Anaplastic Large Cell Lymphoma (ALCL) is an aggressive T-cell lymphoma affecting children and young adults. About 30% of patients develop therapy resistance therefore new precision medicine drugs are highly warranted. Multiple rounds of structure-activity optimization of Caffeic Acid Phenethyl Ester have resulted in CM14. CM14 causes upregulation of genes involved in oxidative stress response and downregulation of DNA replication genes leading to G2/M arrest and subsequent apoptosis induction. In accordance with this, an unbiased proteomics approach, confocal microscopy and molecular modeling showed that TUBGCP2, member of the centrosomal γ-TuRC complex, is a direct interaction partner of CM14. CM14 overcomes ALK inhibitor resistance in ALCL and is also active in T-cell Acute Lymphoblastic Leukemia and Acute Myeloid Leukemia. Interestingly, CM14 also induced cell death in docetaxel-resistant prostate cancer cells thus suggesting an unexpected role in solid cancers. Thus, we synthesized and thoroughly characterized a novel TUBGCP2 targeting drug that is active in ALCL but has also potential for other malignancies.

• MeSH
• apoptóza * účinky léků   MeSH
• centrozom * účinky léků   metabolismus   MeSH
• fenethylalkohol * analogy a deriváty   farmakologie   chemie   MeSH
• kyseliny kávové * farmakologie   chemie   MeSH
• lidé MeSH
• nádorové buněčné linie MeSH
• proliferace buněk účinky léků   MeSH
• protinádorové látky * farmakologie   chemie   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH

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.

• MeSH
• cisplatina * farmakologie   MeSH
• eugenol * farmakologie   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   chemie   MeSH
• synergismus léků MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články 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.

• 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

• MeSH
• eugenol MeSH
• kempferoly MeSH
• léčivé rostliny MeSH
• lidé MeSH
• Syzygium * MeSH
• Check Tag
• lidé 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.

• 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

Phytochemical investigations of Matricaria chamomilla L. (Asteraceae) stated the presence of several compounds with an established therapeutic and antioxidant potential. The chamomile non-enzymatic antioxidant system includes low molecular mass compounds, mainly polyphenols such as cinnamic, hydroxybenzoic and chlorogenic acids, flavonoids and coumarins. The objective of this work was to evaluate the role of the non-enzymatic antioxidant system after stimulation by ethylene in tetraploid chamomile plants. Seven days of ethylene treatment significantly increased the activity of phenylalanine ammonia-lyase, which influenced the biosynthesis of protective polyphenols in the first step of their biosynthetic pathway. Subsequently, considerable enhanced levels of phenolic metabolites with a substantial antioxidant effect (syringic, vanillic and caffeic acid, 1,5-dicaffeoylquinic acid, quercetin, luteolin, daphnin, and herniarin) were determined by HPLC-DAD-MS. The minimal information on the chlorogenic acids function in chamomile led to the isolation and identification of 5-O-feruloylquinic acid. It is accumulated during normal conditions, but after the excessive effect of abiotic stress, its level significantly decreases and levels of other caffeoylquinic acids enhance. Our results suggest that ethephon may act as a stimulant of the production of pharmaceutically important non-enzymatic antioxidants in chamomile leaves and thus, lead to an overall change in phytochemical content and therapeutic effects of chamomile plants, as well.

• MeSH
• antioxidancia metabolismus   MeSH
• biosyntetické dráhy fyziologie   MeSH
• ethyleny metabolismus   MeSH
• fenoly metabolismus   MeSH
• fenylalaninamoniaklyasa metabolismus   MeSH
• fyziologický stres fyziologie   MeSH
• heřmánek, heřmánkovec, rmen, rmenec metabolismus   MeSH
• kyselina chinová analogy a deriváty   metabolismus   MeSH
• kyselina chlorogenová metabolismus   MeSH
• kyseliny kávové metabolismus   MeSH
• listy rostlin metabolismus   MeSH
• Matricaria metabolismus   MeSH
• polyfenoly metabolismus   MeSH
• rostlinné extrakty metabolismus   MeSH
• Publikační typ
• časopisecké články MeSH

Úvod a ciel´: Súčasná endodoncia má k dispozícii nespočetné množstvo materiálov, určených k definitívnemu plneniu koreňových kanálikov, ktoré sa líšia svojím zložením a tiež aj svojimi fyzikálnymi, chemickými a biologickými vlastnosťami. Dentálny trh sa snaží o sústavnú inováciu niektorých materiálov úpravou ich zloženia, čo má za následok zmenu vlastností nových preparátov. Úlohou tohto článku je porovnať vybrané vlastnosti súčasných endodontických sealerov, a sprehľadniť tak klinickým pracovníkom situáciu, ktorá momentálne na trhu s týmito materiálmi panuje. V prvej časti tohto článku sa pojednáva o materiáloch založených na hydroxide vápenatom, zinkoxid eugenole, a na záver je pozornosť venovaná zlatému štandardu v endodoncii – polyepoxidovým materiálom. Pri porovnávaní jednotlivých vlastností týchto materiálov bola sledovaná ich doba tuhnutia, pH pri tuhnutí, radioopacita, rozpustnosť a náchylnosť k vzniku netesností koreňovej výplne v čase, objemové zmeny prebiehajúce pri a po stuhnutí týchto materiálov, cytotoxicita, antibakteriálne vlastnosti a schopnosť týchto materiálov zafarbovať tvrdé zubné tkanivá. Metódy, materiály: Porovnaním jednotlivých vlastností týchto materiálov možno konštatovať, že každý zo súčasných endodontických sealerov vyniká vlastnosťami, ktorými sa od ostatných výrazne odlišuje. Sealery na báze hydroxidu vápenatého vynikajú predovšetkým výrazným antibakteriálnym pôsobením a nízkou náchylnosťou k zafarbovaniu tvrdých zubných tkanív a nízkou, prípadne miernou cytotoxicitou, spôsobenou ich vysokým pH, prípadne ďalšími látkami obsiahnutými v zložení sealeru, naopak ale ich vysoká rozpustnosť a náchylnosť k vzniku netesností výrazne zhoršuje kvalitu koreňovej výplne. Zinkoxid eugenolové sealery majú výborné antibakteriálne vlastnosti, len v prvých dňoch svojho pôsobenia, ale negatívne ovplyvňujú prognózu endodontického ošetrenia svojou vysokou náchylnosťou k vzniku netesností a cytotoxicitou a taktiež nepriaznivo ovplyvňujú zafarbenie zvyšných tvrdých zubných tkanív. Polyepoxidové sealery svojou nízkou rozpustnosťou a nízkou náchylnosťou k vzniku netesností sú zárukou kvalitnej koreňovej výplne, avšak ich antibakteriálne vlastnosti sú len krátkodobé. Ich vysoká cytotoxicita nepriaznivo vplýva na bunky periapikálneho periodoncia a je vysoká náchylnosť k zafarbovaniu tvrdých zubných tkanív. Pri nedostatočnom odstránení prebytkov sealeru sa zhoršuje estetika endodonticky preliečeného zubu. Záver: Výber vhodného materiálu nie je jednoduchý a klinický pracovník musí zvážiť, ktoré z vlastností bude pri tomto výbere preferovať a ktorým bude naopak pripisovať menšiu mieru dôležitosti.

Introduction and aims: Today's endodontics has at its disposal a myriad of materials intended for the definitive filling of root canals, which differ in their composition as well as in their physical, chemical and biological properties. The dental market strives for continuous innovation of some materials by modifying their composition, which results in a change in the properties of new preparations. The aim of this article is to compare selected properties of current endodontic sealers and thus make it clear to clinicians about the current situation on the market with these materials. The first part of this article deals with materials based on calcium hydroxide, zinc oxide eugenol and finally, attention was paid to the gold standard in endodontics – polyepoxide material. When comparing the individual properties of these materials, their setting time, pH during solidification, radiopacity, solubility and susceptibility to root filling leaks over time, volume changes occurring during and after solidification of these materials, cytotoxicity, antibacterial properties and ability of these materials to color hard teeth were monitored tissues. Methods, materials: By comparing the individual properties of these materials, it can be stated that each of the current endodontic sealers excels in properties that significantly differ from the others. Sealers based on calcium hydroxide thus excel mainly in strong antibacterial action and low susceptibility to discoloration of hard dental tissues and low or mild cytotoxicity due to their high pH, or other substances contained in the sealer composition, but their high solubility and susceptibility to leaks significantly deteriorates the quality of the root filling. Zinc oxide eugenol sealers have excellent antibacterial properties, but only in the first days of their action, but on the other hand they negatively affect the prognosis of endodontic treatment with their high susceptibility to leaks and cytotoxicity and also adversely affect the staining of remaining hard dental tissues. Polyepoxide sealers, due to their low solubility and low susceptibility to leakage, guarantee a quality root filling, but their antibacterial properties, however high, are only short-lived, their high cytotoxicity adversely affects periapical periodontal cells and high susceptibility to hard tooth discoloration. Excess of sealer worsens the aesthetics of an endodontically treated tooth. Conclusion: The selection of a suitable material is therefore not easy and the clinician must consider which of the properties he will prefer in this selection and which he will instead attribute less importance to.

• Klíčová slova
• polyepoxid,
• MeSH
• eugenol MeSH
• hydroxid vápenatý MeSH
• lidé MeSH
• pečetidlo pro jamky a fisury * MeSH
• zubní materiály MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• přehledy 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.

• 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

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
• 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

Warfarin is a commonly used anticoagulant drug and is a derivate of coumarin. Cytochrome P450 2C9 (CYP2C9) plays the key role in transformation of coumarin and thus, influences determination of warfarin dosage. A number of factors including dietary compounds such as sesamin, caffeic acid and ferulic acids can regulate the activity of CYP2C9. The present study tested the hypothesis that sesamin, episesamin, caffeic acid and ferulic acid decreases the rate of warfarin 7-hydroxylation via inhibition of hepatic CYP2C9. The experiments were conducted on hepatic microsomes from human donors. It was demonstrated that the rate of 7-hydroxylation of warfarin was significantly decreased in the presence of sesamin in the range of concentrations from 5 to 500 nM, and was not affected by episesamin, caffeic acid and ferulic acid in the same range of concentrations. The kinetic analysis indicated non-competitive type of inhibition by sesamin with Ki = 202 ± 18 nM. In conclusion, the results of our in vitro study revealed that sesamin was able to inhibit formation of a major metabolite of warfarin, 7-hydroxywarfarin. The potentially negative consequences of the consumption of high amounts of sesamin-containing food or dietary supplements in warfarin-treated patients need to be further studied.

• MeSH
• antikoagulancia metabolismus   MeSH
• dioxoly chemie   farmakologie   MeSH
• hydroxylace MeSH
• inhibiční koncentrace 50 MeSH
• jaterní mikrozomy metabolismus   MeSH
• kinetika MeSH
• kyseliny kávové farmakologie   MeSH
• kyseliny kumarové farmakologie   MeSH
• lidé MeSH
• lignany chemie   farmakologie   MeSH
• potraviny MeSH
• potravní doplňky MeSH
• warfarin metabolismus   MeSH
• Check Tag
• lidé MeSH
• mužské pohlaví MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH