Biological characterization of a novel and potent gonadotropin releasing hormone (GnRH) antagonist LXT-101 |
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作者姓名: | Xiao-liCHI Wen-xiaZHOU Jun-pingCHENG Yong-xiangZHANG Ke-liangLIU |
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作者单位: | BeijinglnsUtuteofPharmacologyandToxicology,Beijing100850 |
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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.
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关 键 词: | 生物学作用 促性腺激素释放激素 GnRH LXT-101 皮下注射 |
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