RESUMEN
The purpose of this study is to determine the nutraceutic potential of different Capsicum sp, capsaicin, capsanthin and lutein and provide data in order to clarify the conflicting results obtained for capsaicin by different authors. To achieve these objectives, in vivo (geno/antigenotoxicity and lifespan assays in the animal model Drosophila) and in vitro (cytotoxicity and DNA-fragmentation assays in HL60 promyelocytic cell line) assays were carried out. Results showed that i) none of the tested substances were genotoxic except green hot pepper and capsaicin at the highest tested concentration (5 mg/mL and 11.5 µM respectively), ii) all tested substances except green hot pepper are antimutagenic against H2O2-induced damage, iii) only red sweet pepper significantly extend the lifespan and healthspan of D. melanogaster at 1.25 and 2.5 mg/mL, iv) all pepper varieties induce dose-depended cytotoxic effect in HL60 cells with different IC50, and v) all pepper varieties and capsaicin exerted proapoptotic effect on HL60 cells. IN CONCLUSION: (i) sweet peppers could be suggested as nutraceutical food, (ii) hot peppers should be moderately consumed, and (iii) supplementary studies are necessary to clarify the synergic effect of the carotenoids and capsaicinoids in the hot pepper food matrix.
Asunto(s)
Capsaicina/análisis , Supervivencia Celular/efectos de los fármacos , Suplementos Dietéticos/análisis , Drosophila melanogaster/crecimiento & desarrollo , Luteína/análisis , Piper nigrum/química , Animales , Antipruriginosos/análisis , Antipruriginosos/farmacología , Capsaicina/farmacología , Capsicum/química , Drosophila melanogaster/efectos de los fármacos , Femenino , Células HL-60 , Humanos , Técnicas In Vitro , Luteína/farmacología , Masculino , Piper nigrum/clasificación , Verduras/química , Xantófilas/análisis , Xantófilas/farmacologíaRESUMEN
Munchausen syndrome by proxy (MSBP), also known as fabricated or induced illness in a child by a caretaker, is a form of abuse where a caregiver deliberately produces or feigns illness in a person under his or her care, so that the proxy will receive medical care that gratifies the caregiver. The affected children are often hospitalized for long periods and endure repetitive, painful and expensive diagnostic attempts. We present an analytically confirmed case of MSBP by alimemazine. A 3-year-old boy was brought repetitively to a Pediatric Emergency Department by his mother because he presented limb tremors, dysarthria, obnubilation, and ataxia and generalized tonic-clonic seizures coinciding with intermittent fever. Neither the rest of the physical examination nor the complementary tests showed any significant alterations. MSBP was suspected and a routine systematic toxicological analysis in urine and blood was requested. Alimemazine was detected in all biological samples. The administration of this drug was never mentioned by the mother and the subsequent interview with her corroborated the suspicion of MSBP. Clinically, after separation from the mother, the child's neurological symptoms gradually improved until the complete disappearance of the cerebellar symptoms. Alimemazine was quantified in serum, urine, gastric content and cerebrospinal fluid samples by gas chromatography-mass spectrometry (maximum serum level was 0.42µg/ml). Hair quantification of alimemazine was performed by ultra-performance liquid chromatography-tandem mass spectrometry in different segments of hair. The results confirmed regular substance use during the at least eight last months (8.8, 14.7, 19.7 and 4.6ng/mg hair starting from most proximal segment). This patient represents the first case published with analytical data of alimemazine in blood, urine, gastric content, cerebrospinal fluid and hair, which allowed us to prove an acute and repetitive poisoning with alimemazine as evidence of MSBP.
Asunto(s)
Antipruriginosos/envenenamiento , Síndrome de Munchausen Causado por Tercero/diagnóstico , Trimeprazina/envenenamiento , Antipruriginosos/análisis , Maltrato a los Niños/diagnóstico , Preescolar , Cromatografía Liquida , Cromatografía de Gases y Espectrometría de Masas , Contenido Digestivo/química , Cabello/química , Humanos , Masculino , Trimeprazina/análisisRESUMEN
Dimemorfan was extracted from human plasma samples (100 µL) using MonoTip C(18) tips, which were packed with a C(18)-bonded monolithic silica gel attached to the inside of the tip. The samples, which contained dimemorfan and trimeprazine as an internal standard (IS), were mixed with 300 µL of distilled water and 50 µL of 1M glycine-sodium hydroxide buffer (pH 10). The mixture was extracted onto the C(18) phase of the tip by 20 sequential aspirating/dispensing cycles using a manual micropipettor. The analytes retained on the C(18) phase were then eluted with methanol by five sequential aspirating/dispensing cycles. The eluate was injected directly into a gas chromatograph and detected by a mass spectrometer with selected ion monitoring in positive electron ionization mode. An Equity-5 fused silica capillary column (30 m × 0.32 mm i.d., film thickness 0.25 µm) gave adequate separation of the dimemorfan, IS, and impurities. The recoveries of dimemorfan and the IS spiked into plasma were ≥83%. The regression equation for dimemorfan showed excellent linearity from 0.25 to 32.0 ng/100 µL of plasma, and the limit of detection was 0.125 ng/100 µL of plasma. The maximum intra-day and inter-day relative standard deviations were 13%, while accuracy ranged from 88% to 105%. Dimemorfan was stable for at least 12 h at 4°C, 4 weeks at -80°C, and three freeze-thaw cycles in plasma. This new method is expected to have application as a pretreatment for the rapid, simple, and quantitative determination of dimemorfan in plasma samples.
Asunto(s)
Morfinanos/análisis , Plasma/química , Extracción en Fase Sólida/métodos , Trimeprazina/análisis , Antipruriginosos/análisis , Antitusígenos/análisis , Humanos , Extracción en Fase Sólida/instrumentaciónRESUMEN
AIM: To explore whether intestinal microflora plays a role in anti-pruritic activity of baicalin, a main constituent of the rhizome of Scutellaria baicalensis (SB). METHODS: Baicalin was anaerobically incubated with human fecal microflora, and its metabolites, baicalein and oroxylin A, were isolated. The inhibitory effect of baicalin and its metabolites was accessed in histamine- or compound 48/80-induced scratching behavior in mice. RESULTS: Baicalin was metabolized to baicalein and oroxylin A, with metabolic activities of 40.2+/-26.2 and 1.2+/-1.1 nmol.h(-1).mg(-1) wet weight of human fecal microflora, respectively. Baicalin (20, 50 mg/kg) showed more potent inhibitory effect on histamine-induced scratching behavior when orally administered than intraperitoneally. In contrast, baicalein and oroxylin A had more potent inhibitory effect when the intraperitoneally administered. The anti-scratching behavior activity of oral baicalin and its metabolites was in proportion to their inhibition on histamine-induced increase of vascular permeability with oroxylin A more potent than baicalein and baicalin. In Magnus test using guinea pig ileum, oroxylin A is more potent than baicalein and baicalin in inhibition of histamine-induced contraction. The anti-scratching behavioral effect of oral baicalin was significantly reduced when oral antibiotics were simultaneously administered, whereas the effect of baicalein and oroxylin A were not affected. CONCLUSION: Oral baicalin may be metabolized by intestinal microflora into baicalein and oroxylin A, which ameliorate pruritic reactions through anti-histamine action.
Asunto(s)
Antipruriginosos/uso terapéutico , Flavanonas/uso terapéutico , Flavonoides/uso terapéutico , Antagonistas de los Receptores Histamínicos/uso terapéutico , Prurito/tratamiento farmacológico , Animales , Antibacterianos/administración & dosificación , Antipruriginosos/análisis , Antipruriginosos/metabolismo , Heces/microbiología , Flavanonas/análisis , Flavonoides/análisis , Flavonoides/metabolismo , Cobayas , Histamina/administración & dosificación , Antagonistas de los Receptores Histamínicos/análisis , Antagonistas de los Receptores Histamínicos/metabolismo , Intestinos/microbiología , Masculino , Ratones , Ratones Endogámicos BALB C , Ratones Endogámicos ICR , Fitoterapia , Scutellaria baicalensis/química , Scutellaria baicalensis/metabolismo , Estreptomicina/administración & dosificación , Tetraciclina/administración & dosificaciónRESUMEN
The anti-pruritic effect of red ginseng (the steamed root of Panax ginseng C.A. Meyer, Araliaceae), a traditional medicine in Asian countries, was investigated in mouse scratching behavior models induced by either compound 48/80 or histamine. Red ginseng and its saponin fraction, but not its polysaccharide fraction, showed an anti-pruritic effect. Representative constituents in the saponin fraction, ginsenosides Rg3 and Rh2, inhibited scratching behavior and vascular permeability. These ginsenosides also inhibited the expression of TNF-alpha and IL-4 induced by IgE-antigen complex in RBL-2H3 cells, as well as acetic acid-induced writhing in mice. These results suggest that red ginseng and its ingredients, ginsenosides Rg3 and Rh2, may inhibit scratching behavior by inhibiting IL-4 and TNF-alpha expression, promoting membrane stability, and inhibiting Ca (++) influx.
Asunto(s)
Antipruriginosos/análisis , Ginsenósidos/uso terapéutico , Panax/química , Fitoterapia , Prurito/tratamiento farmacológico , Ácido Acético , Animales , Antipruriginosos/uso terapéutico , Ginsenósidos/aislamiento & purificación , Histamina , Inmunoglobulina E , Interleucina-4/metabolismo , Ratones , Extractos Vegetales/uso terapéutico , Raíces de Plantas/química , Prurito/inducido químicamente , Ratas , Factor de Necrosis Tumoral alfa/metabolismo , p-Metoxi-N-metilfenetilaminaRESUMEN
A case of fatal poisoning with cyamemazine is presented. The cyamemazine was identified in post-mortem blood using a specific gas chromatographic/mass spectrometry method. The autopsy blood concentration of cyamemazine was 1800 ng/ml. Chronic use of cyamemazine was demonstrated by the presence of the drug in hair. Two other drugs were also detected (bromazepam and trimeprazine). We think that this current blood concentration (1800 ng/ml) is a fatal blood concentration because of the negativity of the other parameters, but careful interpretation of analytical findings are important, the possibility that this death was a consequence of the toxicity of combined drugs could not be excluded. Not many therapeutics and toxic levels were previously reported in overdosage cases in which cyamemazine was involved. We consider that this concentration is only of guidance value for a fatal cyamemazine poisoning.
Asunto(s)
Antipsicóticos/envenenamiento , Fenotiazinas/envenenamiento , Ansiolíticos/análisis , Antipruriginosos/análisis , Antipsicóticos/análisis , Bromazepam/análisis , Femenino , Cromatografía de Gases y Espectrometría de Masas , Cabello/química , Humanos , Persona de Mediana Edad , Fenotiazinas/análisis , Trimeprazina/análisisRESUMEN
Camphor and m-cresol mixtures are used in antiseptic and anti-itching creams. No compendial method exists for these preparations. This paper reports a capillary gas chromatographic method using FID detection with 2,6-di-tert-butyl-4-methylphenol as internal standard on a 30 m x 0.32 mm Supelcowax -10 column (0.25 micron film) with helium as carrier gas. Ramped temperature programming was applied. The method allows simultaneous quantitation of camphor and m-cresol in the presence of o- and p-cresols, calamine and zinc oxide. Overall percent recoveries (+/- SD, n = 9) of camphor, o-, p- and m-cresol from spiked placebo creams, at a labeled amount of 10 (w/w)% were 96.9 +/- 0.6, 98.2 +/- 0.6, 99.2 +/- 0.5 and 101.0 +/- 0.9%, respectively, and at a labeled amount of 1% were 96.7 +/- 0.6, 97.8 +/- 0.9, 97.8 +/- 0.6, and 100.3 +/- 1.0%, respectively. The recovery studies were carried out at +/- 30% of the labeled amounts. Linear peak area or height ratios were obtained (r > 0.999) for camphor, o-, p- and m-cresol covering a concentration range of 10-200% of the labeled amount. Linearity (r > 0.999) was also obtained for m-cresol when the relative concentration of o- and p-cresol was varied from 5 to 100% of the m-cresol concentration. The resolution between the 'critical pair' of p- and m-cresol was > or = 1.1. The limit of quantitation was 23 pg for m-cresol and 9.3 pg for camphor using an injection split of 1:50. The repeatability (%RSD) for all compounds were < 2% for peak area and < 1.4% for peak height ratios. System suitability and robustness of the method were established. The method was successively applied to the assay of available commercial products and allows assay of camphor and the three cresol isomers.
Asunto(s)
Antipruriginosos/análisis , Alcanfor/análisis , Cromatografía de Gases/métodos , Cresoles/análisis , Fármacos Dermatológicos/química , Etiquetado de Medicamentos , Pomadas/química , Reproducibilidad de los ResultadosRESUMEN
Crotamiton, which is a mixture of cis and trans isomers, was investigated by several separation techniques. One of the HPLC modes, in which crotamiton eluted as a single peak, was selected for the determination of five active ingredients (crotamiton, prednisolone, glycyrrhetinic acid, dibucaine and chlorhexidine hydrochloride) in an ointment. The simultaneous determination was performed using isocratic reversed-phase mode within 20 min by employing an octyl (C8) column and a mobile phase containing sodium dodecyl sulfate (SDS) and 2-propanol. The method was successfully applied to quality control and stability testing of the ointment.
Asunto(s)
Antipruriginosos/análisis , Cromatografía Líquida de Alta Presión , Insecticidas/análisis , Toluidinas/análisis , Clorhexidina/análisis , Dibucaína/análisis , Estabilidad de Medicamentos , Ácido Glicirretínico/análisis , Estructura Molecular , Pomadas , Prednisolona/análisis , Control de Calidad , Reproducibilidad de los Resultados , EstereoisomerismoRESUMEN
High-pressure liquid chromatography was used with a 5-micrometer silica gel column to quantitate the phenol in phenolated calamine lotion USP and a commercial antiseptic solution. This method requires less than 10 min/assay, and other compounds present in the products analyzed did not interfere.