Andrade Juliana Maria de Mello, Biegelmeyer Renata, Dresch Roger Remy, Maurmann Natasha, Pranke Patrícia, Henriques Amélia T
Laboratory of Pharmacognosy, School of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil.
Hematology and Stem Cell Laboratory, School of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil; Stem Cell Research Institute, School of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil.
Pharmacogn Mag. 2016 Jul-Sep;12(47):171-7. doi: 10.4103/0973-1296.186349.
Investigation of selected plant extracts on multi-targets related to neurodegeneration, such as monoamine oxidases (MAO), cholinesterase enzymes, and antioxidant activities (AOA) is a useful tool for identification of new scaffolds.
This work investigated biological effects of three Blechnum methanol extracts from Brazil and chemical profile of the most active sample.
AOA included scavenging of hydroxyl and nitric oxide radicals, also lipid peroxidation inhibition. Enzymatic modulation of Blechnum binervatum, Blechnum brasiliense, and Blechnum occidentale extracts on MAO and cholinesterases was conducted. Moreover, total phenol content was performed with all samples, and high-performance liquid chromatography-diode array detection mass spectrometry HPLC-DAD-MS analysis was carried out with B. brasiliense. Possible toxic effects were evaluated on Wistar rats polymorphonuclear cells (PMN) and human stem cells.
B. brasiliense extract presented the highest phenolic amount (9.25 g gallic acid equivalent/100 g extract) and lowest IC50 values (112.3 ± 2.61 and 176.1 ± 1.19 μg/mL) against hydroxyl radicals and on lipid peroxidation, respectively, showing strong AO effects. On nitric oxide assay and cholinesterase inhibition, all extracts were considered inactive. MAO-A selective action was evidenced, being B. brasiliense powerful against this enzyme (IC50: 72.7 μg/mL), followed by B. occidentale and B. binervatum (IC50: 130.85 and 165.2 μg/mL). No cytotoxic effects were observed on PMN and human stem cells treated with Blechnum extracts. HPLC-DAD-MS analysis of B. brasiliense allowed the identification of chlorogenic and rosmarinic acids.
Our results especially highlight B. brasiliense, with pronounced phenols content and strong effects on selected targets related to neurodegeneration, being characterized as a natural safe source of bioactive hydroxycinnamic acids.
Blechnum crude extracts showed high phenolic amounts and valuable IC50 values on targets related with neurodegenerative disordersBlechnum brasiliense was the most active sample, with strong radical scavenging and lipid peroxidation inhibition, also with monoamine oxidases: A selective modulationNo cytotoxic effects were observed on polymorphonuclear cells rat cells and human stem cells treated with Blechnum extractsHigh-performance liquid chromatography-diode array detection-mass spectrometry analysis of Blechnum brasiliense allowed the identification of hydroxycinnamic derivatives: Chlorogenic and rosmarinic acids. Abbreviations used: IC50: half maximal inhibitory concentration; MAO: monoamine oxidase; MAO-A: monoamine oxidase isoform A; MAO-B: monoamine oxidase isoform B; HO•: hydroxyl radical.
研究选定植物提取物对与神经退行性变相关的多靶点的作用,如单胺氧化酶(MAO)、胆碱酯酶以及抗氧化活性(AOA),是鉴定新支架的有用工具。
本研究调查了来自巴西的三种 Blechnum 甲醇提取物的生物学效应以及最具活性样品的化学特征。
抗氧化活性包括清除羟基自由基和一氧化氮自由基,以及抑制脂质过氧化。对二叉 Blechnum、巴西 Blechnum 和西方 Blechnum 提取物对 MAO 和胆碱酯酶的酶促调节作用进行了研究。此外,对所有样品进行了总酚含量测定,并对巴西 Blechnum 进行了高效液相色谱 - 二极管阵列检测质谱(HPLC - DAD - MS)分析。对 Wistar 大鼠多形核细胞(PMN)和人类干细胞评估了可能的毒性作用。
巴西 Blechnum 提取物的酚含量最高(9.25 g 没食子酸当量/100 g 提取物),对羟基自由基和脂质过氧化的半数抑制浓度(IC50)值分别最低(112.3 ± 2.61 和 176.1 ± 1.19 μg/mL),显示出较强的抗氧化作用。在一氧化氮检测和胆碱酯酶抑制方面,所有提取物均被认为无活性。证实了 MAO - A 的选择性作用,巴西 Blechnum 对该酶的抑制作用较强(IC50:72.7 μg/mL),其次是西方 Blechnum 和二叉 Blechnum(IC50:130.85 和 165.2 μg/mL)。用 Blechnum 提取物处理的 PMN 和人类干细胞未观察到细胞毒性作用。对巴西 Blechnum 的 HPLC - DAD - MS 分析鉴定出了绿原酸和迷迭香酸。
我们的结果特别突出了巴西 Blechnum,其酚含量显著,对与神经退行性变相关的选定靶点有较强作用,被表征为生物活性羟基肉桂酸的天然安全来源。
Blechnum 粗提物在与神经退行性疾病相关的靶点上显示出高酚含量和有价值的 IC50 值。巴西 Blechnum 是最具活性样品,具有较强的自由基清除和脂质过氧化抑制作用,对单胺氧化酶也有选择性调节作用。用 Blechnum 提取物处理的大鼠多形核细胞和人类干细胞未观察到细胞毒性作用。对巴西 Blechnum 的高效液相色谱 - 二极管阵列检测 - 质谱分析鉴定出了羟基肉桂酸衍生物:绿原酸和迷迭香酸。使用的缩写:IC50:半数最大抑制浓度;MAO:单胺氧化酶;MAO - A:单胺氧化酶同工酶 A;MAO - B:单胺氧化酶同工酶 B;HO•:羟基自由基。