Four new depsidones, mollicellins V-Y (1-4), together with eight known depsidones (5-12) were isolated from the endophytic fungus, Chaetomium brasiliense, detached from stems of Thai rice. Their structures were determined by extensive spectroscopic methods. Mollicellins X, H, and F (3, 8 and 10) showed potent cytotoxicity against the human oral epidermoid carcinoma (KB) cell line, and mollicellin F (10) also showed a potent cytotoxicity against the human hepatocellular carcinoma (HepG2) cell line. Besides, mollicellin B (11) exhibited cytotoxicity against the colorectal adenocarcinoma (HT-29) cell line. Moreover, most of the isolated depsidones displayed potent antibacterial activity against Gram-positive bacteria, Bacillus cereus and Bacillus subtilis, and several of them showed moderate activity against Methicillin-resistant Staphylococcus aureus (MRSA) and clinical isolates of S. aureus. In addition, a few of them also showed moderate activity against a Gram-negative bacteria Pseudomonas aeruginosa.

• MeSH
• antibakteriální látky chemie   MeSH
• Chaetomium * chemie   MeSH
• depsidy MeSH
• laktony MeSH
• lidé MeSH
• methicilin rezistentní Staphylococcus aureus * MeSH
• mikrobiální testy citlivosti MeSH
• molekulární struktura MeSH
• protinádorové látky * chemie   MeSH
• rýže (rod) * MeSH
• Sordariales MeSH
• Staphylococcus aureus MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Geografické názvy
• Thajsko 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.

• 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
• 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

SCOPE: Aberrant vascular smooth muscle cell (VSMC) proliferation is involved in atherosclerotic plaque formation and restenosis. Mediterranean spices have been reported to confer cardioprotection, but their direct influence on VSMCs has largely not been investigated. This study aims at examining rosmarinic acid (RA) and 11 related constituents for inhibition of VSMC proliferation in vitro, and at characterizing the most promising compound for their mode of action and influence on neointima formation in vivo. METHODS AND RESULTS: RA, rosmarinic acid methyl ester (RAME), and caffeic acid methyl ester inhibit VSMC proliferation in a resazurin conversion assay with IC50 s of 5.79, 3.12, and 6.78 µm, respectively. RAME significantly reduced neointima formation in vivo in a mouse femoral artery cuff model. Accordingly, RAME leads to an accumulation of VSMCs in the G0 /G1 cell-cycle phase, as indicated by blunted retinoblastoma protein phosphorylation upon mitogen stimulation and inhibition of cyclin-dependent kinase 2 in vitro. CONCLUSION: RAME represses PDGF-induced VSMC proliferation in vitro and reduces neointima formation in vivo. These results recommend RAME as an interesting compound with VSMC-inhibiting potential. Future metabolism and pharmacokinetics studies might help to further evaluate the potential relevance of RAME and other spice-derived polyphenolics for vasoprotection.

• MeSH
• cévní endotel cytologie   účinky léků   patologie   MeSH
• cinnamáty aplikace a dávkování   škodlivé účinky   farmakologie   terapeutické užití   MeSH
• depsidy aplikace a dávkování   škodlivé účinky   farmakologie   terapeutické užití   MeSH
• endoteliální buňky pupečníkové žíly (lidské) cytologie   MeSH
• fosforylace účinky léků   MeSH
• kardiovaskulární látky škodlivé účinky   farmakologie   terapeutické užití   MeSH
• koření analýza   MeSH
• krysa rodu rattus MeSH
• kultivované buňky MeSH
• lidé MeSH
• metylace MeSH
• myši inbrední C57BL MeSH
• náhodné rozdělení MeSH
• patologická angiogeneze metabolismus   patologie   prevence a kontrola   MeSH
• posttranslační úpravy proteinů účinky léků   MeSH
• proliferace buněk účinky léků   MeSH
• retinoblastomový protein metabolismus   MeSH
• rozmarýn chemie   růst a vývoj   MeSH
• strava středomořská MeSH
• svaly hladké cévní cytologie   účinky léků   metabolismus   patologie   MeSH
• viabilita buněk účinky léků   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu rattus MeSH
• lidé MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Geografické názvy
• Středomoří MeSH

The aim of our study was to increase the extraction efficiency of carvacrol, rosmarinic, oleanolic and ursolic acid from the different species of oregano herbs (Origanum onites L., Origanum vulgare spp. hirtum and Origanum vulgare L.). Various extraction methods (ultrasound-assisted, heat-reflux, continuous stirring, maceration, percolation) and extraction conditions (different solvent, material:solvent ratio, extraction temperature, extraction time) were used, and the active substances were determined by HPLC. The lowest content of carvacrol, rosmarinic, oleanolic and ursolic acid was obtained by percolation. During heat-reflux extraction, the content of active substances depended on the solvent used: ethanol/non-aqueous solvent (glycerol or propylene glycol) mixture was more effective compared with ethanol alone. The results showed that for each species of oregano the most optimal extraction method should be selected to maximize the content of biologically active substances in the extracts.

• MeSH
• cinnamáty izolace a purifikace   MeSH
• depsidy izolace a purifikace   MeSH
• dobromysl (rod) chemie   klasifikace   MeSH
• kyselina olenalová izolace a purifikace   MeSH
• molekulární struktura MeSH
• monoterpeny izolace a purifikace   MeSH
• rostlinné extrakty chemie   MeSH
• rozpouštědla MeSH
• triterpeny izolace a purifikace   MeSH
• vysokoúčinná kapalinová chromatografie MeSH
• Publikační typ
• časopisecké články MeSH

The anti-proliferative activitiy of Hypogymnia physodes methanol extracts (ME) and its main constituents, physodalic acid (P1), physodic acid (P2), and 3-hydroxy physodic acid (P3), was tested on human cancer HeLa cell lines. Three lichen depsidones, P1, P2 and P3, were isolated from H. physodes ME using column chromatography and their structures were determined by UV, ESI TOF MS, 1H and 13C NMR. The content of P1, P2 and P3 in ME was determined using reversed-phase highperformance liquid chromatography with photodiode array detection. P1-3 represented even 70 % of the studied extract. The HeLa cells were incubated during 24 and 72 h in the presence of ME and depsidones P1, P2 and P3, at concentrations of 10-1000 μg/ml. Compounds P2 and P3 showed higher activity than compound P1. Half maximal inhibitory concentrations (IC50, μg/ml) of P1, P2, P3 and ME for 24-h incubation were 964, 171, 97 and 254 μg/ml, respectively, while for 72-h incubation they were 283, 66, 63 and 68 μg/ml. As far as we know, this is the first report on the effect of H. physodes ME and their depsidones on HeLa cells.

• MeSH
• depsidy chemie   farmakologie   MeSH
• HeLa buňky MeSH
• inhibiční koncentrace 50 MeSH
• laktony chemie   farmakologie   MeSH
• lidé MeSH
• lišejníky chemie   MeSH
• viabilita buněk účinky léků   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

Solar radiation is a very important exogenous factor in skin pathogenesis and can lead to the development of a number of skin disorders. UVB irradiation is known to induce oxidative stress, inflammation and especially DNA lesions in exposed cells. It is important, therefore, to identify agents that can offer protection against UVB-caused skin damage. Natural compounds have been studied for their possible ability to control/modulate various lifestyle-related diseases. The application of plant compounds/extracts with screening, antioxidant and anti-inflammatory activities may also successfully protect the skin against UV-caused injury. We assessed the potency of Prunella vulgaris extract (PVE) and its main phenolic acid component, rosmarinic acid (RA), to suppress UVB-induced (295-315 nm) alterations to human keratinocytes HaCaT using a solar simulator. Pre- and post-treatment of HaCaT cells with PVE (5-50 mg/l) and RA (0.18-1.8 mg/l) reduced breakage together with the apoptotic process. PVE and RA also significantly eliminated ROS production and diminished IL-6 release. Taken together, both PVE and RA prevent UVB-caused injury to keratinocytes. However their efficacy needs to be demonstrated in vivo.

• MeSH
• antioxidancia farmakologie   MeSH
• apoptóza účinky léků   účinky záření   MeSH
• buněčná membrána účinky léků   účinky záření   MeSH
• cinnamáty farmakologie   MeSH
• depsidy farmakologie   MeSH
• interleukin-6 metabolismus   MeSH
• keratinocyty účinky léků   metabolismus   patologie   účinky záření   MeSH
• lidé MeSH
• nadzemní části rostlin MeSH
• oxidační stres účinky léků   účinky záření   MeSH
• poškození DNA účinky léků   MeSH
• přípravky chránící proti slunci farmakologie   MeSH
• proliferace buněk účinky léků   účinky záření   MeSH
• Prunella MeSH
• reaktivní formy kyslíku metabolismus   MeSH
• rostlinné extrakty farmakologie   MeSH
• transformované buněčné linie MeSH
• ultrafialové záření MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

Periodontitis is a chronic disease associated with inflammation of the tooth-supporting tissues. The inflammation is initiated by a group of gram-negative anaerobic bacteria. These express a number of irritating factors including a lipopolysaccharide (LPS), which plays a key role in periodontal disease development. Plant extracts with anti-inflammatory and anti-microbial properties have been shown to inhibit bacterial plaque formation and thus prevent chronic gingivitis. In this study we tested effects of Prunella vulgaris L. extract (PVE; 5, 10, 25microg/ml) and its component rosmarinic acid (RA; 1microg/ml) on LPS-induced oxidative damage and inflammation in human gingival fibroblasts. PVE and RA reduced reactive oxygen species (ROS) production, intracellular glutathione (GSH) depletion as well as lipid peroxidation in LPS-treated cells. Treatment with PVE and RA also inhibited LPS-induced up-regulation of interleukin 1beta (IL-1beta), interleukin 6 (IL-6), tumor necrosis factor-alpha (TNF-alpha) and suppressed expression of inducible nitric oxide synthase (iNOS). The results indicate that PVE and RA are able to suppress LPS-induced biological changes in gingival fibroblasts. The effects of PVE and RA are presumably linked to their anti-inflammatory activities and thus use of PVE and RA may be relevant in modulating the inflammation process, including periodontal disease.

• MeSH
• antagonismus léků MeSH
• antioxidancia analýza   farmakologie   MeSH
• cinnamáty analýza   farmakologie   MeSH
• depsidy analýza   farmakologie   MeSH
• fibroblasty metabolismus   patologie   účinky léků   MeSH
• financování organizované MeSH
• gingiva metabolismus   patologie   účinky léků   MeSH
• glutathion metabolismus   MeSH
• kultivované buňky MeSH
• lidé MeSH
• lipopolysacharidy agonisté   toxicita   MeSH
• oxidační stres účinky léků   MeSH
• Prunella chemie   MeSH
• reaktivní formy kyslíku metabolismus   MeSH
• rostlinné extrakty farmakologie   MeSH
• viabilita buněk účinky léků   MeSH
• Check Tag
• lidé MeSH

UVA radiation provokes the generation of reactive oxygen species (ROS), which induce oxidative stress in the exposed cells leading to extensive cellular damage and cell death either by apoptosis or necrosis. One approach to protecting human skin against the harmful effects of UV radiation is by using herbal compounds as photoprotectants. This study evaluated the protective effects of Prunella vulgaris L. (Labiatae) and its main phenolic acid component, rosmarinic acid (RA), against UVA-induced changes in a human keratinocyte cell line (HaCaT). Human keratinocytes exposed to UVA (10-30 J/cm(2)) were treated with an extract of P. vulgaris (1-75 mg/l) or RA (0.9-18 mg/l) for 4h. P. vulgaris and RA exhibited ability to reduce the UVA-caused decrease in a cell viability monitored by neutral red retention and by LDH release into medium. The P. vulgaris extract and RA significantly suppressed UVA-induced ROS production, which manifests as a decrease in intracellular lipid peroxidation, elevation of ATP and reduced glutathione. Post-treatment with P. vulgaris extract and RA also significantly reduced DNA damage. In addition, UVA-induced activation of caspase-3 was inhibited by treatment with P. vulgaris and RA. The P. vulgaris extract and RA demonstrated a concentration-dependent photoprotection (maximum at 25-50 mg/l and 9 mg/l, respectively). These results suggest that P. vulgaris and RA, used in skin care cosmetics, may offer protection against UVA-induced oxidative stress and may be beneficial as a supplement in photoprotective dermatological preparations.

• MeSH
• apoptóza účinky léků   účinky záření   MeSH
• buněčné linie MeSH
• cinnamáty farmakologie   MeSH
• depsidy MeSH
• financování organizované MeSH
• fotobiologie MeSH
• keratinocyty cytologie   metabolismus   účinky léků   účinky záření   MeSH
• lidé MeSH
• oxidační stres účinky léků   účinky záření   MeSH
• poškození DNA účinky léků   MeSH
• proliferace buněk účinky léků   účinky záření   MeSH
• Prunella MeSH
• radioprotektivní látky farmakologie   MeSH
• rostlinné extrakty farmakologie   MeSH
• ultrafialové záření škodlivé účinky   MeSH
• viabilita buněk účinky léků   účinky záření   MeSH
• Check Tag
• lidé MeSH