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含有三萜类化合物的（L.）Spreng茎皮乙酸乙酯提取物的α-葡萄糖苷酶抑制活性

α-Glucosidase Inhibitory Activity from Ethyl Acetate Extract of (L.) Spreng Stem Bark Containing Triterpenoids.

作者信息

Mauldina Marista Gilang, Sauriasari Rani, Elya Berna

机构信息

Department of Pharmacy, Faculty of Pharmacy, Universitas Indonesia, Depok, Indonesia.

出版信息

Pharmacogn Mag. 2017 Oct-Dec;13(52):590-594. doi: 10.4103/pm.pm_25_17. Epub 2017 Nov 13.

DOI:10.4103/pm.pm_25_17
PMID:29200718
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5701396/
Abstract

BACKGROUND

Buni ( [L.] Spreng) has been used as a traditional antidiabetic agent in Asia.

OBJECTIVE

The mechanism of antidiabetic properties was studied in this study by determine its α-glucosidase inhibitory activity.

METHOD

Inhibition of α-glucosidase was performed in all fraction of Buni stem bark with acarbose and miglitol as standards. The half maximal inhibitory concentration (IC) value of acarbose and miglitol was 5.75 and 59.76 μg/mL respectively while ethyl acetate (EtOAc) fraction was the most active fraction with IC of 19.33 μg/mL. Three isolates (B1, B2, and B3) were found in the EtOAc fraction and elucidated by infrared, hydrogen-nuclear magnetic resonance, carbon-nuclear magnetic resonance, and two-dimensional nuclear magnetic resonance.

RESULT

The chemical structures of the isolates were identified by the spectrum then compared with literature which concluded that B1 is friedelin, B2 is β-sitosterol, and B3 is betulinic acid. Inhibition of the α-glucosidase assay showed IC values of B1, B2, and B3 were 19.51, 49.85, and 18.49 μg/mL, respectively.

SUMMARY

α-Glucosidase inhibitory activity assay was performed in n-hexane, ethyl acetate (EtOAc), methanol fraction of Buni ( (L.) Spreng) stem bark and miglitolEtOAc fraction from the liquid chromatography has the highest inhibitory activity against α-glucosidaseThe chemical structures of the isolates were identified by the spectrums infrared, hydrogen-nuclear magnetic resonance, carbon-nuclear magnetic resonance, and two-dimensional nuclear magnetic resonance, then compared with literature which concluded that B1 is friedelin, B2 is β-sitosterol, and B3 is betulinic acidBetulinic acid and friedelin showed the highest α-glucosidase inhibitory activity. IC: Half maximal inhibitory concentration; H-NMR: Hydrogen-nuclear magnetic resonance; C-NMR: Carbon nuclear magnetic resonance; 2D-NMR: Two dimensional-nuclear magnetic resonance; EtOH: Ethanol; EtOAc: Ethyl acetate; MeOH: Methanol; CHCl: Chloroform; DMSO: Dimethyl sulfoxide; EtF: Ethyl acetate fraction; NaCO: Sodium carbonate; IR: Infrared; TGR5: Transmembrane G protein-coupled receptor 5; EC: Half maximal effective concentration.

摘要

背景

布尼（[L.] 施普伦格）在亚洲一直被用作传统抗糖尿病药物。

目的

本研究通过测定其α-葡萄糖苷酶抑制活性来研究其抗糖尿病特性的机制。

方法

以阿卡波糖和米格列醇为标准品，对布尼茎皮的所有馏分进行α-葡萄糖苷酶抑制实验。阿卡波糖和米格列醇的半数最大抑制浓度（IC）值分别为5.75和59.76 μg/mL，而乙酸乙酯（EtOAc）馏分是活性最高的馏分，IC为19.33 μg/mL。在乙酸乙酯馏分中发现了三种分离物（B1、B2和B3），并通过红外光谱、氢核磁共振、碳核磁共振和二维核磁共振进行了鉴定。

结果

通过光谱鉴定了分离物的化学结构，然后与文献进行比较，得出B1是木栓酮，B2是β-谷甾醇，B3是桦木酸。α-葡萄糖苷酶抑制实验表明，B1、B2和B3的IC值分别为19.51、49.85和18.49 μg/mL。

总结

对布尼（[L.] 施普伦格）茎皮的正己烷、乙酸乙酯（EtOAc）、甲醇馏分进行了α-葡萄糖苷酶抑制活性实验，液相色谱法得到的乙酸乙酯馏分对α-葡萄糖苷酶的抑制活性最高。通过红外光谱、氢核磁共振、碳核磁共振和二维核磁共振光谱鉴定了分离物的化学结构，然后与文献进行比较，得出B1是木栓酮，B2是β-谷甾醇，B3是桦木酸。桦木酸和木栓酮表现出最高的α-葡萄糖苷酶抑制活性。IC：半数最大抑制浓度；H-NMR：氢核磁共振；C-NMR：碳核磁共振；2D-NMR：二维核磁共振；EtOH：乙醇；EtOAc：乙酸乙酯；MeOH：甲醇；CHCl：氯仿；DMSO：二甲基亚砜；EtF：乙酸乙酯馏分；NaCO：碳酸钠；IR：红外光谱；TGR5：跨膜G蛋白偶联受体5；EC：半数最大有效浓度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1b0/5701396/834dc50a72a9/PM-13-590-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1b0/5701396/f127a013e035/PM-13-590-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1b0/5701396/6cd9ddf326d9/PM-13-590-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1b0/5701396/aceeb2e3b80e/PM-13-590-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1b0/5701396/834dc50a72a9/PM-13-590-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1b0/5701396/f127a013e035/PM-13-590-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1b0/5701396/6cd9ddf326d9/PM-13-590-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1b0/5701396/aceeb2e3b80e/PM-13-590-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1b0/5701396/834dc50a72a9/PM-13-590-g011.jpg

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