scholarly journals Penaeidins, antimicrobial peptides with chitin-binding activity, are produced and stored in shrimp granulocytes and released after microbial challenge

2000 ◽  
Vol 113 (3) ◽  
pp. 461-469 ◽  
Author(s):  
D. Destoumieux ◽  
M. Munoz ◽  
C. Cosseau ◽  
J. Rodriguez ◽  
P. Bulet ◽  
...  
Keyword(s):  
Antimicrobial Peptides ◽  
Binding Activity ◽  
Penaeus Vannamei ◽  
Mrna Levels ◽  
Cytoplasmic Granules ◽  
Antibacterial And Antifungal Activities ◽  
New Family ◽  
Antibacterial And Antifungal ◽  
And Storage ◽  
Microbial Challenge

Penaeidins are members of a new family of antimicrobial peptides isolated from a crustacean, which present both Gram-positive antibacterial and antifungal activities. We have studied the localization of synthesis and storage of penaeidins in the shrimp Penaeus vannamei. The distribution of penaeidin transcripts and peptides in various tissues reveals that penaeidins are constitutively synthesized and stored in the shrimp haemocytes. It was shown by immunocytochemistry, at both optical and ultrastructural levels, that the peptides are localized in granulocyte cytoplasmic granules. The expression and localization of penaeidins were further analysed in shrimp subjected to microbial challenge. We found that (1) penaeidin mRNA levels decrease in circulating haemocytes in the first 3 hours following stimulation and (2) an increase in plasma penaeidin concentration occurs after microbial challenge, together with (3) a penaeidin immunoreactivity in cuticular tissue, which can be related to the chitin-binding activity we demonstrate here for penaeidins.

scholarly journals Transcriptional Regulation of β-Defensin Gene Expression in Tracheal Epithelial Cells

2000 ◽  
Vol 68 (1) ◽  
pp. 113-119 ◽  
Author(s):  
Gill Diamond ◽  
Vicki Kaiser ◽  
Janice Rhodes ◽  
John P. Russell ◽  
Charles L. Bevins
Keyword(s):  
Innate Immunity ◽  
Transcription Factors ◽  
Epithelial Cells ◽  
Antimicrobial Peptides ◽  
Binding Sites ◽  
Binding Activity ◽  
Mrna Levels ◽  
Tracheal Epithelial Cells ◽  
Tracheal Epithelial ◽  
Flanking Region

ABSTRACT Innate immunity provides an ever-present or rapidly inducible initial defense against microbial infection. Among the effector molecules of this defense in many species are broad-spectrum antimicrobial peptides. Tracheal antimicrobial peptide (TAP) was the first discovered member of the β-defensin family of mammalian antimicrobial peptides. TAP is expressed in the ciliated epithelium of the bovine trachea, and its mRNA levels are dramatically increased upon stimulation with bacteria or bacterial lipopolysaccharide (LPS). We report here that this induction by LPS is regulated at the level of transcription. Furthermore, the transfection of reporter gene constructs into tracheal epithelial cells indicates that DNA sequences in the 5′ flanking region of the TAP gene, within 324 nucleotides of the transcription start site, are responsible in part for mediating gene induction. This region includes consensus binding sites for NF-κB and nuclear factor interleukin-6 (NF IL-6) transcription factors. Gel mobility shift assays indicate that LPS induces NF-κB binding activity in the nuclei of these cells, while NF IL-6 binding activity is constitutively present. The gene encoding human β-defensin 2, a human homologue of TAP with similar inducible expression patterns in the airway, was cloned and found to have conserved NF-κB and NF IL-6 consensus binding sites in its 5′ flanking region. Previous studies of antimicrobial peptides from insects indicated that their induction by infectious microbes and microbial products also occurs via activation of NF-κB-like and NF IL-6-like transcription factors. Together, these observations indicate that a strategy for the induction of peptide-based antimicrobial innate immunity is conserved among evolutionarily diverse organisms.

scholarly journals The Broad-Spectrum Antiviral Potential of the Amphibian Peptide AR-23

2022 ◽  
Vol 23 (2) ◽  
pp. 883
Author(s):  
Annalisa Chianese ◽  
Carla Zannella ◽  
Alessandra Monti ◽  
Anna De Filippis ◽  
Nunzianna Doti ◽  
...  
Keyword(s):  
Antimicrobial Peptides ◽  
Broad Spectrum ◽  
Viral Infections ◽  
Antiviral Agents ◽  
World Population ◽  
Therapeutic Effects ◽  
Amphibian Skin ◽  
Antibacterial And Antifungal Activities ◽  
Dna And Rna ◽  
Antibacterial And Antifungal

Viral infections represent a serious threat to the world population and are becoming more frequent. The search and identification of broad-spectrum antiviral molecules is necessary to ensure new therapeutic options, since there is a limited availability of effective antiviral drugs able to eradicate viral infections, and consequently due to the increase of strains that are resistant to the most used drugs. Recently, several studies on antimicrobial peptides identified them as promising antiviral agents. In detail, amphibian skin secretions serve as a rich source of natural antimicrobial peptides. Their antibacterial and antifungal activities have been widely reported, but their exploitation as potential antiviral agents have yet to be fully investigated. In the present study, the antiviral activity of the peptide derived from the secretion of Rana tagoi, named AR-23, was evaluated against both DNA and RNA viruses, with or without envelope. Different assays were performed to identify in which step of the infectious cycle the peptide could act. AR-23 exhibited a greater inhibitory activity in the early stages of infection against both DNA (HSV-1) and RNA (MeV, HPIV-2, HCoV-229E, and SARS-CoV-2) enveloped viruses and, on the contrary, it was inactive against naked viruses (PV-1). Altogether, the results indicated AR-23 as a peptide with potential therapeutic effects against a wide variety of human viruses.

scholarly journals Identification and Characterization of Antimicrobial Peptides From Butterflies: An Integrated Bioinformatics and Experimental Study

2021 ◽  
Vol 12 ◽  
Author(s):  
Min Wang ◽  
Ziyue Zhou ◽  
Simin Li ◽  
Wei Zhu ◽  
Xianda Hu
Keyword(s):  
Antimicrobial Peptides ◽  
Therapeutic Potential ◽  
Biological Effects ◽  
Future Research ◽  
Nucleic Acid Binding ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Biophysical Changes

Butterflies represent one of the largest animal groups on Earth, yet antimicrobial peptides (AMPs) of this group are less studied in comparison with their moth counterparts. This study employed an integrated bioinformatics approach to survey natural AMPs from publicly available genomic datasets. Numerous AMPs, including cecropins, defensins, and moricins, were identified and subsequently used as templates for the design of a series of synthetic AMPs that mimicked the naturally occurring sequences. Despite differing biological effects among the various sequences, the synthetic AMPs exhibited potent antibacterial and antifungal activities in vitro and in vivo, without inducing hemolysis, which implied their therapeutic potential in infectious diseases. Electron and confocal fluorescence microscopies revealed that the AMPs induced distinct morphological and biophysical changes on microbial cell membranes and nuclei, suggesting that the antimicrobial effects were related to a mechanism of membrane penetration and nucleic acid binding by the peptides. In conclusion, this study not only offers insights into butterfly AMPs but also provides a practical strategy for high-throughput natural AMP discoveries that will have implications for future research in this area.

scholarly journals Microwave Assisted Synthesis of Novel 1,2,3,4-Tetrahydrocarbazolyl thiazolidin-4-ones and Azetidin-2-ones and its Biological Behavior

2009 ◽  
Vol 6 (s1) ◽  
pp. S374-S380 ◽  
Author(s):  
T. Surendiran ◽  
S. Balasubramanian ◽  
Sivaraj D.
Keyword(s):  
Elemental Analysis ◽  
Mass Spectra ◽  
Thioglycolic Acid ◽  
Biological Behavior ◽  
Microwave Assisted Synthesis ◽  
Antifungal Activities ◽  
Microwave Assisted ◽  
Antibacterial And Antifungal Activities ◽  
New Family ◽  
Antibacterial And Antifungal

A new family of 1,2,3,4 – tetrahydrocarbazolyl thiazolidin-4-ones(4a-e)and 1,2,3,4–tetrahydrocarbazolyl azetidin-2-ones(5a-e)were individually derived usingN-[(α-substituted bezylidenehydrazino) acetyl] -1,2,3,4-tetra-hydrocarbazoles3a-eby cyclization with thioglycolic acid and chloro- acetylchloride respectively. The compounds(3a-e)were prepared by condensation ofN-(hydrazinoacetyl) 1,2,3,4-tetrahydrocarbazole (2) with a series of aldehydes. The compound 2 was obtained by the hydrazinolysis ofN-(chloroacetyl)-1,2,3,4-tetrahydrocarbazole (1). These products were characterized by IR, NMR, MASS spectra and by elemental analysis. All the titled compounds(4a-e)and5(a-e)were screened for antibacterial and antifungal activities.

Synthesis, characterization and biological activities of 1,3,4-oxadiazole derivatives of nalidixic acid and their copper complexes

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Nalidixic Acid ◽  
Copper Complexes ◽  
Biological Activities ◽  
Bidentate Coordination ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Oxadiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Substituted 1

A series of novel 1, 3, 4-oxadiazole analogues was synthesized from cyclization of hydrazones of substituted 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carbohydrazides were prepared from nalidixic acid. The structures of synthesized oxadiazole derivatives and their copper complexes were elucidated on the basis of FTIR, elemental analyses, 1H-NMR and atomic absorption spectral analysis. It was observed from spectral data that metal ligand ratio was 1:1 in all copper complexes and they were bidentate, coordination was found to be done through oxygen of 4-oxo group and nitrogen of oxadiazole ring. The synthesized compounds were further evaluated with biological activities and compared with parent hydrazones. Copper complexes possess antibacterial and antifungal activities better than the oxadiazoles while they have better antioxidant activity then copper complexes. Parent hydrazones were better in all biological activities than synthesized oxadiazoles.

Substituted 4-Formyl-2H-chromen-2-ones: Their Reaction with N-(2,3,4,6-Tetra-Oacetyl- β-D-galactopyranosyl)thiosemicarbazide, Antibacterial and Antifungal Activity of Their Thiosemicarbazone Products

2020 ◽  
Vol 24 (19) ◽  
pp. 2272-2282
Author(s):  
Vu Ngoc Toan ◽  
Nguyen Minh Tri ◽  
Nguyen Dinh Thanh
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Selenium Dioxide ◽  
Antibacterial And Antifungal Activity ◽  
E Coli ◽  
Antibacterial And Antifungal Activities ◽  
Alkyl Ethers ◽  
Antibacterial And Antifungal

Several 6- and 7-alkoxy-2-oxo-2H-chromene-4-carbaldehydes were prepared from corresponding alkyl ethers of 6- and 7-hydroxy-4-methyl-2-oxo-2H-chromen-2-ones by oxidation using selenium dioxide. 6- and 7-Alkoxy-4-methyl-2H-chromenes were obtained with yields of 57-85%. Corresponding 4-carbaldehyde derivatives were prepared with yields of 41-67%. Thiosemicarbazones of these aldehydes with D-galactose moiety were synthesized by reaction of these aldehydes with N-(2,3,4,6-tetra-O-acetyl-β-Dgalactopyranosyl) thiosemicarbazide with yields of 62-74%. These thiosemicarbazones were screened for their antibacterial and antifungal activities in vitro against bacteria, such as Staphylococcus aureus, Escherichia coli, and fungi, such as Aspergillus niger, Candida albicans. Several compounds exhibited strong inhibitory activity with MIC values of 0.78- 1.56 μM, including 8a (against S. aureus, E. coli, and C. albicans), 8d (against E. coli and A. niger), 9a (against S. aureus), and 9c (against S. aureus and C. albicans).

Synthesis & Anticancer Evaluation of New Substituted 2-(3,4- Dimethoxyphenyl)benzazoles

2019 ◽  
Vol 15 (3) ◽  
pp. 287-297 ◽  
Author(s):  
Cigdem Karaaslan ◽  
Yalcin Duydu ◽  
Aylin Ustundag ◽  
Can O. Yalcin ◽  
Banu Kaskatepe ◽  
...  
Keyword(s):  
Hela Cells ◽  
Parp Inhibitor ◽  
A549 Cells ◽  
Human Tumor ◽  
Antimicrobial Activities ◽  
Sodium Metabisulfite ◽  
Human Tumor Cell Lines ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Mitotic Inhibitor

Background: The benzazole nucleus is found in many promising small molecules such as anticancer and antibacterial agents. Bendamustine (Alkylating agent), Nocodazole (Mitotic inhibitor), Veliparib (PARP inhibitor), and Glasdegib (SMO inhibitor) are being clinically used as anticancer therapeutic which bear benzimidazole moiety. Based on the principle of bioisosterism, in the present work, 23 compounds belonging to 2-(3,4-dimethoxyphenyl)benzazoles and imidazopyridine series were synthesized and evaluated for their anticancer and antimicrobial activities. Objective: A series of new 2-(3,4-dimethoxyphenyl)-1H-benz(or pyrido)azoles were synthesized and evaluated for their anticancer and antimicrobial activities. Method: N-(5-chloro-2-hdroxyphenyl)-3,4-dimethoxybenzamide 1, was obtained by the amidation of 2-hydroxy-5-chloroaniline with 3,4-dimethoxybenzoic acid by using 1,1&'-carbonyldiimidazole. Cyclization of 1 to benzoxazole derivative 2, was achieved by p-toluenesulfonic acid. Other 1H-benz(or pyrido)azoles were prepared by the reaction between 2-aminothiophenol, ophenylenediamine, o-pyridinediamine with sodium metabisulfite adduct of 3,4-dimethoxybenzaldehyde. The NMR assignments of the dimethoxy groups were established by the NOESY spectra. Results: Compound 12, bearing two chlorine atoms at the 5(4) and 7(6) positions of the benzene moiety of benzimidazole was found the most potent analogue against A549 cells with the GI50 value of 1.5 μg/mL. Moreover, 24 showed remarkable cell growth inhibition against MCF-7 and HeLa cells with the GI50 values of 7 and 5.5 μg/mL, respectively. The synthesized compounds have no important antibacterial and antifungal activities. Conclusion: It could be concluded that the introduction of di-chloro atoms at the phenyl ring of 2-(3,4-dimethoxyphenyl)-1H-benzimidazoles increases significant cytotoxicity to selected human tumor cell lines in comparison to other all benzazoles synthesized. Unsubstituted 2-(3,4- dimethoxyphenyl)-imidazopyridines also gave good inhibitory profile against A549 and HeLa cells.

scholarly journals Synthesis of the Bacteriostatic Poly(L-Lactide) by Using Zinc (II)[(acac)(L)H2O] (L = Aminoacid-Based Chelate Ligands) as an Effective ROP Initiator

2021 ◽  
Vol 22 (13) ◽  
pp. 6950
Author(s):  
Renata Barczyńska-Felusiak ◽  
Małgorzata Pastusiak ◽  
Piotr Rychter ◽  
Bożena Kaczmarczyk ◽  
Michał Sobota ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Antibacterial Properties ◽  
Antimicrobial Effect ◽  
Zinc Complexes ◽  
Antibacterial And Antifungal Activities ◽  
Aspergillus Brasiliensis ◽  
Acetylacetonate Complex ◽  
Distorted Trigonal Bipyramid ◽  
Composition Structure ◽  
Antibacterial And Antifungal

The paper presents a synthesis of poly(l-lactide) with bacteriostatic properties. This polymer was obtained by ring-opening polymerization of the lactide initiated by selected low-toxic zinc complexes, Zn[(acac)(L)H2O], where L represents N-(pyridin-4-ylmethylene) tryptophan or N-(2-pyridin-4-ylethylidene) phenylalanine. These complexes were obtained by reaction of Zn[(acac)2 H2O] and Schiff bases, , the products of the condensation of amino acids and 4-pyridinecarboxaldehyde. The composition, structure, and geometry of the synthesized complexes were determined by NMR and FTIR spectroscopy, elemental analysis, and molecular modeling. Both complexes showed the geometry of a distorted trigonal bipyramid. The antibacterial and antifungal activities of both complexes were found to be much stronger than those of the primary Schiff bases. The present study showed a higher efficiency of polymerization when initiated by the obtained zinc complexes than when initiated by the zinc(II) acetylacetonate complex. The synthesized polylactide showed antibacterial properties, especially the product obtained by polymerization initiated by a zinc(II) complex with a ligand based on l-phenylalanine. The polylactide showed a particularly strong antimicrobial effect against Pseudomonas aeruginosa, Staphylococcus aureus, and Aspergillus brasiliensis. At the same time, this polymer does not exhibit fibroblast cytotoxicity.

scholarly journals Bee Pollen Diet Alters the Bacterial Flora and Antimicrobial Peptides in the Oral Cavities of Mice

Foods ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1282
Author(s):  
Ariuntsetseg Khurelchuluun ◽  
Osamu Uehara ◽  
Durga Paudel ◽  
Tetsuro Morikawa ◽  
Yutaka Kawano ◽  
...  
Keyword(s):  
Antimicrobial Peptides ◽  
Buccal Mucosa ◽  
Bacterial Flora ◽  
Control Group ◽  
Mrna Levels ◽  
Bee Pollen ◽  
Alpha And Beta Diversity ◽  
Beneficial Effects ◽  
Metagenomic Study ◽  
Systemic Health

Background: Bee pollen (BP) has a broad range of beneficial effects on health. The aim of this study was to examine the effect of BP on the oral environment, including the microbiome and antimicrobial peptides. Methods: C57BL/6J mice were randomly divided into two groups: control and BP. The BP group was fed with a 5% BP diet for 1 month. Swabs from the oral and buccal mucosa and samples of the intestinal stool were collected. Genomic DNA was extracted and the microbiome was analyzed via 16S rRNA sequencing. Results: BP inhibited the growth of P. gingivalis at a concentration of >2.5%. The metagenomic study showed that the abundance of genus Lactococcus was significantly elevated in the oral and intestinal microbiomes of the BP group when compared to those of the control group. Significant alterations in alpha and beta diversity were observed between the oral microbiomes of the two groups. The mRNA levels of beta-defensin-2 and -3 were significantly upregulated in the buccal mucosa of the BP group. Conclusion: A BP diet may have a beneficial effect on oral and systemic health by modulating the bacterial flora and antimicrobial peptides of the oral cavity. Further investigations are needed to clarify how a BP diet affects overall human health.

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