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。

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL Fitoterapia Pub Date : 2024-09-30 DOI:10.1016/j.fitote.2024.106221

Wen-Hui Xu , Yi-Ran Jiang , Tian-Tian Bei , Ying-Xiao Xiao , Yuan Gao , Hao Xu , Xue-Feng Wu , Hyun-Sun Lee , Long Cui

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引用次数: 0

摘要

研究人员从喹乙酸鹰嘴豆（Akebia quinate）的茎中分离并阐明了六种新的芝麻木脂素（1-6）以及五种已知的类似物（7-11）。它们的结构是在紫外光谱、红外光谱、核磁共振、HRESIMS 和 CD 光谱实验综合分析的基础上阐明的。评估了所有分离物对 DGAT1 和 DGAT2 的体外抑制活性。其中，化合物 1-11 对 DGAT1 具有选择性抑制活性，其 IC50 值为 60.4 ± 1.3 至 84.6 ± 1.3 μM。此外，还通过分子对接预测了 1 的潜在结合位点。

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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.

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来源期刊

Fitoterapia 医学-药学

CiteScore

5.80

自引率

2.90%

发文量

198

审稿时长

1.5 months

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.