兴奋性和抑制性氨基酸参与α -和β -醋酸amyrin神经药理活性的证据

G. Aragão, L. M. Carneiro, Antônio P.F. Juniora, P. Bandeira, T. L. Lemos, G. Viana
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引用次数: 18

摘要

我们评估了乙酰化α -和β -amyrin (AcAMY)的神经药理学特征,AcAMY是由分离自Protium hephyllum的α -和β -amyrin的异构体混合物乙酰化得到的。给雄性瑞士小鼠注射AcAMY(2.5、5、10和25 mg/kg, ig),并研究抗惊厥药(戊四唑和匹罗卡品诱导的惊厥)、镇静药(巴比妥酸盐诱导的睡眠和开放场试验)和抗焦虑药(升高加迷宫试验)的活性。结果表明,AcAMY腹腔或口服给药对戊四唑有保护作用,但对匹罗卡品诱发的惊厥无保护作用。该药增加了第一次惊厥潜伏期和死亡潜伏期。巴比妥酸盐诱导的睡眠时间也增加,乙醚诱导的睡眠时间也增加,证实了AcAMY的镇静作用。急性给药AcAMY也产生抗溶血作用。亚慢性给药后,两种较高剂量均表现出镇静和抗焦虑作用。用AcAMY (25 mg/kg, i.p, 7天)治疗的小鼠脑区氨基酸测量显示,海马区酪氨酸水平增加89%。纹状体中酪氨酸和牛磺酸分别升高了97%和79%,而天冬氨酸、GABA和谷氨酸分别降低了72%、55%和60%。总之,我们的结果表明,AcAMY具有镇静、抗焦虑和抗惊厥的特性。虽然药物的作用机制尚不完全清楚,但似乎与兴奋性氨基酸的减少和抑制性氨基酸的增加有关。此外,gaba能系统也可能发挥作用。
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Evidence for Excitatory and Inhibitory Amino Acids Participation in theNeuropharmacological Activity of Alpha- and Beta-Amyrin Acetate
We evaluated the neuropharmacological profile of acetylated alpha- and beta-amyrin (AcAMY) obtained by the acetylation of the isomeric mixture of alpha- and beta-amyrin isolated from Protium heptaphyllum. Male Swiss mice were administered with AcAMY (2.5, 5, 10 and 25 mg/kg, i.p.), and anticonvulsant (pentylenetrazole- and pilocarpine-induced convulsions), sedative (barbiturate-induced sleep and open field tests) and anxiolytic (elevated plus maze test) activities were studied. Results showed that AcAMY administered intraperitoneally or orally, protected the animals against penty- lenetetrazole- but not against pilocarpine-induced convulsions. The drug increased both the latency to the 1 st convulsion and the latency to death. The barbiturate-induced sleeping time was also increased, as well as the ethyl ether-induced sleeping time, confirming the sedative nature of AcAMY. The acute administration of AcAMY also produced an anx- iolytic effect. After the sub-chronic administration, both sedative and anxiolytic effects were manifested, at the two higher doses. Amino acids measurements in brain areas of mice treated with AcAMY (25 mg/kg, i.p., for 7 days) showed an 89% increase in tyrosine levels, in the hippocampus. In the striatum, tyrosine and taurine were increased by 97 and 79%, re- spectively, while decreases in the levels of aspartate, GABA and glutamate of 72, 55 and 60%, respectively were ob- served. In conclusion, our results showed that AcAMY presents sedative, anxiolytic and anticonvulsant properties. Al- though the drug mechanism of action is not completely clarified, it seems to involve a decrease in excitatory amino acids and an increase of inhibitory amino acids. Furthermore, the GABAergic system may also play a role.
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