ABSTRACT
BACKGROUND: Point-of-collection testing (POCT) devices for psychoactive substance detection through oral fluid samples are used in several countries for traffic enforcement. However, the reported reliability of such devices is quite heterogeneous among studies, and evaluating and comparing their analytical performance is of paramount importance to guide enforcement policies. AIM: To evaluate the analytical reliability of four POCT devices for the detection of cocaine and cannabinoids using oral fluid samples of Brazilian drivers. METHOD: A total of 168 drivers were recruited during standard roadblockfI procedures in Southern Brazil. Subjects were screened using one of the following POCT devices: the DDS2™, the DOA MultiScreen™, the Dräger Drug Test 5000™ and the Multi-Drug Multi-Line Twist Screen Device™ (MDML). Results of the screening tests were compared with chromatographic analyses in order to obtain the reliability parameters. RESULTS: The prevalence of confirmed positive samples for cocaine and cannabinoids were 9 % and 4.4 %, respectively. For cocaine, three POCT devices (MDML™, Dräger DrugTest 5000™, DOA MultiScreen™) showed good reliability, greater than 80 % of performance measures, using guidelines for research on drugged driving published by Walsh et al. (cutoff 10ng/mL). However, for cannabinoids, the devices had low reliability-only Dräger DrugTest 5000™ had good performance using cut-offs proposed by Walsh et al. (cutoff 2ng/mL). CONCLUSION: We observed a high prevalence of drivers testing positive for cocaine and cannabinoids. Most devices achieved good reliability performance for cocaine detection using cutoffs proposed by Walsh et al. or using the device's own cutoff. Instead, the reliability for cannabinoid detection obtained the desired parameters in just one device using cut-offs proposed by Walsh et al. and its own cutoff. Difficulties in detecting cannabinoids at the roadside should be better evaluated before the implementation of such tests.
Subject(s)
Cannabinoids/analysis , Cocaine/analysis , Driving Under the Influence , Saliva/chemistry , Substance Abuse Detection/methods , Adolescent , Adult , Brazil , Female , Humans , Illicit Drugs/analysis , Male , Middle Aged , Reproducibility of Results , Young AdultABSTRACT
PURPOSE: This study aimed to evaluate the effects of the subchronic consumption of energy drinks and their constituents (caffeine and taurine) in male Wistar rats using behavioural and oxidative measures. METHODS: Energy drinks (ED 5, 7.5, and 10 mL/kg) or their constituents, caffeine (3.2 mg/kg) and taurine (40 mg/kg), either separately or in combination, were administered orally to animals for 28 days. Attention was measured though the ox-maze apparatus and the object recognition memory test. Following behavioural analyses, markers of oxidative stress, including SOD, CAT, GPx, thiol content, and free radicals, were measured in the prefrontal cortex, hippocampus, and striatum. RESULTS: The latency time to find the first reward was lower in animals that received caffeine, taurine, or a combination of both (P = 0.003; ANOVA/Bonferroni). In addition, these animals took less time to complete the ox-maze task (P = 0.0001; ANOVA/Bonferroni), and had better short-term memory (P < 0.01, Kruskal-Wallis). The ED 10 group showed improvement in the attention task, but did not differ on other measures. In addition, there was an imbalance in enzymatic markers of oxidative stress in the prefrontal cortex, the hippocampus, and the striatum. In the group that received both caffeine and taurine, there was a significant increase in the production of free radicals in the prefrontal cortex and in the hippocampus (P < 0.0001; ANOVA/Bonferroni). CONCLUSIONS: Exposure to a combination of caffeine and taurine improved memory and attention, and led to an imbalance in the antioxidant defence system. These results differed from those of the group that was exposed to the energy drink. This might be related to other components contained in the energy drink, such as vitamins and minerals, which may have altered the ability of caffeine and taurine to modulate memory and attention.
Subject(s)
Attention/drug effects , Caffeine/pharmacology , Energy Drinks , Memory/drug effects , Taurine/pharmacology , Animals , Caffeine/administration & dosage , Energy Drinks/analysis , Male , Oxidation-Reduction , Rats , Rats, Wistar , Taurine/administration & dosageABSTRACT
The essential oils extracted from leaves of the Southern Brazilian native species Drimys angustifolia Miers (DA) and Drimys brasiliensis Miers (DB) by Clevenger distillation were analyzed by gas chromatography/mass spectrometry (GC/MS). The oils of DA and DB consisted predominantly of monoterpenoids and sesquiterpenoids. The largest components of DA oil were bicyclogermacrene (19.6%), sabinene (9.7%)and myrcene (5.2%), while DB oil was characterized by cyclocolorenone (18.2%), followed by terpinen-4-ol (8.7%) and alpha-gurjunene (6.9%). Laboratory tests were carried out to determine the repellency of the essential oils to the drywood termite Cryptotermes brevis (Isoptera: Kalotermitidae). It was observed that the oil showed repellency at the concentrations 25, 12.5, and 6.25 μg/mL. The oils of both species exhibited a negative repellency index, which represents repellent activity, except for DA oil at the highest concentration, which was attractive. Five deaths (11% of the termitesample) were observed at 25 μg/mL DA, in the fourhour repellency test, while four deaths occurred at 12.5 μg/mL (approximately 9%). The essential oil of DB did not cause any termite deaths...
Os óleos essenciais obtidos das folhas das árvores nativas do sul do Brasil Drimys angustifolia Miers (DA)e Drimys brasiliensis Miers (DB) foram analisados por cromatografia gasosa acoplada a espectrometria de massas (CG/EM). O óleo de DA foi caracterizado pela presença de monoterpenóides e sesquiterpenóides, biciclogermacreno (19,6%), seguido por sabineno (9,7%) e mirceno (5,2%). O óleo de DB foi caracterizado por sesquiterpenóides e monoterpenóides, ciclocolorenona (18,2%), seguido por terpinen-4-ol (8,7%) e alfagurjuneno(6,9%). Os testes foram realizados a fim de se determinar o potencial repelente dos óleos essenciais contra o cupim de madeira seca Cryptotermes brevis (Isoptera: Kalotermitidae) nas doses de 25, 12,5, e 6,25 μg/mL. Ambas as espécies mostraram índice de repelência negativo, o que representa a ocorrência da atividade repelente, exceto na maior concentração de DA, na qual o óleo mostrou-se atraente. Cinco mortes foram observadas na concentração de 25 μg/mL de DA, correspondendo a 11% do total em quatro horas de análise, sendo que 9% ocorreram na concentração de 12,5 μg/mL. No caso do óleo essencial de DB não foram observadas mortes de cupins...
Subject(s)
Drimys , Insect Repellents , Isoptera , Oils, VolatileABSTRACT
As intoxicações por medicamentos são predominantes no Brasil e frequentes na faixa etária de 0 a 14 anos. O ácido valproico (AV) vem se destacando em virtude do aumento do seu espectro de utilização na terapêutica clínica, porém, a hepatotoxicidade pode ser desencadeada por altas concentrações desse fármaco, apresentando alta incidência em crianças. Logo, tornam-se importantes métodos rápidos de quantificação desse fármaco, a fim de auxiliar o clínico no tratamento da intoxicação. Diante desse cenário, os objetivos deste trabalho foram comparar metodologias analíticas para quantificação de AV por CLAE-F (fluorescência) e CG/DIC (detecção por ionização de chama) em relação à sua potencial aplicação em toxicologia clínico-laboratorial de urgência. Para quantificação de AV por fluorescência, realizou-se a derivatização do AV com 4-(Bromometil)-7-metoxicumarina, sendo o produto da reação analisado em λ de emissão de 325 e detecção de 398 nm, na faixa de calibração de 1-300miug/mL. Com relação à CG/DIC, esta apresentou-se linear na faixa de 100-2000 miug/mL, sem necessidade de derivatização prévia. A técnica de CG/DIC mostrou-se mais apropriada para análises toxicológicas de urgência em casos de intoxicação com AV, tendo em vista o menor tempo de corrida, a linearidade obtida, menor custo, rapidez e praticidade, além de utilizar um equipamento robusto, disponível na grande maioria dos laboratórios de toxicologia de pequeno e médio porte.
Poisoning by drugs is rather frequent in Brazil in the age range of 0 to 14 years. Intoxication by valproic acid (VA) stands out because of an increase in its spectrum of clinical use; hepatotoxicity is an important reaction that can be triggered by high concentrations of this drug and there is a high incidence of toxic events in children. Therefore, fast methods of analysing this drug are essential, in order to help the clinician to treat the intoxication. Given this scenario, the objective of this study was to compare analytical methods to determine VA, by HPLC-F (fluorescence) and GC/FID (flame ionization detection), assessing their potential application in the urgent toxicology clinic. For the fluorometric analysis, the VA was first derivatized with 4-bromomethyl-6, 7-dimethoxycoumarin, and the resulting compound was excited at λ = 325 nm and detected by the emission at 398 nm. The calibration range was 1-300 miug/mL. The GC/FID method showed a linear response in the range 100-2000 miug/mL, without requiring prior derivatization. The technique of GC/FID proved more appropriate for the urgent toxicological analysis of VA, in view of the shorter time of analysis, linearity, lower cost, speed, efficiency and the use of robust equipment that is already available in the great majority of small and medium-sized toxicological clinics.
Subject(s)
Fluorescence , Poisoning , Valproic Acid , Flame IonizationABSTRACT
Dietary supplements containing bitter orange unripe fruit extract/p-synephrine are consumed worldwide for lose weight. This study were conducted to determine the concentration of p-synephrine in unripe fruits and leaves from Citrus aurantium Lin, C. sinensis Osbeck, C. deliciosa Ten, C. limon Burm and C. limonia Osbeck, collected in Southern Brazil, and to evaluate the acute toxicity of C. aurantium extract and p-synephrine. A high performance liquid chromatographic method with diode array detector (HPLC-DAD) was optimized and validated for determination of p-synephrine. The results indicate that all of analyzed samples present p-synephrine in amounts that range from 0.012% to 0.099% in the unripe fruits and 0.029 to 0.438% in the leaves. Acute oral administration of C. aurantium extracts (2.5% p-synephrine, 300-5,000 mg/kg) in mice produced reduction of locomotor activity, p-synephrine (150-2,000 mg/kg) produced piloerection, gasping, salivation, exophtalmia and reduction in locomotor activity, which was confirmed in spontaneous locomotor activity test. All the effects were reversible and persisted for 3-4h. The toxic effects observed seem to be related with adrenergic stimulation and should alert for possible side effects of p-synephrine and C. aurantium.
Subject(s)
Citrus/chemistry , Synephrine/analysis , Synephrine/toxicity , Animals , Body Temperature/drug effects , Brazil , Calibration , Chromatography, High Pressure Liquid , Citrus/growth & development , Fruit/chemistry , Fruit/growth & development , Indicators and Reagents , Male , Mice , Motor Activity/drug effects , Plant Leaves/chemistry , Reference Standards , Reproducibility of Results , Spectrophotometry, UltravioletABSTRACT
The biocatalytic potential of Bipolaris sorokiniana was investigated in its ability to modify the monoterpene geraniol and the sesquiterpene alpha-bisabolol as exogenous substrates, using phosphate buffer as reaction medium. The cultures showed a promising oxidative profile, with conversion of geraniol to 6-methyl-5-hepten-2-one (74.9% yield) in a 5-day incubation and alpha-bisabolol to bisabolol oxide B (84.2% yield), in a 7-day incubation.
Subject(s)
Ascomycota/metabolism , Sesquiterpenes/metabolism , Terpenes/metabolism , Acyclic Monoterpenes , Bioreactors , Biotechnology , Biotransformation , Culture Media , Monocyclic Sesquiterpenes , Sesquiterpenes/chemistry , Terpenes/chemistryABSTRACT
The CNS activity of Lippia alba liquid and spray-dried extracts, containing the non-volatile fraction from the leaves, was investigated. L. alba liquid extracts were prepared by percolation with EtOH 40, 60 or 80%. The liquid extracts, named ES(40%,) ES(60%) and ES(80%,) were concentrated, the ethanol eliminated and then tested in Swiss mice to evaluate its sedative and anticonvulsant effects. The animals received the extracts, orally, in doses corresponding to 200 mg of dry residue by kilogram of body weight. All mice were evaluated in the barbiturate-induced sleep test. Similarly, other groups of mice were submitted to convulsions induced by pentylenetetrazol (PTZ). The concentrated extract obtained from ES(80%) showed the most significant sedative and myorelaxant effects as well as the highest total flavonoid content (66 mg/100 g, expressed in apigenin). Two spray-dried powders, SDP(1) and SDP(2), were prepared from ES(80%) using as excipients, respectively, colloidal silicon dioxide (CSD) and CSD associated to beta-cyclodextrin. Only SDP(1) showed sedative profile similar to that presented by ES(80). In conclusion, we demonstrated that the non-volatile fraction of L. alba, extracted in ethanol 80% (v/v), presents sedative and myorelaxant effects and that, among the tested extracts, this presents the highest flavonoid content. We demonstrated also the technological feasibility of spray-dried extracts and the influence of the excipient on its sedative properties.
Subject(s)
Central Nervous System Agents/pharmacology , Lippia , Animals , Brazil , Central Nervous System Agents/isolation & purification , Central Nervous System Agents/therapeutic use , Drug Evaluation, Preclinical/methods , Male , Mice , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Plant Leaves , Powders , Seizures/drug therapy , Sleep/drug effects , VerbenaceaeABSTRACT
A new alkaloid identified as 3beta,6beta-ditigloyloxynortropane as 3beta,7beta-ditigloyloxynortropane, 4-hydroxyhygrinic acid, methylecgonidine and tropacocaine have been isolated from the leaves of Erythroxylum argentinum. The new structure was established by means of spectroscopic techniques. Four other species E. deciduum, E. microphyllum, E. pelleterianum and E. cuneifolium collected in the state of Rio Grande do Sul were screened for methylecgonidine and tropacocaine by CG/MS. Two of these plants contain tropacocaine and two contain methylecgonidine. GC/MS analysis of all 5 species for cocaine proved fruitless. The chemotaxonomic significance of these results is discussed.
