scholarly journals Nigritanine as a New Potential Antimicrobial Alkaloid for the Treatment of Staphylococcus aureus-Induced Infections

Toxins ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 511 ◽  
Author(s):  
Bruno Casciaro ◽  
Andrea Calcaterra ◽  
Floriana Cappiello ◽  
Mattia Mori ◽  
Maria Loffredo ◽  
...  

Staphylococcus aureus is a major human pathogen causing a wide range of nosocomial infections including pulmonary, urinary, and skin infections. Notably, the emergence of bacterial strains resistant to conventional antibiotics has prompted researchers to find new compounds capable of killing these pathogens. Nature is undoubtedly an invaluable source of bioactive molecules characterized by an ample chemical diversity. They can act as unique platform providing new scaffolds for further chemical modifications in order to obtain compounds with optimized biological activity. A class of natural compounds with a variety of biological activities is represented by alkaloids, important secondary metabolites produced by a large number of organisms including bacteria, fungi, plants, and animals. In this work, starting from the screening of 39 alkaloids retrieved from a unique in-house library, we identified a heterodimer β-carboline alkaloid, nigritanine, with a potent anti-Staphylococcus action. Nigritanine, isolated from Strychnos nigritana, was characterized for its antimicrobial activity against a reference and three clinical isolates of S. aureus. Its potential cytotoxicity was also evaluated at short and long term against mammalian red blood cells and human keratinocytes, respectively. Nigritanine showed a remarkable antimicrobial activity (minimum inhibitory concentration of 128 µM) without being toxic in vitro to both tested cells. The analysis of the antibacterial activity related to the nigritanine scaffold furnished new insights in the structure–activity relationships (SARs) of β-carboline, confirming that dimerization improves its antibacterial activity. Taking into account these interesting results, nigritanine can be considered as a promising candidate for the development of new antimicrobial molecules for the treatment of S. aureus-induced infections.

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 717
Author(s):  
Rita Abou Nader ◽  
Rawan Mackieh ◽  
Rim Wehbe ◽  
Dany El El Obeid ◽  
Jean Marc Sabatier ◽  
...  

Honeybees are one of the most marvelous and economically beneficial insects. As pollinators, they play a vital role in every aspect of the ecosystem. Beehive products have been used for thousands of years in many cultures for the treatment of various diseases. Their healing properties have been documented in many religious texts like the Noble Quran and the Holy Bible. Honey, bee venom, propolis, pollen and royal jelly all demonstrated a richness in their bioactive compounds which make them effective against a variety of bacterial strains. Furthermore, many studies showed that honey and bee venom work as powerful antibacterial agents against a wide range of bacteria including life-threatening bacteria. Several reports documented the biological activities of honeybee products but none of them emphasized on the antibacterial activity of all beehive products. Therefore, this review aims to highlight the antibacterial activity of honey, bee venom, propolis, pollen and royal jelly, that are produced by honeybees.


2017 ◽  
Vol 37 (4) ◽  
pp. 368-378 ◽  
Author(s):  
Jusciêne B. Moura ◽  
Agueda C. de Vargas ◽  
Gisele V. Gouveia ◽  
João J. de S. Gouveia ◽  
Juracy C. Ramos-Júnior ◽  
...  

ABSTRACT: Cladonia substellata Vainio is a lichen found in different regions of the world, including the Northeast of Brazil. It contains several secondary metabolites with biological activity, including usnic acid, which has exhibited a wide range of biological activities. The aim of this study was to evaluate the in vitro antimicrobial activity of the organic extract of C. substellata and purified usnic acid. Initially, Staphylococcus spp., derived from samples of skin and ears of dogs and cats with suspected pyoderma and otitis, were isolated and analyzed. In antimicrobial susceptibility testing against Staphylococcus spp., 77% (105/136) of the isolates were resistant to the antimicrobials tested. In the assessment of biofilm production, 83% (113/136) were classified as producing biofilm. In genetic characterization, 32% (44/136) were positive for blaZ, no isolate (0/136) was positive for the mecA gene, and 2% (3/136) were positive for the icaD gene. The in vitro antimicrobial activity of the organic extract of C. substellata and purified usnic acid against Staphylococcus spp. ranged from 0.25mg/mL to 0.0019mg/mL, inhibiting bacterial growth at low concentrations. The substances were more effective against biofilm-producing bacteria (0.65mg/mL-0.42mg/mL) when compared to non-biofilm producing bacteria (2.52mg/mL-2.71mg/mL). Usnic acid and the organic extract of C. substellata can be effective in the treatment of pyoderma and otitis in dogs and cats caused by Staphylococcus spp.


2016 ◽  
Vol 6 (2) ◽  
pp. 70-76
Author(s):  
Soumia Keddari ◽  
Narimen Benaoum ◽  
Yasmina Mokhtaria Boufadi ◽  
Mansouria Belhocine ◽  
Ali Riazi

Medicinal plants have been used for countries as cures for human diseases because they contain components of therapeutic value. Among these medi-cinal plants, Ammi visnage which have an immense reservoir of potential compounds attributed to the secondary metabolites which have the advan-tage of being of great diversity of chemical structure and have a very wide range of biological activities. The objectives of the present work were to stu-dy the antioxidant and antimicrobial activity of phenolic compounds ex-tracted from A. visnaga L. Its extraction is performed by two methods, etha-nol extraction and water extraction. The results showed that A. visnaga L.. ethanolic extract contains a mixture of phytochemical classes as polyphenol, flavonoids and revealed that this plant has high antioxidant activity (IC50 0.069 mg/ml). Regarding the antimicrobial activity results expressed by the diameter of the inhibition zones by diffusion method AWDT, the most signifi-cant inhibition was observed against to Staphylococcus aureus (12 mm) to the ethanol extract at concentration of 100mg / ml. Thus the aqueous ex-tract had a significant inhibitory activity against on the strains Staphylococ-cus aureus (8 mm), E. coli ATCC 10536 (8 mm) to a concentration of 100 mg / ml. The results for the antibacterial properties have shown that Gram-positive bacteria (Staphylococcus aureus, Listeria monocytogenes and M. luteus.) were more sensitive than gram-negative (Pseudomonas aeruginosa, E. coli ATCC 10536) against from the action of phenolic compounds of the Ammi visnaga ethanolic extract.


2006 ◽  
Vol 50 (2) ◽  
pp. 806-809 ◽  
Author(s):  
Giuseppantonio Maisetta ◽  
Giovanna Batoni ◽  
Semih Esin ◽  
Walter Florio ◽  
Daria Bottai ◽  
...  

ABSTRACT The antimicrobial activity of human β-defensin 3 (hBD-3) against multidrug-resistant clinical isolates of Staphylococcus aureus, Enterococcus faecium, Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter baumannii was evaluated. A fast bactericidal effect (within 20 min) against all bacterial strains tested was observed. The presence of 20% human serum abolished the bactericidal activity of hBD-3 against gram-negative strains and reduced the activity of the peptide against gram-positive strains.


2019 ◽  
Vol 34 (1) ◽  
pp. 80-86 ◽  
Author(s):  
Dionyssia Papadopoulou ◽  
Alicja Dabrowska ◽  
Philip G. Harries ◽  
Jeremy S. Webb ◽  
Raymond N. Allan ◽  
...  

Background Chronic rhinosinusitis (CRS) is a common condition which affects the quality of life of millions of patients worldwide and has a significant impact on health-care resources. While Staphylococcus aureus bacterial biofilms play an important role in this disease, antimicrobial therapy is rarely effective and may promote antibiotic resistance. Thus, development of novel biofilm-targeting and antibiotic-sparing therapies is highly desirable and urgently required. Objective This in vitro study evaluated the antimicrobial activity of a novel synthetic honey-equivalent product which was designed to have the same reactive oxygen release profile as the engineered honey SurgihoneyRO™. Methods Treatment efficacy was investigated by assessment of planktonic growth, biofilm viability, thickness, and biomass using 12 CRS-related S. aureus mucosal bacterial strains. Results Both SurgihoneyRO™ and the synthetic honey-equivalent product inhibited growth of planktonic methicillin-resistant and methicillin-sensitive S. aureus strains, with the synthetic honey-equivalent product exhibiting a lower minimum inhibitory concentration. Treatment of established S. aureus biofilms reduced biofilm viability with 24-hour treatment resulting in a 2-log reduction in viability of biofilms formed by methicillin-resistant strains and a 1-log reduction in biofilms formed by methicillin-sensitive strains. Conclusions This preliminary study shows that the synthetic honey-equivalent product provides marked antimicrobial activity against S. aureus biofilms, with the potential for development in the clinical setting as an adjunctive biofilm-targeted therapy in CRS. The ultimate aim of such a product would be to reduce the need for antibiotics, steroids, and invasive surgical procedures in CRS patients as well as improving clinical outcomes following endoscopic sinus surgery.


2020 ◽  
Vol 17 (36) ◽  
pp. 18-31
Author(s):  
Ahmad khadem HACHIM ◽  
Rashid Rahim HATEET ◽  
Tawfik Muhammad MUHSIN

The purpose of the present work aimed at exploring the potential biochemical components and biological activities of an organic extract of the white truffle Tirmania nivea collected from the Iraqi desert, then test the organic extract against the Cytotoxicity on Human Larynx carcinoma cells and selected strains of pathogenic bacteria. Fourier transform infrared spectroscopy (FTIR) and gas chromatography-mass spectrometry GC/MSS were used to analyze mycochemical compositions. The antibacterial activity and Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) was investigated using a disk diffusion agar method. The truffle extract's cytotoxicity effect against the larynx cell line (Hep-2) was assessed by the MTT assay (in vitro). FTIR results provided the presence of phenol, carboxylic acid, and alkane's functional group, The GC-MS analysis of T. nivea disclose the existence of nineteen compounds that can contribute to the pharmaceutical properties of the truffle. As for antibacterial activity result, A growth inhibition activity of truffle extract at (18-40 mm inhibition zones) against the tested pathogenic bacterial strains was detected, which minimum inhibitory concentration values ranged from 3.12 to 6.25 mg/mL for Escherichia coli (ATCC 25922) and Staphylococcus aureus (ATCC 25923) Respectively. The results of cytotoxicity shown that the organic truffle extract exhibited a high inhibitory rate (52.685%) against cell line (Hep-2) at a concentration of 1.56 ?g/mL. In this work, the results showed that the organic extracts of T. nivea are very promising as cancer cytotoxicity and antibacterial agent for future medical applications.


2019 ◽  
Vol 65 (2) ◽  
pp. 99-102 ◽  
Author(s):  
Yu.V. Butina ◽  
T.V. Kudayarova ◽  
E.A. Danilova ◽  
M.K. Islyaikin

The work is devoted to predicting and studying biological properties of N-substituted analogs of 3,5-diamino-1,2,4-thiadiazole, which, in their turn, include in the composition of many drugs that exhibit a wide range of pharmacological actions. For searching of new alternative drugs with an antibacterial activity, but lacking resistance of microorganism strains to them, a computer screening of 2N-alkyl-substituted 5-amino-3-imino-1,2,4-thiadiazolines previously synthesized by us was carried out. The prediction of the spectrum of biological activity, as well as the determination of the probable toxicity of these compounds, was performed using the freely available computer programs PASS, Anti-Bac-Pred, and GUSAR. The study of the antibacterial activity in vitro against gram-positive (Staphylococcus aureus, Staphylococcus saprophyticus, Staphylococcus epidermidis) and gram-negative (Escherichia coli, Pseudomonas aeruginosae) bacterial strains was performed by the disco-diffusion method. Experimental data roughly correspond to the predictions.


Nanomaterials ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 286 ◽  
Author(s):  
Iris Usach ◽  
Elisabetta Margarucci ◽  
Maria Letizia Manca ◽  
Carla Caddeo ◽  
Matteo Aroffu ◽  
...  

Citrus species extracts are well known sources of bio-functional compounds with health-promoting effects. In particular, essential oils are known for their antibacterial activity due to the high content of terpenes. In this work, the steam-distilled essential oil from the leaves of Citrus limon var. pompia was loaded in phospholipid vesicles. The physico-chemical characteristics of the essential oil loaded vesicles were compared with those of vesicles that were loaded with citral, which is one of the most abundant terpenes of Citrus essential oils. The biocompatibility of the vesicles was assessed in vitro in human keratinocytes. Furthermore, the antimicrobial activity of the vesicles was tested while using different bacterial strains and a yeast: Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Candida albicans, respectively. The vesicles were small in size (~140 nm), slightly polydispersed (PI ~ 0.31), highly negatively charged (~ −73 mV), and able to incorporate high amounts of essential oil or citral (E% ~ 86%). Pompia essential oil and citral exhibited antimicrobial activity against all of the assayed microorganisms, with P. aeruginosa being the least sensitive. Citral was slightly more effective than pompia essential oil against E. coli, S. aureus, and C. albicans. The incorporation of citral in vesicles improved its antifungal activity against C. albicans.


2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Olayinka O. Ajani ◽  
Oluwole B. Familoni ◽  
Feipeng Wu ◽  
Johnbull O. Echeme ◽  
Zheng Sujiang

Sulfonamide drugs which have brought about an antibiotic revolution in medicine are associated with a wide range of biological activities. We have synthesized a series of α-tolylsulfonamide, 1–11 and their substituted N,N-diethyl-2-(phenylmethylsulfonamido) alkanamide derivatives, 12–22 in improved and excellent yields in aqueous medium at room temperature through highly economical synthetic routes. The chemical structures of the synthesized compounds 1–22 were confirmed by analytical and spectral data such as IR, 1H- and 13C-NMR, and mass spectra. The in vitro antibacterial activity of these compounds along with standard clinical reference, streptomycin, was investigated on two key targeted organisms. It was observed that 1-(benzylsulfonyl)pyrrolidine-2-carboxylic acid, 2 emerged as the most active compound against Staphylococcus aureus at MIC value of 1.8 μg/mL while 4-(3-(diethylamino)-3-oxo-2-(phenylmethylsulfonamido) propyl)phenyl phenylmethanesulfonate, 22 was the most active sulfonamide scaffold on Escherichia coli at MIC value of 12.5 μg/mL.


Materials ◽  
2021 ◽  
Vol 14 (11) ◽  
pp. 2723
Author(s):  
Łukasz Popiołek ◽  
Sylwia Szeremeta ◽  
Anna Biernasiuk ◽  
Monika Wujec

This research describes the synthesis and in vitro antimicrobial activity study of a series of 2,4,6-trimethylbenzenesulfonyl hydrazones. Twenty-five hydrazones (2–26) were synthesized on the basis of condensation reaction. The in vitro bioactivity study confirmed the potential application of obtained derivatives as antimicrobial agents. Among the tested compounds, the highest activity was discovered for derivative 24, which possessed minimal inhibitory concentration (MIC) ranging from 7.81 to 15.62 µg/mL against Gram-positive reference bacterial strains. Synthesized benzenesulfonyl hydrazones can be applied as potential ligands for the synthesis of bioactive metal complexes.


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