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1.
Int J Biol Macromol ; 257(Pt 2): 128701, 2024 Feb.
Article in English | MEDLINE | ID: mdl-38072348

ABSTRACT

Trichomoniasis is a common sexually transmitted infection that poses significant complications for women. Challenges in treatment include adverse effects and resistance to standard antimicrobial agents. Given this context, a sesame seed oil nanoemulsion (SONE) was developed and showed anti-Trichomonas vaginalis activity. To facilitate the local application of SONE, a polysaccharide film was developed using xanthan gum (XG) and κ-carrageenan gum (CG). A blend of XG and CG (at 2 %, ratio 1:3) plasticized with glycerol produced a more promising film (XCF) than using the gums individually. The film containing SONE (SONE-XCF) was successfully obtained by replacing the aqueous solvent with SONE via solvent evaporation technique. The hydrophilic SONE-XCF exhibited homogeneity and suitable mechanical properties for vaginal application. Furthermore, SONE-XCF demonstrated mucoadhesive properties and high absorption capacity for excessive vaginal fluids produced in vaginitis. It also had a disintegration time of over 8 h, indicating long retention at the intended site of action. Hemolysis and chorioallantoic membrane tests confirmed the safety of the film. Therefore, SONE-XCF is a biocompatible film with a natural composition and inherent activity against T. vaginalis, possessing exceptional characteristics that make it appropriate for vaginal application, offering an interesting alternative for trichomoniasis treatment.


Subject(s)
Nanocomposites , Sesamum , Trichomonas Infections , Female , Humans , Carrageenan , Prednisone , Polysaccharides, Bacterial , Solvents , Pharmaceutical Preparations , Plant Oils/pharmacology
2.
J Pharm Biomed Anal ; 239: 115889, 2024 Feb 15.
Article in English | MEDLINE | ID: mdl-38056286

ABSTRACT

Aniba canelilla (Kunth) Mez is an aromatic tree from Amazon region whose essential oil presents 1-nitro-2-phenylethane (NP) and methyleugenol (ME) as major compounds. Several properties are attributed to Aniba canelilla essential oil (ACEO), such as antifungal. Onychomycoses are fungal nail infections that require novel therapeutic alternatives, especially topical ones. However, to ensure the success of topical therapy, the active compound should be able to penetrate/permeate the nail plate, which is challenging due to the highly keratinized composition of this structure. Thus, the aims of this article were to develop, validate and apply a high-performance liquid chromatography method (HPLC-UV) to quantify NP and ME in porcine hoof extract (PHE) and receptor fluid (RF) during in vitro permeation/retention studies in nail model, for which porcine hoof membranes were used. For method development, two Designs of Experiment (DoE) were adopted: 23 Full Factorial and Box-Behnken. Retention times of 5.65 and 7.49 min were achieved for NP and ME, respectively. The method was full validated for NP and ME quantification in receptor fluid, in accordance with the recommended parameters by ICH Q2(R1) Guideline. In addition, the method was full validated for NP and ME quantification in porcine hoof extract, considering the parameters and criteria of ICH M10 Guideline. In vitro permeation/retention studies were carried out in nail model, and promising results were obtained. NP reached the receptor fluid in the order of 441.1 ± 92.1 µg/cm2 at 72 h. The amount of NP and ME retained into porcine hoof membrane was 1272.6 ± 225.7 µg/cm2 and 84.7 ± 20.4 µg/cm2, respectively, at 72 h. Our findings open perspective to develop topical formulations containing ACEO as active compound aiming the management of onychomycosis.


Subject(s)
Oils, Volatile , Onychomycosis , Swine , Animals , Chromatography, High Pressure Liquid , Onychomycosis/drug therapy , Antifungal Agents , Oils, Volatile/chemistry , Plant Extracts/therapeutic use , Administration, Topical
3.
Food Chem Toxicol ; 177: 113852, 2023 Jul.
Article in English | MEDLINE | ID: mdl-37244598

ABSTRACT

The ostrich oil (OO) has been topically used for decades to treat skin diseases. Its oral use has been encouraged through e-commerce advertising several health benefits to OO without scientific evidence on its safety or effectiveness. This study presents the chromatographic profile of a commercially available OO and its acute and 28-day repeated dose in vivo toxicological profiles. OO anti-inflammatory and antinociceptive effects were also investigated. Omega-9 (ω-9; oleic acid; 34.6%) and -6 (linoleic acid; 14.9%) were detected as OO main constituents. A high single dose of the OO (2 g/kg of ω-9) demonstrated no or low acute toxicity. However, when orally treated with OO (30-300 mg/kg of ω-9) for 28 consecutive days, mice exhibited altered locomotor and exploratory activities, hepatic damage, and increased hindpaw sensitivity accompanied by increased levels of cytokine and brain-derived neurotrophic factor in their spinal cords and brains. Lack of anti-inflammatory or antinociceptive activities was also evidenced in 15-day-OO treated mice. These results indicate that chronic consumption of OO induces hepatic injury, in addition to neuroinflammation and subsequent hypersensitivity and behavioural changes. Thus, there is no evidence to support OO use to treating illness in humans.


Subject(s)
Struthioniformes , Humans , Animals , Mice , Olive Oil/chemistry , Neuroinflammatory Diseases , Toxicity Tests , Analgesics/toxicity
4.
Toxicol Res (Camb) ; 11(6): 987-1002, 2022 Dec.
Article in English | MEDLINE | ID: mdl-36569486

ABSTRACT

Indonesian clove cigarettes-called "kretek" due to the crackling sound that can be heard when the product burns-are tobacco products containing clove and the "saus", a mixture of essential oils and plant extracts whose ingredients are mostly kept in secret. It is important to determine which ingredients those are to properly assess the effects that clove cigarettes can cause. An organoleptic, qualitative and quantitative analysis was made in 9 different brands of clove cigarettes obtained in Brazil. Nicotine, eugenol, menthol, and ß-caryophyllene were quantified through gas chromatography coupled to mass spectrometry. The samples presented 20 different compounds, and all samples had a different combination of the compounds. Nicotine concentrations were generally higher than eugenol, and lower than nicotine concentration in a conventional cigarette. One sample had menthol even though the cigarette pack did not inform that it was a menthol product. There were traces of 2 unusual substances. Clindamycin is an antibiotic that can be used to treat bacterial infections in respiratory airways, and octodrine is an amphetaminic stimulant used in nutritional supplements, considered as a substance of doping by the World Anti-Doping Association. The presence of both substances was not tested using certified reference materials, but its possible presence raises concern about the compounds in kretek cigarettes. There should be more studies about the contents of clove cigarettes, to improve antitobacco legislations and regulations. This way it would be possible to properly inform the risks of smoking clove cigarettes and to diminish the number of tobacco users throughout the world.

5.
Crit Rev Toxicol ; 52(4): 259-293, 2022 04.
Article in English | MEDLINE | ID: mdl-35971813

ABSTRACT

INTRODUCTION: The general lack of knowledge about the composition of clove cigarettes and the large number of terms that can be used to define different types of cigarettes that contain cloves makes it difficult to find scientific articles focused on the subject. We reviewed the publications that cited clove cigarettes to assess their relevance. METHODS: We searched publications on Scopus, ScienceDirect, PubMed, and Portal CAPES during the first semester of 2021, without date restrictions. Through a quality assessment, the studies found were assorted in ten different categories. RESULTS: Indonesian clove cigarettes-also known as kretek-are a mixture of tobacco and cloves rolled in a cigarette and sprayed with oils, plant extract, and food flavorings, in an unknown quantity and composition, different from each brand, which is usually kept in secret. Due to the relatively low prevalence of use in the general population, most publications on tobacco products tend to ignore clove cigarettes or place them in an existing category. Clove cigarettes can be hand-rolled, machine-made, filtered, unfiltered, and each form can be named differently. The interchangeable use of each term, sometimes grouping conventional cigarettes in the mix, can lead the researcher to consider a publication that should be excluded. CONCLUSION: The existing regulations on flavored cigarettes, although well-intentioned, are still somewhat vague and broad, leaving possible loopholes that can be exploited by the tobacco industries. Fully understanding the precise effects caused by clove cigarettes can be an important tool in future discussions about tobacco control.


Subject(s)
Syzygium , Tobacco Products , Flavoring Agents , Humans , Oils , Plant Extracts , Smoke
6.
Chem Biodivers ; 19(8): e202200369, 2022 Aug.
Article in English | MEDLINE | ID: mdl-35718744

ABSTRACT

Few studies were performed on the volatile components' properties of propolis from native Brazilian stingless bees. This work sought to extract, chemically characterize, and evaluate of the antimicrobial properties of volatile oils from propolis of the stingless bees Melipona quadrifasciata quadrifasciata (MQ) and Tetragonisca angustula (TA). The volatile oils from the pulverized propolis samples were obtained in a Clevenger apparatus and characterized by gas chromatography coupled to mass spectrometry (GC/MS) and to flame ionization detector (GC-FID). All samples showed promising activity against Mycoplasma pneumoniae, with MICs from 103 to 224 µg mL-1 , nonetheless, they were less active against cell walled bacteria. Activity against Candida species was moderate, but one MQ sample showed a MIC value of 103 µg mL-1 against C. tropicallis. Oils' fractionation showed no improvement in antibacterial activity. The promising antibacterial effect against this microorganism is likely related to the synergism between the components of the volatile oils.


Subject(s)
Anti-Infective Agents , Ascomycota , Oils, Volatile , Propolis , Animals , Anti-Bacterial Agents/pharmacology , Anti-Infective Agents/pharmacology , Brazil , Gas Chromatography-Mass Spectrometry , Oils, Volatile/pharmacology , Propolis/chemistry , Propolis/pharmacology
7.
Article in English | MEDLINE | ID: mdl-35447522

ABSTRACT

Psidium cattleyanum has two morphotypes: one with yellow fruits and other with red fruits. The leaves are popularly used as anti-inflammatory. However, no distinction is made between the types. Therefore, this study compared chemical and pharmacological data of both morphotypes to select proper biomarkers to ensure P. cattleyanum leaves quality. After extraction optimization by experimental design, 28 samples were analyzed by HPLC. Using Principal Component Analysis, it was possible to detect two chemotypes, unrelated to the color of the fruits. However, the extracts obtained from both chemotypes seemed to play similar anti-inflammatory effect, demonstrated by anti-chemotactic activity. The compounds common to both chemotypes were isolated and identified as hyperoside, miquelianin and quercitrin; these compounds also demonstrated anti-inflammatory potential. Since both chemotypes played similar activity, along with the isolated flavonoids, these flavonoids were selected as biomarkers for quality control of P. cattleyanum leaves. Following ICH guidelines, a HPLC method was validated. In summary, this study demonstrated that hyperoside, miquelianin and quercitrin can be used as biomarkers for quality control of P. cattleyanum leaves and a method was developed and validated to be used interchangeably for both morpho- and chemotypes.


Subject(s)
Psidium , Biomarkers/analysis , Flavonoids/analysis , Fruit/chemistry , Plant Extracts/chemistry , Plant Leaves/chemistry , Psidium/chemistry
8.
Braz. J. Pharm. Sci. (Online) ; 58: e181097, 2022. tab, graf
Article in English | LILACS | ID: biblio-1374562

ABSTRACT

Abstract Essential oils from four Ocotea species collected in southern Brazil were evaluated for chemical composition using gas chromatography coupled with mass spectrometry. The primary compound identified in O. acutifolia essential oil was an unsaturated tetracyclic diterpene, phyllocladene (67.7%), followed by a sesquiterpene hydrocarbon, ß-selinene (18.0%). The sesquiterpene fraction was predominant in oils from two collections of O. puberula; ß-caryophyllene (25.2%) and globulol (22.6%) were the major compounds identified in collections 1 and 2, respectively. O. silvestris essential oil contained predominantly germacrene D and bicyclogermacrene. These compounds were also predominant in essential oil from O. indecora leaves collected from shady habitats. By contrast, essential oil extracted from O. indecora grown under direct sunlight contained mainly oxygenated sesquiterpenes, such as guaiol (30.2%), α-eudesmol (27.6%), and ß-eudesmol (12.7%). Chemotaxis assays showed that Ocotea essential oils had no significant inhibitory activity on leukocyte migration compared with a chemotactic stimulant (lipopolysaccharide from Escherichia coli). However, the oils exhibited antifungal activity against Candida parapsilosis, with a minimum inhibitory concentration of 500 µg/mL. To our knowledge, this is the first study to investigate the in vitro antifungal and antichemotactic activities of essential oils from Ocotea species native to southern Brazil


Subject(s)
Oils, Volatile/chemistry , Ocotea/anatomy & histology , Biological Products , Ecosystem , Lauraceae/classification , Candida parapsilosis , Gas Chromatography-Mass Spectrometry/methods
9.
Phytomedicine ; 58: 152748, 2019 May.
Article in English | MEDLINE | ID: mdl-31005722

ABSTRACT

BACKGROUND: Several species of Salvia are used as medicinal plants around the world. Biological activities of isolated compounds have been described, being diterpenes frequently responsible for the effects. PURPOSE: Isolation of diterpenes from Salvia uliginosa Benth. and evaluation of the antichemotactic and leishmanicidal activities of the isolated compounds. STUDY DESIGN: To isolate diterpenes from S. uliginosa and evaluate their antichemotactic and leishmanicidal activities in vitro. METHODS: The exudate of S. uliginosa was obtained by rapidly dipping the aerial parts in dichloromethane. The compounds were isolated by repeated column chromatography over silica gel. The effects on L. amazonensis growth, survival, DNA degradation, ROS generation, as well as the antichemotactic activity and cytotoxicity of the compounds towards human erythrocytes and macrophages were evaluated. RESULTS: A novel icetexane diterpene, isoicetexone (IsoICT) along with the known diterpenes icetexone (ICT), and 7-acetoxy-6,7-dihydroicetexone were isolated from the dichloromethane surface exudate of S. uliginosa. The structures were elucidated using NMR and MS experiments, and by comparison with previously reported data. IsoICT and ICT at low concentrations caused completely inhibition of neutrophils migration in vitro. In addition, IsoICT and ICT showed high leishmanicidal activity against L. amazonensis, induced ROS production in parasites and presented low cytotoxicity against macrophages and human erythrocytes, and moderate to high selectivity index. CONCLUSION: These data indicated that IsoICT and ICT exhibit potent antichemotactic and leishmanicidal effects. Further studies are needed in order to evaluate the in vivo activities as well as the toxicity of the compounds.


Subject(s)
Antiprotozoal Agents/chemistry , Chemotaxis/drug effects , Diterpenes/chemistry , Salvia/chemistry , Antiprotozoal Agents/pharmacology , Cells, Cultured , Diterpenes/pharmacology , Drug Evaluation, Preclinical/methods , Erythrocytes/drug effects , Humans , Leishmania/drug effects , Macrophages/drug effects , Molecular Structure , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Reactive Oxygen Species/metabolism
10.
Biomed Chromatogr ; 33(2): e4393, 2019 Feb.
Article in English | MEDLINE | ID: mdl-30239022

ABSTRACT

Pomegranate is of current interest owing to the existing potential for industrial uses of fruit peels. This includes its availability as a raw vegetable material, a byproduct that constitutes residue in the use of the species and is recognized as a functional product, and beneficial health properties, as will be demonstrated in the studies cited. Therefore, it is necessary to ensure its effectiveness and safety. Toward this end, the aim of this study was to develop and validate an analytical method for the separation and quantification of total punicalagin present in the bark of the fruit of Punica granatum by HPLC. Purity tests such as water determination and total ashes were also performed. The ability of the extract and enriched fraction of punicalagin to inhibit leukocyte migration in vitro was determined by the Boyden's chamber method. The developed HPLC method demonstrated good separation and quantification of the punicalagin α and ß anomers. The method is efficient and reliable, and can ultimately be used for the analysis of the extract of pomegranate. The crude extract and the fraction of punicalagins significantly inhibited leukocyte migration at concentrations of 1 and 10 µg/mL in relation to the negative control, indicating potential antichemotactic action.


Subject(s)
Chemotaxis/drug effects , Chromatography, High Pressure Liquid/methods , Fruit , Hydrolyzable Tannins/pharmacology , Lythraceae/chemistry , Plant Extracts/pharmacology , Animals , Cells, Cultured , Fruit/chemistry , Fruit/standards , Hydrolyzable Tannins/analysis , Limit of Detection , Linear Models , Male , Neutrophils/drug effects , Plant Extracts/analysis , Quality Control , Rats , Rats, Wistar , Reproducibility of Results
11.
J Enzyme Inhib Med Chem ; 28(1): 218-22, 2013 Feb.
Article in English | MEDLINE | ID: mdl-22117191

ABSTRACT

The alkaloid extracts of four Huperzia and one Lycopodiella species, from Brazilian habitats, were tested for their in vitro anticholinesterase activities. IC(50) values showed a potent acetylcholinesterase inhibition for H. reflexa (0.11 ± 0.05 µg/mL), followed by H. quadrifariata (2.0 ± 0.3 µg/mL), H. acerosa (5.5 ± 0.9 µg/mL), H. heterocarpon (25.6 ± 2.7 µg/mL) and L. cernua (42.6 ± 1.5 µg/mL). A lower inhibition of butyrylcholinesterase was observed for all species with the exception of H. heterocarpon (8.3 ± 0.9 µg/mL), whose alkaloid extract presented a selectivity for pseudocholinesterase. Moreover, the chemical study of the bioactive extracts performed by GC-MS, revealed the presence of a number of Lycopodium alkaloids belonging to the lycopodane, flabellidane and cernuane groups. Surprisingly, the potent acetylcholinesterase inhibitors huperzines A and B were not detected in the extracts, suggesting that other alkaloids may be responsible for such an effect.


Subject(s)
Alkaloids/pharmacology , Cholinesterase Inhibitors/pharmacology , Lycopodiaceae/chemistry , Brazil , Butyrylcholinesterase/metabolism , Drug Evaluation, Preclinical/methods , Gas Chromatography-Mass Spectrometry , Heterocyclic Compounds, 4 or More Rings/pharmacology , Humans , Huperzia/chemistry , Inhibitory Concentration 50 , Plant Extracts/analysis , Plant Extracts/chemistry , Plant Extracts/pharmacology , Quinolizines/pharmacology , South America
12.
Environ Pollut ; 163: 24-31, 2012 Apr.
Article in English | MEDLINE | ID: mdl-22325427

ABSTRACT

Biological indicators are widely used to monitor genotic compounds and air quality in urban environments. Parmotrema tinctorum and Teloschistes exilis have been used to verify the presence of pollutants and analyze morphophysiological alterations in the thallus of species caused by their action. Species were exposed for seven months, in an urban area, in southern Brazil. Mutagenicity and cytotoxicity of PM10 organic extracts were assessed in the Salmonella/microsome assay at two stations. High concentrations of S, Pb, Cr, Zn and Hg were registered in the last period of exposure and more significant morphophysiological damages were verified in the lichens. Generally a higher mutagenic activity is observed in organic extracts of airborne particulate matter during the first months and in the third period of exposure of lichens. In addition, nitro compounds was detected through nitro-sensitive strains. Lichens and mutagenic biomarkers enabled the evaluation of air quality and the presence of environmentally-aggressive compounds.


Subject(s)
Air Pollutants/analysis , Environmental Monitoring/methods , Mutagens/analysis , Air Pollutants/toxicity , Air Pollution/statistics & numerical data , Atmosphere/chemistry , Brazil , Cities , Lichens/drug effects , Lichens/growth & development , Metals, Heavy/analysis , Metals, Heavy/toxicity , Mutagens/toxicity , Salmonella/drug effects
13.
J Chromatogr A ; 1219: 147-53, 2012 Jan 06.
Article in English | MEDLINE | ID: mdl-22169196

ABSTRACT

Baccharis trimera commonly named 'carqueja', is wide-spread in South America and are used as raw material for herbal medicines. A reversed-phase liquid chromatography (RP-LC) method coupled to diode array detector was developed for the analysis of caffeoylquinic acids (CQAs), the main compounds responsible for its digestive activity. The identity of the quinic acids was established by mass spectrometry and were them: 5-O-[E]-caffeoylquinic acid, 3,4-O-[E]-dicaffeoylquinic acid, 3,5-O-[E]-dicaffeoylquinic acid, 4,5-O-[E]-dicaffeoylquinic acid and a tricaffeoylquinic acid. The RP-LC method for the quantitation of the caffeoylquinic acids was validated according to ICH guidelines, based on the following parameters: linearity, selectivity, robustness, limits of detection and quantification, precision and recovery. Hydroalcoholic extracts were prepared by the maceration of the plant material with ethanol:water 1:1 (v/v) in a 0.1:25 g mL(-1) plant:solvent ratio in a water bath at 40°C. Validation data indicated that the HPLC method proposed is suitable for the analysis of caffeoylquinic acids in B. trimera raw material. The results of the LOD and LOQ analyses for the 5-CQA were 4.1 µg mL(-1) and 12.5 µg mL(-1), respectively, 1.3 µg mL(-1), 3.9 µg mL(-1) for 4,5-diCQA and 1.7 µg mL(-1), 5.1 µg mL(-1) for triCQA. The levels of total CQAs ranged from 2.1 to 4.0 g% (w/w). The influence of season harvest and site collection was also evaluated and variations were observed in the results and can be related to phonologic phase, different locations, seasons and soil. Long term and photostability of plant material were carried out and was observed a stable behavior during the time of the experiments.


Subject(s)
Baccharis/chemistry , Chromatography, Reverse-Phase/methods , Plant Extracts/chemistry , Quinic Acid/analogs & derivatives , Argentina , Brazil , Chromatography, High Pressure Liquid , Drug Stability , Limit of Detection , Photochemical Processes , Quinic Acid/analysis , Quinic Acid/chemistry , Quinic Acid/isolation & purification , Reproducibility of Results , Tandem Mass Spectrometry
14.
Pharm Biol ; 49(3): 306-13, 2011 Mar.
Article in English | MEDLINE | ID: mdl-21323483

ABSTRACT

CONTEXT: Copaiba oil is an oleoresin made up of resin acids and volatile compounds, and it is obtained by tapping the trunks of trees that are members of the Copaifera L. (Leguminoseae) genus and are found in tropical parts of Latin America. OBJECTIVE: This study analyzed the chemical composition of Copaifera multijuga Hayne oil and conducted preclinical trials to investigate anti-inflammatory effects and any action it may have on the central nervous system (CNS) of rats. MATERIALS AND METHODS: The chemical analysis was carried out using gas chromatography with mass spectroscopy. Anti-inflammatory activity was measured by leucocytes mobilization, by chemotaxis assay in Boyden's chamber, and by pleurisy model in rats. CNS effect was determined by plus maze and open-field assays. The statistical test applied was analysis of variance (ANOVA) followed by Tukey's test or ANOVA followed by Duncan's test. RESULTS: The oil was composed of sesquiterpenes with the predominance of ß-caryophyllene (36.0%), followed by α-copaene (18.8%), ß-bisabolene (8.5%), and α-trans-bergamotene (7.0%). Data demonstrated that at 100 and 200 mg/kg doses and at a concentration of 200 µl/ml copaiba essential oil presented anti-inflammatory effects both in vivo and in vitro based on reduced leukocyte migration to the rats' pleural cavity and to the chemotactic agent lipopolysaccharide solution, respectively. During the experiments investigating CNS effects, locomotive and exploratory activities were reduced and the animals' anxiety increased at 100 and 200 mg/kg. CONCLUSION: The results obtained suggest that copaiba oil has an interesting anti-inflammatory effect and important effect on the CNS.


Subject(s)
Fabaceae , Plant Oils/isolation & purification , Plant Oils/pharmacology , Animals , Cell Movement/drug effects , Cell Movement/physiology , Drug Evaluation, Preclinical/methods , Leukocytes, Mononuclear/drug effects , Leukocytes, Mononuclear/physiology , Male , Maze Learning/drug effects , Maze Learning/physiology , Rats , Rats, Wistar
15.
J Food Sci ; 76(7): C991-6, 2011 Sep.
Article in English | MEDLINE | ID: mdl-22417549

ABSTRACT

UNLABELLED: Strawberry guava (Psidium cattleianum Sabine) is a native fruit of Brazil widely consumed fresh and used in the food industry. In this context, the present study deals with the chemical characterization and the antioxidant activity of the red (Psidium cattleianum) and yellow (P. cattleianum var. lucidum Hort.) strawberry guava fruits, cultivars Irapuã and Ya-Cy, respectively. Knowledge of chemical composition is fundamental to human nutrition, contributing to the quality of foods. Phenolic compounds in both fruits were analyzed by HPLC-DAD and the total flavonoid content was determined by the Folin-Ciocalteu assay. The antioxidant activity was evaluated by the total reactive antioxidant (TRAP) method. Psidium cattleianum presented a higher content of polyphenolic compounds than P. cattleianum var. lucidum (501.33 and 292.03 mg/100 g, respectively), with hyperoside being one of the major flavonoids identified for both cultivars. In addition to flavonoids, P. cattleianum presented an anthocyanin, identified as cyanidin. The antioxidant activity varied in a concentration-dependent manner for both strawberry guava species. The volatile oils in fruits and fatty acids in seeds were quantified by GC-EM. The analysis of the essential oil of yellow strawberry guava was compared with a previous study on the red cultivar, revealing ß-caryophyllene as the main component in both oils. The fatty acid composition was also quite similar and was especially characterized by the presence of unsaturated fatty acids (86.25% and 76%, respectively), among which linoleic acid as the most abundant. PRACTICAL APPLICATION: In this study, the chemical characterization and the antioxidant activity of the red (Psidium cattleianum) and yellow (P. cattleianum var. lucidum Hort.) strawberry guava fruits were investigated. This is important for potential application of strawberry guava as functional food. Moreover, it may be the experimental basis for further development and use in food industry.


Subject(s)
Antioxidants/analysis , Fruit/chemistry , Psidium/chemistry , Antioxidants/pharmacology , Brazil , Chromatography, High Pressure Liquid , Fatty Acids/analysis , Flavonoids/analysis , Oils, Volatile/analysis , Phenols/analysis , Plant Oils/analysis , Seeds/chemistry , Species Specificity
16.
Planta Med ; 77(7): 698-704, 2011 May.
Article in English | MEDLINE | ID: mdl-21058242

ABSTRACT

Flavonoids are polyphenols that are ubiquitous in plants and frequently consumed in the diet. They are suggested to have many beneficial actions on human health, including anti-inflammatory activity. Their properties have been studied in a number of cell types, but little is known about their effects on neutrophil biology. Consequently, we selected 25 flavonoids with different structural features to evaluate their in vitro inhibition of rat polymorphonuclear neutrophil (PMN) chemotaxis, employing a modified Boyden chamber. Migratory activity was measured towards a chemotactic stimulant, formyl-Met-Leu-Phe or lipopolysaccharide. Furthermore, the cytotoxic effect of flavonoids on PMNs was determined by the release of cytosolic lactate dehydrogenase (LDH). Ten flavonoids significantly retarded the migration of PMNs with at least one of the concentrations tested in a range between 0.625 and 100 µM; the best antichemotactic agents were flavone, flavonol, quercetin and rutin. None of the flavanones evaluated presented any significant inhibition of migration in this assay. Our findings indicated that non-hydroxylated flavones possess a better antichemotactic activity when compared to flavones with hydroxy groups. The presence of a sugar moiety in rutin did not produce any increase in this effect, when compared to the respective aglycone analogue. Finally, none of the flavonoids exhibited cell toxicity and for many of these flavonoids this is the first report of the inhibition of PMN chemotaxis.


Subject(s)
Chemotaxis, Leukocyte/drug effects , Flavonoids/pharmacology , Neutrophils/drug effects , Plant Extracts/pharmacology , Achyrocline/chemistry , Animals , Anti-Inflammatory Agents/pharmacology , Cell Migration Inhibition/drug effects , Chemotactic Factors/antagonists & inhibitors , Chemotactic Factors/pharmacology , Cytotoxins/pharmacology , Flavonoids/chemistry , Lipopolysaccharides/antagonists & inhibitors , Lipopolysaccharides/pharmacology , N-Formylmethionine Leucyl-Phenylalanine/antagonists & inhibitors , N-Formylmethionine Leucyl-Phenylalanine/pharmacology , Neutrophils/immunology , Plant Extracts/chemistry , Rats
17.
Invest New Drugs ; 27(5): 440-6, 2009 Oct.
Article in English | MEDLINE | ID: mdl-19002382

ABSTRACT

We have studied the apoptotic pathway activated in response to marine sponge extracts of Polymastia janeirensis. The effect on intracellular ROS production was also examined. Exposure of U138MG glioma cell line to doses higher than 5 microg/mL has decreased glioma cell viability, with an IC(50) <15 microg/mL for both aqueous and organic extracts. However, extracts at higher doses (50 and 100 microg/mL) have stronger cytotoxic effects, decreasing more than 90% of glioma cell viability. The antioxidant Trolox (100 microM) reversed the cell death percentage induced by extracts at 10 and 25 microg/mL. The type of cell death induced by such high doses was predominantly necrosis, while a high percentage of apoptotic glioma cells was found at 10 microg/mL. Moreover, inhibition of caspase-8 with Z-IETD (a caspase-8 inhibitor) had no effect on the amount of apoptosis induced by 10 microg/mL, but inhibition of caspase-9 with Z-LEHD (a caspase-9 inhibitor) decreased apoptosis. We also observed a dose-dependent increase in ROS production, and similarly to effects observed on viability of glioma cells, and on cell death, higher doses also had more severe effects. Co-treatment with Trolox significantly reduced ROS production by extracts at doses lower than 50 microg/mL. This is a first report demonstrating that marine sponge extracts of P. janeirensis induce oxidative cell death through a caspase-9 apoptotic pathway.


Subject(s)
Apoptosis/drug effects , Brain Neoplasms/pathology , Caspase 9/metabolism , Glioma/pathology , Porifera/chemistry , Tissue Extracts/pharmacology , Animals , Brain Neoplasms/drug therapy , Flow Cytometry , Glioma/drug therapy , Humans , Reactive Oxygen Species/metabolism , Tumor Cells, Cultured
18.
Invest New Drugs ; 27(1): 13-20, 2009 Feb.
Article in English | MEDLINE | ID: mdl-18454276

ABSTRACT

Marine sponges have been prominently featured in the area of cancer research. Here, we examined the anti-proliferative effects of crude extracts (aqueous and organic) of the Brazilian marine sponge Polymastia janeirensis in the U138MG human glioma cell line. Moreover, we examined the effects of extracts on selective cytotoxicity in the glioma cells in comparison with a normal cell culture. Exposure of glioma cells to treatments (24 h) resulted in cell number decrease at all doses tested, with both aqueous and organic extracts (IC(50) <20 and <30 microg/ml, respectively). Parallel to this result, sponge extracts reduced glioma cell viability (IC(50) <15 microg/ml for both extracts). However, higher doses (50 and 100 microg/ml) induced a stronger cytotoxic effect when compared to the lower dose tested (10 microg/ml), inhibiting more than 80% of cellular growth and viability. Propidium iodide uptake and flow cytometry analysis further showed that sponge extracts caused necrosis in the glioma cell line at higher doses, while a high percentage of apoptotic glioma cells were observed at 10 microg/ml. Moreover, apoptosis was prevented by the pan-caspase inhibitor Z-VAD, suggesting that marine sponge extracts, at lower doses, induce caspase-dependent apoptosis in U138MG glioma cells. Surprisingly the extracts herein tested were more effective than temozolomide, a potent inductor of apoptosis used for the treatment of malignant gliomas. Furthermore, our results suggested a selectivity cytotoxic effect on glioma cell line in comparison with a normal cell culture, since the effect on viability found in glioma cells was not observed in astrocyte cultures with the lower dose (10 microg/ml). Thus, this marine sponge may be considered a good candidate for development of new cancer medicines with antitumor activity against gliomas.


Subject(s)
Antineoplastic Agents/pharmacology , Complex Mixtures/pharmacology , Glioma/drug therapy , Porifera/chemistry , Amino Acid Chloromethyl Ketones/antagonists & inhibitors , Animals , Apoptosis/drug effects , Astrocytes/drug effects , Brazil , Cell Line, Transformed , Cell Line, Tumor , Dacarbazine/analogs & derivatives , Dacarbazine/pharmacology , Humans , Temozolomide
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