Stasiłowicz-Krzemień Anna, Cielecka-Piontek Judyta
Department of Pharmacognosy and Biomaterials, Faculty of Pharmacy, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznan, Poland.
Department of Pharmacology and Phytochemistry, Institute of Natural Fibres and Medicinal Plants, Wojska Polskiego 71b, 60-630 Poznan, Poland.
Antioxidants (Basel). 2023 Sep 5;12(9):1722. doi: 10.3390/antiox12091722.
shows many biological activities like antioxidant potential, extended by a targeted effect on selected enzymes, the expression of which is characteristic for neurodegenerative changes within the nervous system. extracts (LFE) were prepared by supercritical carbon dioxide (scCO) extraction with various pressure and temperature parameters. The antioxidant, chelating activity, and inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase by extracts were studied. The extracts containing ethanol were used as references. The most beneficial neuroprotective effects were shown by the extract obtained under 5000 PSI and 50 °C. The neuroprotective effect of active compounds is limited by poor solubility; therefore, carriers with solubilizing properties were used for scCO extracts, combined with post-scCO ethanol extract. Hydroxypropyl-β-cyclodextrin (HP-β-CD) in combination with magnesium aluminometasilicate (Neusilin US2) in the ratio 1:0.5 improved dissolution profiles to the greatest extent, while the apparent permeability coefficients of these compounds determined using the parallel artificial membrane permeability assay in the gastrointestinal (PAMPA GIT) model were increased the most by only HP-β-CD.
具有许多生物活性,如抗氧化潜力,通过对特定酶的靶向作用得以扩展,这些酶的表达是神经系统神经退行性变化的特征。提取物(LFE)通过超临界二氧化碳(scCO₂)在不同压力和温度参数下萃取制备。研究了提取物的抗氧化、螯合活性以及对乙酰胆碱酯酶(AChE)、丁酰胆碱酯酶(BChE)和酪氨酸酶的抑制作用。含乙醇的提取物用作对照。在5000磅力/平方英寸和50℃条件下获得的提取物显示出最有益的神经保护作用。活性化合物的神经保护作用受溶解度差的限制;因此,具有增溶性质的载体被用于scCO₂提取物,并与scCO₂后乙醇提取物结合使用。羟丙基-β-环糊精(HP-β-CD)与硅铝酸镁(Neusilin US2)以1:0.5的比例组合时,溶解曲线改善程度最大,而在胃肠道(PAMPA GIT)模型中使用平行人工膜通透性测定法测定的这些化合物的表观渗透系数仅在添加HP-β-CD时增加最多。