高效薄层色谱法筛选植物提取物中生物活性天然化合物

Á. Móricz, D. Krüzselyi, Maryam Jamshidi-Aidji, P. Ott, G. Morlock
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摘要

在过去的十年中,效应导向分析(EDA)为从天然来源发现新的潜在药物化合物提供了新的动力。高效薄层色谱(HPTLC)是一种高通量、可靠的分离技术,经常用于筛选高度复杂的样品,如植物粗提取物。HPTLC结合生物和生化分析和高分辨率质谱(HRMS),然后是生物测定引导分离和核磁共振被证明是天然产物生物分析的直接策略[1,2]。糖尿病和阿尔茨海默病(AD)是两个全球性的健康问题。2型糖尿病患者,占糖尿病患者的大多数,患有高血糖症。唾液和胰腺的α-淀粉酶以及α和β-葡萄糖苷酶参与多聚糖和低聚糖的降解和消化,因此,葡萄糖苷酶和淀粉酶抑制剂对2型糖尿病以及超重和肥胖具有治疗意义[3,4]。阿尔茨海默病与大脑胆碱能神经元的丧失和神经递质乙酰胆碱的减少有关。乙酰胆碱酯酶(AChE)和丁基胆碱酯酶(BChE)在乙酰胆碱水解成胆碱的过程中起关键作用。因此,AChE选择性和双重AChE/BChE抑制剂代表了第一代降低AD进展率的药物[5]。传染病是一项重大的全球公害,由于(多重)耐药微生物的出现增加,抗击传染病也是一项挑战[6]。在本研究中,(HP)TLC联合α和β-葡萄糖苷酶、α-淀粉酶和抗菌检测将用于比较入侵性黄花属植物的生物特征(酶抑制和抗菌潜力)。
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High-Throughput Screening for Bioactive Natural Compounds from Plant Extracts by HPTLC Hyphenations
In the last decade, effect-directed analysis (EDA) gave new impetus for the discovery of new potential drug compounds from natural sources. Highperformance thin-layer chromatography (HPTLC) was established as a high-throughput and reliable separation technique that is frequently utilized for screening of highly complex samples, such as crude plant extracts. HPTLC combined with biological and biochemical assays and high-resolution mass spectrometry (HRMS) followed by bioassay-guided isolation and NMR was demonstrated as a straightforward strategy for bioanalysis of natural products [1,2]. Diabetes and Alzheimer’s disease (AD) represent two of the global health issues. Type 2 diabetic patients, the majority of the people with diabetes, suffer from the hyperglycemia. The salivary and pancreatic α-amylases and αand β-glucosidases are involved in the degradation and digestion of polyand oligosaccharides to glucose, hence, glucosidase and amylase inhibitors are of therapeutic interest in type 2 diabetes as well as overweight and obesity [3,4]. AD is associated with the loss of cholinergic neurons in the brain and decrease in the neurotransmitter acetylcholine. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are crucially involved in the hydrolysis of the acetylcholine into choline. Hence, AChE-selective and dual AChE/BChE inhibitors represented the first generation of medicines for the decrease of the AD progression rate [5]. The fight against infectious diseases, a major global public hazard, is also a challenge due to the increase in the emergence of the (multi)drug-resistant microorganisms [6]. In this study (HP)TLC combined with direct αand β-glucosidase, α-amylase and antimicrobial assays will be demonstrated for the comparison of the bio-profiles (the enzyme inhibitory and antibacterial potentials) of invasive goldenrod species.
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