2. Academic Validation
  3. Six new sesquineolignans from the stems of Akebia quinate and their diacylglycerol acyltransferase activity

Six new sesquineolignans from the stems of Akebia quinate and their diacylglycerol acyltransferase activity

  • Fitoterapia. 2024 Dec:179:106221. doi: 10.1016/j.fitote.2024.106221.
Wen-Hui Xu 1,  Yi-Ran Jiang 1,  Tian-Tian Bei 1,  Ying-Xiao Xiao 1,  Yuan Gao 1,  Hao Xu 1,  Xue-Feng Wu 1,  Hyun-Sun Lee 2,  Long Cui 3
Affiliations

Affiliations

  • 1 College of Pharmacy, Beihua University, Jilin Province 132013, China.
  • 2 Molecular Cancer Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), 685-1 Yangcheongri, Ochangeup, Cheongwongun, Chungbuk 363-883, Republic of Korea.
  • 3 College of Pharmacy, Beihua University, Jilin Province 132013, China. Electronic address: cuilong71@beihua.edu.cn.
PMID: 39357777 DOI: 10.1016/j.fitote.2024.106221
Abstract

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.

Keywords

Akebia quinate; DGAT; Inhibitory activity; Lardizabalaceae; Sesquineolignans.

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