Precancerous lesion is one of most important steps in tumorigenesis. It has been shown that retinoids have reliable effects on controlling many kinds of animal tumor and malignant tumor cell lines in vitro, but there is no laboratory report on the biological effect of retinoids on the precancerous lesion of human lung cancer. In this study the methods including of cell serum-free culture, precancerous model of human bronchial epithelium reconstructed in rat trachea/xenotransplanted in nude mice, flowcytometry, immunohistochemistry, TUNEL and pathological observation have been used to study the biological effects of N-(4-hydroxylphenol) retinamide (4-HPR), one new kind of retinoids, on transformed human bronchial epithelial cells in vitro and premalignant human bronchial epithelium in vivo. The results showed that in the study in vitro, the proliferation of transformed human bronchial epithelial cells, the ratio of cells in S phase, and the percentage of cells that positively react to antibody Ki-67 and mpm-2 were inhibited, but apoptotic cells were induced significantly by 4-HPR exposure. At the experiment in vivo, both growth rates and precancerous grades of the reconstructed human bronchial epithelium were reduced, and apoptotic cells were also observed in epithelium after 4-HPR treatment. The results suggested that 4-HPR is one of hopeful chemopreventive medicines to lung cancer.