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对从糙苏中分离得到的甲醇提取物、后续馏分、粗皂苷和黄酮类化合物的抗胆碱酯酶和抗氧化潜力的研究。

Investigations of anticholinestrase and antioxidant potentials of methanolic extract, subsequent fractions, crude saponins and flavonoids isolated from Isodon rugosus.

作者信息

Zeb Anwar, Sadiq Abdul, Ullah Farhat, Ahmad Sajjad, Ayaz Muhammad

机构信息

Department of Pharmacy, University of Malakand, Chakdara, Dir, Pakistan.

出版信息

Biol Res. 2014 Dec 26;47(1):76. doi: 10.1186/0717-6287-47-76.

Abstract

BACKGROUND

Based on the ethnomedicinal uses and the effective outcomes of natural products in various diseases, this study was designed to evaluate Isodon rugosus as possible remedy in oxidative stress, alzheimer's and other neurodegenerative diseases. Acetylecholinestrase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of crude methanolic extract (Ir.Cr), resultant fractions (n-hexane (Ir.Hex), chloroform (Ir.Cf), ethyl acetate (Ir.EtAc), aqueous (Ir.Aq)), flavonoids (Ir.Flv) and crude saponins (Ir.Sp) of I. rugosus were investigated using Ellman's spectrophotometric method. Antioxidant potential of I. rugosus was determined using DPPH, H2O2 and ABTS free radicals scavenging assays. Total phenolic and flavonoids contents of plant extracts were determined and expressed in mg GAE/g dry weight and mg RTE/g of dry sample respectively.

RESULTS

Among different fractions Ir.Flv and Ir.Cf exhibited highest inhibitory activity against AChE (87.44 ± 0.51, 83.73 ± 0.64%) and BChE (82.53 ± 0.71, 88.55 ± 0.77%) enzymes at 1 mg/ml with IC50 values of 45, 50 for AChE and 40, 70 μg/ml for BChE respectively. Activity of these fractions were comparable to galanthamine causing 96.00 ± 0.30 and 88.61 ± 0.43% inhibition of AChE and BChE at 1 mg/ml concentration with IC50 values of 20 and 47 μg/ml respectively. In antioxidant assays, Ir.Flv, Ir.Cf, and Ir.EtAc demonstrated highest radicals scavenging activities in DPPH and H2O2 assays which were comparable to ascorbic acid. Ir.Flv was found most potent with IC50 of 19 and 24 μg/ml against DPPH and H2O2 radicals respectively. Whereas antioxidant activates of plant samples against ABTS free radicals was moderate. Ir.Cf, Ir.EtAc and Ir.Cr showed high phenolic and flavonoid contents and concentrations of these compounds in different fractions correlated well to their antioxidant and anticholinestrase activities.

CONCLUSION

It may be inferred from the current investigations that the Ir.Sp, Ir.Flv and various fractions of I. rugosus are good sources of anticholinesterase and antioxidant compounds. Different fractions can be subjected to activity guided isolation of bioactive compounds effective in neurological disorders.

摘要

背景

基于天然产物在各种疾病中的民族药用用途和有效成果,本研究旨在评估皱叶香茶菜作为氧化应激、阿尔茨海默病和其他神经退行性疾病的可能治疗方法。采用Ellman分光光度法研究了皱叶香茶菜的粗甲醇提取物(Ir.Cr)、所得馏分(正己烷(Ir.Hex)、氯仿(Ir.Cf)、乙酸乙酯(Ir.EtAc)、水相(Ir.Aq))、黄酮类化合物(Ir.Flv)和粗皂苷(Ir.Sp)对乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)的抑制活性。通过DPPH、H2O2和ABTS自由基清除试验测定了皱叶香茶菜的抗氧化潜力。测定了植物提取物中的总酚和黄酮含量,分别以mg GAE/g干重和mg RTE/g干样品表示。

结果

在不同馏分中,Ir.Flv和Ir.Cf在1 mg/ml时对AChE(87.44±0.51,83.73±0.64%)和BChE(82.53±0.71,88.55±0.77%)酶表现出最高的抑制活性,AChE的IC50值分别为45、50,BChE的IC50值分别为40、70 μg/ml。这些馏分的活性与加兰他敏相当,加兰他敏在1 mg/ml浓度下对AChE和BChE的抑制率分别为96.0±0.30和88.61±0.43%,IC50值分别为20和47 μg/ml。在抗氧化试验中,Ir.Flv、Ir.Cf和Ir.EtAc在DPPH和H2O2试验中表现出最高的自由基清除活性,与抗坏血酸相当。发现Ir.Flv最有效,对DPPH和H2O2自由基的IC50分别为19和24 μg/ml。而植物样品对ABTS自由基的抗氧化活性中等。Ir.Cf、Ir.EtAc和Ir.Cr显示出较高的酚类和黄酮类含量,不同馏分中这些化合物的浓度与其抗氧化和抗胆碱酯酶活性密切相关。

结论

从目前的研究中可以推断,皱叶香茶菜的Ir.Sp、Ir.Flv和各种馏分是抗胆碱酯酶和抗氧化化合物的良好来源。不同的馏分可以通过活性导向分离出对神经疾病有效的生物活性化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d47/4297394/72660bc7414e/40659_2014_63_Fig1_HTML.jpg

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