Sun S, Han R
Institute of Materia Medica, Beijing.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 1992 Oct;14(5):365-70.
R8605 belongs to the third generation retinoid and was found during the systematic screening of cancer chemopreventive agents in our institute. Based on the theory of multistage carcinogenesis, the anti-carcinogenic and anti-promoting effects of R8605 as well as its possible anti-promoting mechanisms were studied. Experiments proved that R8605 (50 mg/kg and 25 mg/kg, i.g.) significantly inhibited the growth of skin papillomas induced by 7, 12-dimethylbenz[a]anthracene and croton oil in mice and exhibited a potent anti-promoting action. In addition, R8605 (50 mg/kg and 25 mg/kg, i.g.) strongly inhibited the induction of ornithine decarboxylase (ODC) activity of mouse skin epidermis by croton oil. At a dose of 100 mg/kg of R8605 (i.g.) croton oil-induced ear edema in mice was suppressed. These results suggest that the anti-promoting effect of R8605 might be associated with its anti-inflammatory action and its inhibitory effect on ODC activity.
R8605属于第三代维甲酸，是在本研究所对癌症化学预防剂进行系统筛选过程中发现的。基于多阶段致癌理论，对R8605的抗癌和抗促癌作用及其可能的抗促癌机制进行了研究。实验证明，R8605（50毫克/千克和25毫克/千克，腹腔注射）能显著抑制7,12-二甲基苯并[a]蒽和巴豆油诱导的小鼠皮肤乳头瘤生长，并表现出强大的抗促癌作用。此外，R8605（50毫克/千克和25毫克/千克，腹腔注射）强烈抑制巴豆油诱导的小鼠皮肤表皮鸟氨酸脱羧酶（ODC）活性。当R8605剂量为100毫克/千克（腹腔注射）时，可抑制巴豆油诱导的小鼠耳部水肿。这些结果表明，R8605的抗促癌作用可能与其抗炎作用及其对ODC活性的抑制作用有关。
