RÉSUMÉ
Objective To prepare hydroxycamptothecin-phospholipid complex(HCPT-PC),characterize its physicochemi-cal properties,and evaluate the cytotoxicity. Methods The particle size and morphology of HCPT-PC were characterized by malvern particle size potentiometer,scanning electron microscopy(TEM)and transmission electron microscopy(TEM). Its composite mecha-nism was investigated by X-ray powder diffraction and infrared spectroscopy. The solubility and antitumor activity were also investigat-ed. Results The particle size of HCPT-PC was(145.08±18.37)nm. Scanning electron microscopy and transmission electron micros-copy revealed that HCPT-PC was uniformly distributed with a spherical shape. X-ray powder diffraction indicated that HCPT changed from crystalline to amorphous state in HCPT-PC. Fourier transform infrared spectroscopy showed that there was a weak interaction be-tween HCPT and PC. The solubility of HCPT-PC in water,PBS,ethanol and n-octanol was about 21.91,20.36,1.42 and 6.32 times than that of HCPT,respectively. After treated with HepG2,SMMC-7721 and H22 cells for 48 and 72 hours,IC50 of HCPT-PC was higher than that of HCPT by 3.57,11.14,2.79,37.26,21.23 and 24.49 times,respectively. Conclusion HCPT is compounded into an amorphous-state HCPT-PC by a weak interaction with the polar end of PC. Its solubility and anti-hepatocarcinoma activity are signif-icantly higher than HCPT.
RÉSUMÉ
With the understanding of the development and pro-gress of the cancer,the research of targeted cancer drug devel-opment reaches into a new era.p53 is an important tumor sup-pressor gene,the protein coded by p53 plays a critical role in tumor suppression mainly by inducing cell cycle regulation, DNA repair and apoptosis.Nowadays,p53 becomes a relatively attractive target for anti-cancer drug development and there are some drugs targeting p53,moreover,APR-246 which targets mutant p53 is in Phase II clinical trial.In addition,it facilitates drugs discovery programmes in the challenging area of protein-protein interactions and mutant protein conformational change. The review discusses the research progress of drugs which target p53 and elucidates the characteristics and mechanisms of these compounds.