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来自葡萄牙西南部特有植物的生物活性化合物:乙酰胆碱酯酶抑制和自由基清除活性。

Bioactive compounds from endemic plants of Southwest Portugal: inhibition of acetylcholinesterase and radical scavenging activities.

机构信息

Instituto de Tecnologia Química e Biológica, Universidade Nova de Lisboa, 2780-157 Oeiras, Portugal.

出版信息

Pharm Biol. 2012 Feb;50(2):239-46. doi: 10.3109/13880209.2011.596209.

DOI:10.3109/13880209.2011.596209
PMID:22074503
Abstract

CONTEXT

Natural products are reported to have substantial neuroprotective activity due to their radical scavenging capacity, and also acetylcholinesterase (AChE) inhibitory capacity, both activities important in neurodegeneration.

OBJECTIVE

The undesirable side effects of compounds in pharmacological use make it important to identify natural neuroprotective molecules. This work assesses the potential of five endemic Portuguese plants as sources of neuroprotective compounds.

MATERIALS AND METHODS

Antioxidant capacity for peroxyl radical was determined by Oxygen Radical Absorbance Capacity method and for hydroxyl by Electron Paramagnetic Resonance, as well as AChE inhibitory capacity of the plant hydroethanolic extracts. The molecules responsible for these valuable properties were also tentatively identified by HPLC.

RESULTS AND DISCUSSION

Armeria rouyana and Thymus capitellatus presented some of the highest phenolic contents (76.60 ± 7.19 and 12.82 ± 0.24 mg GAE g−1 dw, respectively) and antioxidant capacities (592 ± 116 and 449 ± 57 μmol TE g−1 dw, respectively). The flavonoids were identified as the phytomolecules related to the antioxidant capacity of these plant extracts; in the case of A. rouyana, l-ascorbic acid also made an important contribution (3.27 ± 0.26 mg g−1 dw). Plant extracts clearly demonstrated effective AChE inhibitory activity (480 ± 98 and 490 ± 46 μg mL−1, respectively), that could be associated to polyphenols.

CONCLUSIONS

The extracts of A. rouyana and T. capitellatus and their active components, especially polyphenols, demonstrate interesting neuroprotective potential. They, therefore, deserve further study as their phytomolecules are promising sources of either natural neuroprotective products and/or novel lead compounds.

摘要

背景

由于其自由基清除能力以及乙酰胆碱酯酶(AChE)抑制能力,天然产物被报道具有显著的神经保护活性,这两种活性在神经退行性变中都很重要。

目的

由于药理作用化合物的不良副作用,识别天然神经保护分子变得非常重要。这项工作评估了五种葡萄牙特有植物作为神经保护化合物来源的潜力。

材料和方法

通过氧自由基吸收能力法测定过氧自由基的抗氧化能力,通过电子顺磁共振法测定羟基自由基的抗氧化能力,以及植物水醇提取物的 AChE 抑制能力。还通过 HPLC 初步鉴定了这些有价值特性的相关分子。

结果与讨论

Armeria rouyana 和 Thymus capitellatus 表现出较高的酚含量(分别为 76.60±7.19 和 12.82±0.24 mg GAE g−1 dw)和抗氧化能力(分别为 592±116 和 449±57 μmol TE g−1 dw)。黄酮类化合物被鉴定为与这些植物提取物抗氧化能力相关的植物分子;在 A. rouyana 的情况下,l-抗坏血酸也做出了重要贡献(3.27±0.26 mg g−1 dw)。植物提取物表现出明显的 AChE 抑制活性(分别为 480±98 和 490±46 μg mL−1),这可能与多酚有关。

结论

A. rouyana 和 T. capitellatus 的提取物及其活性成分,特别是多酚,显示出有趣的神经保护潜力。因此,它们值得进一步研究,因为它们的植物分子是天然神经保护产品和/或新型先导化合物的有前途的来源。

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