Optimization of Rutaecarpine as ABCA1 Up-Regulator for Treating Atherosclerosis

  • ACS Med Chem Lett. 2014 Jun 24;5(8):884-8. doi: 10.1021/ml500131a.
Yongzhen Li  1 ,  Tingting Feng  1 ,  Peng Liu  1 ,  Chang Liu  1 ,  Xiao Wang  1 ,  Dongsheng Li  1 ,  Ni Li  1 ,  Minghua Chen  1 ,  Yanni Xu  1 ,  Shuyi Si  1
Affiliations
  • 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
PMID: 25147608 DOI: 10.1021/ml500131a
Abstract

ATP-binding cassette transporter A1 (ABCA1) is a key transporter and receptor in promoting Cholesterol efflux, and increasing the expression level of ABCA1 is antiatherogenic. In our previous study, rutaecarpine (RUT) was found to protect apoE(-/-) mice from developing atherosclerosis through preferentially up-regulating ABCA1 expression. In the present work, a series of RUT derivatives were synthesized and examined as ABCA1 expression up-regulators. Compounds CD1, CD6, and BCD1-2 were found to possess the most potential activity as antiatherosclerotic agents among all compounds tested.

Keywords
ABCA1; RCT; Rutaecarpine; atherosclerosis.