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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.

SUBMITTER: Li Y 

PROVIDER: S-EPMC4137366 | biostudies-literature | 2014 Aug

REPOSITORIES: biostudies-literature

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Optimization of Rutaecarpine as ABCA1 Up-Regulator for Treating Atherosclerosis.

Li Yongzhen Y   Feng Tingting T   Liu Peng P   Liu Chang C   Wang Xiao X   Li Dongsheng D   Li Ni N   Chen Minghua M   Xu Yanni Y   Si Shuyi S  

ACS medicinal chemistry letters 20140624 8


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  ...[more]

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