LC-MS/MS analysis of determination of strychnine and brucine in formaldehyde fixed tissue / 法医学杂志

OBJECTIVE@#To establish a method for determination of strychnine and brucine in formaldehyde fixed tissue by LC-MS/MS analysis.@*METHODS@#The samples were pretreated with solid phase extraction using SCX cartridges and separated on SB-C18 column with mobile phase 0.1% formic acid : 0.1% formic acid-acetonitrile (75:25). Electrospray ionization (ESI) source was utilized and operated in positive ion mode. Multiple reactions monitoring (MRM) mode was applied. External standard method was applied for quantitation.@*RESULTS@#The chromatographic separation of strychnine and brucine in formaldehyde fixed nephritic and hepatic tissues resulted successfully. The standard curve was linear in the range of 0.002-2.0 microg/g for strychnine and brucine in formaldehyde fixed tissues, and the correlation coefficient was more than 0.996. The limits of detection (LOD) of strychnine and brucine in nephritic tissues were 0.06ng/g and 0.03 ng/g, respectively. The LOD of both chemicals were 0.3 ng/g in hepatic tissues. The extraction recovery rate was more than 74.5%. The precision of intra-day and inter-day were both less than 8.2%.@*CONCLUSION@#Strychnine and brucine can be sensitive to be determined in formaldehyde fixed tissue by LC-MS/MS analysis. It can be applied in the forensic toxicological analysis.

Anticonvulsant activity of bacopa monniera in rodents / Anticonvulsivante atividade de bacopa monniera em roedores

Bacopa monnieri (L), belonging to the Scrophulariaceae family and commonly known as Brahmi, is well known in India for its CNS activity but its neuropharmacological effect has not yet been explored. In the present study, the antiepileptic effects of the plant were investigated. The ethanolic extract of Bacopa monniera was tested for anticonvulsant activity in albino rats, using different convulsive models. The ethanolic extract of leaves produced significant anticonvulsant activity for all the different models studied. The present study shows a probable mechanism of action similar to that of benzodiazepines (GABA agonist). Thus, these results emphasize the need to diversify by using alternative therapeutic approaches pertaining to herbal medicine, where a single easily available plant may provide solutions to several therapeutic challenges, as observed in the anticonvulsant action of ethanolic extract of B. monniera.

Bacopa monniera, da família Scrophulariaceae, e comumente denominada Brahmi, é bem conhecida na Índia por sua atividade no Sistema Nervoso Central, mas seu efeito neurofarmacológico não foi, ainda, explorado. No presente estudo, investigaram-se os efeitos antiepilépticos da planta. O extrato etanólico da Bacopa monniera foi testado quanto à atividade anticonvulsivante em ratos albinos, utilizando-se diferentes modelos de convulsão. O extrato etanólico das folhas produziu atividade anticonvulsivante significativa para todos os diferentes modelos estudados. O presente estudo mostra provável mecanismo de ação semelhante ao dos benzodiazepínicos (agonista do GABA). Assim sendo, esses resultados enfatizam a necessidade de diversificar, utilizando-se abordagens terapêuticas alternativas da medicina natural, em que uma planta facilmente disponível pode fornecer soluções para vários desafios terapêuticos, como o observado na ação anticonvulsivante do extrato etanólico de Bacopa monniera.

Espectro de acción antiepiléptica de la DL-4-hidroxi, 4-etil,4-fenil butiramida y sus homólogos inferiores / Profile of the antiepileptic action of DL-4-hydroxy, 4-ethyl, 4-phenyl butiramide and its inferior homologues

Se estudio la actividad farmacológica en animales de una serie nueva de compuestos anticonvulsionantes, la DL-4-hidroxil, 4-etil, 4-fenil butiramida (HEPB) y sus homólogos inferiores propionamida (HEPP) y acetamida (HEPA). La neurotoxidad fue determinada con un rotarod y se indujeron cuadros convulsivos con electrochoque supramáximo (MES), pentilentetrazol (TSC), estricnina (STR) y picrotoxina (PIC). HEPP es menos neurotóxica que HEPB y HEPA y altera el comportamiento de los ratones solamente a dosis altas. Los tres compuestos presentaron un amplio espectro de acción anticonvulsionante. Ellos son muy potentes para inhibir cuadros convulsivos inducidos con 4-AP, BIC, TSC y PTZ en dosis no tóxicas administradas ip, pero son inefectivas contra convulsiones inducidas con pic y STR. Los índices terapéuticos (IT = DT 50/D 50) fueron más elevados para HEPP. En consecuencia los resultados indican que los tres compuestos probados pueden servir para el tratamiento de convulsiones generalizadas tipo ausencias. Puesto que HEPP es el compuesto menos neurotóxico se ha seleccionado para los estudios toxicológicos y neuroquímicos