脂溶性提取物比传统制剂和提取物更能提高益智活性。

Department of Quality Assurance Technique, Bharati Vidyapeeth University - Poona College of Pharmacy, Maharashtra, India.

J Pharm Pharmacol. 2009 Nov;61(11):1537-44. doi: 10.1211/jpp/61.11.0014.

OBJECTIVES

The aim was to design an alternative solvent-free extraction method using the hydrophilic lipid Gelucire (polyethylene glycol glycerides) for herbal extraction and to confirm the efficacy of extraction using biological screening.

METHODS

Bacopa monniera Linn. (BM) was selected for the study. Conventional methanolic extract (MEBM), Ayurvedic ghrita (AGBM) and lipid extracts (LEBM) were prepared and standardised by high-performance thin-layer chromatography (HPTLC). Nootropic activity in rats was evaluated using the two-trial Y-maze test and the anterograde amnesia induced by scopolamine (1 mg/kg i.p.) determined by the conditioned avoidance response. The extracts were administered daily at doses of 100, 200 and 400 mg/kg orally. At the end of the conditioned avoidance response test, brain monoamine levels were estimated by HPLC.

KEY FINDINGS

The LEBM, MEBM and AGBM contained 3.56%, 4.10% and 0.005% bacoside A, respectively. Significantly greater spatial recognition was observed with LEBM (P < 0.001 at 400 and 200 mg/kg) and MEBM (P < 0.001 at 400 mg/kg, P < 0.01 at 200 mg/kg) than AGBM. The conditioned avoidance response was significantly higher in the groups treated with high doses of LEBM and MEBM than AGBM. There were significant decreases in brain noradrenaline (P < 0.001) and 5-hydroxytryptamine (P < 0.01) levels and an increase in dopamine levels (P < 0.05) in the LEBM-treated groups compared with the stress control group.

CONCLUSIONS

The proposed LEBM is solvent free, does not have the shortcomings associated with conventional extraction, and had comparable nootropic activity to the MEBM.

目的

设计一种使用亲水脂质 Gelucire（聚乙二醇甘油酯）的无溶剂提取方法，用于草药提取，并通过生物筛选确认提取的效果。

方法

选择益智（Bacopa monniera Linn.）进行研究。制备并通过高效薄层色谱（HPTLC）标准化常规甲醇提取物（MEBM）、印度阿育吠陀油（AGBM）和脂溶性提取物（LEBM）。使用双试验 Y 型迷宫测试评估益智的益智活性，并通过条件回避反应确定由东莨菪碱（1mg/kg ip）诱导的顺行性遗忘。提取物以 100、200 和 400mg/kg 口服剂量每天给药。在条件回避反应测试结束时，通过 HPLC 估计脑单胺水平。

主要发现

LEBM、MEBM 和 AGBM 分别含有 3.56%、4.10%和 0.005%的益智皂苷 A。LEBM（400 和 200mg/kg 时 P < 0.001）和 MEBM（400mg/kg 时 P < 0.001，200mg/kg 时 P < 0.01）与 AGBM 相比，空间识别显著增加。LEBM 和 MEBM 高剂量治疗组的条件回避反应显著高于 AGBM 组。与应激对照组相比，LEBM 治疗组脑去甲肾上腺素（P < 0.001）和 5-羟色胺（P < 0.01）水平显著降低，多巴胺水平显著升高（P < 0.05）。