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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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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