实验动物科学 ›› 2021, Vol. 38 ›› Issue (1): 1-.

• 研究报告 •    下一篇

七甲川菁染料与醋酸阿比特龙的化合物应用于小鼠前列腺癌的活体成像和治疗研究

摘要:目的 研究七甲川菁( heptamethine carbocyanine)近红外( near-infrared fluorescence, NIRF)荧光染料与醋酸阿比特龙( abiraterone acetate,ABi)合成化合物( DZ1-ABi 和 783-ABi) 对前列腺癌的治疗及其在活体成像中的应用。方法 化学合成两种化合物 DZ1-ABi 783-ABi;将人前列腺癌细胞 PC-3、LNcaP 和 C4-2 培养至对数生长期后分别加入 DZ1-ABi、783-ABi 和 ABi,观 察 三 种 化 合 物 对 肿 瘤 细 胞 增 殖 的 抑 制 作 用;将 人 源 性 前 列 腺 癌 PDX 肿 瘤(B45354)皮下移植裸鼠随机分组给予 DZ1-ABi、783-ABi 和 ABi 治疗并监测肿瘤生长状况。 荷瘤鼠分别注射 DZ1- ABi 783-ABi(0. 1 nmol / 只),活体成像监测两种化合物在小鼠体内的代谢情况和肿瘤靶向性。 结果相较于ABi 和 783-ABi,DZ1-ABi 能更好地抑制人前列腺癌细胞 PC-3、LNcaP 和 C4-2 的增殖;在荷瘤鼠药敏实验发现,DZ1-ABi 表现出较 783-ABi ABi 更好的治疗效果;活体成像显示,无论是肿瘤的靶向性还是荧光信号强度,DZ1-ABi 均表现出比 783-ABi 更为明显的优势。 结论DZ1-ABi 相较于 783-ABi 和临床药物 ABi 在对肿瘤的抑制和活体成像中均表现出比较明显的优势,有望成为新型的肿瘤显像和治疗双重靶向药物。
  

  1. 空军军医大学实验动物中心,西安 710032
  • 出版日期:2021-02-28 发布日期:2021-04-14

The Key Points of Genotype Identification in Genetically Modified Mice Model

Abstract:Recently, with the development of biomedical research and gene editing technology, there are more and more animal models have been established. Due to the different production methods, the genotype identification technology is also different, resulting genotype identification disordered phenomenon. This paper is based on the method of the genetically modified mice model, introduced the genotype identification key points of the random transgenic mice, conditional knockin mice, and knockout mice. Through this paper, we want to achieve standardize the genotype identification method and ensure the accuracy of animal experimental materials, so as to
promote the application and development of animal models in basic and applied science and technology fields.
  

  • Online:2021-02-28 Published:2021-04-14

摘要:

摘要:目的 研究七甲川菁( heptamethine carbocyanine)近红外( near-infrared fluorescence, NIRF)荧光染料与醋酸阿比特龙( abiraterone acetate,ABi)合成化合物( DZ1-ABi 和 783-ABi) 对前列腺癌的治疗及其在活体成像中的应用。方法 化学合成两种化合物 DZ1-ABi 783-ABi;将人前列腺癌细胞 PC-3、LNcaP 和 C4-2 培养至对数生长期后分别加入 DZ1-ABi、783-ABi 和 ABi,观 察 三 种 化 合 物 对 肿 瘤 细 胞 增 殖 的 抑 制 作 用;将 人 源 性 前 列 腺 癌 PDX 肿 瘤(B45354)皮下移植裸鼠随机分组给予 DZ1-ABi、783-ABi 和 ABi 治疗并监测肿瘤生长状况。 荷瘤鼠分别注射 DZ1- ABi 783-ABi(0. 1 nmol / 只),活体成像监测两种化合物在小鼠体内的代谢情况和肿瘤靶向性。 结果相较于ABi 和 783-ABi,DZ1-ABi 能更好地抑制人前列腺癌细胞 PC-3、LNcaP 和 C4-2 的增殖;在荷瘤鼠药敏实验发现,DZ1-ABi 表现出较 783-ABi ABi 更好的治疗效果;活体成像显示,无论是肿瘤的靶向性还是荧光信号强度,DZ1-ABi 均表现出比 783-ABi 更为明显的优势。 结论DZ1-ABi 相较于 783-ABi 和临床药物 ABi 在对肿瘤的抑制和活体成像中均表现出比较明显的优势,有望成为新型的肿瘤显像和治疗双重靶向药物。

Abstract:

Abstract: Objective To study the therapeutic effect on prostate cancer and possible application in living imaging of synthetic compounds DZ1-ABi and 783-ABi derived from fluorescent dye heptamethine carbocyanine ( nearinfrared fluorescence, NIRF ) and abiraterone acetate respectively. Method DZ1-ABi and 783-ABi were chemically synthesized; Human prostate cancer cells PC-3, LNcaP and C4-2 were cultured to the logarithmic growth phase, then DZ1-ABi, 783-ABi and ABi were added to observe the inhibitory effects on tumor cell
proliferation; Human-derived prostate cancer PDX tumor ( B45354) was subcutaneously transplanted into nude mice, randomly grouped and treated with DZ1-ABi, 783-ABi and ABi to monitor tumor growth. Tumor-bearing mice were injected with DZ1-ABi and 783-ABi ( 0. 1 nmol / mouse) for monitoring metabolism and tumor-targeting ability of these compounds by in vivo imaging. Result Compared with ABi and 783-ABi, better inhibitory effect of DZ1-ABi was observed on the proliferation of human prostate tumor cells; Moreover, DZ1-ABi exhibited better therapeutic effects on the treatment of tumor-bearing mice; In addition, in vivo imaging disclosed that DZ1-Abi has an obvious advantage over 783-ABi in terms of tumor-targeting ability or fluorescence signal intensity. Conclusion Compared with 783-ABi and the clinical drug ABi, DZ1-ABi has obvious advantages in tumor inhibition and in vivo imaging, which potentiates it as a new dual-targeted drug for tumor imaging and treatment.