title: Four new sesqui-lignans isolated from Acanthopanax senticosus and their diacylglycerol acyltransferase (DGAT) inhibitory activity.
abstract: Four new sesqui-lignans, (7R, 7'R, 7″S, 8S, 8'S, 8″S)-4',5″-dihydroxy-3,5,3',4″-tetramethoxy-7,9':7',9-diepoxy-4,8″-oxy-8,8'-sesquineo-lignan-7″,9″-diol (1), (7R, 7'R, 7″S, 8S, 8'S, 8″S)-4',3″-dihydroxy-3,5,3',5',4″-pentamethoxy-7,9':7',9-diepoxy-4,8″-oxy-8,8'-sesquineo-lignan-7″,9″-diol (2), (7R, 7'R, 7″S, 8S, 8'S, 8″S)-3',4″-dihydroxy-3,5,4',5″-tetramethoxy-7,9':7',9-diepoxy-4,8″-oxy-8,8'-sesquineo-lignan-7″,9″-diol (3) and acanthopanax A (7) together with three known compounds (4-6) were isolated from the EtOAc-soluble extract of Acanthopanax senticosus. Their structures were elucidated on the basis of spectroscopic and physicochemical analyses. All the isolates were evaluated for in vitro inhibitory activity against DGAT1 and DGAT2. Among them, compounds 1-6 were found to exhibit selective inhibitory activity on DGAT1 with IC50 values ranging from 61.1 ± 1.3 to 97.7 ± 1.1 μM and compound 7 showed selective inhibition of DGAT2 with IC50 value 93.2 ± 1.2.
authors.affiliation: College of Pharmacy, Beihua University, Jilin Province 132013, People's Republic of China.
authors.forename: Jia-Lin
authors.initials: JL
authors.lastname: Li
authors.affiliation: College of Pharmacy, Beihua University, Jilin Province 132013, People's Republic of China.
authors.forename: Na
authors.initials: N
authors.lastname: Li
authors.affiliation: Chemical Biology Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Chungbuk 363-883, Republic of Korea.
authors.forename: Hyun-Sun
authors.initials: HS
authors.lastname: Lee
authors.affiliation: College of Pharmacy, Beihua University, Jilin Province 132013, People's Republic of China.
authors.forename: Shan-Shan
authors.initials: SS
authors.lastname: Xing
authors.affiliation: College of Pharmacy, Beihua University, Jilin Province 132013, People's Republic of China.
authors.forename: Shi-Zhou
authors.initials: SZ
authors.lastname: Qi
authors.affiliation: College of Pharmacy, Beihua University, Jilin Province 132013, People's Republic of China.
authors.forename: Zhen-Dong
authors.initials: ZD
authors.lastname: Tuo
authors.affiliation: College of Pharmacy, Beihua University, Jilin Province 132013, People's Republic of China.
authors.forename: Le
authors.initials: L
authors.lastname: Zhang
authors.affiliation: College of Pharmacy, Beihua University, Jilin Province 132013, People's Republic of China.
authors.forename: Ban-Ban
authors.initials: BB
authors.lastname: Li
authors.affiliation: College of Pharmacy, Beihua University, Jilin Province 132013, People's Republic of China.
authors.forename: Jian-Guang
authors.initials: JG
authors.lastname: Chen
authors.affiliation: College of Pharmacy, Beihua University, Jilin Province 132013, People's Republic of China. Electronic address: cuilong71@beihua.edu.cn.
authors.forename: Long
authors.initials: L
authors.lastname: Cui
mesh_terms: D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors*; D028001:Eleutherococcus / Q000737:chemistry*; D017705:Lignans / Q000737:chemistry* / Q000302:isolation & purification; D015394:Molecular Structure; D018547:Plant Stems / Q000737:chemistry
chemical_list: D017705:Lignans; D051048:Diacylglycerol O-Acyltransferase
keywords: Acanthopanax senticosus; DGAT; Sesqui-lignans