Affiliation:
1. School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, China
Abstract
:
Berberine (BBR) is a quaternary ammonium alkaloid isolated from the Traditional Chinese
Medicine Coptis chinensis. It possesses a plethora of pharmacological activities because its
unique structure properties make it readily interact with macromolecules through π-π stacking and
electrostatic interaction. Its anti-tumor effects are receiving more and more attention in recent years.
Cytotoxicity and anti-proliferation are the important anti-tumor modes of BBR, which have been
studied by many research groups.
:
This study aims to review the structural modifications of BBR and its cytotoxic derivatives. Also, to
study the corresponding structure-activity relationship. BBR showed potential activities toward tumor
cells, however, its modest activity and poor physicochemical properties hindered its application
in clinical. Structural modification is a common and effective approach to improve BBR's cytotoxic
or anti-proliferative activities.
:
The structural modifications of BBR, the cytotoxic or anti-proliferative activities of its derivatives,
and the corresponding structure-activity relationship (SAR) were summarized in the review.
:
The concluded SAR of BBR derivatives with their cytotoxic or anti-proliferative activities will provide
great prospects for the future anti-tumor drug design with BBR as the lead compound.
Funder
National Natural Science Foundation of China
Publisher
Bentham Science Publishers Ltd.