Biological characterization of a novel and potent gonadotropin releasing hormone （GnRH） antagonist LXT-101

• 作者: Xiao-liCHI Wen-xiaZHOU Jun-pingCHENG Yong-xiangZHANG Ke-liangLIU
• 来源期刊: 中国药理通讯
• 学科: 医学
• 关键词: 生物学作用 促性腺激素释放激素 GNRH LXT-101 皮下注射
• 年，卷（期）: zgyltx,（2）
• 页码范围: 16
• 页数: 1页
• 分类号: R977.1

摘要

AIM The biological characterization of LXT-101 was investigated in vivo using intact male rats and nude mice bearing xenografts of LNCaP prostate cancer. The effect of LXT-101 on the proliferation of androgen -sensitive prostate cancer cell LNCaP and androgen-insensitive DU145 and PC-3M in vitro was also determined. METHODS Rats were injected subcutaneously with LXT-101 while control animals received only vehicle (5% mannitol). Blood samples were collected at different time after adminis-tration of LXT-101. The androgen-dependent LNCaP prostate cancer cells were grown, mixed with Matrigel and injected subcutaneously into nude mice. Experimental group received LXT-101 injectionfor up to 4 weeks. At the end point, blood samples were drawn and the excised tumors and sex organswere weighted. The serum testosterone was determined by specific immunochemiluminescence assay using kits produced by Beckman-Counter Co. The mRNA expressions of the genes of hormone receptor related to the gonadal axis were investigated by real-time RT-PCR technique. Cell viability was determined by MTT method.