Histone deacetylase inhibitory properties of metabolites from leaves of Quercus pontica K. Koch and its metabolites.

IF 2.2 4区 医学 Q3 ENVIRONMENTAL SCIENCES
Gülin Renda, Sezer Sevgi, Michal Šoral, Gamze Bora-Akoğlu, Suat Sari, Özge Çetin, Pelin Zobaroğlu-Özer, Didem Şöhretoğlu
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引用次数: 0

Abstract

The infusions prepared from some Quercus L. species are used in folk medicine for medicinal purposes and consumed as tea. Quercus pontica K. Koch was selected in this study, for which no phytochemical isolation studies have been performed so far. Quercetin 3-O- β-D-glucopyranoside, kaempferol 3-O-(6""-O-galloyl)-β-D-glucopyranoside, kaempferol 3-O-β-D-glucopyranoside, kaempferol 3-O-(6"'-coumaroyl-β-D-glucopyranoside, phlorizin, rosmarinic acid, and catechin were isolated from the titled plant for the first time. Some polyphenolic compounds have been shown to inhibit histone deacetylase (HDAC) enzymes. However, there is no study on the any activities of Quercus species in the literature. In this study, we demonstrated that the extract has in vitro pan-HDAC inhibition activity. Through a virtual screening study, the compounds were found to inhibit HDAC7 more strongly than the other HDAC isoforms; therefore, the HDAC7 inhibition activities were studied in vitro. Kaempferol 3-O-β-D-glucopyranoside and kaempferol 3-O-(6'"-coumaroyl-β-D-glucopyranoside) showed the best anti-HDAC7 activity with 37% and 41% inhibition at 500 μM.

Quercus pontica K. Koch叶片及其代谢物的组蛋白去乙酰化酶抑制特性。
从一些柞树树种中提取的浸泡液在民间医学中用于药用目的,并作为茶饮用。本研究选择了迄今为止尚未进行过植物化学分离研究的 Quercus pontica K. Koch。研究首次从该植物中分离出槲皮素 3-O-β-D-Glucopyranoside 、山柰酚 3-O-(6""-O-galloyl)-β-D-Glucopyranoside 、山柰酚 3-O-β-D-Glucopyranoside 、山柰酚 3-O-(6"'-coumaroyl-β-D-Glucopyranoside, phlorizin, 迷迭香酸和儿茶素。一些多酚化合物已被证明能抑制组蛋白去乙酰化酶(HDAC)。然而,文献中还没有关于柞树的任何活性的研究。在这项研究中,我们证明了槲皮提取物具有体外泛 HDAC 抑制活性。通过虚拟筛选研究,我们发现这些化合物对 HDAC7 的抑制作用比对其他 HDAC 同工酶的抑制作用更强;因此,我们对这些化合物的 HDAC7 抑制活性进行了体外研究。山奈酚 3-O-β-D-吡喃葡萄糖苷和山奈酚 3-O-(6'"-香豆酰-β-D-吡喃葡萄糖苷)显示出最佳的抗 HDAC7 活性,在 500 μM 时的抑制率分别为 37% 和 41%。
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来源期刊
International Journal of Environmental Health Research
International Journal of Environmental Health Research 医学-公共卫生、环境卫生与职业卫生
CiteScore
6.70
自引率
3.10%
发文量
134
审稿时长
>12 weeks
期刊介绍: International Journal of Environmental Health Research ( IJEHR ) is devoted to the rapid publication of research in environmental health, acting as a link between the diverse research communities and practitioners in environmental health. Published articles encompass original research papers, technical notes and review articles. IJEHR publishes articles on all aspects of the interaction between the environment and human health. This interaction can broadly be divided into three areas: the natural environment and health – health implications and monitoring of air, water and soil pollutants and pollution and health improvements and air, water and soil quality standards; the built environment and health – occupational health and safety, exposure limits, monitoring and control of pollutants in the workplace, and standards of health; and communicable diseases – disease spread, control and prevention, food hygiene and control, and health aspects of rodents and insects. IJEHR is published in association with the International Federation of Environmental Health and includes news from the Federation of international meetings, courses and environmental health issues.
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