Anaerobic bacteria, such as Bacteroides fragilis or Clostridium perfringens, are part of indigenous human flora. However, Clostridium difficile represents also an important causative agent of nosocomial infectious antibiotic-associated diarrhoea. Treatment of C. difficile infection is problematic, making it imperative to search for new compounds with antimicrobial properties. Hops (Humulus lupulus L.) contain substances with antibacterial properties. We tested antimicrobial activity of purified hop constituents humulone, lupulone and xanthohumol against anaerobic bacteria. The antimicrobial activity was established against B. fragilis, C. perfringens and C. difficile strains according to standard testing protocols (CLSI, EUCAST), and the minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBC) were calculated. All C. difficile strains were toxigenic and clinically relevant, as they were isolated from patients with diarrhoea. Strongest antimicrobial effects were observed with xanthohumol showing MIC and MBC values of 15-107 μg/mL, which are close to those of conventional antibiotics in the strains of bacteria with increased resistance. Slightly higher MIC and MBC values were obtained with lupulone followed by higher values of humulone. Our study, thus, shows a potential of purified hop compounds, especially xanthohumol, as alternatives for treatment of infections caused by select anaerobic bacteria, namely nosocomial diarrhoea caused by resistant strains.
- MeSH
- anaerobióza fyziologie MeSH
- antibakteriální látky izolace a purifikace farmakologie MeSH
- Bacteroides fragilis účinky léků růst a vývoj MeSH
- Clostridioides difficile účinky léků růst a vývoj patogenita MeSH
- Clostridium perfringens účinky léků růst a vývoj MeSH
- cyklohexeny izolace a purifikace farmakologie MeSH
- flavonoidy izolace a purifikace farmakologie MeSH
- Humulus chemie MeSH
- infekce spojené se zdravotní péčí mikrobiologie MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- propiofenony izolace a purifikace farmakologie MeSH
- průjem mikrobiologie MeSH
- pseudomembranózní enterokolitida mikrobiologie MeSH
- rostlinné extrakty chemie MeSH
- symbióza fyziologie MeSH
- terpeny izolace a purifikace farmakologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
In our continuing search for biologically active natural product(s) of plant origin, Buddleja saligna, a South African medicinal plant, was screened in line with its traditional use for antidiabetic (yeast alpha glucosidase inhibitory) and antiplasmodial (against a chloroquine sensitive strain of Plasmodium falciparum (NF54)) activities. The hexane fraction showed the most promising activity with regards to its antidiabetic (IC(50) = 260 ± 0.112 µg/ml) and antiplasmodial (IC(50) = 8.5 ± 1.6 µg/ml) activities. Using activity guided fractionation three known terpenoids (betulonic acid, betulone and spinasterol) were isolated from this species for the first time. The compounds displayed varying levels of biological activities (antidiabetic: 27.31 µg/ml ≥ IC(50) ≥ 5.6 µg/ml; antiplasmodial: 14 µg/ml ≥ IC(50) ≥ 2 µg/ml) with very minimal toxicity.
- MeSH
- alfa-glukosidasy metabolismus MeSH
- antimalarika chemie izolace a purifikace farmakologie MeSH
- Buddleja chemie MeSH
- inhibitory glykosidových hydrolas chemie izolace a purifikace farmakologie MeSH
- kvasinky enzymologie MeSH
- listy rostlin chemie MeSH
- molekulární struktura MeSH
- parazitické testy citlivosti MeSH
- Plasmodium falciparum účinky léků MeSH
- terpeny chemie izolace a purifikace farmakologie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Safranal and crocin are biologically active compounds isolated from Crocus sativus L., commonly known as saffron. Clinical trials confirm that saffron has antidepressant effect, thus being a potential valuable alternative in the treatment of depression. The aim of the present study was to determine, whether systemic administration of safranal and crocin can influence the metabolic activity of CYP3A, CYP2C11, CYP2B, and CYP2A in rat liver microsomes (RLM). The experiments were carried out on male Wistar albino rats intragastrically administered with safranal (4, 20, and 100 mg/kg/day) or with intraperitoneal injections of crocin (4, 20, and 100 mg/kg/day). Our results demonstrate the ability of safranal and crocin to increase the total protein content and to change the metabolic activity of several CYP enzymes assessed as CYP specific hydroxylations of testosterone in RLM. Crocin significantly decreased the metabolic activity of all selected CYP enzymes, while safranal significantly increased the metabolic activity of CYP2B, CYP2C11 and CYP3A enzymes. Therefore, both substances could increase the risk of interactions with co-administered substances metabolized by cytochrome P450 enzymes.
- MeSH
- aktivace enzymů účinky léků fyziologie MeSH
- Crocus * MeSH
- cyklohexeny izolace a purifikace farmakologie MeSH
- jaterní mikrozomy účinky léků enzymologie MeSH
- karotenoidy izolace a purifikace farmakologie MeSH
- krysa rodu rattus MeSH
- potkani Wistar MeSH
- rostlinné extrakty izolace a purifikace farmakologie MeSH
- systém (enzymů) cytochromů P-450 metabolismus MeSH
- terpeny izolace a purifikace farmakologie 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
- práce podpořená grantem MeSH
- MeSH
- antivirové látky * izolace a purifikace MeSH
- benzofurany farmakologie izolace a purifikace terapeutické užití MeSH
- flavonoidy farmakologie izolace a purifikace terapeutické užití MeSH
- látky proti HIV farmakologie izolace a purifikace terapeutické užití MeSH
- léčivé rostliny chemie MeSH
- lišejníky chemie MeSH
- listy rostlin chemie MeSH
- oleje rostlin farmakologie izolace a purifikace terapeutické užití MeSH
- polyfenoly farmakologie izolace a purifikace terapeutické užití MeSH
- polysacharidy farmakologie izolace a purifikace terapeutické užití MeSH
- rostlinné extrakty * terapeutické užití MeSH
- sinice chemie MeSH
- terpeny farmakologie izolace a purifikace terapeutické užití MeSH
An original method based on capillary zone electrophoresis with fluorimetric detection has been developed for the determination of terpenic compounds. The method is based on the separation of a terpenes dynamically labeled by the non-ionogenic tenside poly(ethylene glycol) pyrenebutanoate, which was used previously for the labeling of biopolymers. The background electrolytes were composed of taurine-Tris buffer (pH 8.4). In addition to the non-ionogenic tenside aceton and poly(ethylene glycol) were used as the additives. The capillary zone electrophoresis with fluorometric detection at the excitation wavelength 335 nm and the emission wavelength 463 nm was successfully applied to the analysis of tonalid, cholesterol, vitamin A, ergosterol, estrone and farnesol at level of 10(-17) mol L(-1). Farnesol, is produced by Candida albicans as an extracellular quorum-sensing molecule that influences expression of a number of virulence factors, especially morphogenesis and biofilm formation. It enables this yeast to cause serious nosocomial infections. The sensitivity of this method was demonstrated on the separation of farnesol directly from the cultivation medium.
- MeSH
- biofilmy MeSH
- butyráty chemie MeSH
- Candida albicans chemie metabolismus MeSH
- cholesterol chemie MeSH
- elektroforéza kapilární metody MeSH
- ergosterol chemie MeSH
- estron chemie MeSH
- farnesol chemie izolace a purifikace metabolismus MeSH
- fluorometrie metody MeSH
- polymery chemie MeSH
- quorum sensing MeSH
- senzitivita a specificita MeSH
- terpeny chemie izolace a purifikace MeSH
- tetrahydronaftaleny chemie MeSH
- vitamin A chemie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Headspace solid-phase microextraction (HS-SPME) and solid-phase microextraction coupled with hydrodistillation (HD-SPME) were used for detection and determination of essential oils in dried leaves of Mentha piperita L., Lavandula augustifolia L. and Salvia officinalis L. The results were compared with those obtained using steam distillation, which is a reference method. The extraction time 15 min and the minimal fibre depth 1.4 cm are suitable for a 50/30 ?m polydimethylsiloxane/divinylbenzene/ carboxen fibre. The method was compared with HS-SPME and steam distillation.
Třezalka (Hypericum perforatum L.) je tradičně využívaná léčivá rostlina v alternativní i klasické medicíně. V současnosti jsou k dispozici poznatky o fyziologické aktivitě jednotlivých sloučenin, které třezalka syntetizuje ve svých pletivech. Nejvyšší pozornost je věnována hypericinu a hyperforinu. Tyto organické sloučeniny nacházejí uplatnění v léčbě depresivních stavů, v protinádorové (fotodynamické) terapii a jako antimikrobiální a virostatické agens. V předkládaném souhrnu jsou ve stručnosti prezentovány současné poznatky o analýze, fyziologickém účinku a praktickém využití hypericinu a hyperforinu ve farmakochemii a biomedicínských oborech.
St. John's Wort (Hypericum perforatum L.) is commonly accepted as a medicinal plant. The data on the physiological activities of the individual substances that are produced in different organs of H. perforatum are well known at present. The highest attention is focused on the characterization and phytochemical properties of hypericin and hyperforin. These organic compounds are used as antidepressant, anticarcinogenic (photodynamic), antimicrobial and virostatic agents. The review paper surveys the present knowledge of chemical and analytical methods for their identification and quantification, physiological activity, and pharmacological and biomedical applications of hypericin and hyperforin.
- MeSH
- antitumorózní látky terapeutické užití MeSH
- depresivní poruchy farmakoterapie terapie MeSH
- lidé MeSH
- perylen analogy a deriváty izolace a purifikace terapeutické užití MeSH
- rostlinné extrakty terapeutické užití MeSH
- terpeny izolace a purifikace terapeutické užití MeSH
- třezalka chemie MeSH
- virové nemoci farmakoterapie terapie MeSH
- Check Tag
- lidé MeSH
