Wen-Hui Xu , Yi-Ran Jiang , Tian-Tian Bei , Ying-Xiao Xiao , Yuan Gao , Hao Xu , Xue-Feng Wu , Hyun-Sun Lee , Long Cui
{"title":"琥珀酸赤萍茎中的六种新芝麻素及其二酰甘油酰基转移酶活性。","authors":"Wen-Hui Xu , Yi-Ran Jiang , Tian-Tian Bei , Ying-Xiao Xiao , Yuan Gao , Hao Xu , Xue-Feng Wu , Hyun-Sun Lee , Long Cui","doi":"10.1016/j.fitote.2024.106221","DOIUrl":null,"url":null,"abstract":"<div><div>Six new sesquineolignans (<strong>1–6</strong>), have been isolated and elucidated from the stems of <em>Akebia quinate</em> together with five known analogues (<strong>7–11</strong>). Their structures were elucidated on the basis of comprehensive analysis of UV, IR, NMR, HRESIMS and CD spectroscopy experiments. All the isolates were evaluated for <em>in vitro</em> inhibitory activity against DGAT1 and DGAT2. Among them, compounds <strong>1–11</strong> were found to exhibit selective inhibitory activity on DGAT1 with IC<sub>50</sub> values ranging from 60.4 ± 1.3 to 84.6 ± 1.3 μM. Besides, the potential binding sites of <strong>1</strong> were predicted by molecular docking.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":null,"pages":null},"PeriodicalIF":2.5000,"publicationDate":"2024-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Six new sesquineolignans from the stems of Akebia quinate and their diacylglycerol acyltransferase activity\",\"authors\":\"Wen-Hui Xu , Yi-Ran Jiang , Tian-Tian Bei , Ying-Xiao Xiao , Yuan Gao , Hao Xu , Xue-Feng Wu , Hyun-Sun Lee , Long Cui\",\"doi\":\"10.1016/j.fitote.2024.106221\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Six new sesquineolignans (<strong>1–6</strong>), have been isolated and elucidated from the stems of <em>Akebia quinate</em> together with five known analogues (<strong>7–11</strong>). Their structures were elucidated on the basis of comprehensive analysis of UV, IR, NMR, HRESIMS and CD spectroscopy experiments. All the isolates were evaluated for <em>in vitro</em> inhibitory activity against DGAT1 and DGAT2. Among them, compounds <strong>1–11</strong> were found to exhibit selective inhibitory activity on DGAT1 with IC<sub>50</sub> values ranging from 60.4 ± 1.3 to 84.6 ± 1.3 μM. Besides, the potential binding sites of <strong>1</strong> were predicted by molecular docking.</div></div>\",\"PeriodicalId\":12147,\"journal\":{\"name\":\"Fitoterapia\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":2.5000,\"publicationDate\":\"2024-09-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Fitoterapia\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0367326X24004040\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Fitoterapia","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0367326X24004040","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Six new sesquineolignans from the stems of Akebia quinate and their diacylglycerol acyltransferase activity
Six new sesquineolignans (1–6), have been isolated and elucidated from the stems of Akebia quinate together with five known analogues (7–11). Their structures were elucidated on the basis of comprehensive analysis of UV, IR, NMR, HRESIMS and CD spectroscopy experiments. All the isolates were evaluated for in vitro inhibitory activity against DGAT1 and DGAT2. Among them, compounds 1–11 were found to exhibit selective inhibitory activity on DGAT1 with IC50 values ranging from 60.4 ± 1.3 to 84.6 ± 1.3 μM. Besides, the potential binding sites of 1 were predicted by molecular docking.
期刊介绍:
Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas:
1. Characterization of active ingredients of medicinal plants
2. Development of standardization method for bioactive plant extracts and natural products
3. Identification of bioactivity in plant extracts
4. Identification of targets and mechanism of activity of plant extracts
5. Production and genomic characterization of medicinal plants biomass
6. Chemistry and biochemistry of bioactive natural products of plant origin
7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.