Issue 4, 2015
From the journal:

MedChemComm

Synthesis and relationship of stability and biological activity of new DSS and TMP conjugates†

Yewei Sun,a   Zicheng Tan,a   Zhibin Liang,a   Liang Wang,b   Luchen Shan,*a   Pei Yu,*a   Simon MingYuen Leeb  and  Yuqiang Wanga  

* Corresponding authors

a Institute of New Drug Research and Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine, Jinan University College of Pharmacy, Guangzhou, China
E-mail: ytysxs@126.com, pennypeiyu@163.com

b State Key Laboratory of Quality Research in Chinese Medicine, University of Macau, Avenue Padre Tomás Pereira S.J., Macao SAR, China

Abstract

A series of novel conjugates of danshensu (DSS) and tetramethylpyrazine (TMP) were designed and synthesized. Their stability toward hydrolysis by carboxylesterase and cardioprotective effect against t-BHP- and doxorubicin-induced damage were evaluated in H9c2 cells. The results revealed that increasing steric hindrance with bulky groups at the linkage position between DSS and TMP prolonged the half-life and also markedly increased the protective effect. Compound 7 was the most potent in protecting against t-BHP- and doxorubicin-induced damage. The protective effect of compound 7 may in part be attributed to its promotion of mitochondrial biogenesis.

Graphical abstract: Synthesis and relationship of stability and biological activity of new DSS and TMP conjugates

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Article information

DOI
https://doi.org/10.1039/C4MD00448E
Article type
Concise Article
Submitted
02 Oct 2014
Accepted
12 Dec 2014
First published
22 Dec 2014

Med. Chem. Commun., 2015,6, 586-591

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Synthesis and relationship of stability and biological activity of new DSS and TMP conjugates

Y. Sun, Z. Tan, Z. Liang, L. Wang, L. Shan, P. Yu, S. M. Lee and Y. Wang, Med. Chem. Commun., 2015, 6, 586 DOI: 10.1039/C4MD00448E

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