The emergence of biofilm-induced drug tolerance poses a critical challenge to public healthcare management. Pseudomonas aeruginosa, a gram-negative opportunistic bacterium, is involved in various biofilm-associated infections in human hosts. Towards this direction, in the present study, a combinatorial approach has been explored as it is a demonstrably effective strategy for managing microbial infections. Thus, P. aeruginosa has been treated with cuminaldehyde (a naturally occurring phytochemical) and gentamicin (an aminoglycoside antibiotic) in connection to the effective management of the biofilm challenges. It was also observed that the test molecules could show increased antimicrobial activity against P. aeruginosa. A fractional inhibitory concentration index (FICI) of 0.65 suggested an additive interaction between cuminaldehyde and gentamicin. Besides, a series of experiments such as crystal violet assay, estimation of extracellular polymeric substance (EPS), and microscopic images indicated that an enhanced antibiofilm activity was obtained when the selected compounds were applied together on P. aeruginosa. Furthermore, the combination of the selected compounds was found to reduce the secretion of virulence factors from P. aeruginosa. Taken together, this study suggested that the combinatorial application of cuminaldehyde and gentamicin could be considered an effective approach towards the control of biofilm-linked infections caused by P. aeruginosa.

• Klíčová slova
• Pseudomonas aeruginosa, Antibiofilm, Antimicrobial, Cuminaldehyde, Gentamicin,
• MeSH
• antibakteriální látky * farmakologie   MeSH
• benzaldehydy * farmakologie   MeSH
• biofilmy * účinky léků   MeSH
• cymeny farmakologie   MeSH
• faktory virulence MeSH
• gentamiciny * farmakologie   MeSH
• lidé MeSH
• mikrobiální testy citlivosti * MeSH
• Pseudomonas aeruginosa * účinky léků   fyziologie   MeSH
• synergismus léků MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antibakteriální látky * MeSH
• benzaldehydy * MeSH
• cuminaldehyde MeSH Prohlížeč
• cymeny MeSH
• faktory virulence MeSH
• gentamiciny * MeSH

Bacterial blight is a serious disease of carrot production worldwide. Under favorable conditions, the causal organism Xanthomonas hortorum pv. carotae causes serious loss especially in seed production because of its seed-borne character. Unlike fungal diseases, the treatment of bacterial diseases is limited and methods such as hot water or sodium hypochlorite (bleach) treatment are mainly used by seed companies. Here, we compared the efficacy of hot water treatment, sodium hypochlorite treatment and treatment with three phenolic compounds-carvacrol, thymol and eugenol, to eliminate Xanthomonas growth in vitro and subsequently in vivo on seeds of Xhc low, medium and highly infested carrot seed lots. The complete elimination of Xhc from germinated plants was obtained only for Xhc low infested seed lot with 1% sodium hypochlorite and carvacrol solutions in concentrations of 0.0196%- 0.313%. The significant reduction of Xhc presence in germinated plants of Xhc medium infested seed lot was achieved with 1% sodium hypochlorite treatment and hot water treatment. However, hot water treatment resulted in a significant reduction of seed germination percentage as well. Considering the elimination of Xhc infection from germinated plants and the effect on seed germination and plant vigor, 0.0196% carvacrol solution was suggested as an alternative to 1% sodium hypochlorite treatment regarding additional costs related to the liquidation of used treated water and to hot water treatment that has been proved to be insufficient to obtain disease-free plants.

• MeSH
• chlornan sodný farmakologie   MeSH
• cymeny MeSH
• mrkev obecná * MeSH
• semena rostlinná mikrobiologie   MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• carvacrol MeSH Prohlížeč
• chlornan sodný MeSH
• cymeny MeSH

Carbapenem resistance observed in Klebsiella pneumoniae strains limits treatment options. Therefore, use of antibiotics combined with bioactive compounds may be an important strategy to control K. pneumoniae. The purpose of this study was to evaluate the activity of combination of carvacrol and meropenem on carbapenem-resistant K. pneumoniae (CRKP) strains. The presence of blaOXA-48 carbapenemase in all 25 CRKP strains was identified using the PCR technique. The combination of carvacrol and meropenem was tested for antimicrobial activity on CRKP strains. The minimum inhibitory concentrations of carvacrol and meropenem were detected within a range of 32-128 µg/mL using the broth microdilution method. Synergy between carvacrol and meropenem was observed on 8 of the 25 CRKP strains by checkerboard assay (FICI = 0.5) and confirmed by time-kill assay. According to the live-dead test results, the viability percentage of the cells exposed to synergistic combination was 35.47% at the end of 24 h. The membrane damage caused by the synergistic combination was spectrophotometrically measured (A = 0.21) and further confirmed by SEM analysis. According to the MTT assay, both carvacrol and meropenem did not show any statistically significant cytotoxic effect on Vero cells (p > 0.05). In conclusion, the results suggest that carvacrol and meropenem can act synergistically to inhibit the growth of CRKP.

• MeSH
• antibakteriální látky farmakologie   MeSH
• beta-laktamasy * genetika   MeSH
• Cercopithecus aethiops MeSH
• cymeny MeSH
• karbapenemy farmakologie   MeSH
• Klebsiella pneumoniae * MeSH
• meropenem farmakologie   MeSH
• mikrobiální testy citlivosti MeSH
• synergismus léků MeSH
• Vero buňky MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antibakteriální látky MeSH
• beta-laktamasy * MeSH
• carvacrol MeSH Prohlížeč
• cymeny MeSH
• karbapenemy MeSH
• meropenem MeSH

Carvacrol (CAR) is a natural bioactive compound with antioxidant and antimicrobial activity that is present in essential oils. The application of CAR in food preservation is hampered by its high volatility, low solubility in water, and susceptibility to light, heat and oxygen degradation. Polylactide (PLA) is an FDA-approved polymer derived from renewable resources. Controlled release of CAR from PLA nanoparticles (NPs) could improve its antimicrobial efficacy and storage. In this study, negatively charged CAR-NPs and positively charged polyethylenimine (PEI)-coated CAR-(PEI)NPs were formulated by nanoprecipitation methods and characterised by dynamic light scattering, electron microscopy, encapsulation efficiency, and drug loading capacity. The positively charged (PEI)NPs enhanced the in vitro antimicrobial activity of CAR against Escherichia coli, Listeria monocytogenes, Salmonella enterica and Staphylococcus aureus. Bacterial uptake, evaporation tests, release studies and NP stability after storage were assessed to provide evidence supporting CAR-(PEI)NPs as a potential nanocarrier for further development in food preservation.

• Klíčová slova
• Acetone (PubChem CID: 180), Antimicrobial nanoparticles, Carvacrol, Carvacrol (PubChem CID: 10364), Food preservatives, PEI-coating, PLA, Polyethylenimine (PEI) (CID: 86276476), Polylactide (PubChem CID: 11039), Polyvinyl alcohol (PubChem CID: 11199), Tetrahydrofuran (PubChem CID: 7272), rac-lactide (PubChem CID: 7272),
• MeSH
• antibakteriální látky chemie   farmakologie   MeSH
• cymeny chemie   farmakokinetika   farmakologie   MeSH
• Escherichia coli účinky léků   MeSH
• Listeria monocytogenes MeSH
• mikrobiální testy citlivosti MeSH
• nanočástice chemie   MeSH
• nosiče léků chemie   MeSH
• polyestery chemie   MeSH
• polyethylenimin chemie   MeSH
• potravinářská mikrobiologie MeSH
• rozpustnost MeSH
• Salmonella enterica účinky léků   MeSH
• Staphylococcus aureus účinky léků   MeSH
• velikost částic MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antibakteriální látky MeSH
• carvacrol MeSH Prohlížeč
• cymeny MeSH
• nosiče léků MeSH
• poly(lactide) MeSH Prohlížeč
• polyestery MeSH
• polyethylenimin MeSH

Aluminum accumulation, glutathione (GSH) and malondialdehyde (MDA) concentrations as well as catalase (CAT) and superoxide dismutase (SOD) activities were determined in erythrocytes and brain and liver homogenates of BALB/c mice treated with Al3+ (7.5 mg/kg/day (0.15 LD50) as AlCl3 (37.08 mg/kg/day), whereas HCl (30.41 mg/kg/day) was used as Cl- control, the treatments were performed for 21 days, i.p., in the presence and absence of rosmarinic acid (0.2805 mg/kg/day (0.05 LD50), 21 days, i.g.) or carvacrol (0.0405 mg/kg/day (0.05 LD50), 21 days, i.g.). The treatment with AlCl3 increased GSH concentration in erythrocytes only slightly and had no effect on brain and liver homogenates. Rosmarinic acid and carvacrol strongly increased GSH concentration in erythrocytes but decreased it in brain and liver homogenates. However, AlCl3 treatment led to Al accumulation in mice blood, brain, and liver and induced oxidative stress, assessed based on MDA concentration in the brain and liver. Both rosmarinic acid and carvacrol were able to counteract the negative Al effect by decreasing its accumulation and protecting tissues from lipid peroxidation. AlCl3 treatment increased CAT activity in mice brain and liver homogenates, whereas the administration of either rosmarinic acid or carvacrol alone or in combination with AlCl3 had no significant effect on CAT activity. SOD activity remained unchanged after all the treatments in our study. We propose that natural herbal phenolic compounds rosmarinic acid and carvacrol could be used to protect brain and liver against aluminum induced oxidative stress leading to lipid peroxidation.

• Klíčová slova
• aluminum toxicity, brain, carvacrol, lipid peroxidation, liver, oxidative stress, rosmarinic acid,
• MeSH
• antioxidancia farmakologie   MeSH
• biologické přípravky chemie   farmakologie   MeSH
• cinnamáty chemie   farmakologie   MeSH
• cymeny chemie   farmakologie   MeSH
• depsidy chemie   farmakologie   MeSH
• erytrocyty účinky léků   metabolismus   MeSH
• hliník škodlivé účinky   chemie   MeSH
• játra účinky léků   metabolismus   MeSH
• kyselina rozmarýnová MeSH
• malondialdehyd metabolismus   MeSH
• mozek účinky léků   metabolismus   MeSH
• myši MeSH
• oxidační stres účinky léků   MeSH
• peroxidace lipidů účinky léků   MeSH
• zvířata MeSH
• Check Tag
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antioxidancia MeSH
• biologické přípravky MeSH
• carvacrol MeSH Prohlížeč
• cinnamáty MeSH
• cymeny MeSH
• depsidy MeSH
• hliník MeSH
• malondialdehyd MeSH

Marsh rosemary (Ledum palustre, Ericaceae) has been widely used in the traditional medicine of various regions worldwide, and as insect repellent. Little is known on its essential oil insecticidal potential. This study explored the insecticidal effects of the essential oil obtained from L. palustre growing in Poland on selected insect pests and vectors. GC-MS analysis evidenced an uncommon chemotype characterized by ascaridole (35.3% as sum of cis-ascaridole and isoascaridole) and p-cymene (25.5%). The essential oil was effective against Culex quinquefasciatus, Spodoptera littoralis and Musca domestica, showing LC50/LD50 of 66.6 mg L-1, 117.2 μg larva-1 and 61.4 μg adult-1, respectively. It was not toxic to non-target Eisenia fetida earthworms and moderately toxic to Daphnia magna microcrustaceans, over the positive control α-cypermethrin. The essential oil cytotoxicity on human keratinocytes and fibroblasts showed high IC50 values (71.3 and 84.4 μg mL-1, respectively). Comet assay data highlighted no DNA damages. Based on our findings, this essential oil, characterized by the ascaridole/p-cymene chemotype, could be a candidate for the formulation of botanical insecticides; large-scale production of green insecticides by this rare species may be assured by ex situ cultivation and biotechnological techniques.

• Klíčová slova
• Adulticide, Botanical pesticide, Culex quinquefasciatus, Housefly, Larvicide, Spodoptera littoralis,
• MeSH
• buněčné linie MeSH
• Culex účinky léků   MeSH
• Culicidae účinky léků   MeSH
• cymeny analýza   farmakologie   MeSH
• Daphnia účinky léků   MeSH
• insekticidy analýza   farmakologie   MeSH
• keratinocyty cytologie   účinky léků   MeSH
• komáří přenašeči účinky léků   MeSH
• kometový test MeSH
• larva účinky léků   MeSH
• lidé MeSH
• monoterpeny s cyklohexanovým kruhem analýza   farmakologie   MeSH
• moucha domácí účinky léků   MeSH
• můry účinky léků   MeSH
• oleje prchavé analýza   farmakologie   MeSH
• Oligochaeta účinky léků   MeSH
• peroxidy analýza   farmakologie   MeSH
• pyrethriny analýza   farmakologie   MeSH
• repelenty proti hmyzu analýza   farmakologie   MeSH
• rozmarýn chemie   MeSH
• Spodoptera účinky léků   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Geografické názvy
• Polsko MeSH
• Názvy látek
• 4-cymene MeSH Prohlížeč
• ascaridole MeSH Prohlížeč
• cymeny MeSH
• cypermethrin MeSH Prohlížeč
• insekticidy MeSH
• monoterpeny s cyklohexanovým kruhem MeSH
• oleje prchavé MeSH
• peroxidy MeSH
• pyrethriny MeSH
• repelenty proti hmyzu MeSH

Conventional chemotherapy is mostly effective in the treatment of rapidly-dividing differentiated tumor cells but has limited application toward eliminating cancer stem cell (CSC) population. The presence of a very small number of CSCs may contribute to the development of therapeutic resistance, metastases, and relapse. Thus, treatment failure by developing novel anticancer drugs capable of effective targeting of CSCs is at present a major challenge for research focused on chemotherapy of cancer. Here, we show that Os(II) complex 2 [Os(η6-pcym)(bphen)(dca)]PF6 (pcym = p-cymene, bphen = bathophenanthroline, and dca = dichloroacetate), is capable of efficient and selective killing CSCs in heterogeneous populations of human breast cancer cells MCF-7 and SKBR-3. Notably, its remarkable submicromolar potency to kill CSCs is considerably higher than that of its Ru analog, [Ru(η6-pcym)(bphen)(dca)]PF6 (complex 1) and salinomycin, one of the most selective CSC-targeting compounds hitherto identified. Furthermore, Os(II) complex 2 reduces the formation, size, and viability of three-dimensional mammospheres which more closely reflect the tumor microenvironment than cells in traditional two-dimensional cultures. The antiproliferation studies and propidium iodide staining using flow cytometry suggest that Os(II) complex 2 induces human breast cancer stem cell death predominantly by necroptosis, a programmed form of necrosis. The results of this study demonstrate the promise of Os(II) complex 2 in treating human breast tumors. They also represent the foundation for further preclinical and clinical studies and applications of Os(II) complex 2 to comply with the emergent need for human breast CSCs-specific chemotherapeutics capable to treat chemotherapy-resistant and relapsed human breast tumors.

• MeSH
• apoptóza účinky léků   MeSH
• chloracetáty farmakologie   MeSH
• cymeny farmakologie   MeSH
• fenantroliny farmakologie   MeSH
• komplexní sloučeniny farmakologie   MeSH
• lidé MeSH
• lokální recidiva nádoru patologie   MeSH
• nádorové buněčné linie MeSH
• nádorové kmenové buňky účinky léků   metabolismus   MeSH
• nádorové mikroprostředí účinky léků   MeSH
• nádory prsu farmakoterapie   patologie   MeSH
• nekroptóza účinky léků   MeSH
• nekróza metabolismus   MeSH
• organoplatinové sloučeniny farmakologie   MeSH
• osmium farmakologie   MeSH
• proliferace buněk účinky léků   MeSH
• protinádorové látky farmakologie   MeSH
• Check Tag
• lidé MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• 4-cymene MeSH Prohlížeč
• bathophenanthroline MeSH Prohlížeč
• chloracetáty MeSH
• cymeny MeSH
• diammine(dichloroacetato)platinum(II) MeSH Prohlížeč
• fenantroliny MeSH
• komplexní sloučeniny MeSH
• organoplatinové sloučeniny MeSH
• osmium MeSH
• protinádorové látky MeSH

Developing effective and eco-friendly antiparasitic drugs and insecticides is an issue of high importance nowadays. In this study, we evaluated the anthelminthic and insecticidal potential of the leaf essential oil obtained from Origanum syriacum against the L3 larvae of the parasitic nematode Anisakis simplex and larvae and adults of the mosquito Culex quinquefasciatus. Tests on A. simplex were performed by standard larvicidal and penetration assays, while mosquito toxicity was assessed relying on larvicidal, tarsal contact, and fumigation tests. To shed light on the possible mode of action, we analyzed the oil impact as acetylcholinesterase (AChE) inhibitor. This oil was particularly active on L3 larvae of A. simplex, showing a LC50 of 0.087 and 0.067 mg mL-1 after 24 and 48 h treatment, respectively. O. syriacum essential oil was highly effective on both larvae and adults of C. quinquefasciatus, showing LC50 values of 32.4 mg L-1 and 28.1 µg cm-2, respectively. Its main constituent, carvacrol, achieved larvicidal LC50(90) of 29.5 and 39.2 mg L-1, while contact toxicity assays on adults had an LC50(90) of 25.5 and 35.8 µg cm-2, respectively. In fumigation assays, the LC50 was 12.1 µL L-1 after 1 h and decreased to 1.3 µL L-1 in 24 h of exposure. Similarly, the fumigation LC50 of carvacrol was 8.2 µL L-1 after 1 h of exposure, strongly decreasing to 0.8 µL L-1 after 24 h of exposure. These results support the folk usage of Lebanese oregano as an antiparasitic agent, providing new insights about its utilization for developing new effective and eco-friendly nematocidal and insecticidal products.

• Klíčová slova
• anisakiasis, contact toxicity, enzyme inhibition, fumigation toxicity, larvicide, mosquito control, penetration assay,
• MeSH
• Anisakis účinky léků   MeSH
• cholinesterasové inhibitory chemie   farmakologie   MeSH
• Culex účinky léků   MeSH
• cymeny farmakologie   MeSH
• dobromysl (rod) chemie   MeSH
• komáří přenašeči účinky léků   MeSH
• larva účinky léků   MeSH
• listy rostlin chemie   MeSH
• oleje prchavé chemie   farmakologie   MeSH
• oleje rostlin chemie   farmakologie   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• carvacrol MeSH Prohlížeč
• cholinesterasové inhibitory MeSH
• cymeny MeSH
• oleje prchavé MeSH
• oleje rostlin MeSH

Every year Chile exports about 2000 tons of boldo folium (Peumus boldus), which is used around the world as a traditional herbal medicinal product (THMP), mostly to relieve gastrointestinal disorders. This biomass may be a resource for the agrochemical industry to manufacture botanical insecticides. In this regard, the insecticidal potential of boldo has been poorly investigated. In the present work, hydrodistillation of a commercial boldo folium gave 1.5% (w/w) of a yellowish essential oil (boldo essential oil, BEO) containing 1,8-cineole (20.7%), p-cymene (18.5%), limonene (9.1%), ascaridole (9.1%) and β-phellandrene (6.4%) as the main constituents, as determined by gas chromatography-mass spectrometry (GC-MS). NMR analysis allowed us to determine that ascaridole was mainly represented by the cis-isomer. BEO was toxic to larvae of the filariasis vector Culex quinquefasciatus and adults of the housefly Musca domestica, showing LC50/LD50 values of 67.9 mg·L-1 and 98.5 µg·adult-1, respectively. On the other hand, lower insecticidal activity was observed against larvae of the moth pest Spodoptera littoralis (LD50 of 268.9 µg·larva-1). It is worth noting that, when tested at LC90 concentration, BEO was significantly less toxic to aquatic microcrustacean Daphnia magna than the conventional insecticide α-cypermethrin. Finally, in the attempt to explore the BEO mode of action, we tested it for acetylcholinesterase (AChE) inhibitory properties using the Ellman method, obtaining negligible effects (IC50 = 0.45 mg·mL-1). Taken together, these results gave new insights into the potential of BEO as a future ingredient of botanical insecticides.

• Klíčová slova
• Culex quinquefasciatus, Musca domestica, aquatic ecotoxicology, ascaridole, insecticide,
• MeSH
• Culex účinky léků   MeSH
• cyklohexeny chemie   MeSH
• cymeny MeSH
• Daphnia účinky léků   MeSH
• insekticidy chemie   farmakologie   MeSH
• komáří přenašeči účinky léků   MeSH
• larva účinky léků   MeSH
• LD50 MeSH
• lidé MeSH
• monoterpeny s cyklohexanovým kruhem MeSH
• monoterpeny chemie   MeSH
• moucha domácí účinky léků   MeSH
• můry účinky léků   MeSH
• oleje prchavé chemie   farmakologie   MeSH
• peroxidy chemie   MeSH
• Peumus chemie   MeSH
• plynová chromatografie s hmotnostně spektrometrickou detekcí MeSH
• pyrethriny chemie   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• 4-cymene MeSH Prohlížeč
• ascaridole MeSH Prohlížeč
• beta-phellandrene MeSH Prohlížeč
• cyklohexeny MeSH
• cymeny MeSH
• cypermethrin MeSH Prohlížeč
• insekticidy MeSH
• monoterpeny s cyklohexanovým kruhem MeSH
• monoterpeny MeSH
• oleje prchavé MeSH
• peroxidy MeSH
• pyrethriny 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.

• Klíčová slova
• Combinatory antimicrobial effect, Essential oil, Fractional inhibitory concentration, Vapour phase, Volatile compound,
• MeSH
• cymeny MeSH
• mikrobiální testy citlivosti metody   MeSH
• monoterpeny farmakologie   MeSH
• rychlé screeningové testy MeSH
• Staphylococcus aureus účinky léků   MeSH
• thymol farmakologie   MeSH
• volatilizace MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• carvacrol MeSH Prohlížeč
• cymeny MeSH
• monoterpeny MeSH
• thymol MeSH