Gossypol, a natural product extracted from the seed, roots, and stem of cotton, was initially used as a male contraceptive but was subsequently investigated as a novel antitumor agent. This review depicts the current status of gossypol and its derivatives as novel antitumor agents as well as presents their preparation and characteristics, especially of some gossypol Schiff bases, through quantitative and structural analyses. The main attractive target sites of gossypol and its derivatives are Bcl-2 family proteins containing the anti-apoptosis proteins Bcl-2 and Bcl-XL. The molecular mechanism of gossypol analogs not only involves cell apoptosis but also autophagy, cell cycle arrest, and other abnormal cellular phenomena. Gossypol and its derivatives exert antitumor effects on different cancer types in vitro and in vivo, and demonstrate synergistic effects with other chemo- and radio- therapeutic treatments. In addition, several nanocarriers have been designed to load gossypol or its derivatives in order to expand the range of their applications and evaluate their combination effects with other anti-tumor agents. This review may serve as a reference for the rational application of gossypol analogs as anti-tumor agents.
Keywords: Anti-tumor effects, Apoptosis, Autophagy, Bcl-2 family proteins, Gossypol, Nanocarriers, Synergistic effects.
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