scholarly journals Selective Modification of Streptozotocin at the C3 Position to Improve Its Bioactivity as Antibiotic and Reduce Its Cytotoxicity towards Insulin-Producing β Cells

2020 ◽  
Author(s):  
Ji Zhang ◽  
Liubov Yakovlieva ◽  
Bart J. de Haan ◽  
Paul de Vos ◽  
Adriaan J. Minnaard ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Natural Product ◽  
Beta Cells ◽  
Bacterial Infections ◽  
Structural Modification ◽  
Antimicrobial Effect ◽  
Antibiotic Activity ◽  
Broad Spectrum Antibiotic ◽  
Cytotoxic Compound ◽  
Regioselective Oxidation

With the increasing resistance of bacteria to current antibiotics, novel compounds are urgently needed to treat bacterial infections. Streptozotocin (STZ) is a natural product that has broad-spectrum antibiotic activity, albeit with limited use because of its toxicity to pancreatic β cells. In an attempt to derivatize STZ through structural modification at the C3 position, we performed the synthesis of three novel STZ analogues by making use of our recently developed regioselective oxidation protocol. Keto-STZ (2) shows the highest inhibition of bacterial growth (MIC and viability assays), but is also the most cytotoxic compound. Pre-sensitizing the bacteria with GlcNAc increased the antimicrobial effect, but did not result in complete killing. Interestingly, allo-STZ (3) revealed moderate concentration-dependent antimicrobial activity and no cytotoxicity towards β cells, and deoxy-STZ (4) showed no activity at all.

scholarly journals Selective Modification of Streptozotocin at the C3 Position to Improve Its Bioactivity as Antibiotic and Reduce Its Cytotoxicity towards Insulin-Producing β Cells

Antibiotics ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 182
Author(s):  
Ji Zhang ◽  
Liubov Yakovlieva ◽  
Bart J. de Haan ◽  
Paul de Vos ◽  
Adriaan J. Minnaard ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Structural Modification ◽  
Inhibitory Concentration ◽  
Antimicrobial Effect ◽  
Antibiotic Activity ◽  
Β Cells ◽  
Broad Spectrum Antibiotic ◽  
Pancreatic Β Cells ◽  
Cytotoxic Compound ◽  
Regioselective Oxidation

With the increasing resistance of bacteria to current antibiotics, novel compounds are urgently needed to treat bacterial infections. Streptozotocin (STZ) is a natural product that has broad-spectrum antibiotic activity, albeit with limited use because of its toxicity to pancreatic β cells. In an attempt to derivatize STZ through structural modification at the C3 position, we performed the synthesis of three novel STZ analogues by making use of our recently developed regioselective oxidation protocol. Keto-STZ (2) shows the highest inhibition of bacterial growth (minimum inhibitory concentration (MIC) and viability assays), but is also the most cytotoxic compound. Pre-sensitizing the bacteria with GlcNAc increased the antimicrobial effect, but did not result in complete killing. Interestingly, allo-STZ (3) revealed moderate concentration-dependent antimicrobial activity and no cytotoxicity towards β cells, and deoxy-STZ (4) showed no activity at all.

scholarly journals Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening

2021 ◽  
Vol 11 (3) ◽  
pp. 1180
Author(s):  
Kinga Paruch ◽  
Łukasz Popiołek ◽  
Anna Biernasiuk ◽  
Anna Berecka-Rycerz ◽  
Anna Malm ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Carboxylic Acid ◽  
Bacterial Infections ◽  
Acid Hydrazide ◽  
Antimicrobial Effect ◽  
In Vitro Antimicrobial Activity ◽  
Research Goal ◽  
New Compounds ◽  
Derivatives Of

Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound 15, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL.

scholarly journals Composition and Antimicrobial Activity ofEuphrasia rostkovianaHayne Essential Oil

2015 ◽  
Vol 2015 ◽  
pp. 1-5 ◽  
Author(s):  
Pavel Novy ◽  
Hana Davidova ◽  
Cecilia Suqued Serrano-Rojero ◽  
Johana Rondevaldova ◽  
Josef Pulkrabek ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Chemical Composition ◽  
Essential Oil ◽  
Bacterial Infections ◽  
Antimicrobial Effect ◽  
Main Constituent ◽  
Hexadecanoic Acid ◽  
Eye Infections ◽  
Gram Positive Bacteria ◽  
Health Disorders

Eyebright,Euphrasia rostkovianaHayne (Scrophulariaceae), is a medicinal plant traditionally used in Europe for the treatment of various health disorders, especially as eyewash to treat eye ailments such as conjunctivitis and blepharitis that can be associated with bacterial infections. SomeEuphrasiaspecies have been previously reported to contain essential oil. However, the composition and bioactivity ofE. rostkovianaoil are unknown. Therefore, in this study, we investigated the chemical composition and antimicrobial activity of the eyebright essential oil against some organisms associated with eye infections:Enterococcus faecalis,Escherichia coli,Klebsiella pneumoniae,Staphylococcus aureus,S. epidermidis,Pseudomonas aeruginosa, andCandida albicans. GC-MS analysis revealed more than 70 constituents, with n-hexadecanoic acid (18.47%) as the main constituent followed by thymol (7.97%), myristic acid (4.71%), linalool (4.65%), and anethole (4.09%). The essential oil showed antimicrobial effect against all organisms tested with the exception ofP. aeruginosa. The best activity was observed against all Gram-positive bacteria tested with the minimum inhibitory concentrations of 512 µg/mL. This is the first report on the chemical composition ofE. rostkovianaessential oil and its antimicrobial activity.

scholarly journals Antibiotic activity and resistance of lactic acid bacteria and other antagonistic bacteriocin-producing microorganisms

2020 ◽  
Vol 8 (2) ◽  
pp. 377-384
Author(s):  
Yong Yang ◽  
Olga Babich ◽  
Stanislav Sukhikh ◽  
Mariya Zimina ◽  
Irina Milentyeva
Keyword(s):  
Antimicrobial Activity ◽  
Lactic Acid ◽  
Lactic Acid Bacteria ◽  
Leuconostoc Mesenteroides ◽  
Antimicrobial Effect ◽  
Alcaligenes Faecalis ◽  
Inhibitory Effect ◽  
Antibiotic Activity ◽  
Antibiotic Drugs ◽  
New Antibiotics

Introduction. Increased resistance of microorganisms to traditional antibiotics has created a practical need for isolating and synthesizing new antibiotics. We aimed to study the antibiotic activity and resistance of bacteriocins produced by lactic acid bacteria and other microorganisms. Study objects and methods. We studied the isolates of the following microorganism strains: Bacillus subtilis, Penicillium glabrum, Penicillium lagena, Pseudomonas koreenis, Penicillium ochrochloron, Leuconostoc lactis, Lactobacillus plantarum, Leuconostoc mesenteroides, Pediococcus acidilactici, Leuconostoc mesenteroides, Pediococcus pentosaceus, Lactobacillus casei, Lactobacillus fermentum, Bacteroides hypermegas, Bacteroides ruminicola, Pediococcus damnosus, Bacteroides paurosaccharolyticus, Halobacillus profundi, Geobacillus stearothermophilus, and Bacillus caldotenax. Pathogenic test strains included Escherichia coli, Salmonella enterica, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus mycoides, Alcaligenes faecalis, and Proteus vulgaris. The titer of microorganisms was determined by optical density measurements at 595 nm. Results and discussion. We found that eleven microorganisms out of twenty showed high antimicrobial activity against all test strains of pathogenic and opportunistic microorganisms. All the Bacteroides strains exhibited little antimicrobial activity against Gramnegative test strains, while Halobacillus profundi had an inhibitory effect on Gram-positive species only. The Penicillium strains also displayed a slight antimicrobial effect on pathogenic test strains. Conclusion. The antibiotic resistance of the studied lactic acid bacteria and other bacteriocin-producing microorganisms allows for their use in the production of pharmaceutical antibiotic drugs.

scholarly journals Characterization and Antimicrobial Activity of the Teleost Chemokine CXCL20b

Antibiotics ◽  
2020 ◽  
Vol 9 (2) ◽  
pp. 78
Author(s):  
Xun Xiao ◽  
Yanqi Zhang ◽  
Zhiwei Liao ◽  
Jianguo Su
Keyword(s):  
Antimicrobial Activity ◽  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Early Stage ◽  
Biological Activities ◽  
Antimicrobial Effect ◽  
Ctenopharyngodon Idella ◽  
Random Coil ◽  
Grass Carp Ctenopharyngodon Idella ◽  
Short Time

Fish are a potential source of diverse organic compounds with a broad spectrum of biological activities. Many fish-derived antimicrobial peptides and proteins are key components of the fish innate immune system. They are also potential candidates for development of new antimicrobial agents. CXCL20b is a grass carp (Ctenopharyngodon idella) CXC chemokine strongly transcribed at the early stage of bacterial infections, for which the immune role had not been reported to date. In the present study, we found that CXCL20b is a cationic amphipathic protein that displays potent antimicrobial activity against both Gram-positive and Gram-negative bacteria. The results of DiOC2(3) and atomic force microscopy (AFM) assays indicated that CXCL20b could induce bacterial membrane depolarization and disruption in a short time. By performing further structure-activity studies, we found that the antimicrobial activity of CXCL20b was mainly relative to the N-terminal random coil region. The central part of this cytokine representing β-sheet region was insoluble in water and the C-terminal α-helical region did not show an antimicrobial effect. The results presented in this article support the poorly understood function of CXCL20b, which fulfills an important role in bony fish antimicrobial immunity.

scholarly journals Concise synthesis of spergualin-inspired molecules with broad-spectrum antibiotic activity

MedChemComm ◽  
2015 ◽  
Vol 6 (5) ◽  
pp. 912-918 ◽  
Author(s):  
Victoria A. Assimon ◽  
Hao Shao ◽  
Sylvie Garneau-Tsodikova ◽  
Jason E. Gestwicki
Keyword(s):  
Natural Product ◽  
Broad Spectrum ◽  
Antibiotic Activity ◽  
Broad Spectrum Antibiotic ◽  
Broad Spectrum Antibiotics ◽  
Privileged Structure

There is a growing need to identify new, broad-spectrum antibiotics. Here, we report a concise route to an antibiotic based on the privileged structure of the natural product spergualin.

Evaluation of antimicrobial potential of some spices from apiaceae sold in herbal shops

2019 ◽  
Author(s):  
Alev ONDER ◽  
Suna Sibel GURPINAR, Mujde ERYILMAZ ◽  
Bayram Kagan AKAY, Ahsen Sevde CINAR
Keyword(s):  
Antimicrobial Activity ◽  
Daucus Carota ◽  
Antimicrobial Effect ◽  
Coriandrum Sativum ◽  
Apium Graveolens ◽  
Dilution Method ◽  
Anethum Graveolens ◽  
Foeniculum Vulgare ◽  
Pimpinella Anisum ◽  
Hexane Extracts

Spices are a part of the plants used for many purposes as preservatives and as colorants in foods or as medicinal intention. Main aim of the present research was to estimate the potential antimicrobial activity of some spices from Apiaceae family such as Amni visnaga (Diş otu, Hıltan), Anethum graveolens (Dereotu), Apium graveolens (Kereviz), Coriandrum sativum (Kişniş), Cuminum cyminum (Kimyon), Daucus carota (Havuç), Foeniculum vulgare (Rezene), Petroselinum sativum (Maydanoz), Pimpinella anisum (Anason). Thus, the fruits of the plants are used in the experiments. The fruits have been extracted by n-hexane, and all extracts have been subjected to TLC (Thin Layer Chromatography). The n-hexane extracts were screened for their potential in vitro antibacterial activity against Staphylococcus aureus ATCC 29213, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 13883, Pseudomonas aeruginosa ATCC 27853 and antifungal activity against Candida albicans ATCC 10231 by microbroth dilution method. The hexane extracts of the fruits of Coriandrum sativum, Anethum graveolens, Daucus carota, and Pimpinella anisum did not show antimicrobial activity against tested microorganisms. Except these, the other extracts having MIC values of 2.5-5-10 mg/mL exhibited antimicrobial effect against some tested microorganisms. These results demonstrate that the extracts which have an antimicrobial effect can probably play a role as an antimicrobial agent owing to their nonpolar components which are accumulated to the n-hexane extracts.

scholarly journals Synergistic Antimicrobial Activities of Combinations of Vanillin and Essential Oils of Cinnamon Bark, Cinnamon Leaves and Cloves

Foods ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1406
Author(s):  
Rita Cava-Roda ◽  
Amaury Taboada-Rodríguez ◽  
Antonio López-Gómez ◽  
Ginés Benito Martínez-Hernández ◽  
Fulgencio Marín-Iniesta
Keyword(s):  
Antimicrobial Activity ◽  
Essential Oils ◽  
Food Packaging ◽  
Antimicrobial Effect ◽  
Antimicrobial Activities ◽  
Inhibitory Effects ◽  
Cinnamon Bark ◽  
E Coli ◽  
Pure Compounds ◽  
Main Component

Plant bioactive compounds have antimicrobial and antioxidant activities that allow them to be used as a substitute for synthetic chemical additives in both food and food packaging. To improve its sensory and bactericidal effects, its use in the form of effective combinations has emerged as an interesting possibility in the food industry. In this study, the antimicrobial activities of essential oils (EOs) of cinnamon bark, cinnamon leaves, and clove and the pure compounds vanillin, eugenol, and cinnamaldehyde were investigated individually and in combination against Listeria monocytogenes and Escherichia coli O157:H7. The possible interactions of combinations of pure compounds and EOs were performed by the two-dimensional checkerboard assay and isobologram methods. Vanillin exhibited the lowest antimicrobial activity (MIC of 3002 ppm against L. monocytogenes and 2795 ppm against E. coli O157:H7), while clove and cinnamon bark EOs exhibited the highest antimicrobial activity (402–404 against L. monocytogenes and 778–721 against E. coli O157:H7). For L. monocytogenes, pure compound eugenol, the main component of cinnamon leaves and clove, showed lower antimicrobial activity than EOs, which was attributed to the influence of the minor components of the EOs. The same was observed with cinnamaldehyde, the main component of cinnamon bark EO. The combinations of vanillin/clove EO and vanillin/cinnamon bark EO showed the most synergistic antimicrobial effect. The combination of the EOs of cinnamon bark/clove and cinnamon bark/cinnamon leaves showed additive effect against L. monocytogenes but indifferent effect against E. coli O157:H7. For L. monocytogenes, the best inhibitory effects were achieved by cinnamon bark EO (85 ppm)/vanillin (910 ppm) and clove EO (121 ppm)/vanillin (691 ppm) combinations. For E. coli, the inhibitory effects of clove EO (104 ppm)/vanillin (1006 ppm) and cinnamon leaves EO (118 ppm)/vanillin (979 ppm) combinations were noteworthy. Some of the tested combinations increased the antimicrobial effect and would allow the effective doses to be reduced, thereby offering possible new applications for food and active food packaging.

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