synthesis and biological activity of trans-tiliroside derivatives as potent anti-diabetic agentstrans-tiliroside衍生物的合成和生物活性的抗糖尿病药物.pdf

Molecules 2010, 15, 9174-9183; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Biological Activity of trans-Tiliroside Derivatives as Potent Anti-Diabetic Agents Yujin Zhu 1,2, Yanjun Zhang 3, Yi Liu 1, Hongwan Chu 1 and Hongquan Duan 1,* 1 School of Pharmaceutical Sciences, Research Center of Basic Medical Sciences, Tianjin Medical University, Tianjin 300070, China; E-Mails: wjyxyzyj@ (Y.J.Z.); aliu_yi@ (Y.L.); ch (H.W.C.) 2 Chinese People’s Armed Police Forces, Tianjin Provincial Corps Hospital, Tianjin 300162, China 3 Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; E-Mail: zyjsunye@163.com (Y.J.Z.)  Author to whom correspondence should be addressed; E-Mail: duanhq@; Tel.:+86-022 Fax: +86-022 Received: 29 October 2010; in revised form: 7 December 2010 / Accepted: 8 December 2010 / Published: 10 December 2010 Abstract: A set of novel trans-tiliroside derivatives were synthesized. The structures of the derivatives were identified by their IR, 1H-NMR, and MS spectra analysis. Their anti-diabetic activities were evaluated on the insulin resistant (IR) HepG2 cell model. As a result, compounds 7a, 7c, 7h, and trans-tiliroside exhibited significant glucose consumption-enhancing effects in IR-HepG2 cells compared with the positive control (metformin). This research provides useful clues for further design and discovery of anti-diabetic agents. Keywords: