Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar, MP, 470003, India.
Drug Deliv Transl Res. 2012 Aug;2(4):265-71. doi: 10.1007/s13346-012-0082-2.
Goserelin acetate (Gos) is a synthetic analogue of luteinizing hormone-releasing hormone (LHRH) used in treatment of prostate cancer. The objective of this study is to investigate the in vitro cytotoxic effect of Goserelin loaded nanoparticles on both androgen dependent and androgen independent cell lines. Goserelin causes cell death of prostate cancer cell lines by inducing apoptosis. Treatment of Goserelin loaded nanoparticles inhibited the proliferation of LNCaP and DU145 in the dose-dependent manner, however did not affect the cell proliferation in PC-3 cell lines. Blank nanoparticles exhibited negligible cytotoxicity on cell lines. In addition, immunocytochemical studies indicated that Gos induced apoptosis in prostate cancer cells. The presence and characteristics of LHRH receptors and their messenger ribonucleic acid (mRNA) expression in human prostate cancer cell line LNCaP were investigated by polymerase chain reaction. Changes in nuclear morphology and DNA fragmentation associated with Gos induced apoptosis were clearly seen in both LNCaP and DU145 cell lines by DNA studies. The PCR product of the expected size of 319 bp for human LHRH receptors was obtained in cell line sample. Goserelin loaded nanoparticles are the potential tool for site specific delivery for prostate cancer treatment.
醋酸戈舍瑞林(Gos)是一种促黄体激素释放激素(LHRH)的合成类似物,用于治疗前列腺癌。本研究旨在研究载戈舍瑞林纳米粒对雄激素依赖性和非依赖性细胞系的体外细胞毒性作用。戈舍瑞林通过诱导细胞凋亡导致前列腺癌细胞系死亡。载戈舍瑞林纳米粒处理以剂量依赖性方式抑制 LNCaP 和 DU145 的增殖,但不影响 PC-3 细胞系的细胞增殖。空白纳米粒对细胞系表现出轻微的细胞毒性。此外,免疫细胞化学研究表明 Gos 诱导前列腺癌细胞凋亡。通过聚合酶链反应研究人前列腺癌细胞系 LNCaP 中 LHRH 受体的存在及其信使核糖核酸(mRNA)表达的特征。通过 DNA 研究,在 LNCaP 和 DU145 细胞系中均清楚地观察到与 Gos 诱导的凋亡相关的核形态变化和 DNA 片段化。在细胞系样本中获得了预期大小为 319bp 的人 LHRH 受体的 PCR 产物。载戈舍瑞林纳米粒是用于前列腺癌治疗的局部递药的潜在工具。