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从富含多酚的番荔枝叶提取物中鉴定抗糖尿病化合物

Identification of Antidiabetic Compounds from Polyphenolic-rich Fractions of A. Rich Leaves.

作者信息

Odeyemi Samuel Wale, Afolayan Anthony Jiede

机构信息

Department of Botany, Medicinal Plants and Economic Development Research Centre, University of Fort Hare, Eastern Cape, South Africa.

出版信息

Pharmacognosy Res. 2018 Jan-Mar;10(1):72-80. doi: 10.4103/pr.pr_55_17.

Abstract

BACKGROUND

has been reported to possess a variety of pharmacological activities traditionally. Previous work suggested its antidiabetic properties, but information on the antidiabetic compounds is still lacking.

OBJECTIVE

The present research exertion was aimed to isolate and identify biologically active polyphenols from leaves and to evaluate their efficacy on carbohydrate digesting enzymes.

MATERIALS AND METHODS

Fractionation of the polyphenolic contents from the methanolic extract of leaves was executed by the silica gel column chromatography to yield different fractions. The antioxidant activities of these fractions were carried out against 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) diammonium salt (ABTS), 2,2-diphenyl-1-picrylhydrazyl radicals, and ferric ion-reducing antioxidant power (FRAP). antidiabetic experimentation was performed by evaluating the α-amylase and α-glucosidase inhibitory capacity. The isolated polyphenols were then identified using liquid chromatography and mass spectroscopy (LC/MS).

RESULTS

Out of the eight polyphenolic fractions (BAL 1-8), BAL-4 has the highest inhibitory activity against ABTS radicals whereas BAL-6 showed potent ferric ion-reducing capacity. BAL-5 was the most effective fraction with antidiabetic activity with ICof 140.0 and 68.58 ± 3.2 μg/ml for α-amylase and α-glucosidase inhibitory activities, respectively. All the fractions competitively inhibited α-amylase, BAL-5 and BAL-6 also inhibited α-glucosidase competitively, while BAL-4 and BAL-1 exhibited noncompetitive and near competitive inhibitions against α-glucosidase, respectively. The LC/MS analysis revealed the presence of carvone in all the fractions.

CONCLUSIONS

The present study demonstrates the antioxidant and antidiabetic activities of the isolated polyphenols from .

SUMMARY

Polyphenols were successfully isolated and identified from leavesThe isolated polyphenols are biologically active with high antioxidant as well as inhibitor of carbohydrate-digesting enzymes can be a good source of amylase and glucosidase inhibitors can be used as complementary or alternative therapeutic agents especially for the treatment of diabetesCarvone, quercetin, and psoralen could be the compounds responsible for the α-amylase and α-glucosidase inhibitory activities. ABTS: 2,2'-Azino-bis (3-ethylbenzthiazoline-6-sulfonic acid), DPPH: 2,2-diphenyl-1-picrylhydrazyl, FRAP: Ferric ion-reducing antioxidant power, LC/MS: Liquid chromatography and mass spectroscopy, AGEs: Advanced glycation end products, TLC: Thin-layer chromatography, MeOH: Methanol, PNP-G: ρ-Nitrophenyl-α-D-Glucoside, : Coefficient of determination, mgQE: Milligram quercetin equivalent, mgTAE: Milligram tannic acid equivalent, mgCE: Milligram catechin equivalent, g: Gram.

摘要

背景

据报道,传统上其具有多种药理活性。先前的研究表明其具有抗糖尿病特性,但关于抗糖尿病化合物的信息仍然缺乏。

目的

本研究旨在从[植物名称]叶中分离并鉴定具有生物活性的多酚,并评估它们对碳水化合物消化酶的功效。

材料与方法

通过硅胶柱色谱法对[植物名称]叶甲醇提取物中的多酚成分进行分离,得到不同的馏分。采用2,2'-联氮-双(3-乙基苯并噻唑啉-6-磺酸)二铵盐(ABTS)、2,2-二苯基-1-苦基肼自由基和铁离子还原抗氧化能力(FRAP)对这些馏分的抗氧化活性进行测定。通过评估α-淀粉酶和α-葡萄糖苷酶抑制能力进行抗糖尿病实验。然后使用液相色谱和质谱(LC/MS)对分离出的多酚进行鉴定。

结果

在8个多酚馏分(BAL 1-8)中,BAL-4对ABTS自由基具有最高的抑制活性,而BAL-6显示出较强的铁离子还原能力。BAL-5是具有抗糖尿病活性的最有效馏分,对α-淀粉酶和α-葡萄糖苷酶抑制活性的IC50分别为140.0和68.58±3.2μg/ml。所有馏分均竞争性抑制α-淀粉酶,BAL-5和BAL-6也竞争性抑制α-葡萄糖苷酶,而BAL-4和BAL-1分别对α-葡萄糖苷酶表现出非竞争性和近竞争性抑制。LC/MS分析表明所有馏分中均存在香芹酮。

结论

本研究证明了从[植物名称]中分离出的多酚具有抗氧化和抗糖尿病活性。

总结

成功从[植物名称]叶中分离并鉴定出多酚。分离出的多酚具有生物活性,具有高抗氧化性,并且是碳水化合物消化酶的抑制剂,可能是淀粉酶和葡萄糖苷酶抑制剂的良好来源,可作为补充或替代治疗剂,特别是用于治疗糖尿病。香芹酮、槲皮素和补骨脂素可能是负责α-淀粉酶和α-葡萄糖苷酶抑制活性的化合物。ABTS:2,2'-联氮-双(3-乙基苯并噻唑啉-6-磺酸);DPPH:2,2-二苯基-1-苦基肼;FRAP:铁离子还原抗氧化能力;LC/MS:液相色谱和质谱;AGEs:晚期糖基化终产物;TLC:薄层色谱;MeOH:甲醇;PNP-G:ρ-硝基苯基-α-D-葡萄糖苷;IC50:半数抑制浓度;mgQE:毫克槲皮素当量;mgTAE:毫克单宁酸当量;mgCE:毫克儿茶素当量;g:克

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d111/5855377/598d50301a22/PR-10-72-g002.jpg

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