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比较曲普瑞林与一种新型促性腺激素释放激素类似物的抗癌活性。

The anticancer activity compared between triptorelin and a new gonadotropin releasing hormone analogue.

作者信息

Saleh-Abady Mohammad Mirzaei, Alizadeh Abdolali, Shamsipour Fereshteh, Naderi-Manesh Hossein

机构信息

Department of Biophysics, School of Basic Science, Tarbiat Modares University, Tehran, Iran.

出版信息

Avicenna J Med Biotechnol. 2009 Jul;1(2):105-10.

PMID:23407883
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3558131/
Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/49916e961e9f/AJMB-1-105-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/5495a394ec57/AJMB-1-105-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/503267094530/AJMB-1-105-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/21628cfe0c59/AJMB-1-105-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/0e7aa3e297d8/AJMB-1-105-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/49916e961e9f/AJMB-1-105-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/5495a394ec57/AJMB-1-105-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/503267094530/AJMB-1-105-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/21628cfe0c59/AJMB-1-105-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/0e7aa3e297d8/AJMB-1-105-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/339d/3558131/49916e961e9f/AJMB-1-105-g005.jpg

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本文引用的文献

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Synthesis of novel Gn-RH analogues using Ugi-4MCR.使用 Ugi-4MCR 合成新型 Gn-RH 类似物。
Bioorg Med Chem Lett. 2009 Feb 1;19(3):887-90. doi: 10.1016/j.bmcl.2008.11.111. Epub 2008 Dec 6.
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Gonadotropin-releasing hormone type II antagonists induce apoptotic cell death in human endometrial and ovarian cancer cells in vitro and in vivo.II型促性腺激素释放激素拮抗剂在体外和体内均可诱导人子宫内膜癌细胞和卵巢癌细胞发生凋亡性细胞死亡。
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促性腺激素释放激素(GnRH)-III类似物的促黄体生成素(LH)和促卵泡生成素(FSH)释放及抗癌作用的构效关系研究
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Gonadotropin-releasing hormone (GnRH) antagonists promote proapoptotic signaling in peripheral reproductive tumor cells by activating a Galphai-coupling state of the type I GnRH receptor.促性腺激素释放激素(GnRH)拮抗剂通过激活I型GnRH受体的Gαi偶联状态,在外周生殖肿瘤细胞中促进促凋亡信号传导。
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