In vitro and in vivo antimicrobial activity of Ulva lactuca Linn. (Green algae) associated endophytic bacterial Strains

Humiria balsamifera (Aubl), commonly known as “mirim”, is a plant of the Humiriaceae family, which consists of 39 species divided between eight genera: Duckesia, Endopleura, Humiria, Humiriastrum, Hylocara, Sacoglottis, Schistostemon, and Vantenea. This study aimed to characterize H. balsamifera extracts by LC-MS/MS and evaluate their antimicrobial potential through in vitro and in vivo assays. The leaves and stem bark of H. balsamifera were collected and dried at room temperature and then ground in a knife mill. The extracts were prepared with organic solvents in order to increase the polarity index (hexane, ethyl acetate, and methanol). The antimicrobial effects of these extracts were evaluated against the following bacterial strains: Escherichia coli ATCC 25922, Listeria monocytogenes ATCC 15313, Salmonella enterica Typhimurium ATCC 14028, and Staphylococcus aureus ATCC 6538. The best activity was observed in the ethyl acetate (EALE = 780 µg/mL), methanol (MLE = 780 µg/mL), and hexane (HLE = 1560 µg/mL) leaf extracts against S. aureus. Considering the results for both antimicrobial and antibiofilm activities, the EALE extract was chosen to proceed to the infection assays, which used Tenebrio molitor larvae. The EALE treatment was able to extend the average lifespan of the larvae (6.5 days) in comparison to S. aureus-infected larvae (1 day). Next, the samples were characterized by High-Performance Liquid Chromatography coupled to a mass spectrometer, allowing the identification of 11 substances, including seven flavonoids, substances whose antimicrobial activity is already well-reported in the literature. The number of bioactive compounds found in the chemical composition of H. balsamifera emphasizes its significance in both traditional medicine and scientific research that studies new treatments based on substances from the Brazilian flora.

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In vitro Assessment of Bacterial Strains Associated with Microalgae as Potential Probiotics

Pertanika Journal of Tropical Agricultural Science ◽

10.47836/pjtas.44.1.12 ◽

2021 ◽

Vol 44 (1) ◽

Author(s):

Aimi Zabidi ◽

Natasya-Ain Rosland ◽

Jasmin Yaminudin ◽

Murni Karim

Keyword(s):

Antimicrobial Activity ◽

In Vitro Assays ◽

Disc Diffusion ◽

Bacterial Strains ◽

Pathogenic Vibrio ◽

Fish And Shellfish ◽

Diffusion Assay ◽

Vibrio Spp

Bacteria and microalgae are essential elements in the aquatic ecosystem, co-existing and having constant interactions with each other which help microalgae to exert its beneficial effect as probiotics in aquaculture. This research aims to isolate and identify potential probiotics from different species of microalgae and to evaluate their antimicrobial activity against pathogenic Vibrio spp. via series of in vitro assays; disc diffusion, well diffusion, and co-culture assays. A total of 18 bacterial strains were isolated from five species of microalgae; Chlorella sp., Nannochloropsis sp., Amphora sp., Chaetoceros sp., and Spirulina sp.. The isolated strains were tested in in vitro antagonistic assay against four Vibrio spp. (Vibrio harveyi, Vibrio alginolyticus, Vibrio vulnificus, and Vibrio parahaemolyticus). Seventeen strains demonstrated antimicrobial activity with the highest inhibition was observed by strain SPS11 against V. parahaemolyticus (12.6 ± 0.36 mm) in disc diffusion assay and strain NAS32 showed 13.2 ± 0.45 mm clear zone against V. vulnificus in well diffusion assay. In co-culture assay, both the SPS11 and NAS32 were able to reduce the growth of V. parahaemolyticus and V. harveyi at concentration of 106 and 108 CFU mL-1, respectively. Strains SPS11 and NAS32 were characterized as gram positive bacteria with rod shape and further identified as Lysinibacillus fusiformis (SPS11) and Lysinibacillus sphaericus (NAS32) using 16s rRNA. These two strains should be further studied in in vivo challenged experiments in fish and shellfish to explore their probiotic effects.

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In vitro antimicrobial activity of marbofloxacin and enrofloxacin against bacterial strains isolated from companion animals

Schweizer Archiv für Tierheilkunde ◽

10.1024/0036-7281.149.6.265 ◽

2007 ◽

Vol 149 (6) ◽

pp. 265-271 ◽

Cited By ~ 7

Author(s):

A. M. Farca ◽

P. Cavana ◽

P. Robino ◽

P. Nebbia

Keyword(s):

Antimicrobial Activity ◽

Companion Animals ◽

Bacterial Strains ◽

In Vitro Antimicrobial Activity

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Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents

Current Bioactive Compounds ◽

10.2174/1573407214666180226130957 ◽

2019 ◽

Vol 15 (1) ◽

pp. 63-70

Author(s):

Shiv Dev Singh ◽

Arvind Kumar ◽

Firoz Babar ◽

Neetu Sachan ◽

Arun Kumar Sharma

Keyword(s):

Antimicrobial Activity ◽

Potassium Hydroxide ◽

Antimicrobial Agents ◽

Pyrimidine Ring ◽

Antimicrobial Activities ◽

Screening Methods ◽

Chlorpheniramine Maleate ◽

In Vivo Screening

Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial activity. Objective: Synthesis of novel 3(N,N-dialkylamino)alkyl/phenyl substituted thieno[2,3-d]pyrimidinones as H1-anti-histaminic and antimicrobial agents. Methods: A series of 3-[(N,N-dialkylamino)alkyl/phenyl]-2-(1H)thioxo-5,6,7,8-tetrahydrobenzo(b) thieno(2,3-d)pyrimidine-4(3H)-ones[4a-d], their oxo analogous [5a-d] and 3-[(N,N-dialkylamino)alkyl]- 2-chlorophenyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidine- 4 (3H)-ones[6a-d]derivative were synthesized from 2-amino-4,5,6,7-tetrahydrobenzo(b)thiophene-3-carboxylic acid by nucleophilic substitution of different N,N-dialkyl alkylene/phenylene diamines on activated 3-acylchloride moiety followed by cyclocondensation with carbon disulfide and ethanolic potassium hydroxide to get [4a-d] and in second reaction by condensation with 4-chlorobenzoyl chloride to get [6a-d] by single pot novel innovative route. The oxo analogous [5a-d] were prepared by treating derivatives [4a-d] with potassium permagnate in ethanolic KOH. The synthesized compound were evaluated for H1-antihistaminic and antimicrobial activities. Results: All synthesized compounds exhibited significant H1-antihistaminic activity by in vitro and in vivo screening methods and data were verified analytically and statistically. The compound 4a, 4b, 5a and 5b showed significant H1-antihistaminiic activity than the reference standard chlorpheniramine maleate. The compound 6d, 6c, 5c and 4c exhibited significant antimicrobial activity.

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Synthesis, characterization, and pharmacological evaluation of thiourea derivatives

Open Chemistry ◽

10.1515/chem-2020-0139 ◽

2020 ◽

Vol 18 (1) ◽

pp. 764-777

Author(s):

Sumaira Naz ◽

Muhammad Zahoor ◽

Muhammad Naveed Umar ◽

Saad Alghamdi ◽

Muhammad Umar Khayam Sahibzada ◽

...

Keyword(s):

Spectroscopic Techniques ◽

Organosulfur Compounds ◽

Bacterial Strains ◽

Thiourea Derivatives ◽

Toxicological Effects ◽

Pharmaceutical Industries ◽

Uv Visible ◽

Hematological And Biochemical Parameters

AbstractThioureas and their derivatives are organosulfur compounds having applications in numerous fields such as organic synthesis and pharmaceutical industries. Symmetric thiourea derivatives were synthesized by the reaction of various anilines with CS2. The synthesized compounds were characterized using the UV-visible and nuclear magnetic resonance (NMR) spectroscopic techniques. The compounds were screened for in vitro inhibition of α-amylase, α-glucosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BuChE) enzymes and for their antibacterial and antioxidant potentials. These compounds were fed to Swiss male albino mice to evaluate their toxicological effects and potential to inhibit glucose-6-phosphatase (G6Pase) inhibition. The antibacterial studies revealed that compound 4 was more active against the selected bacterial strains. Compound 1 was more active against 2,2-diphenyl-1-picrylhydrazyl and 2,2’-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radicals, AChE, BuChE, and α-glucosidase. Compound 2 was more potent against α-amylase and G6Pase. Toxicity studies showed that compound 4 is safe as it exerted no toxic effect on any of the hematological and biochemical parameters or on liver histology of the experimental animals at any studied dose rate. The synthesized compounds showed promising antibacterial and antioxidant potential and were very active (both in vitro and in vivo) against G6Pase and moderately active against the other selected enzymes used in this study.

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Fabrication and Characterization of Antimicrobial Magnetron Cosputtered TiO2/Ag/Cu Composite Coatings

Coatings ◽

10.3390/coatings11040473 ◽

2021 ◽

Vol 11 (4) ◽

pp. 473

Author(s):

Dilyana Gospodonova ◽

Iliana Ivanova ◽

Todorka Vladkova

Keyword(s):

Antimicrobial Activity ◽

Composite Coatings ◽

Surface Characteristics ◽

Standard Test ◽

Most Probable Number ◽

Bacterial Strains ◽

Probable Number ◽

Fabrication And Characterization

The aim of this study was to prepare TiO2/Ag/Cu magnetron co-sputtered coatings with controlled characteristics and to correlate them with the antimicrobial activity of the coated glass samples. The elemental composition and distribution, surface morphology, wettability, surface energy and its component were estimated as the surface characteristics influencing the bioadhesion. Well expressed, specific, Ag/Cu concentration-dependent antimicrobial activity in vitro was demonstrated toward Gram-negative and Gram-positive standard test bacterial strains both by diffusion 21 assay and by Most Probable Number of surviving cells. Direct contact and eluted silver/coper nanoparticles killing were experimentally demonstrated as a mode of the antimicrobial action of the studied TiO2/Ag/Cu thin composite coatings. It is expected that they would ensure a broad spectrum bactericidal activity during the indwelling of the coated medical devices and for at least 12 h after that, with the supposition that the benefits will be over a longer time.

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High-throughput screening and rational design of biofunctionalized surfaces with optimized biocompatibility and antimicrobial activity

Nature Communications ◽

10.1038/s41467-021-23954-8 ◽

2021 ◽

Vol 12 (1) ◽

Author(s):

Zhou Fang ◽

Junjian Chen ◽

Ye Zhu ◽

Guansong Hu ◽

Haoqian Xin ◽

...

Keyword(s):

Antimicrobial Activity ◽

High Throughput ◽

High Throughput Screening ◽

Rational Design ◽

Click Reaction ◽

Reaction Times ◽

Great Promise ◽

Biomaterial Surfaces

AbstractPeptides are widely used for surface modification to develop improved implants, such as cell adhesion RGD peptide and antimicrobial peptide (AMP). However, it is a daunting challenge to identify an optimized condition with the two peptides showing their intended activities and the parameters for reaching such a condition. Herein, we develop a high-throughput strategy, preparing titanium (Ti) surfaces with a gradient in peptide density by click reaction as a platform, to screen the positions with desired functions. Such positions are corresponding to optimized molecular parameters (peptide densities/ratios) and associated preparation parameters (reaction times/reactant concentrations). These parameters are then extracted to prepare nongradient mono- and dual-peptide functionalized Ti surfaces with desired biocompatibility or/and antimicrobial activity in vitro and in vivo. We also demonstrate this strategy could be extended to other materials. Here, we show that the high-throughput versatile strategy holds great promise for rational design and preparation of functional biomaterial surfaces.

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Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

Acta Pharmaceutica ◽

10.2478/acph-2013-0001 ◽

2013 ◽

Vol 63 (1) ◽

pp. 19-30 ◽

Cited By ~ 11

Author(s):

Mohammed Afzal Azam ◽

Loganathan Dharanya ◽

Charu Chandrakant Mehta ◽

Sumit Sachdeva

Keyword(s):

Antimicrobial Activity ◽

Diclofenac Sodium ◽

Biological Evaluation ◽

Ring System ◽

Standard Drug ◽

Anti Inflammatory ◽

Pyrimidine Moiety ◽

Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

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Macrophage oxygen-dependent antimicrobial activity. III. Enhanced oxidative metabolism as an expression of macrophage activation.

Journal of Experimental Medicine ◽

10.1084/jem.152.6.1596 ◽

1980 ◽

Vol 152 (6) ◽

pp. 1596-1609 ◽

Cited By ~ 126

Author(s):

H W Murray ◽

Z A Cohn

Keyword(s):

Antimicrobial Activity ◽

Oxidative Metabolism ◽

Macrophage Activation ◽

Systemic Infection ◽

Peritoneal Macrophages ◽

H2o2 Production ◽

Oxygen Intermediates ◽

Cultivation In Vitro

The capacity of 15 separate populations of mouse peritoneal macrophages to generate and release H2O2 (an index of oxidative metabolism) was compared with their ability to inhibit the intracellular replication of virulent Toxoplasma gondii. Resident macrophages and those elicited by inflammatory agents readily supported toxoplasma multiplication and released 4-20X less H2O2 than macrophages activated in vivo by systemic infection with Bacille Calmette-Guérin or T. gondii, or by immunization with Corynebacterium parvum. Immunologically activated cells consistently displayed both enhanced H2O2 production and antitoxoplasma activity. Exposure to lymphokines generated from cultures of spleen cells from T. gondii immune mice and toxoplasma antigen preserved both the antitoxoplasma activity and the heightened H2O2 release of toxoplasma immune and immune-boosted macrophages, which otherwise were lost after 48-72 h of cultivation. In vitro activation of resident and chemically-elicited cells by 72 h of exposure to mitogen- and antigen-prepared lymphokines, conditions that induce trypanocidal (5) and leishmanicidal activity (14), stimulated O2- and H2O2 release, and enhanced nitroblue tetrazolium reduction in response to toxoplasma ingestion. Such treatment, however, failed to confer any antitoxoplasma activity, indicating that intracellular pathogens may vary in their susceptibility to macrophage microbicidal mechanisms, including specific oxygen intermediates. In contrast, cocultivating normal macrophages with lymphokine plus heart infusion broth for 18H rendered these cells toxoplasmastatic. This in vitro-acquired activity was inhibited by scavengers of O2-, H2O2, OH., and 1O2, demonstrating a role for oxidative metabolites in lymphokine-induced enhancement of macrophage antimicrobial activity. These findings indicate that augmented oxidative metabolism is an consistent marker of macrophage activation, and that oxygen intermediates participate in the resistance of both in vivo- and vitro-activated macrophages toward the intracellular parasite, T. gondii.

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