Anticancer And Radiosensitizing Effects Of Sodium Rhein-amino Acids

Objective:to investigate the anticancer and radiosensitizing effects of sodium rhein derivatives in vitro, various sodium amino acids derives of rhein were been synthesized by modification in structure, and their radiosensitizing effects were further investigated to find radiosensitizer with higher efficiency and less toxicity.Methods:rhein was the lead compound, and its carboxyl condensed with amino group of leucine (Leu), isoleucine (Ile), aspartic acid (Asp), glutamic acid (Glu), tryptophan (Trp), methionine (Met), proline (Pro),2-amino butyric acid, resulting in8amide derivatives. MTT assay was used to measure the inhibition of compounds on proliferation of pulmonary carcinoma H460cells. Compounds with better activity were selected to investigate their radiosensitizing activities in corresponding IC15and IC20concentration.Results:Inhibitory effects of sodium rhein-Leu,-Ile,-Asp,-Glu, and-Met on proliferation of H460cells manifested in a dose and time-dependent manner. The half inhibitory concentrations (IC50) of the sodium rhein-Leu are279.863MM (24h)、92.735μM (48h)、65.567μM (72h), rhein-Ile205.251μM (24h)、164.222μM (48h)、77.442μM (72h), both lower than corresponding IC50values of sodium rhein. Preliminary radiosensitizing test demonstrated that inhibiting rates to H460cells are higher after treatment with the combination of Epirubicin, sodium rhein-Ile with y ray than that of radiation alone.Conclusion:Sodium rhein-Leu and sodium rhein-Ile demonstrated better activity than sodium rhein in inhibiting proliferation on H460cells. Sodium rhein-Ile were tested with preliminary radiosensitizing effect on H460cells in vitro.