ETHNOPHARMACOLOGICAL RELEVANCE: The use of Hazomalania voyronii, popularly known as hazomalana, to repel mosquitoes and resist against insect attacks is handed down from generation to generation in Madagascar. In the present study, we investigated the ability of the essential oils (EOs) obtained from the stem wood, fresh and dry bark of H. voyronii to keep important mosquito vectors (Aedes aegypti and Culex quinquefasciatus) away, as well as their toxicity on three insect species of agricultural and public health importance (Cx. quinquefasciatus, Musca domestica and Spodoptera littoralis). MATERIALS AND METHODS: Hydrodistillation was used to obtain EOs from stem wood, fresh and dry bark. The chemical compositions were achieved by gas chromatography-mass spectrometry (GC-MS). Toxicity assays using stem wood and bark EOs were performed on larvae of Cx. quinquefasciatus and S. littoralis, and adults of M. domestica by WHO and topical application methods, respectively. Mosquito repellent activity of the most effective EO, i.e. the bark one, was determined on human volunteers by arm-in-cage tests, and results were compared with that of the commercial repellent N,N-ddiethyl-m-toluamide (DEET). RESULTS: The H. voyronii EOs were characterized by oxygenated monoterpenes with perilla aldehyde (30.9-47.9%) and 1,8-cineole (19.7-33.2%) as the main constituents. The fresh and dry bark EOs were the most active on Cx. quinquefasciatus and S. littoralis larvae, respectively, with LC50/LD50 of 65.5 mg L-1, and 50.5 μg larva-1; the EOs from wood and fresh bark displayed the highest toxicity on M. domestica (LD50 values 60.8 and 65.8 μg adult-1, respectively). Repellence assay revealed an almost complete protection (>80%) from both mosquito species for 30 min when pure fresh bark EO was applied on the volunteers' arm, while DEET 10% repelled >80% of the mosquitoes up to 120 min from application. CONCLUSION: The traditional use of the bark EO to repel insects has been demonstrated although an extended-release formulation based on H. voyronii EOs is needed to increase the repellent effect over time. A wide spectrum of insecticidal activity has been provided as well, suggesting a possible use of H. voyronii EOs in the fabrication of green repellents and insecticides useful to control mosquito vectors and agricultural pests.
- MeSH
- Aedes účinky léků růst a vývoj MeSH
- časové faktory MeSH
- Culex účinky léků embryologie MeSH
- diethyltoluamid farmakologie MeSH
- dřevo * chemie MeSH
- Hernandiaceae * chemie MeSH
- kůra rostlin * chemie MeSH
- larva účinky léků růst a vývoj MeSH
- lidé MeSH
- moskyti - kontrola * MeSH
- moucha domácí účinky léků růst a vývoj MeSH
- oleje prchavé izolace a purifikace farmakologie MeSH
- oleje rostlin izolace a purifikace farmakologie MeSH
- repelenty proti hmyzu izolace a purifikace farmakologie MeSH
- Spodoptera účinky léků embryologie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- srovnávací studie MeSH
Comprehensive oncology research suggests an important role of phytochemicals or whole plant foods in the modulation of signaling pathways associated with anticancer action. The goal of this study is to assess the anticancer activities of Cinnamomum zeylanicum L. using rat, mouse, and cell line breast carcinoma models. C. zeylanicum (as bark powder) was administered in the diet at two concentrations of 0.1% (w/w) and 1% (w/w) during the whole experiment in chemically induced rat mammary carcinomas and a syngeneic 4T1 mouse model. After autopsy, histopathological and molecular evaluations of mammary gland tumors in rodents were carried out. Moreover, in vitro analyses using MCF-7 and MDA-MB-231 cells were performed. The dominant metabolites present in the tested C. zeylanicum essential oil (with relative content over 1%) were cinnamaldehyde, cinnamaldehyde dimethyl acetal, cinnamyl acetate, eugenol, linalool, eucalyptol, limonene, o-cymol, and α-terpineol. The natural mixture of mentioned molecules demonstrated significant anticancer effects in our study. In the mouse model, C. zeylanicum at a higher dose (1%) significantly decreased tumor volume by 44% when compared to controls. In addition, treated tumors showed a significant dose-dependent decrease in mitotic activity index by 29% (0.1%) and 45.5% (1%) in comparison with the control group. In rats, C. zeylanicum in both doses significantly reduced the tumor incidence by 15.5% and non-significantly suppressed tumor frequency by more than 30% when compared to controls. An evaluation of the mechanism of anticancer action using valid oncological markers showed several positive changes after treatment with C. zeylanicum. Histopathological analysis of treated rat tumor specimens showed a significant decrease in the ratio of high-/low-grade carcinomas compared to controls. In treated rat carcinomas, we found caspase-3 and Bax expression increase. On the other hand, we observed a decrease in Bcl-2, Ki67, VEGF, and CD24 expressions and MDA levels. Assessment of epigenetic changes in rat tumor cells in vivo showed a significant decrease in lysine methylation status of H3K4m3 and H3K9m3 in the high-dose treated group, a dose-dependent increase in H4K16ac levels (H4K20m3 was not changed), down-regulations of miR21 and miR155 in low-dose cinnamon groups (miR22 and miR34a were not modulated), and significant reduction of the methylation status of two out of five gene promoters-ATM and TIMP3 (PITX2, RASSF1, PTEN promoters were not changed). In vitro study confirmed results of animal studies, in that the essential oil of C. zeylanicum displayed significant anticancer efficacy in MCF-7 and MDA-MB-231 cells (using MTS, BrdU, cell cycle, annexin V/PI, caspase-3/7, Bcl-2, PARP, and mitochondrial membrane potential analyses). As a conclusion, C. zeylanicum L. showed chemopreventive and therapeutic activities in animal breast carcinoma models that were also significantly confirmed by mechanistic evaluations in vitro and in vivo.
- MeSH
- antitumorózní látky fytogenní aplikace a dávkování chemie farmakologie MeSH
- histony metabolismus MeSH
- krysa rodu rattus MeSH
- kůra rostlin chemie MeSH
- lidé MeSH
- MFC-7 buňky MeSH
- mikro RNA genetika MeSH
- myši MeSH
- nádorové buněčné linie MeSH
- nádory prsu farmakoterapie genetika metabolismus MeSH
- oleje prchavé aplikace a dávkování chemie farmakologie MeSH
- oleje rostlin aplikace a dávkování chemie farmakologie MeSH
- proliferace buněk účinky léků MeSH
- skořicovník ceylonský chemie MeSH
- viabilita buněk účinky léků MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- xenogenní modely - testy antitumorózní aktivity MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- lidé MeSH
- myši MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
The diet rich in fruits and vegetables reduces the risk of metabolic syndrome, including diabetes development by various mechanisms of action, mainly due to the presence of polyphenolic compounds. Extracts from different conifer species are known to be a rich source of various polyphenols. In the present study we elucidated the in vitro mechanism of anti-diabetic activity of silver fir (Abies alba) wood and bark extracts and compared their activity to non-coniferous sweet chestnut wood extract and standardized maritime pine bark extract. Extracts and lignans were tested for their inhibitory activity of enzymes involved in the regulation of blood glucose in vitro. The ability of extracts to protect against oxidative stress in high glucose environment was tested on mouse myoblast cell line. Silver fir wood and bark extracts were shown to be effective inhibitors of α-glucosidase, α-amylase and dipeptidyl peptidase 4, three enzymes involved in the regulation of blood glucose levels. Coniferous extracts also showed protection against oxidative stress generated in high glucose environment. Lignans, particularly pinoresinol diglucoside, isolariciresinol and secolariciresinol were shown to be important contributors of antihyperglycemic activity through inhibition of dipeptidyl peptidase 4. This corroborates previously published in vivo results on blood glucose level obtained with silver fir wood extract and supports the use of silver fir wood and bark extracts as food supplements or functional foods in borderline diabetes.
- MeSH
- alfa-amylasy antagonisté a inhibitory MeSH
- alfa-glukosidasy metabolismus MeSH
- buněčné linie MeSH
- dipeptidylpeptidasa 4 metabolismus MeSH
- dřevo chemie MeSH
- hypoglykemika izolace a purifikace farmakologie MeSH
- inhibitory dipeptidylpeptidasy 4 izolace a purifikace farmakologie MeSH
- inhibitory glykosidových hydrolas izolace a purifikace farmakologie MeSH
- jedle chemie MeSH
- krevní glukóza účinky léků MeSH
- kůra rostlin chemie MeSH
- lidé MeSH
- myši MeSH
- oxidační stres účinky léků MeSH
- rostlinné extrakty izolace a purifikace farmakologie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
Maytenus macrocarpa (Celastraceae) is a tree native to Amazonia. Its roots, leaves, bark, and combinations of these are used in traditional medicine mainly to treat rheumatism and, to a lesser extent, to heal wounds and to combat bronchitis and diarrhea. To date, mainly triterpenes and dihydro-β-agarofuran sesquiterpenes were isolated from M. macrocarpa. Extracts and selected pure compounds isolated from the leaves, roots, and stem bark showed antibacterial, antiviral, antiparasitic, anti-inflammatory, and cytotoxic activities in vitro. The aim of this review is to summarize the available ethnobotanical, phytochemical, and pharmacological information about this traditional Amazonian medicinal tree, as well as to attract the attention of phytochemists and pharmacognosists to this potentially interesting source of ethnopharmaceuticals.
- MeSH
- antibakteriální látky chemie terapeutické užití MeSH
- antivirové látky chemie terapeutické užití MeSH
- hojení ran účinky léků MeSH
- kořeny rostlin chemie MeSH
- kůra rostlin chemie MeSH
- lidé MeSH
- listy rostlin chemie MeSH
- Maytenus chemie MeSH
- revmatické nemoci farmakoterapie patologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy 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
V extraktu kůry Sorbus aucuparia byl stanoven metodou GC-MS kvantitativní obsah 40 karboxylových kyselin s prevalencí hexadekandiové, lignocerové, behenové, azelaové, palmitové a benzoové kyseliny, a 39 složek silice. V etanolickém extraktu kůry Sorbus aucuparia byl metodou HPLC kvantitativně stanoven obsah šesti fenolických sloučenin, tj. kyseliny chlorogenové, kávové a galové, katechinu, kvercetinu a apigenin-7-glukosidu.
The quantitative contents of 40 carboxylic acids, with the prevalence of hexadecanedioic, lignocerinic, behenic, azelaic, palmitic and benzoic acids, and 39 components of essential oil were determined in the extracts of the bark of Sorbus aucuparia by the GC-MS method. The quantitative contents of 6 phenolic compounds, i.e., chlorogenic, caffeic, and gallic acids, catechin, quercetin, and apigenin-7-glucoside were determined by the HPLC method in the ethanolic extract of the bark of Sorbus aucuparia.
The Czech Republic (CZ) had extremely high emissions and atmospheric deposition of pollutants in the second half of the 1980s. Since the beginning of the 1990s, moss, spruce bark and forest floor humus have been used as bioindicators of air quality. In the first half of the 1990s, seven larger areas were found to be affected by high atmospheric deposition loads. Six of these "hot spots" were caused by industrial pollution sources, mainly situated in coal basins in the NW and NE part of the country, and one large area in the SE was affected by increased deposition loads of eroded soil particles. After restructuring of industry in CZ, these hot spots were substantially reduced or even disappeared between 1995 and 2000. Since 2000, only two larger areas with slightly increased levels of industrial pollutant deposition and a larger area affected by soil dust have repeatedly been identified by biomonitoring. The distribution of lead isotope ratios in moss showed the main deposition zones around important emission sources. Very high SO2 emissions led to extreme acidity of spruce bark extracts (pH of about 2.3) at the end of the 1980s. The rate of increasing bark pH was strikingly similar to the rate of recovery of acid wet deposition measured at forest stations in CZ. By about 2005, when the median pH value in bark increased to about 3.2, the re-colonisation of trees by several epiphyte lichen species was observed throughout CZ. An increase in the accumulation of Chernobyl-derived (137)Cs in bark was detected at about ten sites affected by precipitation during the time when radioactive plumes crossed CZ (1986). Accumulated deposition loads in forest floor humus corresponded to the position of the moss and bark hot spots.
- MeSH
- Bryophyta chemie MeSH
- kůra rostlin chemie MeSH
- látky znečišťující vzduch analýza MeSH
- monitorování životního prostředí * MeSH
- půda chemie MeSH
- smrk chemie MeSH
- Publikační typ
- časopisecké články MeSH
- Geografické názvy
- Česká republika MeSH
A new and relatively simple method for purification of betulin from birch bark extract was developed in this study. Its five purification steps are based on the differential solubility of extract components in various solvents and their crystallization and/or precipitation, on their affinity for Ca(OH)2 in ethanol, and on the affinity of some impurities for silica gel in chloroform. In addition, all used solvents can be simply recycled. Betulin of more than 99% purity can be prepared by this method with minimal costs. Various observations including crystallization of betulin, changes in crystals during heating, and attempt of localization of betulin in outer birch bark are also described in this work. The original extract, fraction without betulinic acid and lupeol, amorphous fraction of pure betulin, final crystalline fraction of pure betulin and commercial betulin as a standard were employed to determine the antiproliferative/cytotoxic effect. We used WST-1 tetrazolium-based assays with triple negative breast cancer cell line BT-549. The decrease in cell survival showed clear relationship with the purity of the samples, being most pronounced using our final product of pure crystalline betulin. WST-1 proliferation/cytotoxicity test using triple negative breast cancer cell line BT-549 clearly showed the importance of purity of betulin for biological experiments and, apparently, for its medicinal use.
- MeSH
- bříza chemie MeSH
- krystalizace MeSH
- kůra rostlin chemie MeSH
- lidé MeSH
- nádorové buněčné linie MeSH
- proliferace buněk účinky léků MeSH
- triple-negativní karcinom prsu farmakoterapie patologie MeSH
- triterpeny chemie izolace a purifikace farmakologie terapeutické užití MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Chromatographic separation of root extracts of Morus alba and M. nigra led to the identification of the 2-arylbenzofurans moracin C (1), mulberrofuran Y (2), and mulberrofuran H (3), and the prenylated flavonoids kuwanon E (4), kuwanon C (5), sanggenon H (6), cudraflavone B (7), and morusinol (8), and the Diels-Alder adducts soroceal (9), and sanggenon E (10). The cytotoxicity and their antiphlogistic activity, determined as the attenuation of the secretion of TNF-α and IL-1β and the inhibition of NF-κB nuclear translocation in LPS-stimulated macrophages, were evaluated for compounds 1-10.
- MeSH
- antiflogistika farmakologie MeSH
- benzofurany chemie izolace a purifikace farmakologie MeSH
- benzopyrany chemie izolace a purifikace farmakologie MeSH
- flavonoidy chemie izolace a purifikace farmakologie MeSH
- kořeny rostlin chemie MeSH
- kůra rostlin chemie MeSH
- lidé MeSH
- lipopolysacharidy farmakologie MeSH
- makrofágy účinky léků MeSH
- molekulární struktura MeSH
- Morus chemie MeSH
- myši MeSH
- NF-kappa B účinky léků MeSH
- prenylace MeSH
- TNF-alfa farmakologie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
The effects of condensed tannins (CTs) extracted from pine bark on egg hatching, larval development and the viability of infective L3 larvae of Trichostrongylus colubriformis (Giles, 1892) and Teladorsagia circumcincta (Stadelmann, 1894) (syn. Ostertagia circumcincta) were evaluated using in vitro bioassays. Significant inhibitory effects of CTs were obtained on the viability of the infective larvae, egg hatching and larval development of both nematodes. In all bioassays, the larval stages of Te. circumcincta were significantly (P < 0.05) more susceptible to the inhibitory effects of CT than those of Tr. colubriformis. At 1 000 microg/ml, CTs from pine bark inhibited 48% and 69% of the infective larvae of Tr. colubriformis and Te. circumcincta, respectively, from passing through the sieve relative to the control incubations (no CT added; P < 0.0001). At the same concentration, CTs were able to inhibit 36% and 47% of the eggs of the two parasites, respectively, from hatching relative to the control incubations without CTs. Moreover, at 150 microg/ml, the CTs were able to inhibit 88% and 95% (P < 0.0001 relative to control incubation) of L1 larvae of the two nematodes, respectively, from attaining the full development to L3 larvae in comparison with the control incubations without CTs. At 200 microg/ml, CTs were able to inhibit completely the larval development in both nematodes. Addition of 2 microg polyethylene glycol (PEG; tannin inhibitor) per microg CT eliminated up to 87% of the CT activity (P < 0.0001) compared to incubations without PEG. In conclusion, this study shows that CTs are able to disrupt the life cycle of nematodes and their effects varied according to the parasite species and stage.
- MeSH
- borovice chemie MeSH
- druhová specificita MeSH
- fylogeneze MeSH
- hlístice účinky léků MeSH
- kůra rostlin chemie MeSH
- larva účinky léků růst a vývoj fyziologie MeSH
- ovum účinky léků MeSH
- pohybová aktivita účinky léků MeSH
- proantokyanidiny chemie farmakologie MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
