Research on the in vitro anticancer activity and in vivo tissue distribution of Amoitone B nanocrystals.

Amoitone B, a natural agonist to Nur77, is a promising anticancer drug. However, its application is seriously restricted due to the water-insolubility and short biological half-life. Amoitone B nanocrystals (AmB-NC) were formulated by microfluidization method to overcome the above obstacles. This study aims to evaluate the cytotoxicity and tissue distribution of AmB-NC. MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay revealed the improved in vitro antitumor activity of AmB-NC against stomach, colon, liver and lung cancer cells compared with Amoitone B solution. Meanwhile, observation of morphological changes, cell cycle and apoptosis examination using flow cytometry exhibited that AmB-NC could induce G1 cycle arrest and markedly enhance the apoptosis of human gastric cancer BGC-823 cell line. Tissue distribution study demonstrated that AmB-NC had a higher distribution in liver and lung, which was helpful for relevant cancer treatment. In conclusion, AmB-NC could be a potential delivery system for treatment of human cancer.