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来自厄瓜多尔物种 Taxifolium 属(Kunth)Govaerts 的次生代谢产物的α-葡萄糖苷酶抑制和抗菌活性。

α-Glucosidase Inhibition and Antibacterial Activity of Secondary Metabolites from the Ecuadorian Species Clinopodium taxifolium (Kunth) Govaerts.

机构信息

Departamento de Química y Ciencias Exactas, Universidad Técnica Particular de Loja (UTPL), Loja 1101608, Ecuador.

Facultad de Farmacia, Universidad Central de Venezuela, Caracas 1040, Venezuela.

出版信息

Molecules. 2018 Jan 11;23(1):146. doi: 10.3390/molecules23010146.

DOI:10.3390/molecules23010146
PMID:29324657
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6017263/
Abstract

The phytochemical investigation of both volatile and fixed metabolites of (Kunth) Govaerts (Lamiaceae) was performed for the first time. It allowed the isolation and characterization of the essential oil and six known compounds: carvacrol (), squalane (), uvaol (), erythrodiol (), ursolic acid (), and salvigenin (). Their structures were identified and characterized by Nuclear Magnetic Resonance (NMR) and Gas Chromatography coupled to Mass Spectroscopy (GC-MS), and corroborated by literature. The essential oil of the leaves was obtained by hydrodistillation in two different periods and analyzed by GC-MS and GC coupled to Flame Ionization Detector (GC-FID). A total of 54 compounds were detected, of which 42 were identified (including trace constituents). The major constituents were carvacrol methyl ether (18.9-23.2%), carvacrol (13.8-16.3%) and, carvacryl acetate (11.4-4.8%). The antibacterial activities were determined as Minimum Inhibition Concentration (MIC) against , , , , , and . The hexane and methanol extracts exhibited activity only against (250 and 500 μg/mL respectively), while the ethyl acetate extract was inactive. The hypoglycemic activity was evaluated by the in vitro inhibition of α-glucosidase. The ethyl acetate (EtOAc) extract showed strong inhibitory activity with IC = 24.88 µg/mL, however methanolic and hexanic extracts showed weak activity. As a pure compound, only ursolic acid showed a strong inhibitory activity, with IC = 72.71 μM.

摘要

首次对 (Kunth)Govaerts(唇形科)的挥发性和固定代谢产物的植物化学进行了研究。这使得分离和鉴定精油和六种已知化合物成为可能:香芹酚()、角鲨烷()、乌苏酸()、熊果酸()和 salvigenin()。它们的结构通过核磁共振(NMR)和气相色谱与质谱联用(GC-MS)进行鉴定和表征,并通过文献得到证实。叶精油通过两段不同时期的水蒸馏获得,并通过 GC-MS 和气相色谱与火焰离子化检测器(GC-FID)进行分析。共检测到 54 种化合物,其中 42 种被鉴定(包括痕量成分)。主要成分是香芹酚甲基醚(18.9-23.2%)、香芹酚(13.8-16.3%)和香芹醇乙酸酯(11.4-4.8%)。抗菌活性通过最低抑菌浓度(MIC)来确定,对抗 、 、 、 、 和 。正己烷和甲醇提取物仅对 (分别为 250 和 500μg/mL)具有活性,而乙酸乙酯提取物则没有活性。通过体外抑制α-葡萄糖苷酶评估降血糖活性。乙酸乙酯(EtOAc)提取物具有很强的抑制活性,IC = 24.88 µg/mL,而甲醇和正己烷提取物则具有较弱的活性。作为纯化合物,只有熊果酸表现出很强的抑制活性,IC = 72.71 μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be7/6017263/43dbb7b1293f/molecules-23-00146-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be7/6017263/43dbb7b1293f/molecules-23-00146-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be7/6017263/43dbb7b1293f/molecules-23-00146-g001.jpg

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