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A series of b-cyclodextrin inclusion complexes of 4-hydroxyquinoline derivatives was designed and their activities on free-radical-induced hemolysis were studied. The hemolysis of human erythrocytes was initiated by 2,2'-azobis(2-amidinopropane hydrochloride) (AAPH). A novel distributive status was designed: 7-chloro-4-hydroxyquinoline-3-carboxylic acid (CA), 7-fluoro-4-hydroxyquinoline-3-carboxylic acid (FA), 7-chloro-4-hydroxyquinoline (CQ) and 7-fluoro-4-hydroxy quinoline (FQ) were included into b-cyclodextrin to form host-guest complexes, CACD, FACD, CQCD and FQCD, respectively. The hemolysis process was expressed mathematically by Boltzmann equation. Three complexes acted as concentrationdependent antioxidants, and the order of concentrationsensitivity was CQCD > FACD > FQCD. CACD did not show activity. The order of 50% inhibitory concentration (IC 50 ) was FQCD < FACD < CQCD, which was different from that dissolved in dimethyl sulfoxide (DMSO) remarkably. FQCD may be a candidate for a novel antitumor drug.

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