Saleh-Abady Mohammad Mirzaei, Alizadeh Abdolali, Shamsipour Fereshteh, Naderi-Manesh Hossein
Department of Biophysics, School of Basic Science, Tarbiat Modares University, Tehran, Iran.
Avicenna J Med Biotechnol. 2009 Jul;1(2):105-10.
Gonadotropin releasing hormone (GnRH) plays a key role in reproduction. This decapeptide is synthesized and released by hypothalamus and induces the pituitary gonadotrop cells to release pituitary gonadotropin hormones. In some extrapituitary compartments GnRH and its receptor act as part of the autocrine regulatory system of cell proliferation. The anticancer activity of GnRH and its analogues has been observed by many researchers. In this study the anticancer activity of a new analogue of GnRH and triptorelin was investigated by cell proliferation assay. Results indicate that proliferation of human breast and ovarian cancer cell lines are dose-dependently inhibited. The inhibitory efficiency of the new analogue is proved to be higher than the original triptorelin. In addition to its antimitogenic activity, evidence was found for the involvement of the apoptotic mechanism in the action of the new analogue and triptorelin. In conclusion, the new analogue can be considered as a good pharmaceutical candidate.
促性腺激素释放激素(GnRH)在生殖过程中起关键作用。这种十肽由下丘脑合成并释放,可诱导垂体促性腺细胞释放垂体促性腺激素。在一些垂体外区域,GnRH及其受体作为细胞增殖自分泌调节系统的一部分发挥作用。许多研究人员已经观察到GnRH及其类似物的抗癌活性。在本研究中,通过细胞增殖试验研究了一种新的GnRH类似物和曲普瑞林的抗癌活性。结果表明,人乳腺癌和卵巢癌细胞系的增殖受到剂量依赖性抑制。新类似物的抑制效率被证明高于原始的曲普瑞林。除了其抗有丝分裂活性外,还发现新类似物和曲普瑞林的作用涉及凋亡机制。总之,新类似物可被视为一种良好的药物候选物。