{"title":"葎草酚类新苷类及其对DGKζ的抑制活性","authors":"Y. Wang, H. A. Aisa, G. Zou, Z. Li","doi":"10.1007/s10600-025-04730-2","DOIUrl":null,"url":null,"abstract":"<p>The new chromone derivative 1-[(2-methylpropanoyl)chromone]-<i>β</i>-D-glucopyranoside (<b>1</b>) together with eight known compounds (<b>2–9</b>) were isolated from <i>Humulus lupulus</i> (common hops). The structures of the isolated compounds were confirmed by detailed analyses of NMR and HR-ESI-MS data. The glucose fragment in <b>1</b> was determined as the D-glucoside based on GC analysis. Compounds <b>2</b>, <b>4</b>, and <b>5</b> exhibited significant inhibitory activity against diacylglycerol kinase ζ (DGKζ). Compound <b>5</b> demonstrated strong inhibition of DGKζ with an IC<sub>50</sub> value of 1.60 μM. Molecular docking studies gave important information about the role of the galloyl group in DGKζ inhibition.</p>","PeriodicalId":514,"journal":{"name":"Chemistry of Natural Compounds","volume":"61 4","pages":"653 - 658"},"PeriodicalIF":0.9000,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"New Phenolic Glycosides from Humulus lupulus and Their Inhibitory Activity Against DGKζ\",\"authors\":\"Y. Wang, H. A. Aisa, G. Zou, Z. Li\",\"doi\":\"10.1007/s10600-025-04730-2\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>The new chromone derivative 1-[(2-methylpropanoyl)chromone]-<i>β</i>-D-glucopyranoside (<b>1</b>) together with eight known compounds (<b>2–9</b>) were isolated from <i>Humulus lupulus</i> (common hops). The structures of the isolated compounds were confirmed by detailed analyses of NMR and HR-ESI-MS data. The glucose fragment in <b>1</b> was determined as the D-glucoside based on GC analysis. Compounds <b>2</b>, <b>4</b>, and <b>5</b> exhibited significant inhibitory activity against diacylglycerol kinase ζ (DGKζ). Compound <b>5</b> demonstrated strong inhibition of DGKζ with an IC<sub>50</sub> value of 1.60 μM. Molecular docking studies gave important information about the role of the galloyl group in DGKζ inhibition.</p>\",\"PeriodicalId\":514,\"journal\":{\"name\":\"Chemistry of Natural Compounds\",\"volume\":\"61 4\",\"pages\":\"653 - 658\"},\"PeriodicalIF\":0.9000,\"publicationDate\":\"2025-07-22\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Chemistry of Natural Compounds\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s10600-025-04730-2\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemistry of Natural Compounds","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1007/s10600-025-04730-2","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
摘要
从葎草中分离得到新的色素衍生物1-[(2-甲基丙炔基)色素]-β- d -葡萄糖吡喃苷(1)及8个已知化合物(2-9)。化合物的结构通过NMR和HR-ESI-MS进行了详细的分析。通过GC分析确定1中的葡萄糖片段为d -葡萄糖苷。化合物2、4和5对二酰基甘油激酶ζ (DGKζ)具有显著的抑制活性。化合物5对DGKζ具有较强的抑制作用,IC50值为1.60 μM。分子对接研究为没食子酰基在DGKζ抑制中的作用提供了重要信息。
New Phenolic Glycosides from Humulus lupulus and Their Inhibitory Activity Against DGKζ
The new chromone derivative 1-[(2-methylpropanoyl)chromone]-β-D-glucopyranoside (1) together with eight known compounds (2–9) were isolated from Humulus lupulus (common hops). The structures of the isolated compounds were confirmed by detailed analyses of NMR and HR-ESI-MS data. The glucose fragment in 1 was determined as the D-glucoside based on GC analysis. Compounds 2, 4, and 5 exhibited significant inhibitory activity against diacylglycerol kinase ζ (DGKζ). Compound 5 demonstrated strong inhibition of DGKζ with an IC50 value of 1.60 μM. Molecular docking studies gave important information about the role of the galloyl group in DGKζ inhibition.
期刊介绍:
Chemistry of Natural Compounds publishes reviews and general articles about the structure of different classes of natural compounds, the chemical characteristics of botanical families, genus, and species, to establish the comparative laws and connection between physiological activity and the structure of substances.