The Anti-mycobacterial Activity of a Diterpenoid-Like Molecule Operates Through Nitrogen and Amino Acid Starvation

A library of 14 nontoxic diterpenoid-like compounds (CC50> 70 µM on HepG2 human liver cells) was screened against Mycobacterium smegmatis, Staphylococcus aureus and Escherichia coli to determine antimicrobial activity. Some compounds with a phenethyl alcohol core substituted with a β-cyclocitral derivative demonstrated anti-mycobacterial activity, with the most active being compound 1 (MIC = 23.4 mg/L, IC50 = 0.6 mg/L). Lower activity was exhibited against S. aureus, while no activity was displayed against E. coli. Low cytotoxicity was confirmed on HepG2 cells and newly derived for RAW 264.7 murine macrophages (SI> 38). The sub-lethal (IC50 at 6 h) effect of compound 1 on M. smegmatis was examined through untargeted metabolomics and compared to untreated bacteria and bacteria treated with sub-lethal (IC50 at 6 h) concentrations of the antituberculosis drugs ethambutol, isoniazid, kanamycin and streptomycin. The study revealed that compound 1 acts differently from the reference antibiotics and that it significantly affects amino acid, nitrogen, nucleotides and folate-dependent one-carbon metabolism of M. smegmatis, giving some insights about the mode of action of this molecule. A future medicinal chemistry optimization of this new anti-mycobacterial core could lead to more potent molecules.
Source: Frontiers in Microbiology - Category: Microbiology Source Type: research

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This study estimated the prevalence of bacterial pneumonia in HIV patients, antimicrobial susceptibility patterns of pathogens implicated in pneumonia, and associated risk factors in Mekelle zone, Tigray, Northern Ethiopia, during August-December 2016. Methods: Sputum specimens were collected from 252 HIV seropositive individuals with suspected pneumonia. Data on sociodemographics and risk factors were also collected using a structured questionnaire. Blood, Chocolate, and Mac Conkey agar plates (Oxoid, Hampshire, UK) were used to grow the isolates. The isolated colonies were identified based on Gram stain, colony morp...
Source: Biomed Res - Category: Research Authors: Tags: Biomed Res Int Source Type: research
Publication date: October 2019Source: Materials Science and Engineering: C, Volume 103Author(s): Jyoti Ahlawat, Vinay Kumar, P. GopinathAbstractBioactive polymers are highly used polymers for preparing electrospun nanofiber based scaffold in the field of wound dressing to treat chronic non-healing wounds. Here, we report, the fabrication and evaluation of Carica papaya incorporated poly (vinyl) alcohol (PVA) blended gelatin nanofibers. PVA/Gelatin/Carica papaya nanofibrous scaffold was fabricated by electrospinning method. The obtained nanofibrous scaffold was characterized by using various analytical techniques such as FT...
Source: Materials Science and Engineering: C - Category: Materials Science Source Type: research
Abstract Starch, and silver nitrate were used for one pot facile synthesis of starch capped silver nanoparticles. Transmission electron microscopy (TEM), dynamic light scattering (DLS), iodometry titration, and UV-visible spectroscopy were used for the characterization and encapsulation of silver nanoparticles into the helix of amylose. TEM images confirm that morphology of nanoparticles changed entirely (from spherical and chain-like aggregated to only chain like beautiful silver) in excess of starch concentration. Starch capped nanoparticles were used for detection of hydrogen peroxide. The results reveal that s...
Source: International Journal of Biological Macromolecules - Category: Biochemistry Authors: Tags: Int J Biol Macromol Source Type: research
Publication date: Available online 18 May 2019Source: European Polymer JournalAuthor(s): Aiswarya Devi Sekar, Vinay Kumar, Harshiny Muthukumar, P. Gopinath, Manickam MatheswaranAbstractPoly Vinyl Alcohol (PVA) nanofibers incorporated with various weight percentages of Fe-doped ZnO nanoparticles were successfully fabricated by electrospinning technique and examined for its antibacterial with cytotoxic properties. The analytical characterization of fabricated nanofibers has revealed virtuous physicochemical traits such as bead less uniform nanofibers with diameter ranges from 120-250nm and hydrophilic in nature. A prominent ...
Source: European Polymer Journal - Category: Chemistry Source Type: research
In this study, Schiff bases of chitosan (CS) were synthesized using citronellal, citral, and their derivatives containing selenium and sulfur. Organoselenium and organosulfur compounds show attractive biological and pharmaceutical activities, which can be beneficial to CS-based materials. From the characterization analyses, it was found that the CS-derivatives containing organoselenium and organosulfur compounds exhibited the highest conversion degrees (23 and 28%). Biological assays were conducted using films prepared by the blending of CS-derivatives and poly(vinyl alcohol). The antimicrobial evaluation indicated that th...
Source: Carbohydrate Polymers - Category: Biomedical Science Source Type: research
In this study, poly(vinyl alcohol)/silver nanoparticles-graphene oxide (PVA/AgNPs-GO) nanocomposites were synthesized by a one-step process with l-ascorbic acid as environmentally friendly reductant agent of a mixture of AgNO3, GO and PVA aqueous solutions. PVA/GO nanocomposites were also prepared for comparison. The structure, morphology, thermal, mechanical, water resistance and antibacterial properties of the samples were investigated as a function of GO and silver precursor contents. GO sheets decorated with spherical AgNPs were uniformly dispersed in the polymer matrix. The size range of most AgNPs was below 10 nm. ...
Source: Carbon - Category: Materials Science Source Type: research
In conclusion, potential biological applications of PF-SeNPs were explored by antibacterial, antifungal, antioxidant and biocompatibility assays. Materials and Methods Chemicals and Reagents Sodium selenite (98%), 2,2-diphenyl-1-picrylhydrazyl (DPPH), 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT), Tween 80, methanol, acetate buffer, tetracycline, nystatin, rhodamine 123, caspase-3 kit, Dulbecco’s modified Eagle media (DMEM), Folin-Ciocalteu reagent, 2,2-azinobis-(3-ethylbenzothiazoline-6-sulfonate) (ABTS), Dulbecco’s phosphate buffered saline pH 7.4 (DPBS) and fetal bovine serum (FBS) w...
Source: Frontiers in Microbiology - Category: Microbiology Source Type: research
Publication date: Available online 18 April 2019Source: Journal of Industrial and Engineering ChemistryAuthor(s): Katarina Nešović, Ana Janković, Aleksandra Perić-Grujić, Maja Vukašinović-Sekulić, Tamara Radetić, Ljiljana Živković, Soo-Jin Park, Kyong Yop Rhee, Vesna Mišković-StankovićAbstractSilver nanoparticles (AgNPs) were synthesized by in situ electrochemical reduction of Ag+ ions in poly(vinyl alcohol)/chitosan/graphene (PVA/CHI/Gr) hydrogel matrices with different concentrations of chitosan. The physicochemical properties of nanocomposite hydrogels were investigated by ultraviolet-vis...
Source: Journal of Industrial and Engineering Chemistry - Category: Chemistry Source Type: research
Conclusion γPGA-producing Bacillus spp. were isolated during fermentation of OSL and LOSL at 0–12 h. These isolates exhibited antibacterial and ACE inhibitory activities at different concentrations. The individual antibacterial activities of γPGA were bacteriostatic while the combined use exhibited bactericidal characteristics. Although the ACE inhibitory activities were low, OSL and LOSL are promising sources for developing functional microorganisms with a beneficial impact on health. The importance lies in the benefits derived from the use of local resources. Author Contributions TA contributed to th...
Source: Frontiers in Microbiology - Category: Microbiology Source Type: research
François Chassagne1†, Xinyi Huang1†, James T. Lyles1 and Cassandra L. Quave1,2* 1Center for the Study of Human Health, Emory University, Atlanta, GA, United States 2Department of Dermatology, Emory University, Atlanta, GA, United States In the search for new therapeutic solutions to address an increasing number of multidrug-resistant bacterial pathogens, secondary metabolites from plants have proven to be a rich source of antimicrobial compounds. Ginkgo biloba, a tree native to China, has been spread around the world as an ornamental tree. Its seeds have been used as snacks and medical mater...
Source: Frontiers in Microbiology - Category: Microbiology Source Type: research
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