A polyacetylene from Gymnaster koraiensis exerts hepatoprotective effects in vivo and in vitro.
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.
Lee
Saet Byoul
SB
Natural Products Research Center, Korea Institute of Science and Technology, 290 Daejeon-dong, Gangneung, South Korea.
Kang
Kyungsu
K
Oidovsambuu
Sarangerel
S
Jho
Eun Hye
EH
Yun
Ji Ho
JH
Yoo
Ji-Hye
JH
Lee
En-Ha
EH
Pan
Cheol-Ho
CH
Lee
Jae Kwon
JK
Jung
Sang Hoon
SH
Nho
Chu Won
CW
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
D000975:Antioxidants; D010936:Plant Extracts; D012333:RNA, Messenger; D053279:Polyynes; D024483:Vitamin K 3; D010088:Oxidoreductases; D005978:Glutathione