Screening of Actinobacterial Cultures for Antimycobacterial Activity Using Mycobacterium smegmatis

2022 ◽  
pp. 391-393
Author(s):  
Ramachandran Chelliah ◽  
Deog-Hwan Oh
Keyword(s):  
Mycobacterium Smegmatis ◽  
Antimycobacterial Activity

scholarly journals Conserved Structure and Function in the Granulysin and NK-Lysin Peptide Family

2005 ◽  
Vol 73 (10) ◽  
pp. 6332-6339 ◽  
Author(s):  
Charlotte M. A. Linde ◽  
Susanna Grundström ◽  
Erik Nordling ◽  
Essam Refai ◽  
Patrick J. Brennan ◽  
...  
Keyword(s):  
Mycobacterium Smegmatis ◽  
Three Dimensional ◽  
Antimycobacterial Activity ◽  
Structure And Function ◽  
Loop Structure ◽  
E Coli ◽  
Short Loop ◽  
Peptide Family ◽  
And Function ◽  
Related Proteins

ABSTRACT Granulysin and NK-lysin are homologous bactericidal proteins with a moderate residue identity (35%), both of which have antimycobacterial activity. Short loop peptides derived from the antimycobacterial domains of granulysin, NK-lysin, and a putative chicken NK-lysin were examined and shown to have comparable antimycobacterial but variable Escherichia coli activities. The known structure of the NK-lysin loop peptide was used to predict the structure of the equivalent peptides of granulysin and chicken NK-lysin by homology modeling. The last two adopted a secondary structure almost identical to that of NK-lysin. All three peptides form very similar three-dimensional (3-D) architectures in which the important basic residues assume the same positions in space. The basic residues in granulysin are arginine, while those in NK-lysin and chicken NK-lysin are a mixture of arginine and lysine. We altered the ratio of arginine to lysine in the granulysin fragment to examine the importance of basic residues for antimycobacterial activity. The alteration of the amino acids reduced the activity against E. coli to a larger extent than that against Mycobacterium smegmatis. In granulysin, the arginines in the loop structure are not crucial for antimycobacterial activity but are important for cytotoxicity. We suggest that the antibacterial domains of the related proteins granulysin, NK-lysin, and chicken NK-lysin have conserved their 3-D structure and their function against mycobacteria.

scholarly journals Structure-activity relationships of quinolone agents against mycobacteria: effect of structural modifications at the 8 position.

1996 ◽  
Vol 40 (10) ◽  
pp. 2363-2368 ◽  
Author(s):  
T E Renau ◽  
J W Gage ◽  
J A Dever ◽  
G E Roland ◽  
E T Joannides ◽  
...  
Keyword(s):  
Mycobacterium Smegmatis ◽  
Antimycobacterial Activity ◽  
Mycobacterium Fortuitum ◽  
Structural Modifications ◽  
Structure Activity ◽  
Mycobacterium Aurum ◽  
The Relationship ◽  
Tuberculosis Activity ◽  
Better Than ◽  
Positive Controls

A series of quinolones with substitutions at the 8 position has been prepared as part of a study to examine the relationship between structural modifications at this position and activity against mycobacteria. The compounds were prepared by procedures described in the literature and were evaluated for their activities against Mycobacterium fortuitum and Mycobacterium smegmatis. The activities of the compounds against these two organisms were used as a measure of Mycobacterium tuberculosis activity. The results demonstrate that the contribution of the 8 position to antimycobacterial activity was dependent on the substituent at N-1 and was in the order (i) COMe approximately CBr > CCI > CH approximately CF approximately COEt > N > CCF3 when N-1 was cyclopropyl; (ii) N approximately CH > CF > COMe when N-1 was 2,4-difluorophenyl; (iii) N > or = CH when N-1 was tert-butyl; and (iv) N > CH when N-1 was ethyl. In general, derivatives with piperazine substitutions at C-7 were slightly less active against mycobacteria than the analogs with pyrrolidine substitutions, regardless of the pattern of substitution at the 8 position. Several of the best compounds were evaluated for their potential side effects as well as their activities against Mycobacterium aurum, Mycobacterium avium-M. intracellulare, and M. tuberculosis. These agents exhibited biological profiles similar to or better than those of the positive controls ciprofloxacin and sparfloxacin.

scholarly journals Synthesis of Antimycobacterial Agents that Harness Mycothiol and Cysteine conjugate β-lyase Metabolic Pathways

2021 ◽  
Author(s):  
◽  
Scott W. Riordan
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Mycobacterium Smegmatis ◽  
Antimycobacterial Activity ◽  
New Drugs ◽  
Bacillus Calmette Guerin ◽  
Antimycobacterial Agents ◽  
Resistant Strains ◽  
Drug Resistant Strains ◽  
Related Compounds ◽  
Synthetic Target

<p>Mycobacterium tuberculosis kills approximately two million people each year and is second only to HIV/AIDs in terms of death from infectious disease. The most pertinent problem in regards to Mycobacterium tuberculosis today is the increasing prevalence of drug resistant strains. Thus, there is a great need for the development of new drugs with novel targets. This thesis aimed to address this problem by synthesizing a compound that could exploit the mycothiol detoxification pathway, unique to Mycobacterium, in order to cause cell death, through the release of a harmful halothioketene.  The research described herein involved the successful synthesis of the desired mycothiol analogue, along with three other related compounds. The target compounds were synthesised via protection of N-acetyl glucosamine, followed by thioglycosidation with cyclohexane thiol. Subsequent deprotection and coupling to Boc protected Strichlorovinyl cysteine provided access to the synthetic target and its β-anomer, as well as their Boc protected precursors.  The original synthetic target demonstrated weak antimycobacterial activity against Mycobacterium smegmatis and an encouraging sub 100 μM MIC against Mycobacterium bovis derived Bacillus Calmette–Guérin. Unexpectedly the beta anomer of the synthetic target also displayed antimycobacterial activity against Bacillus Calmette–Guérin (MIC 125 - 250 μM). All compounds proved to be active against HL60 cells (16-114 μM).  Whilst further work is required to improve efficacy, the work presented here demonstrates the potential of these compounds as leads for the generation of new antimycobacterial agents.</p>

scholarly journals Novel Cyclic Lipodepsipeptide from Pseudomonas syringae pv. lachrymans Strain 508 and Syringopeptin Antimicrobial Activities

2005 ◽  
Vol 49 (12) ◽  
pp. 5037-5045 ◽  
Author(s):  
Ingeborg Grgurina ◽  
Mekki Bensaci ◽  
Gabriella Pocsfalvi ◽  
Luisa Mannina ◽  
Oscar Cruciani ◽  
...  
Keyword(s):  
Pseudomonas Syringae ◽  
Mycobacterium Smegmatis ◽  
Acyl Chain ◽  
Antimycobacterial Activity ◽  
Structural Features ◽  
Antimicrobial Activities ◽  
Gram Negative Bacteria ◽  
Gram Positive Bacteria ◽  
Growth Inhibitory ◽  
Unsaturated Amino Acids

ABSTRACT The syringopeptins are a group of antimicrobial cyclic lipodepsipeptides produced by several plant-associated pseudomonads. A novel syringopeptin, SP508, was shown to be produced as two homologs (A and B) by Pseudomonas syringae pv. lachrymans strain 508 from apple and to structurally resemble syringopeptin SP22. SP508 differed from SP22 and other syringopeptins by having three instead of four α,β-unsaturated amino acids and a longer β-hydroxy acyl chain. Both SP508 and SP22 displayed growth-inhibitory activities against Mycobacterium smegmatis, other gram-positive bacteria, and yeasts but not against gram-negative bacteria. Structure-activity analyses of the SP508 and SP22 homologs indicated chemical structural features that lead to enhanced antimycobacterial activity by these pseudomonad cyclic lipodepsipeptides.

scholarly journals Phytochemical Investigation, Antioxidant and Antimycobacterial Activities of Schkuhria pinnata (Lam) Thell Extracts Against Mycobacterium smegmatis

2019 ◽  
Vol 24 ◽  
pp. 2515690X1986610 ◽  
Author(s):  
Peter Masoko ◽  
Maano V. Masiphephethu
Keyword(s):  
Ethyl Acetate ◽  
Mycobacterium Smegmatis ◽  
Extraction Procedure ◽  
Radical Scavenging ◽  
Ammonium Hydroxide ◽  
Antimycobacterial Activity ◽  
Antioxidant Compounds ◽  
Total Phenol Content ◽  
Isolation And Purification ◽  
High Antioxidant Activity

The focus of this study was to evaluate the antioxidants and antimycobacterial activities of extracts of Schkuhria pinnata. Serial exhaustive extraction procedure was employed using solvents of varying polarity to obtain the desired extracts. Thin layer chromatography and standard chemical tests were used to analyze phytochemicals constituents. Free radical scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) methods were used to detect the presence of antioxidant compounds. Antimycobacterial activity was evaluated using microdilution and bioautography assays. A variety of secondary metabolites such as flavonoids, tannins, and alkaloids were detected in the extract. Ethyl acetate and acetone extracts had high antioxidant activity on chromatograms eluted in ethyl acetate/methanol/water while methanol extract at various concentrations had the best scavenging activity. The minimum inhibitory concentration (MIC) values ranged from 0.02 to 2.50 mg/mL. Total phenol content was 55.33 ± 3.51 mg of gallic acid equivalent (GAE)/g and higher when compared with flavonoids (4.00 ± 0.35 mg of quercetin equivalent [QE]/mg) and tannin content (28.00 ± 1.73 mg of GAE/g). The most effective antimycobacterial activity against Mycobacterium smegmatis was observed with the lowest inhibitory concentrations of acetone (0.27 mg/mL), dichloromethane (0.32 mg/mL), and ethyl acetate (0.32 mg/mL) in that order. In massive extraction, hexane and dichloromethane had the greatest inhibitory bands on benzene/ethanol/ammonium hydroxide bioautograms. Antimmycobacterial activity gives promising potential leads of S pinnata extracts to be used in the development of antimycobacterial drugs. The presence of antioxidant and antimycobacterial compounds requires further isolation and purification.

scholarly journals Antimicrobial Activity of Pyrazinamide Coordination Frameworks Synthesized by Mechanochemistry

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1904
Author(s):  
Sílvia Quaresma ◽  
Paula C. Alves ◽  
Patrícia Rijo ◽  
M. Teresa Duarte ◽  
Vânia André
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Mycobacterium Smegmatis ◽  
Antimycobacterial Activity ◽  
The Novel ◽  
Stability Studies ◽  
New Compounds ◽  
Crystalline Forms ◽  
Coordination Frameworks

The urge for the development of a more efficient antibiotic crystalline forms led us to the disclosure of new antibiotic coordination frameworks of pyrazinamide, a well-known drug used for the treatment of tuberculosis, with some of the novel compounds unravelling improved antimycobacterial activity. Mechanochemistry was the preferred synthetic technique to yield novel compounds, allowing the reproduction of a 1D zinc framework, the synthesis of a novel hydrogen bonding manganese framework, and three new compounds with silver. The structural characterization of the novel forms is presented along with stability studies. The increased antimicrobial activity of the new silver-based frameworks against Escherichia coli, Staphylococcus aureus, and Mycobacterium smegmatis is particularly relevant.

scholarly journals Antimicrobial Diterpenes from Azorella Species against Gram-Positive Bacteria

2015 ◽  
Vol 10 (11) ◽  
pp. 1934578X1501001 ◽  
Author(s):  
Viviana Donoso ◽  
Mitchell Bacho ◽  
Solange Núñez ◽  
Juana Rovirosa ◽  
Aurelio San-Martín ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Mycobacterium Smegmatis ◽  
Antimycobacterial Activity ◽  
Multidrug Resistant ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Resistant Strains ◽  
Andean Plants

The present study was aimed at evaluating the antibacterial activity of mulinane and azorellane diterpenes isolated from the Andean plants Azorella compacta and A. trifoliolata and semisynthetic derivatives against reference and multidrug-resistant strains. The results revealed that the semisynthetic compound 7-acetoxy-mulin-9,12-diene (5) exhibited antibacterial activity against reference and multidrug-resistant strains of Staphylococcus aureus and moderate antimycobacterial activity against Mycobacterium smegmatis ATCC 14468.

scholarly journals Sutherlandia frutescens (Fabaceae) extracts used for treating tuberculosis do not have high activity against Mycobacterium smegmatis

2017 ◽  
Vol 36 (1) ◽  
Author(s):  
Itumeleng H. Mabusa ◽  
Rachmond Howard ◽  
Peter Masoko
Keyword(s):  
Bioactive Compounds ◽  
Mycobacterium Smegmatis ◽  
High Performance ◽  
Antimycobacterial Activity ◽  
Chemical Profiling ◽  
Aerial Parts ◽  
Medicinal Use ◽  
Tlc Plates ◽  
Ethanol Extracts ◽  
Sutherlandia Frutescens

Sutherlandia frutescens (L) R. Br. contains several essential, bioactive compounds with clinically proven pharmacological activities. Sutherlandia is prescribed for people with tuberculosis but it is still not known what compounds in this plant act against Mycobacterium tuberculosis and its mode of action. This study is aimed at determining if S. frutescens extracts contain antimycobacterial compounds. Aerial parts of S. frutescens were dried, ground and extracted with ethanol, dichloromethane: methanol 1:1 (v/v) and water. The chemical profiling was done using high-performance liquid chromatography-mass spectroscopy (HPLC-MS) and thin layer chromatography (TLC). TLC plates were developed in butanol:acetic acid:water (BAW) to the ratio of 21:6:3; chloroform:methanol:water:formic acid (CMWF1) [60:15:2:1] and (CMWF2) [21:9:1:0.3]. Qualitative antioxidant activity was done, using 2.2-diphenylpacryl-1-hydrazyl (DPPH). Antimycobacterial activity of the plant extracts was evaluated, using micro-dilution and bioautographic methods against Mycobacterium smegmatis. Low antimycobacterial activity against M. smegmatis was observed on the bioautograms. The ethanol extracts contained more compounds compared to water extracts on HPLC-MS chromatographic profiles. The average Minimum Inhibitory Concentration (MIC) values for all the extracts were 0.61 mg/mL units and the DCM:MeOH (1:1) extract had the lowest MIC value of 0.28 mg/mL. The results showed that the plant could be further explored for possible antimycobacterial agents. Low activity was observed, possibly due to low replication of bacilli and non-replicating organisms. The study provides preliminary scientific validation of the traditional medicinal use of this plant. Further studies are required to identify the bioactive compounds in the DCM:MeOH 1:1 extract which showed significant antimycobacterial activities. Research correlation: This article is the original version, of which an Afrikaans translation was made available to provide access to a larger readership, available here: https://doi.org/10.4102/satnt.v36i1.1494

scholarly journals Antibacterial and Antimycobacterial Activity of Crude Extracts, Fractions, and Isolated Compounds From Leaves of Sneezewood, Ptaeroxylon obliquum (Rutaceae)

2019 ◽  
Vol 14 (11) ◽  
pp. 1934578X1987292 ◽  
Author(s):  
Thanyani E. Ramadwa ◽  
Maurice D. Awouafack ◽  
Molahlehi S. Sonopo ◽  
Jacobus N. Eloff
Keyword(s):  
Antimicrobial Activity ◽  
Mycobacterium Smegmatis ◽  
Antimycobacterial Activity ◽  
Culture Collection ◽  
Chloroform Fraction ◽  
Leaf Extracts ◽  
Excellent Activity ◽  
Liquid Fractionation ◽  
Isolated Compound ◽  
Human And Animal Diseases

Ptaeroxylon obliquum (Thunb.) Radlk. (Rutaceae) is traditionally used to treat human and animal diseases in South Africa. In this study, the activity of leaf extracts, fractions, and isolated compounds was determined against nonpathogenic mycobacterial species and nosocomial bacterial pathogens. An acetone leaf extract was partitioned by liquid-liquid fractionation, and obliquumol, a mixture of lupeol and β-amyrin, and eranthin were isolated. Antimicrobial activity was determined using a serial microdilution assay against Mycobacterium smegmatis (American Type Culture Collection [ATCC] 1441), M. bovis (BCG P1172), M. aurum (NCTC 10437), M. fortuitum (ATCC 6841), Staphylococcus aureus (ATCC 29213), Enterococcus faecalis (ATCC 29212), Pseudomonas aeruginosa (ATCC 25922), and Escherichia coli (ATCC 27853). The n-hexane fraction had minimal inhibitory concentration (MIC) values as low as 20 and 40 µg/mL against M. fortuitum and S. aureus, respectively. The chloroform fraction also had promising activity with an MIC value of 80 µg/mL against both P. aeruginosa and M. fortuitum. Obliquumol had excellent activity (MIC 8 µg/mL) against M. fortuitum. Fractionation of the crude extract potentiated the antimicrobial activity of the nonpolar fractions. The isolated compound, obliquumol, had good antimicrobial and excellent antimycobacterial activities. The antimicrobial activity provides some scientific rationale for the use of P. obliquum against infectious diseases and related symptoms. This is the first report on the antibacterial activity of obliquumol.

In vitro antimycobacterial activity of synthetic 1-methyl-2-alkenyl-4(1H)-quinolones against Mycobacterium smegmatis

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
A Wube ◽  
A Hüfner ◽  
C Hochfellner ◽  
C Thomaschitz ◽  
R Bauer ◽  
...  
Keyword(s):  
Mycobacterium Smegmatis ◽  
Antimycobacterial Activity
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