Diethylcarbamazine-related antimicrobial activity in Mycobacterium tuberculosis-infected blood

Granulysin is an antimicrobial peptide (AMP) expressed by human T-lymphocytes and natural killer cells. Despite a remarkably broad antimicrobial spectrum, its implementation into clinical practice has been hampered by its large size and off-target effects. To circumvent these limitations, we synthesized a 29 amino acid fragment within the putative cytolytic site of Granulysin (termed “Gran1”). We evaluated the antimicrobial activity of Gran1 against the major human pathogen Mycobacterium tuberculosis (Mtb) and a panel of clinically relevant non-tuberculous mycobacteria which are notoriously difficult to treat. Gran1 efficiently inhibited the mycobacterial proliferation in the low micro molar range. Super-resolution fluorescence microscopy and scanning electron microscopy indicated that Gran1 interacts with the surface of Mtb, causing lethal distortions of the cell wall. Importantly, Gran1 showed no off-target effects (cytokine release, chemotaxis, cell death) in primary human cells or zebrafish embryos (cytotoxicity, developmental toxicity, neurotoxicity, cardiotoxicity). Gran1 was selectively internalized by macrophages, the major host cell of Mtb, and restricted the proliferation of the pathogen. Our results demonstrate that the hypothesis-driven design of AMPs is a powerful approach for the identification of small bioactive compounds with specific antimicrobial activity. Gran1 is a promising component for the design of AMP-containing nanoparticles with selective activity and favorable pharmacokinetics to be pushed forward into experimental in vivo models of infectious diseases, most notably tuberculosis.

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2-aminoimidazoles potentiate ß-lactam antimicrobial activity against Mycobacterium tuberculosis by reducing ß-lactamase secretion and increasing cell envelope permeability

PLoS ONE ◽

10.1371/journal.pone.0180925 ◽

2017 ◽

Vol 12 (7) ◽

pp. e0180925 ◽

Cited By ~ 7

Author(s):

Albert B. Jeon ◽

Andrés Obregón-Henao ◽

David F. Ackart ◽

Brendan K. Podell ◽

Juan M. Belardinelli ◽

...

Keyword(s):

Antimicrobial Activity ◽

Mycobacterium Tuberculosis ◽

Cell Envelope

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SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME NEW 1,3,4- OXADIAZOLES, 1,2,4-TRIAZOLES AND 1,3,4-THIADIAZOLES

INDIAN DRUGS ◽

10.53879/id.53.06.10489 ◽

2016 ◽

Vol 53 (06) ◽

pp. 18-23

Author(s):

U. V. Laddi ◽

◽

S. R. Desai

Keyword(s):

Escherichia Coli ◽

Antimicrobial Activity ◽

Mycobacterium Tuberculosis ◽

Antitubercular Activity ◽

Tuberculosis H37rv ◽

Research Centre ◽

Methyl Ethyl ◽

Rhizoctonia Bataticola ◽

Mycobacterium Tuberculosis H37rv ◽

H37rv Strain

Some new 5-[(((α-phenyl/methyl)benzylidene)amino)oxy]methyl/ethyl-2-[4-(substituted aryl)/allyl)] amino-1,3,4-oxadiazoles (4a-p), 3-[(((α-phenyl/methyl)- benzylidene) amino)oxy]methyl/ethyl-4-(4- substitutedaryl)/allyl-5-mercapto-1,2,4-triazoles (5a-p) and 5-[(((α-phenyl/methyl)-benzylidene)amino) oxy]- methyl/ethyl-2-[4-(substituted aryl)/allyl)]amino-1,3,4-thiadiazoles (6a-p) were prepared starting from α/β-[((α-(phenyl/methyl)benzylidene)amino)oxy acetic/propionic acid hydrazides (1a-d). The structures of all the compounds have been established by elemental and spectral (IR, 1HNMR and mass) analysis. All the newly synthesised compounds have been screened for their antimicrobial activity against Escherichia coli, Bacillus cirroflagellosus, Aspergillus niger and Rhizoctonia bataticola. Some of the newly synthesised compounds have been evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv strain by BACTEC radiometric system at Southern Research Institute, Birmingham, AL and Frederick Research Centre, Frederick, MD. Significant antimicrobial activity is observed against Escherichia coli and Rhizoctonia bataticola. A few compounds also exhibited interesting antitubercular activity against Mycobacterium tuberculosis H37Rv strain.

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Polyketides from an Endophytic Aspergillus fumigatus Isolate Inhibit the Growth of Mycobacterium tuberculosis and MRSA

Natural Product Communications ◽

10.1177/1934578x1501001009 ◽

2015 ◽

Vol 10 (10) ◽

pp. 1934578X1501001 ◽

Cited By ~ 4

Author(s):

Andrew J. Flewelling ◽

Amanda L Bishop ◽

John A. Johnson ◽

Christopher A. Gray

Keyword(s):

Staphylococcus Aureus ◽

Antimicrobial Activity ◽

Mycobacterium Tuberculosis ◽

Aspergillus Fumigatus ◽

Crude Extract ◽

Antimycobacterial Activity ◽

Methicillin Resistant ◽

Bioassay Guided Fractionation ◽

Chaetoglobosin A

The crude extract of Aspergillus fumigatus isolate AF3-093A, an endophyte of the brown algaFucus vesiculosus, showed significant antimicrobial activity in initial bioactivity screens. Bioassay-guided fractionation of the extract led to the isolation of flavipin, chaetoglobosin A and chaetoglobosin B, all of which inhibited the growth of Staphylococcus aureus, methicillin-resistant S. aureus and Mycobacterium tuberculosis H37Ra. The antimycobacterial activity of these compounds has not been previously reported.

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The antimicrobial activity of copper and copper alloys against nosocomial pathogens and Mycobacterium tuberculosis isolated from healthcare facilities in the Western Cape: an in-vitro study

Journal of Hospital Infection ◽

10.1016/j.jhin.2007.10.009 ◽

2008 ◽

Vol 68 (1) ◽

pp. 45-51 ◽

Cited By ~ 116

Author(s):

S. Mehtar ◽

I. Wiid ◽

S.D. Todorov

Keyword(s):

Antimicrobial Activity ◽

Mycobacterium Tuberculosis ◽

Copper Alloys ◽

In Vitro Study ◽

Vitro Study ◽

Western Cape ◽

Nosocomial Pathogens ◽

Healthcare Facilities

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Synthesis of Some New Pyrimidine-Azitidinone Analogues and Their Antioxidant,In VitroAntimicrobial, and Antitubercular Activities

Journal of Chemistry ◽

10.1155/2014/847180 ◽

2014 ◽

Vol 2014 ◽

pp. 1-9 ◽

Cited By ~ 3

Author(s):

Mallikarjunaswamy Chandrashekaraiah ◽

Mallesha Lingappa ◽

Vathsala Deepu Channe Gowda ◽

Doddamedur Giddegowda Bhadregowda

Keyword(s):

Antimicrobial Activity ◽

Mycobacterium Tuberculosis ◽

Schiff Base ◽

Aromatic Amines ◽

Dimethyl Formamide ◽

Chloroacetyl Chloride ◽

Antituberculosis Activity ◽

Sodium Sulphide ◽

Molecular Studies

A series of 1-(3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)-4-methylphenyl)-3-chloro-4-(2-mercaptoquinolin-3-yl)azetidin-2-one (7a-j) have been synthesized from the condensation of aromatic amines withN-phenylacetamide. The thione nucleus formed from 2-chloroquionoline-3-carbadehyde using sodium sulphide in dimethyl formamide (DMF) was followed by the reaction with pyrimidine amine to form the Schiff base intermediates. Attempt has been made to derive final azetidinone analogues from Schiff bases by using chloroacetyl chloride. The newly synthesized analogues were examined for the antimicrobial activity against some bacterial and fungal strains andin vitroantituberculosis activity against mycobacterium tuberculosis. These observations provide some predictions to design further antibacterial and antituberculosis active compounds prior to their synthesis according to molecular studies.

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Analysis of Antimicrobial Activity of Monocytic Myeloid-Derived Suppressor Cells in Infection with Mycobacterium tuberculosis and Human Immunodeficiency Virus

Methods in Molecular Biology - Myeloid-Derived Suppressor Cells ◽

10.1007/978-1-0716-1060-2_11 ◽

2020 ◽

pp. 115-127

Author(s):

Ankita Garg

Keyword(s):

Human Immunodeficiency Virus ◽

Antimicrobial Activity ◽

Mycobacterium Tuberculosis ◽

Suppressor Cells ◽

Myeloid Derived Suppressor Cells ◽

Immunodeficiency Virus

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Antimicrobial Lavandulylated Flavonoids from a Sponge-Derived Streptomyces sp. G248 in East Vietnam Sea

Marine Drugs ◽

10.3390/md17090529 ◽

2019 ◽

Vol 17 (9) ◽

pp. 529 ◽

Cited By ~ 5

Author(s):

Cao ◽

Trinh ◽

Mai ◽

Vu ◽

Le ◽

...

Keyword(s):

Mass Spectrometry ◽

Nuclear Magnetic Resonance ◽

Antimicrobial Activity ◽

Mycobacterium Tuberculosis ◽

Spectroscopic Data ◽

Inhibitory Concentration ◽

Culture Broth ◽

Ionization Mass ◽

Streptomyces Sp ◽

Mycobacterium Tuberculosis H37rv

Three new lavandulylated flavonoids, (2S,2′’S)-6-lavandulyl-7,4′-dimethoxy-5,2′-dihydroxylflavanone (1), (2S,2′’S)-6-lavandulyl-5,7,2′,4′-tetrahydroxylflavanone (2), and (2′’S)-5′-lavandulyl-2′-methoxy-2,4,4′,6′-tetrahydroxylchalcone (3), along with seven known compounds 4–10 were isolated from culture broth of Streptomyces sp. G248. Their structures were established by spectroscopic data analysis, including 1D and 2D nuclear magnetic resonance (NMR), and high-resolution electrospray ionization mass spectrometry (HR-ESI-MS). The absolute configurations of 1–3 were resolved by comparison of their experimental and calculated electronic circular dichroism spectra. Compounds 1–3 exhibited remarkable antimicrobial activity. Whereas, two known compounds 4 and 5 exhibited inhibitory activity against Mycobacterium tuberculosis H37Rv with minimum inhibitory concentration (MIC) values of 6.0 µg/mL and 11.1 µg/mL, respectively.

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Vitamins and tuberculosis

Farmacist ro ◽

10.26416/farm.187.2.2019.2338 ◽

2019 ◽

Vol 187 (2) (1) ◽

pp. 38-45

Author(s):

Nicolae Bacinschi ◽

Sofia Alexandru ◽

Anna Donica ◽

Ina Guţu

Keyword(s):

Antimicrobial Activity ◽

Mycobacterium Tuberculosis ◽

Multidrug Resistance ◽

Mechanisms Of Action ◽

Vitamin Deficiency ◽

Antituberculous Drugs

The importance of vitamins to the development, progression and treatment of tuberculosis is indisputable due to the presence of hypovitaminosis in people with malnutrition or the increase of vitamin deficiency in the setting of the disease. It was established that vitamin preparations exhibit antimicrobial activity, potentiate efficacy and reduce the toxicity of antituberculous drugs. Recent studies have proved the role of vitamins in the metabolism and multiplication of mycobacteria, suggesting the possibility of developing antitubercular compounds based on vitamin preparations with new mechanisms of action. These data are important for the possibility of combating resistance and multidrug resistance in Mycobacterium tuberculosis.

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EFFECTISAN FOR DISINFECTION OF OBJECTS OF VETERINARY SUPERVISION

Problems of Veterinary Sanitation, Hygiene and Ecology ◽

10.36871/vet.san.hyg.ecol.201802006 ◽

2018 ◽

Vol 1 (2) ◽

pp. 36-41

Author(s):

D. I. Udavliev ◽

◽

A. M. Abdullaeva ◽

S. S. Shikhov ◽

N. E. Vanner ◽

...

Keyword(s):

Antimicrobial Activity ◽

Quality Control ◽

Mycobacterium Tuberculosis ◽

Consumption Rate ◽

High Antimicrobial Activity ◽

E Coli ◽

Selection Of Cultures ◽

Selection Of ◽

Test Cultures

The article provides information about the effectiveness of the drug is Effectisan in the laboratory. As a result of the conducted researches it is established that the tested preparation possesses a certain high antimicrobial activity. The drug (in vitro) is effective at concentrations from 0.2 to 1.0% against E. coli (pcs 1257), St. aureus (pcs 209-P), Mycobacterium B-5, Bac. cereus (pcs 96). With wet disinfection at a concentration of 0.5% and a consumption rate of 350 ml/m2, the drug has a pronounced disinfection activity against surfaces made of various materials, the quality control of disinfection in which is carried out by the presence or absence of growth in the washouts of test cultures E. coli, S. aureus. At a concentration of 2.0% and the rate of 350 ml/m2 Effectisan has a pronounced disinfectant activity during processing objects and for quality control of disinfection by selection of cultures of Mycobacterium tuberculosis (pcs-5).

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