2O$ (M=Fe(III), Cr(III) or Ru(III)), or dibasic hexadentate ligand as in complexes 6-9 with the general formula $[H_2LM_2Cl_2(H_2O)_4]{\cdot}nH_2O$ (M = Cu(II), Ni(II), Co(II) or Mn(II), and 13 with general formula $[H_4L(ZrO)_2Cl_2]{\cdot}8H_2O$. Molar conductance in DMF solution indicated the non-ionic nature of the complexes. The ESR spectra of solid copper(II) complexes 2, 5, and 6 showed $g_{\parallel}$ >g> $g_e$, indicating distorted octahedral structure and the presence of the unpaired electron in the $N^1,N^2$ orbital with significant covalent bond character. For the dimeric copper(II) complex $[H_2LCu_2Cl_2(H_2O)_4]{\cdot}3H_2O$ (6), the distance between the two copper centers was calculated using field zero splitting parameter for the parallel component that was estimated from the ESR spectrum. The antibacterial and antifungal activities of the compounds showed that, some of metal complexes exhibited a greater inhibitory effect than standard drug as tetracycline (bacteria) and Amphotricene B (fungi).

Antibacterial Effect of Cinnamon (Cinnamomum cassia) Bark Extract against Fish Pathogenic Bacteria (계피 추출물의 어류 질병 세균에 대한 항균 효과)

  • MOK Jong-Soo;SONG Ki-Cheol;CHOI Nack-Joong;YANG Ho-Shik
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.34 no.5
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    • pp.545-549
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    • 2001
  • To develop a natural antibacterial agent for fish bacterial diseases, antibacterial activity, minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and bactericidal effect of cinnamon bark extract were examined against fish pathogenic bacteria. The antimicrobial effect of the extract to the fish diet was also estimated, Cinnamon bark extract showed the broad spectrum of antibacterial activity against fish pathogenic bacteria, especially, it had strong activity against Streptococcus iniae, Edwardsiella tarda and Listonella anguillarum. Its MIC was $75.8\sim189.6{\mu}g/mL$ against Cram positive bacteria, and $75.8\sim113.8{\mu}g/mL$ against Gram negative bacteria in liquid medium, It was found to show stronger bactericidal action against Gram negative bacteria than Cram positive bacteria. According to increasing concentrations of the extract, it resulted in a proportional reduction of viable cell counts of both S. iniae and L. anguillarum. The former was not detected by addition of $189.6{\mu}g/mL$ after 12 hours incubation and the latter by addition of $151.6{\mu}g/mL$ after 24 hours incubation, respectively. It was reasonable that fish diet was soaked in cinnamon bark extract for ten minutes. The relationship formula between the weight of fish diet and the extract absorbed to fish diet was Y=7.2726X+4.5083 ($R^2=0.9998$). The fish diet soaked in the extract inhibited the growth of all strains used in this study. Its antibacterial activity was stable at the range from $10^{\circ}C\;to\;35^{\circ}C$ during the storage period of 28 days. When the diet soaked in the extract was incubated in liquid medium at $35^{\circ}C$, it inhibited the growth of microorganisms inhabited in the diet.

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Synergistic action of pesticide mixtures using glutathione-s-transferase- and esterase-inhibiting properties in diamondback moth (Plutella xylostella L.) (Glutathione-S-transferase와 esterase 효소 저해특성을 이용한 농약의 혼합 상승효과)

  • Yu, Yong-Man;Hong, S.S.;Kim, S.;Hur, J.H.
    • The Korean Journal of Pesticide Science
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    • v.7 no.1
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    • pp.38-44
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    • 2003
  • In vitro inhibitory activity of 34 insecticides and 31 fungicides to glutathione-S-transferase and esterases extracted from rats was determined. Of tested pesticides, the pesticides with high activity on both detoxifying enzymes were mixed with pesticides that are known to be detoxified by detoxifying enzymes. Glutathione-S-transferase was inhibited by thiodicarb $(I_{50}:1.87\times10^{-4}M)$, thiocyclam $(7.40\times10^{-4}M)$, dithianon $(7.55\times10^{-5}M)$, and tolylfluanide $(8.66\times10^{-5}M)$, while esterases by dichlorvos $(8.95\times10^{-8}M)$, pirimicarb $(2.74\times10^{-6}M)$, pyrazophos $(3.31\times10^{-5}M)$, and benomyl $(4.96\times10^{-5}M)$. After acephate known to be detoxified by glutathione-S-transferase was mixed with glutathione-S-transferase-inhibiting pesticides and phenthoate known to be detoxified by esterases was mixed with esterases-inhibiting pesticides, insecticidal activities of such mixtures were determined against diamondback moth (PlutelLa xylostella L.). Synergistic action was observed in all pesticide combinations. The highest synergistic action was obtained when phenthoate was combined with dichlorvos, showing that co-toxicity coefficients were 1512 and 1877 after 24 and 48 hours of treatment, respectively. Several other combinations of pesticides, such as phenthoate with benomyl, and acephate with dithianon, also showed synergism, showing that their co-toxicity coefficients were about 1,000 and 500, after 24 hours of treatment, respectively. Our results showed that combinations of pesticides inhibited by detoxifying enzymes and ones detoxified by detoxifying enzymes resulted in increased toxicities of pesticides, suggesting that such combinations could be used to develop pesticide mixtures with more broad spectrum and high effectiveness.