ABSTRACT
A new series of 3-phenyl-3-pyrrolylpentane derivatives are synthesized through modifying the structure of lead compound LG19055,a nonsecosteroidal vitamin D receptor(VDR)agonist.The VDR-agonistic ability of target compounds was measured indirectly by evaluating the differentiation ability of HL-60 cell.The results showed that compounds 13a,13c,13d,13h,13i,13j have excellent VDR-agonistic ability(EC50 <50 μmol /L), especially for compound 13j (EC50 =0.10 μmol /L),which was more potential than that of lead compound LG190155.Their proliferation inhibitory activities in vitro were evaluated by MTT assay in MCF-7,PC-3,Caco-2, HepG2 and L02 cell lines.Compound 13a exhibited significant inhibitory effects on HepG2 cell line(IC50 =0.11μmol /L).Moreover,the inhibitory effect of compound 13a on non-tumor liver L02 cell line was relatively weak (IC50 =15.24 μmol /L ),suggesting that compound 13a has selective inhibitory effects on liver cancer cells.Additionally,HL-60 cell differentiation-inducing activity and the inhibitory effect of cancer cells were posi-tively related.
ABSTRACT
AIM: To study the quality standard for Ganmao Qingre Granules(Herba Schizonepetae,Radix Saposhnikoviae,Radix Puerariae,etc). METHODS: Radix Saposhnikoviae,Spica Schizonepetae,Radix Bupleuri,Herba Platycodonis in Ganmao Qingre Granules were identified by TLC,and the content of puerarin was determined by HPLC. RESULTS: Radix Saposhnikoviae,Herba Schizonepetae,Radix Bupleuri,Herba Platycodonis could be identified by TLC.The concentration curve of hesperdin showed linearity over the range of 0.086 8-8.680 ?g(r=0.999 9).The average recovery was 99.09%,RSD was 1.12%(n=9). CONCLUSION: The method is simple,specific and accurate and can be used effectively for the quality control of Ganmao Qingre Granules.