Pharmacokinetics of acteoside following single dose intragastric and intravenous administrations in dogs / 中国天然药物

Acteoside (verbascoside), a phenylethanoid glycoside widely distributed in various plants, has been shown to have potential activity against Alzheimer's disease, attracting great attentions recently. The present study was designed to develop a selective and sensitive LC-MS/MS method for the determination of acteoside in biological samples and carry our a pharmacokinetic (PK) study in beagle dogs. The PK parameters were calculated using non-compartmental models. Following a single-dose oral administration, acteoside was rapidly absorbed and eliminated, with Tmax being between 30 to 45 min and terminal half-life being about 90 min. The areas under the time-concentration curve (AUC) were 47.28 ± 8.74, 87.86 ± 13.33, and 183.14 ± 28.69 mg · min · L(-1) for oral administration of 10, 20, and 40 mg · kg(-1), respectively, demonstrating that the exposure of acteoside proportionally increased with the dose level. The absolute bioavailability of acteoside was around 4%. For all the PK parameters, there were large variations between individual dogs. In conclusion, the pharmacokinetic characteristics observed in the present study can be of great value to help better understand the pharmacological properties of acteoside and to improve the outcome of its clinical use.

Effect of acteoside on learning and memory impairment induced by scopolamine in mice / 中国中药杂志

<p><b>OBJECTIVE</b>To study on the effect of acteoside on learning and memory of dementia mice.</p><p><b>METHOD</b>Mice were orally administered with acteoside for 10 days. Scopolamine was used to establish the acquired learning disability in mice. Their learning and memory were detected with a behavioral experiment (step-down test). After the behavior test, corticocerebral and hippocampus tissues of mice were detected with biochemical indexes, including GSH-Px, T-SOD, MDA, TChE and contents of protein in brain tissues.</p><p><b>RESULT</b>Mice were administered with acteoside for 10 d in advance to alleviate the acquired learning disability induced by scopolamine. Compared with the model group, acteoside increased the latency period in the step-down test and reduced error times. Besides, acteoside increased the activity of GSH-Px, T-SOD, TChE and protein content in their brain tissues, but decreased MDA content.</p><p><b>CONCLUSION</b>Acteoside can significantly alleviate the acquired learning disability in mice induced by scopolamine. Its mechanism may be related with its effect of inhibiting the generation of free radicals in mice and improving the function of the central cholinergic system.</p>