Preliminary Study On Antitumor Mechanism And Nanoparticles Formulation Of A Kind Of Pyrano[2,3-c] Pyrazole Heterocyclic Compound

The compounds with good anti-tumor activity were screened from 9 kinds of dihydropyrazopyrazole derivatives and named as 6-amino-4-(2-hydroxyphenyl)-3-methyl-1,4-Dihydropyrano[2,3-c]pyrazole-5-carbon itrile(hereinafter abbreviated as AMDPC).The IC50 of AMDPC is 46.52?g/mL.the effect of AMDPC on the gene,protein,cycle and apoptosis of BCAP-37 cells shows that the anti-tumor mechanism of AMDPC may be to stimulate the expression of P21 gene and protein in BCAP-37 cells and then to block the cell cycle through the P53-independent pathway in the S phase.That could be how AMDPC to inhibit cell growth and exert anti-tumor effect.Using MPEG-PLGA as raw material,AMDPC-NP was prepared by encapsulating AMDPC in polymer micelles.The average particle size of AMDPC-NP was 68.16 ± 0.67nm,PDI was 0.139 ± 0.014,and Zeta potential was-16.87 ± 1.10mv.Drug loading rate and entrapment efficiency were 1.28 ± 0.46%and 64.3 ± 7.89%,respectively.The in vitro drug release curves showed that the AMDPC can release slowly from AMDPC-NP.The loading of AMDPC polymer micelles could significantly improve the solubility of AMDPC and make AMDPC release slowly.Its potential anti-tumor activity remains to be further studied and developed.