{"title":"Hypericum empetrifolium and H. lydium as Health Promoting Nutraceuticals: Assessing Their Role Combining In Vitro In Silico and Chemical Approaches","authors":"Stefania Sut, Stefano Dall'Acqua, Giancarlo Angeles Flores, Gaia Cusumano, İsmail Koyuncu, Ozgur Yuksekdag, Carla Emiliani, Roberto Venanzoni, Paola Angelini, Selami Selvi, Evren Yildiztugay, Adriano Mollica, Eleonora Procino, Gregorio Peron, Lorenza Marinaccio, Gokhan Zengin","doi":"10.1002/fsn3.70053","DOIUrl":null,"url":null,"abstract":"<p><i>Hypericum</i> species are known for their ability to produce multiple classes of secondary metabolite and in this article the possible health-promoting role of <i>H. empetrifolium</i> and <i>H. lydium</i> have been evaluated combining in vitro and in silico approaches. <i>H. empetrifolium</i> and <i>H. lydium</i> extracts were obtained using different solvents (ethyl acetate, aceton, aceton/water, and water) and the composition was compared using NMR and LC–MS based approaches. Myricetin-3-<i>O</i>-glucoside, Kaemempferol -3-<i>O</i>-glucoside, and hyperopliphylirrin were present only in <i>H. empetrifolium.</i> Rutin, quercetin-3-<i>O</i>-rhamnoside ant the triterpenoids oleanolic and ursolic acid were only detected in <i>H. lydium</i>. To establish a possible role against degenerative diseases antioxidant, antiradical activities of the extracts were studied and <i>H. empetrifolium</i> acetone/water and water extracts were the more active regarding these effects. The extracts were also evaluated for the inhibition of key-enzymes involved in degenerative diseases namely cholinesterase and tyrosinase for CNS-related pathologies and amylase for metabolic-related diseases. Significant inhibition of acetylcholinesterase was observed for the extracts obtained with lipophilic solvents. The extracts were also studied for their possible antiproliferative activity on cell lines including tumor (DU-145, A549, and MCF-7) and non-tumoral cells (HEK-293) revealing moderate activities. <i>H. lydium</i> ethyl acetate showed late apoptotic (17.5%) and necrotic (46.6%) effects in the Annexin V/PI assay. Molecular docking was used to establish possible interaction of identified compounds with target enzymes and a good interaction between rutin and tyrosinase, myricetin-7-<i>O</i>-glucoside and amylase, was reported. In conclusion, <i>Hypericum empetrifolium</i> and <i>H. lydium</i> thanks to their complex pattern of phytoconstituents and thanks to their significant antioxidant effects as well as with the ability to act on some key-target enzymes involved in degenerative diseases can be considered a good vegetal source for the preparation of nutraceuticals and food supplements useful as health-promoting products against oxidative stress-related diseases such as diabetes, cancer, and Alzheimer's disease.</p>","PeriodicalId":12418,"journal":{"name":"Food Science & Nutrition","volume":"13 4","pages":""},"PeriodicalIF":3.5000,"publicationDate":"2025-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/fsn3.70053","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Food Science & Nutrition","FirstCategoryId":"97","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/fsn3.70053","RegionNum":2,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"FOOD SCIENCE & TECHNOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
Hypericum species are known for their ability to produce multiple classes of secondary metabolite and in this article the possible health-promoting role of H. empetrifolium and H. lydium have been evaluated combining in vitro and in silico approaches. H. empetrifolium and H. lydium extracts were obtained using different solvents (ethyl acetate, aceton, aceton/water, and water) and the composition was compared using NMR and LC–MS based approaches. Myricetin-3-O-glucoside, Kaemempferol -3-O-glucoside, and hyperopliphylirrin were present only in H. empetrifolium. Rutin, quercetin-3-O-rhamnoside ant the triterpenoids oleanolic and ursolic acid were only detected in H. lydium. To establish a possible role against degenerative diseases antioxidant, antiradical activities of the extracts were studied and H. empetrifolium acetone/water and water extracts were the more active regarding these effects. The extracts were also evaluated for the inhibition of key-enzymes involved in degenerative diseases namely cholinesterase and tyrosinase for CNS-related pathologies and amylase for metabolic-related diseases. Significant inhibition of acetylcholinesterase was observed for the extracts obtained with lipophilic solvents. The extracts were also studied for their possible antiproliferative activity on cell lines including tumor (DU-145, A549, and MCF-7) and non-tumoral cells (HEK-293) revealing moderate activities. H. lydium ethyl acetate showed late apoptotic (17.5%) and necrotic (46.6%) effects in the Annexin V/PI assay. Molecular docking was used to establish possible interaction of identified compounds with target enzymes and a good interaction between rutin and tyrosinase, myricetin-7-O-glucoside and amylase, was reported. In conclusion, Hypericum empetrifolium and H. lydium thanks to their complex pattern of phytoconstituents and thanks to their significant antioxidant effects as well as with the ability to act on some key-target enzymes involved in degenerative diseases can be considered a good vegetal source for the preparation of nutraceuticals and food supplements useful as health-promoting products against oxidative stress-related diseases such as diabetes, cancer, and Alzheimer's disease.
金丝桃属植物以其产生多种次生代谢物的能力而闻名,本文结合体外和室内方法评估了金丝桃属植物和金丝桃属植物可能的健康促进作用。采用不同的溶剂(乙酸乙酯、丙酮、丙酮/水和水)得到了石竹和石竹提取物,并采用NMR和LC-MS方法对其组成进行了比较。杨梅素-3- o -葡萄糖苷、山奈酚-3- o -葡萄糖苷和高卟啉仅存在于叶黄素中。芦丁、槲皮素-3- o -鼠李糖苷、齐墩果酸和熊果酸三萜仅在枸杞中检测到。为了确定其对退行性疾病的抗氧化作用,对其提取物的抗自由基活性进行了研究,结果表明,石首草丙酮/水提取物和水提取物的抗自由基活性更强。还评估了提取物对涉及退行性疾病的关键酶的抑制作用,即对中枢神经系统相关病理的胆碱酯酶和酪氨酸酶以及对代谢相关疾病的淀粉酶。用亲脂溶剂提取的提取物对乙酰胆碱酯酶有明显抑制作用。研究了其对肿瘤细胞(DU-145、A549和MCF-7)和非肿瘤细胞(HEK-293)的抗增殖活性。在Annexin V/PI实验中,H.乙酸乙酯显示出晚期凋亡(17.5%)和坏死(46.6%)的作用。利用分子对接方法确定了化合物与目标酶可能的相互作用,并报道了芦丁与酪氨酸酶、杨梅素-7- o -葡萄糖苷和淀粉酶的良好相互作用。综上所述,由于其复杂的植物成分模式和显著的抗氧化作用,以及对退行性疾病中一些关键靶酶的作用能力,金丝桃和黄金丝桃可以被认为是制备营养保健品和食品补充剂的良好植物来源,这些营养保健品和食品补充剂有助于预防氧化应激相关疾病,如糖尿病、癌症和阿尔茨海默病。
期刊介绍:
Food Science & Nutrition is the peer-reviewed journal for rapid dissemination of research in all areas of food science and nutrition. The Journal will consider submissions of quality papers describing the results of fundamental and applied research related to all aspects of human food and nutrition, as well as interdisciplinary research that spans these two fields.