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贯叶连翘和贯叶金丝桃中的生物活性化合物:多酚对乙酰胆碱酯酶和 2 型糖尿病相关关键酶的抑制潜力。

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

机构信息

a Laboratory of Plant Biotechnology , National Institute of Applied Sciences and Technology , Tunis , Tunisia.

c National Centre for Nuclear Science and Technology (CNSTN) , Ariana , Tunisia.

出版信息

Pharm Biol. 2017 Dec;55(1):906-911. doi: 10.1080/13880209.2016.1270973.

DOI:10.1080/13880209.2016.1270973
PMID:28147885
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6130493/
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.

摘要

背景

天然产物被报道具有广泛的药理活性,如抗菌、抗炎和抗胆碱酯酶。贯叶金丝桃属(金丝桃科)是多种具有不同生物活性的分子的来源,特别是金丝桃素和各种类黄酮。

目的

本工作的目的是测定总酚和类黄酮含量、金丝桃素和贯叶连翘素的浓度,并评价贯叶金丝桃(Hhu)和贯叶连翘(Hper)的生物学特性。

材料和方法

将地上部分的各种提取物磨碎,然后用甲醇提取。根据最小抑菌浓度(MIC)和最小杀菌浓度(MBC)方法,对四种革兰氏阳性菌、四种革兰氏阴性菌和酵母进行了抗菌活性测定。

结果

结果表明,贯叶金丝桃(H. humifusum)总酚和类黄酮含量(分别为 48-113mgGAE/g 和 8-41mgRE/g)以及金丝桃素(60-90mg/g)和贯叶连翘素(8-30mg/g)浓度最高。两种植物均表现出较强的抗氧化活性,DPPH、FRAP、ABTS 和金属螯合试验均有显示。贯叶金丝桃(H. humifusum)表现出较强的乙酰胆碱酯酶(3.86-4.57mgGALAEs/g)、α-葡萄糖苷酶(0.73-2.55mmolACEs/g)和α-淀粉酶(3-8mmolACEs/g)抑制活性。贯叶金丝桃提取物对表皮葡萄球菌、金黄色葡萄球菌和粪肠球菌具有较强的抗菌活性(MIC 值范围为 200-250μg/mL)。贯叶连翘提取物的抗真菌活性最高(MIC 值=250μg/mL)。

结论

数据表明,贯叶金丝桃(H. humifusum)可作为具有功能特性的有价值的新型天然药物,用于制药行业。

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