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Molecules 2010, 15(8), 5273-5281; doi:10.3390/molecules15085273
Article

2-(Penta-1,3-diynyl)-5-(3,4-dihydroxybut-1-ynyl)thiophene, a Novel NQO1 Inducing Agent from Echinops grijsii Hance

1,†
,
2,†
 and
3,*
1 Department of Pharmacy, Zhejiang Medical College, No.481 Binwen Rd., Hangzhou 310053, China 2 School of Pharmaceutical Sciences, Zhejiang University, Zijingang Campus, No.388 Yuhangtang Rd., Hangzhou 310058, China 3 Department of Urology, First Affiliated Hospital, School of Medicine, Zhejiang University, No.79 Qingchun Rd., Hangzhou 310003, China These authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 15 July 2010 / Revised: 27 July 2010 / Accepted: 2 August 2010 / Published: 3 August 2010
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Abstract

A natural alkynol group-substituted thiophene, 2-(penta-1,3-diynyl)-5-(3,4-dihydroxybut-1-ynyl)-thiophene (PDDYT), was isolated from the roots of Echinops grijsii Hance. It possessed potent NAD(P)H: quinone oxidoreductase1 (NQO1) inducing activity and could activate Keap1-Nrf2 pathway effectively in murine hepatoma Hepa 1c1c7 cells. Further investigations indicated that the activation of Keap1-Nrf2 pathway by PDDYT might be attributed to the activation of Akt and depleting the cellular glutathione (GSH).
Keywords: Echinops grijsii hance; PDDYT; NQO1; Nrf2; glutathione; Akt Echinops grijsii hance; PDDYT; NQO1; Nrf2; glutathione; Akt
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Shi, J.; Zhang, X.; Jiang, H. 2-(Penta-1,3-diynyl)-5-(3,4-dihydroxybut-1-ynyl)thiophene, a Novel NQO1 Inducing Agent from Echinops grijsii Hance. Molecules 2010, 15, 5273-5281.

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