title: Optimization of Rutaecarpine as ABCA1 Up-Regulator for Treating Atherosclerosis.
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.
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
authors.forename: Yongzhen
authors.initials: Y
authors.lastname: Li
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Feng
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
authors.forename: Peng
authors.initials: P
authors.lastname: Liu
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
authors.forename: Chang
authors.initials: C
authors.lastname: Liu
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Wang
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
authors.forename: Dongsheng
authors.initials: D
authors.lastname: Li
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
authors.forename: Ni
authors.initials: N
authors.lastname: Li
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
authors.forename: Minghua
authors.initials: M
authors.lastname: Chen
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
authors.forename: Yanni
authors.initials: Y
authors.lastname: Xu
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Tiantanxili No. 1, Beijing 100050, China.
authors.forename: Shuyi
authors.initials: S
authors.lastname: Si
keywords: ABCA1; RCT; Rutaecarpine; atherosclerosis