Natural products are widely used in different aspects of our lives - from household cleaners and food production, via cosmetics and aromatherapy, to both alternative and traditional medicine. In our research group, we have recently described several monoterpenoids with potential in the antiviral and anticancer therapy by allosteric targeting of aryl hydrocarbon receptor (AhR). Prior to any practical application, biological effects on human organism must be taken in concern. This review article is focused on the biological effects of 5 monoterpenoids on the human health previously identified as AhR antagonists with a therapeutic potential as antiviral and anticancer agents. We have thoroughly described cytotoxic, anti-inflammatory, anti-proliferative, and anticancer effects, as well as known interactions with nuclear receptors. As clearly demonstrated, monoterpenoids in general represent almost an inexhaustible reservoir of natural compounds possessing the ability to influence, modulate and improve human health.
- MeSH
- antitumorózní látky farmakologie terapeutické užití MeSH
- antivirové látky farmakologie terapeutické užití chemie MeSH
- lidé MeSH
- monoterpeny * farmakologie chemie terapeutické užití MeSH
- nádory farmakoterapie metabolismus MeSH
- receptory aromatických uhlovodíků * metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Thymus alternans and Teucrium montanum subsp. jailae are medicinal and aromatic plants, typical of Slovakian flora, producing bioactive essential oils. In the present study, we evaluated the insecticidal potential of the essential oils, obtained by hydrodistillation from the plant aerial parts and analysed by GC-MS, as insecticidal agents. For the purpose, they were assayed against three insect species acting as agricultural pests or vectors of medical relevance, such as the common housefly, Musca domestica L., the lymphatic filariasis vector, Culex quinquefasciatus and the Egyptian cotton leafworm Spodoptera littoralis; α-cypermethrin was tested as positive control. The two essential oils exhibited a different chemical profile, with monoterpenes and sesquiterpenes being the main fractions in the essential oils from Th. alternans and T. montanum subsp. jailae, respectively. Insecticidal tests showed that the T. montanum essential oil was effective against S. littoralis (LD50(90) = 56.7 (170.0) μg larva-1) and Cx. quinquefasciatus larvae (LC50(90) = 180.5 (268.7) mg L-1), whereas T. alternans essential oil displayed good toxicity against M. domestica adults (LD50(90) = 103.7 (223.9) μg adult-1). Overall, our results add useful knowledge about the potential of Slovakian flora as a source of botanicals for the eco-friendly management of insect pests and vectors.
- MeSH
- Culex účinky léků metabolismus MeSH
- insekticidy analýza farmakologie MeSH
- larva účinky léků metabolismus MeSH
- léčivé rostliny chemie MeSH
- monoterpeny analýza farmakologie MeSH
- moucha domácí účinky léků metabolismus MeSH
- oleje prchavé analýza farmakologie MeSH
- ožanka chemie MeSH
- plynová chromatografie s hmotnostně spektrometrickou detekcí MeSH
- pyrethriny analýza farmakologie MeSH
- seskviterpeny analýza farmakologie MeSH
- Spodoptera účinky léků metabolismus MeSH
- Thymus (rostlina) chemie MeSH
- zvířata MeSH
- Check Tag
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Geografické názvy
- Slovenská republika MeSH
Bark beetles kill apparently vigorous conifers during epidemics by means of pheromone-mediated aggregation. During non-endemic conditions the beetles are limited to use trees with poor defense, like wind-thrown. To find olfactory cues that help beetles to distinguish between trees with strong or weak defense, we collected volatiles from the bark surface of healthy felled or standing Picea abies trees. Furthermore, living trees were treated with methyl jasmonate in order to induce defense responses. Volatiles were analyzed by combined gas chromatography and electroantennographic detection (GC-EAD) on Ips typographus antennae. Compounds eliciting antennal responses were characterized by single sensillum recording for identification of specific olfactory sensory neurons (OSN). Release of monoterpene hydrocarbons decreased, while oxygenated compounds increased, from spring to early summer in felled trees. In both beetle sexes particular strong EAD activity was elicited by trace amounts of terpene alcohols and ketones. 4-Thujanol gave a very strong response and the absolute configuration of the tested natural product was assigned to be (+)-trans-(1R,4S,5S)-thujanol by stereoselective synthesis and enantioselective gas chromatography. One type of OSN responded to all ketones and five other OSN were characterized by the type of compounds that elicited responses. Three new OSN classes were found. Of the eight EAD-active compounds found in methyl jasmonate-treated bark, the known anti-attractant 1,8-cineole was the one most strongly induced. Our data support the hypothesis that highly active oxygenated host volatiles could serve as positive or negative cues for host selection in I. typographus and in other bark beetles.
- MeSH
- acetáty farmakologie MeSH
- brouci fyziologie MeSH
- cyklopentany farmakologie MeSH
- elektrofyziologické jevy účinky léků MeSH
- kůra rostlin chemie účinky léků metabolismus MeSH
- monoterpeny chemická syntéza chemie farmakologie MeSH
- oxylipiny farmakologie MeSH
- plynová chromatografie s hmotnostně spektrometrickou detekcí MeSH
- smrk chemie metabolismus MeSH
- stereoizomerie MeSH
- styren chemie farmakologie MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
Carvacrol and thymol, both plant-derived volatile compounds, have extensively been studied individually as well as in combination with other agents for their antimicrobial activity in liquid phase. However, in contrast to well-established assays for testing of antimicrobial combinatory effects in liquid media, there are no standardized methods for evaluation of interactions between volatile compounds in vapour phase. The objective of this study was to verify new broth volatilization chequerboard method by testing the combination of carvacrol and thymol and to determine in vitro inhibitory effect of these compounds in liquid and vapour phase against twelve Staphylococcus aureus strains. The new method, based on combination of standard microdilution chequerboard and new broth volatilization tests allowing calculation of fractional inhibitory concentrations (FICs), was used. Combination of carvacrol and thymol produced the additive antimicrobial effect against all strains tested. In several cases, they reached ΣFIC values lower than 0.6, which can be considered as a strong additive interaction. The best result was found in vapour phase against one standard strain at combination of 128 μg/mL of carvacrol and 16-256 μg/mL of thymol (ΣFIC = 0.51) and in liquid phase against one clinical isolate at combination of 256 μg/mL of carvacrol and 256 μg/mL of thymol (ΣFIC = 0.53). The study verified that the new technique is suitable for simple and rapid high-throughput combinatory antimicrobial screening of volatile compounds simultaneously in vapour and liquid phase and that it allows determination and comparison of MIC and FIC values in both, liquid and solid media.
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
The transient receptor potential vanilloid 3 (TRPV3) channel is a Ca2+-permeable thermosensitive ion channel widely expressed in keratinocytes, where together with epidermal growth factor receptor (EGFR) forms a signaling complex regulating epidermal homeostasis. Proper signaling through this complex is achieved and maintained via several pathways in which TRPV3 activation is absolutely required. Results of recent studies have suggested that low-level constitutive activity of TRPV3 induces EGFR-dependent signaling that, in turn, amplifies TRPV3 via activation of the mitogen-activated protein kinase ERK in a positive feedback loop. Here, we explored the molecular mechanism that increases TRPV3 activity through EGFR activation. We used mutagenesis and whole-cell patch clamp experiments on TRPV3 channels endogenously expressed in an immortalized human keratinocyte cell line (HaCaT) and in transiently transfected HEK293T cells and found that the sensitizing effect of EGFR on TRPV3 is mediated by ERK. We observed that ERK-mediated phosphorylation of TRPV3 alters its responsiveness to repeated chemical stimuli. Among several putative ERK phosphorylation sites, we identified threonine 264 in the N-terminal ankyrin repeat domain as the most critical site for the ERK-dependent modulation of TRPV3 channel activity. Of note, Thr264 is in close vicinity to a structurally and functionally important TRPV3 region comprising an atypical finger 3 and oxygen-dependent hydroxylation site. In summary, our findings indicate that Thr264 in TRPV3 is a key ERK phosphorylation site mediating EGFR-induced sensitization of the channel to stimulate signaling pathways involved in regulating skin homeostasis.
- MeSH
- epidermální růstový faktor metabolismus MeSH
- erbB receptory agonisté metabolismus MeSH
- fosforylace účinky léků MeSH
- HEK293 buňky MeSH
- interakční proteinové domény a motivy MeSH
- kationtové kanály TRPV agonisté chemie genetika metabolismus MeSH
- keratinocyty účinky léků enzymologie metabolismus MeSH
- lidé MeSH
- MAP kinasový signální systém * účinky léků MeSH
- metoda terčíkového zámku MeSH
- mitogenem aktivovaná proteinkinasa 3 chemie genetika metabolismus MeSH
- modulátory membránového transportu farmakologie MeSH
- monoterpeny farmakologie MeSH
- mutace MeSH
- mutageneze cílená MeSH
- posttranslační úpravy proteinů účinky léků MeSH
- rekombinantní proteiny chemie metabolismus MeSH
- sloučeniny boru farmakologie MeSH
- threonin metabolismus MeSH
- transformované buněčné linie MeSH
- upregulace * účinky léků MeSH
- zelené fluorescenční proteiny genetika metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
(-)-Linalool is the major floral scent occurring mainly in families Lamiaceae, Lauraceae and Rutaceae and is the main active compound of lavender oil. The purpose of this study was to reveal the influence of subchronic systemic treatment with (-)-linalool on the metabolic activity of CYP2A, 2B, 2C6, 2C11 and 3A in rat liver microsomes (RLM). The second aim was to reveal possible inhibitory effect of (-)-linalool on CYP2C6 in vitro. Wistar albino male rats were treated with (-)-linalool intragastrically at the doses of 40, 120, and 360 mg/kg/day for 13 days. Treatment with (-)-linalool at the dose of 360 mg/kg increased the metabolic activity of CYP2A assessed with testosterone as a probe substrate. (-)-Linalool showed weak competitive inhibition of CYP2C6 in rat liver microsomes, with IC(50) of 84 microM with use of diclofenac as a probe substrate.
- MeSH
- insekticidy farmakologie MeSH
- jaterní mikrozomy účinky léků enzymologie MeSH
- játra účinky léků enzymologie MeSH
- krysa rodu rattus MeSH
- monoterpeny farmakologie MeSH
- potkani Wistar MeSH
- systém (enzymů) cytochromů P-450 účinky léků metabolismus MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
The effect of the combination of α-pinene and β-caryophyllene on the proliferation of the Trypanosoma evansi was analyzed. These compounds were added individually and in combination at different concentrations to T. evansi cultures, and the in vivo study used mice of 1.0 and 1.5 mL kg−1 of α-pinene and β-caryophyllene individually and in combination against T. evansi. In order to evaluate the in vitro safety, lymphocytes and VERO cells were assessed using tetrazolium salt (MTT) assay. The trypanocidal effect of α-pinene and β-caryophyllene was observed in vitro when applied independently or combined at 0.5, 1 and 2% concentrations. The combination effect showed a faster trypanocidal effect when compared to chemotherapy (diminazene aceturate – D.A.). Concerning the in vivo evaluation, α-pinene + β-caryophyllene at 1.0 mL kg−1 was able to extend animal longevity and showed 83.33% curative efficacy, a superior result when compared to D.A. (16.66%). The MTT assay showed that the assessed compounds do not present toxicity to used cells. Also, in vivo safety evaluation of α-pinene + β-caryophyllene at 1.0 mL kg−1 not altered the aminotransferases levels in serum. Combination between α-pinene and β-caryophyllene shows in vitro and in vivo trypanocidal activity against T. evansi, in a safe dose.
- MeSH
- modely u zvířat MeSH
- monoterpeny aplikace a dávkování farmakologie chemie MeSH
- myši MeSH
- seskviterpeny aplikace a dávkování farmakologie chemie MeSH
- trypanocidální látky aplikace a dávkování MeSH
- Trypanosoma izolace a purifikace účinky léků MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- ženské pohlaví MeSH
- zvířata MeSH
BACKGROUND: Essential oil components (EOCs) are known for their antifungal properties; however, their high volatility limits their application as antimicrobial agents. Strategies used for controlling the volatility of EOCs include encapsulation or loading into porous materials. This study evaluated the in vitro antifungal activity of selected EOCs (carvacrol, cinnamaldehyde, eugenol and thymol) against the fungus Aspergillus niger when loaded into MCM-41 and β-cyclodextrin (β-CD). RESULTS: Carvacrol and thymol in Mobil Composition of Matter No. 41 (MCM-41) displayed remarkable enhanced antifungal properties in comparison to the pure or β-CD-encapsulated EOCs. In fact, carvacrol and thymol were able to maintain antifungal activity and inhibit fungal growth for 30 days, suggesting better applicability of these EOCs as natural preservatives. CONCLUSIONS: The sustained antifungal effect of EOCs encapsulated into silica mesoporous supports was described.
- MeSH
- antifungální látky chemie farmakologie MeSH
- Aspergillus niger účinky léků růst a vývoj MeSH
- beta-cyklodextriny MeSH
- cinnamáty chemie farmakologie MeSH
- konzervace potravin metody MeSH
- lidé MeSH
- monoterpeny chemie farmakologie MeSH
- oleje prchavé chemie farmakologie MeSH
- oleje rostlin chemie farmakologie MeSH
- oxid křemičitý MeSH
- potravinářská mikrobiologie MeSH
- potravinářské konzervační látky chemie farmakologie MeSH
- rostlinné extrakty chemie farmakologie MeSH
- volatilizace MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
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
- anisoly farmakologie MeSH
- azuleny farmakologie MeSH
- eugenol farmakologie MeSH
- mikrobiální testy citlivosti MeSH
- monoterpeny farmakologie MeSH
- Mycoplasma hominis účinky léků MeSH
- oleje prchavé farmakologie MeSH
- seskviterpeny farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
