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UPLC-TOF-MS 分析拉拉藤对其神经保护和抗惊厥活性的影响。

UPLC-TOF-MS analysis of Galium spurium towards its neuroprotective and anticonvulsant activities.

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, 06330 Hipodrom, Ankara, Turkey.

出版信息

J Ethnopharmacol. 2012 May 7;141(1):220-7. doi: 10.1016/j.jep.2012.01.056. Epub 2012 Feb 18.

DOI:10.1016/j.jep.2012.01.056
PMID:22348922
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Galium species have been reported to be used against epilepsy in traditional Turkish folk medicine.

AIM OF STUDY

The present work was undertaken to evaluate the in vivo anticonvulsant and in vitro neuroprotective effects of Galium spurium L. and to determine the major constituents by UPLC-TOF-MS.

MATERIALS AND METHODS

Anticonvulsant activity of the aerial parts of Galium spurium was investigated using pentylenetetrazole, picrotoxin, and maximal electroshock-induced seizure animal models. In order to evaluate the safety, neurotoxicity (Rota rod test) of the ethanol extract was also determined. In vitro neuroprotective effect of the ethanol extract of Galium spurium was assessed by acetylcholinesterase and butrylcholinesterase inhibitions. Ultra Performance Liquid Chromatography-Time of Flight Mass Spectrometer (UPLC-TOF-MS) was used to identify the major compounds in the extract.

RESULTS

In pentylenetetrazole-induced seizure, the ethanol extract at doses of 250 and 1000mg/kg prolonged the onset of seizures. Similarly, Galium spurium (250 and 500mg/kg) significantly delayed the onset of picrotoxin-induced seizures in mice and these doses also exhibited 12.5% and 17% protection, respectively, against picrotoxin-induced seizures. Furthermore, Galium spurium extract showed a significant protective effect against maximal electroshock-induced seizures at doses of 250 and 1000mg/kg (50% and 37.5%, respectively) and also all tested doses prolonged the onset of seizures. No motor co-ordination was observed with intraperitoneal injection of Galium spurium extract at doses of 500 and 1000mg/kg. The extract exhibited 16.2% inhibition against butrylcholinesterase at 200μg/mL concentration, whereas it did not inhibit acetylcholinesterase. Phytochemical analysis of the extract based on the MS data by UPLC-TOF-MS, ten major compounds (phenolic and triterpenic acids, flavonoids and iridoids) were determined.

CONCLUSIONS

The results indicate that Galium spurium may have anticonvulsant activity against picrotoxin and maximal electroshock-induced seizures in mice. Phenolic acids, flavonoids and iridoids might be responsible for anticonvulsant activity. The results offer possible beneficial effects by the plant's aerial parts and may suggest a realistic explanation for its traditonal usage in epilepsy.

摘要

民族药理学相关性

Galium 物种已被报道在传统的土耳其民间医学中用于治疗癫痫。

目的

本研究旨在评估 Galium spurium L. 的体内抗惊厥和体外神经保护作用,并通过 UPLC-TOF-MS 确定主要成分。

材料和方法

使用戊四氮、苦毒素和最大电休克诱导的惊厥动物模型研究 Galium spurium 地上部分的抗惊厥活性。为了评估乙醇提取物的安全性和神经毒性(旋转棒试验),也对其进行了测定。通过乙酰胆碱酯酶和丁酰胆碱酯酶抑制作用评估 Galium spurium 乙醇提取物的体外神经保护作用。采用超高效液相色谱-飞行时间质谱联用仪(UPLC-TOF-MS)鉴定提取物中的主要化合物。

结果

在戊四氮诱导的惊厥中,乙醇提取物在 250 和 1000mg/kg 剂量下可延长惊厥发作的潜伏期。同样,Galium spurium(250 和 500mg/kg)显著延迟了小鼠苦毒素诱导的惊厥发作的发作,这些剂量对苦毒素诱导的惊厥发作的保护率分别为 12.5%和 17%。此外,Galium spurium 提取物在 250 和 1000mg/kg 剂量下对最大电休克诱导的惊厥发作具有显著的保护作用(分别为 50%和 37.5%),并且所有测试剂量均延长了惊厥发作的潜伏期。腹腔注射 Galium spurium 提取物 500 和 1000mg/kg 时未观察到运动协调。提取物在 200μg/mL 浓度下对丁酰胆碱酯酶的抑制率为 16.2%,而对乙酰胆碱酯酶没有抑制作用。基于 UPLC-TOF-MS 的 MS 数据的提取物的植物化学分析,确定了十种主要化合物(酚酸、三萜酸、类黄酮和环烯醚萜)。

结论

结果表明,Galium spurium 可能对苦毒素和最大电休克诱导的小鼠惊厥具有抗惊厥活性。酚酸、类黄酮和环烯醚萜可能是其抗惊厥活性的原因。这些结果提供了植物地上部分可能有益的影响,并可能为其在癫痫中的传统应用提供现实的解释。

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