Zhou Wan-Qi, Zhang Hai-Jing, Jin Jing, Li Yan, Li Chao, Chen Xiao-Guang
State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
Yao Xue Xue Bao. 2012 Apr;47(4):546-50.
FTY720 is a synthetic compound derived from the metabolites of Isaria sinclairii. Its unique chemical structure and mechanism appear to be distinctive from other known immunosuppressors. In the present study, the effect of FTY720 on immunosuppression and toxicity to heart was evaluated by detection of lymphocytes count, heart rate in rats, the survival time of the allografts of skin slice in mice and binding to S1P1 and S1P3 receptors by confocal. The results showed that FTY720 could induce lymphopenia, reduce the heart rates in rats and prolong the survival time of the allografts of skin slice in mice. The assay results on confocal showed that FTY720 can bind with S1P1 and S1P3 on surface of CHO-S1P1 and CHO-S1P3 cells. FTY720 could be developed for wide application for organ transplantation and self-immunity diseases.
FTY720是一种从蝉拟青霉代谢产物中衍生而来的合成化合物。其独特的化学结构和作用机制似乎与其他已知的免疫抑制剂不同。在本研究中，通过检测大鼠淋巴细胞计数、心率、小鼠皮肤切片同种异体移植物的存活时间以及利用共聚焦显微镜检测FTY720与S1P1和S1P3受体的结合情况，评估了FTY720对免疫抑制的作用以及对心脏的毒性。结果表明，FTY720可诱导淋巴细胞减少，降低大鼠心率，并延长小鼠皮肤切片同种异体移植物的存活时间。共聚焦显微镜检测结果显示，FTY720可与CHO-S1P1和CHO-S1P3细胞表面的S1P1和S1P3结合。FTY720有望在器官移植和自身免疫性疾病中得到广泛应用。
