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基于代谢组学的贯叶金丝桃化学型指纹图谱分析及其细胞毒性评价

Metabolomics assisted fingerprint of Hypericum perforatum chemotypes and assessment of their cytotoxic activity.

机构信息

Hellenic Agricultural Organization "DEMETER", Institute of Plant Breeding and Genetic Recourses, Department of Medicinal and Aromatic Plants, Thermi 57001, Thessaloniki, Greece.

Laboratory of Pharmacology, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.

出版信息

Food Chem Toxicol. 2018 Apr;114:325-333. doi: 10.1016/j.fct.2018.02.057. Epub 2018 Feb 27.

DOI:10.1016/j.fct.2018.02.057
PMID:29499307
Abstract

Hypericum perforatum is known as an important medicinal plant, used for the treatment of several diseases, while its pharmacological properties are attributed to the presence of a wide range of secondary metabolites. Due to the great chemotypic variability of Hypericum species in the nature, and the demand for standardized herbal products, a detailed phytochemical investigation was carried out on different parts (herba, leaf, flowers) from wild collected and cultivated populations, using advanced chromatographic tools. Liquid Chromatographic analysis (LC-MS/MS MRM) revealed significant variability in the secondary metabolites content of the examined methanolic extracts. The most common derivatives belong to 9 groups i.e. benzoic acids, phenylpropanoids, coumarins, flavones, flavonols, flavan-3-ols, anthocyanins, phloroglucinols and naphtodianthrones. The main polyphenolic compounds were catechin, epicatechin, quercetin, quercetin 3-O-rhamnoside, quercetin 3-O-glucoside, neochlorogenic acid, proanthocyanidins (A and B series) and cyanidin-3-O-glucoside. In addition, the content of the characteristic compounds hypericin and hyperforin in herba crude extracts ranged between 0.5 and 1.7 mg/g and 0.6-3.3 mg/g respectively. The cytotoxic activity of the crude extracts was assessed at concentrations ranged between 0.01 and 100 μg/mL, on Caco-2 intestinal cancer cell cultures, and a cytotoxic behavior was shown only at the highest concentration of 100 μg/mL.

摘要

贯叶金丝桃是一种重要的药用植物,用于治疗多种疾病,而其药理学特性归因于存在广泛的次生代谢物。由于贯叶金丝桃属植物在自然界中的化学型变异性很大,以及对标准化草药产品的需求,因此对野生和栽培种群的不同部位(全草、叶、花)进行了详细的植物化学研究,使用了先进的色谱工具。液相色谱分析(LC-MS/MS MRM)表明,所检查的甲醇提取物中次生代谢物的含量存在显著差异。最常见的衍生物属于 9 组,即苯甲酸、苯丙素、香豆素、黄酮、黄酮醇、黄烷-3-醇、花青素、根皮苷和萘二蒽酮。主要的多酚类化合物为儿茶素、表儿茶素、槲皮素、槲皮素 3-O-鼠李糖苷、槲皮素 3-O-葡萄糖苷、新绿原酸、原花青素(A 和 B 系列)和矢车菊素 3-O-葡萄糖苷。此外,贯叶金丝桃全草粗提取物中特征化合物金丝桃素和金丝桃素的含量在 0.5 至 1.7 mg/g 之间,0.6 至 3.3 mg/g 之间。在 0.01 至 100 μg/mL 的浓度范围内,用 Caco-2 肠癌细胞培养物评估了粗提取物的细胞毒性,仅在 100 μg/mL 的最高浓度下显示出细胞毒性行为。

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