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Bioactive compounds from Hypericum humifusum and Hypericum perfoliatum : inhibition potential of polyphenols with acetylcholinesterase and key enzymes linked to type-2 diabetes

机译:贯叶连翘和贯叶连翘的生物活性化合物:乙酰胆碱酯酶和与2型糖尿病有关的关键酶对多酚的抑制潜力

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Abstract Context: Natural products are reported to have a wide spectrum of pharmacological properties such as antimicrobial, anti-inflammatory and anti-cholinesterase. The genus Hypericum (Hypericaceae) is a source of a variety of molecules with different biological activities, notably hypericin and various phenolics. Objectives: The goals of the present work were the determination of total phenolic and flavonoid content, hypericin and hyperforin concentration as well as the evaluation of biological of Hypericum humifusum L. (Hhu) and Hypericum perfoliatum L. (Hper). Materials and methods: The various extracts of aerial parts were powdered, and then extracted with methanol. Antibacterial activity was performed according to minimum inhibitory concentration (MIC) and minimum bactericidal (MBC) methods against four Gram-positive bacteria, four Gram-negative bacteria and yeast. Results: The results revealed that H. humifusum, bear the highest total phenolic and flavonoid content (48–113?mg GAE/g and 8–41?mg RE/g, respectively) as well as hypericin (60–90?mg/g) and hyperforin (8–30?mg/g) concentration. Both species showed significant antioxidant activity as revealed by DPPH, FRAP, ABTS, and metal chelating assays. H. humifusum exhibited a strong acetylcholinesterase (3.86–4.57?mg GALAEs/g), α-glucosidase (0.73–2.55?mmol ACEs/g) and α-amylase (3–8?mmol ACEs/g) inhibitory activity. The extract of H. humifusum exhibited strong antibacterial activity mainly against Staphylococcus epidermidis, Staphylococus aureus, and Enterococcus faecium (MIC values ranging from 200 to 250?μg/mL). The highest antifungal activity was showed for H. perfoliatum extract (MIC value = 250?μg/mL). Conclusion: The data suggest that H. humifusum could be used as valuable new natural agents with functional properties for pharmacology industries.
机译:摘要背景:据报道,天然产物具有广泛的药理特性,例如抗微生物,抗炎和抗胆碱酯酶。金丝桃属(Hypericaceae)是具有不同生物活性的各种分子的来源,特别是金丝桃素和各种酚类。目的:目前工作的目标是测定总酚和类黄酮含量,金丝桃素和金丝桃素的浓度,以及评价贯叶连翘和贯叶连翘的生物学特性。材料和方法:将地上部分的各种提取物制成粉末,然后用甲醇提取。根据最小抑菌浓度(MIC)和最小杀菌(MBC)方法对四种革兰氏阳性菌,四种革兰氏阴性菌和酵母菌进行抗菌活性。结果:结果表明,H。humifusum的总酚和类黄酮含量最高(分别为48-113?mg GAE / g和8-41?mg RE / g)以及金丝桃素(60-90?mg / g)。 g)和hyperforin(8–30?mg / g)浓度。如DPPH,FRAP,ABTS和金属螯合测定所揭示,两种物质均显示出显着的抗氧化活性。 H. humifusum表现出很强的乙酰胆碱酯酶(3.86-4.57?mg GALAEs / g),α-葡萄糖苷酶(0.73-2.55?mmol ACEs / g)和α-淀粉酶(3-8?mmol ACEs / g)抑制活性。潮腐提取物主要对表皮葡萄球菌,金黄色葡萄球菌和粪肠球菌具有很强的抗菌活性(MIC值为200至250μg/ mL)。对叶提取物H.perfoliatum提取物具有最高的抗真菌活性(MIC值=250μg/ mL)。结论:数据表明,H。humifusum可用作具有药理学功能的有价值的新型天然药物。

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