title: Diarylheptanoid glycosides from Tacca plantaginea and their effects on NF-κB activation and PPAR transcriptional activity.
abstract: In the screening search for NF-κB inhibitory and PPAR transactivational agents from medicinal plants, a methanol extract of the whole plant of Tacca plantaginea and its aqueous fraction showed the significant activities. Bioassay-guided fractionation combined with repeated chromatographic separation of the aqueous fraction of the methanol extract of T. plantaginea resulted in the isolation of two new diarylheptanoid glycosides, plantagineosides A (1) and B (2), an unusual new cyclic diarylheptanoid glycoside, plantagineoside C (3), and three known compounds (4-6). Their structures were determined by extensive spectroscopic and chemical methods. Compounds 3-6 significantly inhibited TNFα-induced NF-κB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC(50) values ranging from 0.9 to 9.4 μM. Compounds 1-6 significantly activated the transcriptional activity of PPARs in a dose-dependent manner, with EC(50) values ranging from 0.30 to 10.4 μM. In addition, the transactivational effects of compounds 1-6 were evaluated on three individual PPAR subtypes, including PPARα, γ, and β(δ). Compounds 1-6 significantly enhanced the transcriptional activity of PPARβ(δ), with EC(50) values in a range of 11.0-30.1 μM. These data provide the rationale for using T. plantaginea and its components for the prevention and treatment of inflammatory and metabolic diseases.
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea; Institute of Marine Biochemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Caugiay, Hanoi, Vietnam.
authors.forename: Tran Hong
authors.initials: TH
authors.lastname: Quang
authors.forename: Nguyen Thi Thanh
authors.initials: NT
authors.lastname: Ngan
authors.forename: Chau Van
authors.initials: CV
authors.lastname: Minh
authors.forename: Phan Van
authors.initials: PV
authors.lastname: Kiem
authors.forename: Pham Hai
authors.initials: PH
authors.lastname: Yen
authors.forename: Bui Huu
authors.initials: BH
authors.lastname: Tai
authors.forename: Nguyen Xuan
authors.initials: NX
authors.lastname: Nhiem
authors.forename: Nguyen Phuong
authors.initials: NP
authors.lastname: Thao
authors.forename: Hoang Le Tuan
authors.initials: Hle T
authors.lastname: Anh
authors.forename: Bui Thi Thuy
authors.initials: BT
authors.lastname: Luyen
authors.forename: Seo Young
authors.initials: SY
authors.lastname: Yang
authors.forename: Chun Whan
authors.initials: CW
authors.lastname: Choi
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
mesh_terms: D000963:Antimetabolites / Q000737:chemistry / Q000494:pharmacology; D036381:Diarylheptanoids / Q000737:chemistry* / Q000494:pharmacology; D027743:Dioscoreaceae / Q000737:chemistry*; D004789:Enzyme Activation / Q000187:drug effects; D006027:Glycosides / Q000737:chemistry* / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D000432:Methanol / Q000737:chemistry; D015394:Molecular Structure; D016328:NF-kappa B / Q000378:metabolism*; D047492:Peroxisome Proliferator-Activated Receptors / Q000378:metabolism*; D014158:Transcription, Genetic / Q000187:drug effects*
chemical_list: D000963:Antimetabolites; D036381:Diarylheptanoids; D006027:Glycosides; D016328:NF-kappa B; D047492:Peroxisome Proliferator-Activated Receptors; C578930:plantagineoside A; C578932:plantagineoside B; C578931:plantagineoside C; D000432:Methanol