Platinum(IV) compounds possess distinct properties that set them apart from platinum(II) compounds. Often designed as prodrugs, they are reduced within cancer cells to their active platinum(II) form, enabling their cytotoxic effects. Their versatility also lies in their ability to be functionalized and conjugated with bioactive molecules to enhance cancer cell targeting. This report introduces new prodrugs that combine antitumor cisplatin with axially coordinated eugenol, leveraging their synergistic action to target cancer stem cells. A third bioactive ligand, 4-phenylbutyrate or octanoate, was added to further enhance biological activity, creating 'triple action' prodrugs. These new platinum(IV) prodrugs offer a novel approach to cancer therapy by improving targeting, increasing efficacy, overcoming drug resistance, and reducing tumor invasiveness while sparing healthy tissue.
- Klíčová slova
- Cancer stem cells, Cisplatin, Eugenol, Platinum(IV), Spheroids,
- MeSH
- cisplatina * farmakologie chemie aplikace a dávkování MeSH
- eugenol * farmakologie chemie aplikace a dávkování MeSH
- lidé MeSH
- nádorové buněčné linie MeSH
- nádorové kmenové buňky * účinky léků patologie MeSH
- nádory tračníku * farmakoterapie patologie MeSH
- prekurzory léčiv * farmakologie chemie MeSH
- protinádorové látky * farmakologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- cisplatina * MeSH
- eugenol * MeSH
- prekurzory léčiv * MeSH
- protinádorové látky * MeSH
In the constant search for new pharmacological compounds, molecular hybridisation is a well-known technique whereby two or more known pharmacophoric subunits are combined to create a new "hybrid" compound. This hybrid is expected to maintain the characteristics of the original compounds whilst demonstrating improvements to their pharmacological action. Accordingly, we report here a series of molecular hybrid compounds based upon eugenol and chloramphenicol pharmacophores. The hybrid compounds were screened for their in vitro antimicrobial potential against Gram-negative and Gram-positive bacteria and also rapidly growing mycobacteria (RGM). The results highlight that the antimicrobial profiles of the hybrid compounds improve in a very clear fashion when moving through the series. The most prominent results were found when comparing the activity of the hybrid compounds against some of the multidrug-resistant clinical isolates of Pseudomonas aeruginosa, methicillin-resistant clinical isolates of Staphylococcus aureus (MRSA) and clinical isolates of rapidly growing mycobacteria.
- Klíčová slova
- Antimicrobial, Chloramphenicol, Eugenol, Hybridisation, Rapidly growing mycobacteria,
- MeSH
- antibakteriální látky terapeutické užití MeSH
- antiinfekční látky * farmakologie MeSH
- chloramfenikol farmakologie MeSH
- eugenol farmakologie MeSH
- farmakofor MeSH
- methicilin rezistentní Staphylococcus aureus * MeSH
- mikrobiální testy citlivosti MeSH
- Staphylococcus aureus MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- antibakteriální látky MeSH
- antiinfekční látky * MeSH
- chloramfenikol MeSH
- eugenol MeSH
Nanofibers have become a promising material in many industries in recent years, mainly due to their various properties. The only disadvantage of nanofibers as a potential filtration membrane is their short life due to clogging by bacteria in water treatment. The enrichment of nanofibers with active molecules could prevent these negative effects, represented by essential oils components such as Thymol, Eugenol, Linalool, Cinnamaldehyde and Carvacrol. Our study deals with the preparation of electrospun polyvinylidene difluoride (PVDF)-based nanofibers with incorporated essential oils, their characterization, testing their antibacterial properties and the evaluation of biofilm formation on the membrane surface. The study of the nanofibers' morphology points to the nanofibers' diverse fiber diameters ranging from 570 to 900 nm. Besides that, the nanofibers were detected as hydrophobic material with wettability over 130°. The satisfactory results of PVDF membranes were observed in nanofibers enriched with Thymol and Eugenol that showed their antifouling activity against the tested bacteria Escherichia coli ATCC 25922 and Staphylococcus aureus ATCC 25923. Therefore, these PVDF membranes could find potential applications as filtration membranes in healthcare or the environment.
- Klíčová slova
- PVDF, antibacterial activity, antifouling activity, essential oil, nanofiber,
- MeSH
- antibakteriální látky farmakologie chemie MeSH
- bioznečištění * prevence a kontrola MeSH
- Escherichia coli MeSH
- eugenol farmakologie MeSH
- nanovlákna * MeSH
- oleje prchavé * farmakologie MeSH
- thymol farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- antibakteriální látky MeSH
- eugenol MeSH
- oleje prchavé * MeSH
- polyvinylidene fluoride MeSH Prohlížeč
- thymol MeSH
Zein is renewable plant protein with valuable film-forming properties that can be used as a packaging material. It is known that the addition of natural cross-linkers can enhance a film's tensile properties. In this study, we aimed to prepare antimicrobial zein-based films enriched with monolaurin, eugenol, oregano, and thyme essential oil. Films were prepared using the solvent casting technique from ethanol solution. Their physicochemical properties were investigated using structural, morphological, and thermal techniques. Polar and dispersive components were analyzed using two models to evaluate the effects on the surface free energy values. The antimicrobial activity was proven using a disk diffusion method and the suppression of bacterial growth was confirmed via a growth kinetics study with the Gompertz function. The films' morphological characteristics led to systems with uniform distribution of essential oils or eugenol droplets combined with a flat-plated structure of monolaurin. A unique combination of polyphenolic eugenol and amphiphilic monoglyceride provided highly stretchable films with enhanced barrier properties and efficiency against Gram-positive and Gram-negative bacteria, yeasts, and molds. The prepared zein-based films with tunable surface properties represent an alternative to non-renewable resources with a potential application as active packaging materials.
- Klíčová slova
- antibacterial activity, essential oils, eugenol, film, mechanical properties, monoglyceride, wettability, zein,
- MeSH
- antibakteriální látky farmakologie MeSH
- antifungální látky farmakologie MeSH
- biomechanika účinky léků MeSH
- diferenciální skenovací kalorimetrie MeSH
- Escherichia coli účinky léků MeSH
- eugenol farmakologie MeSH
- laurany farmakologie MeSH
- mikroskopie atomárních sil MeSH
- monoglyceridy farmakologie MeSH
- obaly potravin * MeSH
- oleje prchavé farmakologie MeSH
- pára MeSH
- permeabilita MeSH
- povrchové vlastnosti MeSH
- smáčivost MeSH
- spektroskopie infračervená s Fourierovou transformací MeSH
- Staphylococcus aureus účinky léků MeSH
- zein farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- antibakteriální látky MeSH
- antifungální látky MeSH
- eugenol MeSH
- laurany MeSH
- monoglyceridy MeSH
- monolaurin MeSH Prohlížeč
- oleje prchavé MeSH
- pára MeSH
- zein MeSH
The onion thrips, Thrips tabaci Lindeman (Thysanoptera: Thripidae), is a polyphagous pest that causes serious damage to agricultural crops, vegetables, and ornamental plants worldwide. Farmers rely on the extensive usage of synthetic chemical insecticides to control T. tabaci. There is a dire need to develop alternative control strategies to overcome the problems posed by chemical insecticides. Efficient traps would allow sensitive monitoring and possibly mass trapping. A field experiment was conducted to evaluate the potential of three plant compounds with known release rates (ranging from 6-30 mg/d); eugenol (Eug), 1, 8-cineole (eucalyptol), and linalool in all possible combinations with a thrips attractant, ethyl iso-nicotinate (EI). A combination of EI with Eug increased the effect of EI by attracting 100% more thrips (effect size, 1.95) as compared to the control of EI alone. Catches in remaining treatments were lower and or not significantly different from EI alone. The results from our study could be used to develop improved volatile blends to be used for monitoring traps. Our data suggests that these traps could be effective even at very low populations.
- MeSH
- acyklické monoterpeny MeSH
- eugenol farmakologie MeSH
- feromony farmakologie MeSH
- kyseliny isonikotinové farmakologie MeSH
- monoterpeny farmakologie MeSH
- synergismus léků MeSH
- Thysanoptera účinky léků MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- hodnotící studie MeSH
- práce podpořená grantem MeSH
- Názvy látek
- acyklické monoterpeny MeSH
- ethyl isonicotinate MeSH Prohlížeč
- eugenol MeSH
- feromony MeSH
- insect attractants MeSH Prohlížeč
- kyseliny isonikotinové MeSH
- linalool MeSH Prohlížeč
- monoterpeny MeSH
The rise of the mosquitoes-transmitted diseases, like dengue, zika and chikungunya in Brazil in the last years has increased concerns on protection against mosquitoes bites. However, the prohibitive prices of the commercially available repellents for the majority of the Brazilian population has provoked a search for cheaper solutions, like the use of the homemade ethanolic extract of Indian clove (Syzygium aromaticum L.) as repellent, which has been reported as quite efficient by the local press. In order to verify this, we performed here the quantification of the main components of this extract through high-performance thin-layer chromatography (HPTLC)-densitometry and evaluated its efficiency as a repellent and its acetylcholinesterase (AChE) inhibition capacity. Our results have proved HPTLC-densitometry as an efficient and appropriate method for this quantification and confirmed the repellency activity, as well as its capacity of AChE inhibition.
- Klíčová slova
- Aedes aegypti, Syzygium aromaticum L, anticholinesterase, eugenol, insect repellent,
- MeSH
- acetylcholinesterasa metabolismus MeSH
- Aedes účinky léků MeSH
- cholinesterasové inhibitory * analýza chemie farmakologie MeSH
- chování zvířat účinky léků MeSH
- chromatografie na tenké vrstvě metody MeSH
- denzitometrie MeSH
- dospělí MeSH
- eugenol analýza chemie farmakologie MeSH
- lidé MeSH
- limita detekce MeSH
- lineární modely MeSH
- mladý dospělý MeSH
- repelenty proti hmyzu * analýza chemie farmakologie MeSH
- reprodukovatelnost výsledků MeSH
- rostlinné extrakty * analýza chemie farmakologie MeSH
- Syzygium chemie MeSH
- zvířata MeSH
- Check Tag
- dospělí MeSH
- lidé MeSH
- mladý dospělý MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- acetylcholinesterasa MeSH
- cholinesterasové inhibitory * MeSH
- eugenol MeSH
- repelenty proti hmyzu * MeSH
- rostlinné extrakty * MeSH
Cronobacter sakazakii and C. malonaticus are opportunistic pathogens that cause infections in children and immunocompromised adults. In the present study, the antibacterial activity of 19 plant-derived compounds, 5 essential oils, and an extract of propolis were assessed against C. sakazakii and C. malonaticus. The effects of most of these antimicrobials have not been reported previously. Both strains were susceptible to thymol, carvacrol, thymoquinone, p-cymene, linalool, camphor, citral, eugenol, and trans-cinnamaldehyde as well as cinnamon, lemongrass, oregano, clove, and laurel essential oils; their minimum inhibitory concentrations varied between 0.1 and 2.0 mg/mL. As an alternative treatment method, vapors of the volatiles were tested as an indirect treatment. Vapors of trans-cinnamaldehyde, eugenol, oregano, and cinnamon essential oils inhibited both tested strains, while vapors of linalool were only active against C. sakazakii. To our knowledge, this study is the first time that the inhibitory activity of the vapors of these compounds and essential oils has been reported against Cronobacter spp.
- MeSH
- acyklické monoterpeny MeSH
- akrolein analogy a deriváty chemie farmakologie MeSH
- antibakteriální látky chemie farmakologie MeSH
- benzochinony chemie farmakologie MeSH
- Cronobacter sakazakii účinky léků MeSH
- Cronobacter účinky léků MeSH
- Cymbopogon chemie MeSH
- cymeny MeSH
- dobromysl (rod) chemie MeSH
- eugenol chemie farmakologie MeSH
- kafr chemie farmakologie MeSH
- mikrobiální testy citlivosti MeSH
- monoterpeny chemie farmakologie MeSH
- oleje prchavé chemie farmakologie MeSH
- oleje rostlin chemie farmakologie MeSH
- rostlinné extrakty chemie farmakologie MeSH
- seskviterpeny chemie farmakologie MeSH
- skořicovník ceylonský chemie MeSH
- Syzygium chemie MeSH
- thymol chemie farmakologie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 4-cymene MeSH Prohlížeč
- acyklické monoterpeny MeSH
- akrolein MeSH
- antibakteriální látky MeSH
- benzochinony MeSH
- carvacrol MeSH Prohlížeč
- cinnamaldehyde MeSH Prohlížeč
- citral MeSH Prohlížeč
- cymeny MeSH
- eugenol MeSH
- kafr MeSH
- laurel oil MeSH Prohlížeč
- linalool MeSH Prohlížeč
- monoterpeny MeSH
- oleje prchavé MeSH
- oleje rostlin MeSH
- rostlinné extrakty MeSH
- seskviterpeny MeSH
- thymol MeSH
- thymoquinone MeSH Prohlížeč
AIMS: The aim of this study was to evaluate the antimicrobial effects of five natural substances against 50 clinical isolates of Mycoplasma hominis. METHODS AND RESULTS: The in vitro activity of selected natural compounds, cinnamon bark oil, anethole, carvacrol, eugenol and guaiazulene, was investigated against 50 M. hominis isolates cultivated from cervical swabs by the broth dilution method. All showed valuable antimicrobial activity against the tested isolates. Oil from the bark of Cinnamomum zeylanicum (MBC90 = 500 µg/mL) however was found to be the most effective. Carvacrol (MBC90 = 600 µg/mL) and eugenol (MBC90 = 1000 µg/mL) also possessed strong antimycoplasmal activity. CONCLUSIONS: The results indicate that cinnamon bark oil, carvacrol and eugenol have strong antimycoplasmal activity and the potential for use as antimicrobial agents in the treatment of mycoplasmal infections.
- MeSH
- allylbenzenové deriváty MeSH
- anisoly farmakologie MeSH
- azuleny farmakologie MeSH
- cymeny MeSH
- eugenol farmakologie MeSH
- mikrobiální testy citlivosti MeSH
- monoterpeny farmakologie MeSH
- Mycoplasma hominis účinky léků MeSH
- oleje prchavé farmakologie MeSH
- seskviterpeny guajanové MeSH
- seskviterpeny farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- allylbenzenové deriváty MeSH
- anethole MeSH Prohlížeč
- anisoly MeSH
- azuleny MeSH
- carvacrol MeSH Prohlížeč
- cinnamon oil, bark MeSH Prohlížeč
- cymeny MeSH
- eugenol MeSH
- guaiazulene MeSH Prohlížeč
- monoterpeny MeSH
- oleje prchavé MeSH
- seskviterpeny guajanové MeSH
- seskviterpeny MeSH
The inhibitory effect of some plant oil aromatics against three strains of Arcobacter butzleri, two strains of Arcobacter cryaerophilus, and one strain of Arcobacter skirrowii was evaluated. When MICs were determined using the broth macrodilution method, cinnamaldehyde was most inhibitory followed by thymol, carvacrol, caffeic acid, tannic acid, and eugenol (P < 0.001). Sublethal concentrations of the three most potent plant oil aromatics also were examined. Overall, cinnamaldehyde was the most bacteriostatic against all arcobacters tested except A. butzleri when these strains were exposed to the MIC25 of this aromatic aldehyde. The bacteriostatic activities of thymol and carvacrol were concentration and species dependent.
- MeSH
- akrolein analogy a deriváty farmakologie MeSH
- Arcobacter účinky léků růst a vývoj MeSH
- cymeny MeSH
- druhová specificita MeSH
- eugenol farmakologie MeSH
- konzervace potravin metody MeSH
- kyseliny kávové farmakologie MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- monoterpeny farmakologie MeSH
- oleje rostlin chemie farmakologie MeSH
- počet mikrobiálních kolonií MeSH
- potravinářské konzervační látky farmakologie MeSH
- spotřebitelská bezpečnost produktů MeSH
- taniny farmakologie MeSH
- thymol farmakologie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- akrolein MeSH
- caffeic acid MeSH Prohlížeč
- carvacrol MeSH Prohlížeč
- cinnamaldehyde MeSH Prohlížeč
- cymeny MeSH
- eugenol MeSH
- kyseliny kávové MeSH
- monoterpeny MeSH
- oleje rostlin MeSH
- potravinářské konzervační látky MeSH
- taniny MeSH
- thymol MeSH
Inhibitory effects of compounds with guaiacyl and syringyl structure, representing the structure of native lignin, were studied on model cultures of bacteria, yeasts, yeast-like microorganisms and moulds. Isoeugenol exhibited the most pronounced inhibitory effect on growth of the studied microorganisms.
- MeSH
- antibakteriální látky farmakologie MeSH
- antifungální látky farmakologie MeSH
- Aspergillus niger účinky léků MeSH
- Bacillus účinky léků MeSH
- Candida albicans účinky léků MeSH
- chemické jevy MeSH
- chemie MeSH
- Escherichia coli účinky léků MeSH
- eugenol farmakologie MeSH
- guajakol analogy a deriváty farmakologie MeSH
- isomerie MeSH
- kyselina gallová analogy a deriváty farmakologie MeSH
- lignin analogy a deriváty analýza farmakologie MeSH
- Micrococcus účinky léků MeSH
- mikrobiální testy citlivosti MeSH
- Saccharomyces cerevisiae účinky léků MeSH
- terpeny farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- antibakteriální látky MeSH
- antifungální látky MeSH
- eugenol MeSH
- guajakol MeSH
- kyselina gallová MeSH
- lignin MeSH
- terpeny MeSH
