Silva Fo, Silva Mgv, Cerqueira Gs, Sabino Eb, Almeida Aac, Costa Jp, Freitas Rm
Department of Organic and Inorganic Chemistry of Federal University of Piauí, CEP 64.049-550, Teresina, Piauí, Brazil.
J Young Pharm. 2011 Jul;3(3):232-6. doi: 10.4103/0975-1483.83772.
The central nervous system (CNS) depressant and anticonvulsant activities of iso-6-spectaline (SPEC) were investigated in animal models. The SPEC from Senna spectabilis var. excelsa (Schrad) (0.1, 0.5 and 1.0 mg/ kg) injected by oral route (p.o.) in mice caused a significant decrease in the motor activity up to 30 days after the administration and in the dose of 1.0 mg/kg significantly reduced the remaining time on the Rota-rod apparatus. Additionally, SPEC (0.1, 0.5 and 1.0 mg/kg, p.o.) was also capable of promoting increase of latency for development of convulsions induced by pentylenetetrazole. This SPEC was also capable of promoting an increase of latency for development of convulsions induced by picrotoxin at highest dose. In the same way, the anticonvulsant effect of SPEC was affected by pretreatment with flumazenil, a selective antagonist of the benzodiazepine site of the GABA(A) receptor. These results suggest possible CNS depressant and anticonvulsant activities in mice that needs further investigation.
在动物模型中研究了异-6-番泻灵(SPEC)的中枢神经系统抑制和抗惊厥活性。将来自番泻叶变种(Schrad)的SPEC(0.1、0.5和1.0毫克/千克)经口(p.o.)注射到小鼠体内,给药后30天内可显著降低运动活性,1.0毫克/千克剂量可显著缩短小鼠在转棒试验中的停留时间。此外,SPEC(0.1、0.5和1.0毫克/千克,p.o.)还能够延长戊四氮诱导惊厥发作的潜伏期。在最高剂量下,这种SPEC也能够延长印防己毒素诱导惊厥发作的潜伏期。同样,氟马西尼(一种GABA(A)受体苯二氮䓬位点的选择性拮抗剂)预处理会影响SPEC的抗惊厥作用。这些结果表明SPEC在小鼠中可能具有中枢神经系统抑制和抗惊厥活性,需要进一步研究。