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苦马豆根中二氯甲烷提取物及其成分对α-淀粉酶和α-葡萄糖苷酶的抑制活性。

The α-amylase and α-glucosidase inhibitory activities of the dichloromethane extracts and constituents of Ferulago bracteata roots.

机构信息

a Department of Pharmacognosy, Faculty of Pharmacy , Atatürk University , Erzurum , Turkey.

b Department of Pharmacognosy, Faculty of Pharmacy , Erzincan University , Erzincan , Turkey.

出版信息

Pharm Biol. 2018 Dec;56(1):18-24. doi: 10.1080/13880209.2017.1414857.

Abstract

CONTEXT

Ferulago (Apiaceae) species have been used since ancient times for the treatment of intestinal worms, hemorrhoids, and as a tonic, digestive, aphrodisiac, or sedative, as well as in salads or as a spice due to their special odors.

OBJECTIVES

This study reports the α-amylase and α-glucosidase inhibitory activities of dichloromethane extract and bioactive compounds isolated from Ferulago bracteata Boiss. & Hausskn. roots.

MATERIALS AND METHODS

The isolated compounds obtained from dichloromethane extract of Ferulago bracteata roots through bioassay-guided fractionation and isolation process were evaluated for their in vitro α-amylase and α-glucosidase inhibitory activities at 5000-400 µg/mL concentrations. Compound structures were elucidated by detailed analyses (NMR and MS).

RESULTS

A new coumarin, peucedanol-2'-benzoate (1), along with nine known ones, osthole (2), imperatorin (3), bergapten (4), prantschimgin (5), grandivitinol (6), suberosin (7), xanthotoxin (8), felamidin (9), umbelliferone (10), and a sterol mixture consisted of stigmasterol (11), β-sitosterol (12) was isolated from the roots of F. bracteata. Felamidin and suberosin showed significant α-glucosidase inhibitory activity (IC 0.42 and 0.89 mg/mL, respectively) when compared to the reference standard acarbose (IC 4.95 mg/mL). However, none of the tested extracts were found to be active on α-amylase inhibition.

DISCUSSION AND CONCLUSIONS

The present study demonstrated that among the compounds isolated from CHCl fraction of F. bracteata roots, coumarins were determined as the main chemical constituents of this fraction. This is the first report on isolation and characterization of the bioactive compounds from root extracts of F. bracteata and on their α-amylase and α-glucosidase inhibitory activities.

摘要

背景

Ferulago(伞形科)物种自古以来就被用于治疗肠道蠕虫、痔疮,并作为补品、消化剂、壮阳药或镇静剂,由于其特殊的气味,也可用于沙拉或作为香料。

目的

本研究报告了二氯甲烷提取物及从 Ferulago bracteata Boiss. & Hausskn. 根中分离得到的生物活性化合物对α-淀粉酶和α-葡萄糖苷酶的抑制活性。

材料和方法

通过生物测定指导的分步分离和分离过程,从 Ferulago bracteata 根的二氯甲烷提取物中获得的分离化合物,在 5000-400µg/mL 浓度下,对其体外α-淀粉酶和α-葡萄糖苷酶抑制活性进行了评价。通过详细分析(NMR 和 MS)阐明了化合物的结构。

结果

从 F. bracteata 的根部分离得到一个新的香豆素,peucedanol-2'-benzoate(1),以及 9 个已知的化合物,欧前胡素(2)、异茴芹素(3)、佛手柑内酯(4)、 Prantschimgin(5)、大根香叶醇(6)、suberosin(7)、花椒毒素(8)、felamidin(9)、umbelliferone(10)和由豆甾醇(11)、β-谷甾醇(12)组成的甾醇混合物。与对照标准阿卡波糖(IC 4.95mg/mL)相比,felamidin 和 suberosin 对α-葡萄糖苷酶抑制活性具有显著的抑制作用(IC 0.42 和 0.89mg/mL)。然而,测试的提取物均未表现出对α-淀粉酶抑制的活性。

讨论和结论

本研究表明,在所分离的 F. bracteata 根中二氯甲烷部分的化合物中,香豆素被确定为该部分的主要化学成分。这是首次从 Ferulago bracteata 根提取物中分离和鉴定生物活性化合物,并对其α-淀粉酶和α-葡萄糖苷酶抑制活性进行研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c85d/6130714/cfb49d2c2137/IPHB_A_1414857_F0001_B.jpg

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