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来自蓝灰景天的具有抗氧化、抗胆碱酯酶和抗菌活性的化合物。

Compounds from Sedum caeruleum with antioxidant, anticholinesterase, and antibacterial activities.

作者信息

Bensouici Chawki, Kabouche Ahmed, Karioti Anastasia, Öztürk Mehmet, Duru Mehmet Emin, Bilia Anna Rita, Kabouche Zahia

机构信息

a Université Mentouri - Constantine, Département de Chimie, Laboratoire d'Obtention de Substances Thérapeutiques (LOST), Constantine 1 , Constantine , Algeria .

b Department of Pharmaceutical Sciences , University of Florence , Sesto , Fiorentino (FI) , Italy , and.

出版信息

Pharm Biol. 2016;54(1):174-9. doi: 10.3109/13880209.2015.1028078. Epub 2015 Apr 7.

Abstract

CONTEXT

This is the first study on the phytochemistry, antioxidant, anticholinesterase, and antibacterial activities of Sedum caeruleum L. (Crassulaceae).

OBJECTIVE

The objective of this study is to isolate the secondary metabolites and determine the antioxidant, anticholinesterase, and antibacterial activities of S. caeruleum.

MATERIALS AND METHODS

Six compounds (1-6) were isolated from the extracts of S. caeruleum and elucidated using UV, 1D-, 2D-NMR, and MS techniques. Antioxidant activity was investigated using DPPH(•), CUPRAC, and ferrous-ions chelating assays. Anticholinesterase activity was determined against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes using the Ellman method. Antibacterial activity was performed according to disc diffusion and minimum inhibitory concentration (MIC) methods.

RESULTS

Isolated compounds were elucidated as ursolic acid (1), daucosterol (2), β-sitosterol-3-O-β-D-galactopyranoside (3), apigenin (4), apigetrin (5), and apiin (6). The butanol extract exhibited highest antioxidant activity in all tests (IC50 value: 28.35 ± 1.22 µg/mL in DPPH assay, IC50 value: 40.83 ± 2.24 µg/L in metal chelating activity, and IC50 value: 23.52 ± 0.44 µg/L in CUPRAC), and the highest BChE inhibitory activity (IC50 value: 36.89 ± 0.15 µg/L). Moreover, the chloroform extract mildly inhibited (MIC value: 80 µg/mL) the growth of all the tested bacterial strains.

DISCUSSION AND CONCLUSION

Ursolic acid (1), daucosterol (2), β-sitosterol-3-O-β-D-galactopyranoside (3), apigenin (4), apigetrin (5), and apiin (6) were isolated from Sedum caeruleum for the first time. In addition, a correlation was observed between antioxidant and anticholinesterase activities of bioactive ingredients of this plant.

摘要

背景

这是关于蓝景天(景天科)植物化学、抗氧化、抗胆碱酯酶及抗菌活性的首次研究。

目的

本研究旨在分离次生代谢产物并测定蓝景天的抗氧化、抗胆碱酯酶及抗菌活性。

材料与方法

从蓝景天提取物中分离出六种化合物(1 - 6),并采用紫外、一维、二维核磁共振及质谱技术进行鉴定。通过二苯基苦味酰基自由基(DPPH(•))、铜离子还原抗氧化能力(CUPRAC)及亚铁离子螯合试验研究抗氧化活性。采用埃尔曼法测定对乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)的抗胆碱酯酶活性。根据纸片扩散法和最低抑菌浓度(MIC)法进行抗菌活性测试。

结果

分离得到的化合物鉴定为熊果酸(1)、胡萝卜苷(2)、β - 谷甾醇 - 3 - O - β - D - 吡喃半乳糖苷(3)、芹菜素(4)、芹菜苷元(5)和芹糖异黄酮(6)。正丁醇提取物在所有测试中表现出最高的抗氧化活性(DPPH试验中IC50值:28.35 ± 1.22 µg/mL,金属螯合活性中IC50值:40.83 ± 2.24 µg/L,CUPRAC中IC50值:23.52 ± 0.44 µg/L),以及最高的BChE抑制活性(IC50值:36.89 ± 0.15 µg/L)。此外,氯仿提取物对所有测试菌株的生长有轻度抑制作用(MIC值:80 µg/mL)。

讨论与结论

首次从蓝景天中分离出熊果酸(1)、胡萝卜苷(2)、β -谷甾醇 - 3 - O - β - D - 吡喃半乳糖苷(3)、芹菜素(4)、芹菜苷元(5)和芹糖异黄酮(6)。此外,观察到该植物生物活性成分的抗氧化和抗胆碱酯酶活性之间存在相关性。

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