DGAT inhibitory three new lignans from the stem of Eleutherococcus senticosus

• Published in: Phytochemistry letters 2020-12, Vol.40, p.67-71
• Main Authors: Li, Zhi, Li, Ban-Ban, Xiu, Meng-Xue, Wang, Dong, Xiong, Da-Xi, Lee, Hyun-Sun, Cui, Long
• Format: Article
• Language: English
• Subjects: DGAT; Eleutherococcus senticosus (Rupt. & Maxim.) Maxim; Lignans
• ISSN: 1874-3900; 1876-7486
• DOI: 10.1016/j.phytol.2020.09.002

[Display omitted] •Three new compounds were isolated from the stems of Eleutherococcus senticosus for the first time.•Compound 5 was a special lignan that the acetyl group was attached to the dihydrofuran structure.•Eight compounds displayed a high selectivity for inhibitory against DGAT1. Eleutherococcus senticosus (Rupt. & Maxim.) Maxim is a shrub plant, it is the traditional medicine which is used to treat numerous diseases such as rheumatism, diabetes and hepatitis. In this study, a new furofuran lignan 1/2,5/6-trans-2-(3”,4”-methylenedioxyphenyl)-6-(3',4'-methylenedioxyphenyl)-8-oxo-3,7-dioxabicyclo[3.3.0]octane (1) and two new neolignans cis-7,8-dihydro-8-acetylmethyl-7-(4-hydroxy-3,5'-methoxyphenyl)-1'-benzofuranpropanol (5) and 7,8-erythro-5,9-dihydroxy-4,3'-dimethoxy-5,8'-oxyneolign-1'-propanol (8) together with seven known compounds (2-4, 6, 7, 9, 10) were obtained from the EtOAc-soluble extract of Eleutherococcus senticosus. Their structures were determined by analysis of basis of spectroscopic and physicochemical. All the compounds were evaluated for in vitro inhibitory activity against DGAT1 and DGAT2. The in vitro inhibitory activity of all isolated were found to exhibited significant selective inhibitory activity on DGAT1 with IC50 values ranging from 78.8 ± 1.0–132.1 ± 1.1 μM.