title: A polyacetylene from Gymnaster koraiensis exerts hepatoprotective effects in vivo and in vitro.
abstract: In the present study, we isolated a polyacetylene, gymnasterkoreayne B (GKB), from Gymnaster koraiensis and investigated the effect of GKB on the protection from oxidative stress-induced cytotoxicity through induction of the expression of cellular defense enzymes. GKB induced mRNA expression and enzyme activity of NAD(P)H:quinone oxidoreductase (NQO1) in vitro and in vivo, and potently increased expression of many cellular defense genes including glutathione-S-transferases, UDP-glucuronosyltransferase, and glutathione reductase (GSR) in normal rat liver. The nuclear factor erythroid 2-related factor 2 (Nrf2) which is known to induce various antioxidant and cytoprotective genes, and the genes containing the antioxidant response element (ARE), including NQO1, hemeoxygenease-1, GSR were induced by GKB in HepG2 human hepatocarcinoma cells. Pre-treatment of the cells with GKB accelerated the production of glutathione and mitigated menadione-induced cytotoxicity in HepG2 cells. Taken together, we found that GKB was a novel inducer of phase II detoxification enzymes and cellular defense enzymes, resulting in protection of the cells from oxidative stress and hepatotoxicity through regulation of detoxifying and antioxidant systems.
authors.affiliation: Natural Products Research Center, Korea Institute of Science and Technology, 290 Daejeon-dong, Gangneung, South Korea.
authors.forename: Saet Byoul
authors.initials: SB
authors.lastname: Lee
authors.forename: Kyungsu
authors.initials: K
authors.lastname: Kang
authors.forename: Sarangerel
authors.initials: S
authors.lastname: Oidovsambuu
authors.forename: Eun Hye
authors.initials: EH
authors.lastname: Jho
authors.forename: Ji Ho
authors.initials: JH
authors.lastname: Yun
authors.forename: Ji-Hye
authors.initials: JH
authors.lastname: Yoo
authors.forename: En-Ha
authors.initials: EH
authors.lastname: Lee
authors.forename: Cheol-Ho
authors.initials: CH
authors.lastname: Pan
authors.forename: Jae Kwon
authors.initials: JK
authors.lastname: Lee
authors.forename: Sang Hoon
authors.initials: SH
authors.lastname: Jung
authors.forename: Chu Won
authors.initials: CW
authors.lastname: Nho
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000494:pharmacology*; D019659:Asteraceae / Q000737:chemistry*; D002470:Cell Survival / Q000187:drug effects; D018890:Chemoprevention; D004790:Enzyme Induction / Q000187:drug effects; D015971:Gene Expression Regulation, Enzymologic / Q000187:drug effects; D005978:Glutathione / Q000378:metabolism; D056945:Hep G2 Cells / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D006801:Humans; D008099:Liver / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D008297:Male; D020411:Oligonucleotide Array Sequence Analysis; D018384:Oxidative Stress / Q000187:drug effects; D010088:Oxidoreductases / Q000235:genetics / Q000378:metabolism; D010936:Plant Extracts / Q000494:pharmacology; D053279:Polyynes / Q000494:pharmacology*; D012333:RNA, Messenger / Q000378:metabolism; D051381:Rats; D011916:Rats, Inbred F344; D024483:Vitamin K 3 / Q000037:antagonists & inhibitors / Q000633:toxicity
chemical_list: D000975:Antioxidants; D010936:Plant Extracts; D012333:RNA, Messenger; D053279:Polyynes; D024483:Vitamin K 3; D010088:Oxidoreductases; D005978:Glutathione