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LyP-1肽的^(131)碘标记及其生物分布研究
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作者 陈月华 于明明 郑瑞强 《医学理论与实践》 2014年第1期1-3,8,共4页
目的:探讨Na131I标记LyP-1肽的可能性以及Na131I标记的LyP-1肽在乳腺癌裸鼠体内的生物分布。方法:包含LyP-1序列的十环肽(YCGNKRTRGC)通过固相合成法合成。在两个半胱氨酸之间形成二硫键以维持肽的环形结构。LyP-1肽通过氯胺-T法进行Na1... 目的:探讨Na131I标记LyP-1肽的可能性以及Na131I标记的LyP-1肽在乳腺癌裸鼠体内的生物分布。方法:包含LyP-1序列的十环肽(YCGNKRTRGC)通过固相合成法合成。在两个半胱氨酸之间形成二硫键以维持肽的环形结构。LyP-1肽通过氯胺-T法进行Na131I标记。通过尾静脉途径将Na131I标记LyP-1肽以及对照肽注射于荷MDA-MB-435乳腺癌裸鼠体内并测量其生物分布情况。结果:LyP-1肽的Na131I标记率可达80%±5%(n=5),放射化学纯度约96%。在37℃新鲜人血清中Na131I标记LyP-1肽24h其放射化学纯度仍然达92%。在生物分布研究中,Na131I标记LyP-1肽在肿瘤中的聚集水平明显高于其他组织。结论:通过氯胺-T法可以成功的将131I标记于LyP-1肽。131I标记的LyP-1肽在37℃新鲜人血清中24h仍然保持稳定,并可被肿瘤组织高度摄取。 展开更多
关键词 LyP_1肽MDA-MB-435乳腺癌生物分布
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LyP-1修饰的肿瘤靶向脂质体制备及抗肿瘤活性评价 被引量:2
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作者 吴美霖 王飞 +1 位作者 黄园 陆伟跃 《中国医药工业杂志》 CAS CSCD 北大核心 2013年第7期694-701,740,共9页
利用固相合成法合成了LyP-1,一种对肿瘤细胞具有靶向能力的环状九肽,及其荧光素标记物(LyP-1-FAM)。利用巯基和马来酰亚胺的专属性反应制备了功能化脂质材料LyP-1-PEG 3400-DSPE。用成膜水化法制备了LyP-1修饰的多柔比星(1)、荧光素(FAM... 利用固相合成法合成了LyP-1,一种对肿瘤细胞具有靶向能力的环状九肽,及其荧光素标记物(LyP-1-FAM)。利用巯基和马来酰亚胺的专属性反应制备了功能化脂质材料LyP-1-PEG 3400-DSPE。用成膜水化法制备了LyP-1修饰的多柔比星(1)、荧光素(FAM)和近红外染料(DiR)脂质体,并评价其对SCI 375黑素瘤细胞的体内外靶向性、细胞毒性和体内抑瘤效果。体外试验表明,SCI 375细胞对LyP-1-FAM或LyP-1修饰的FAM脂质体的摄取显著高于5-FAM或普通FAM脂质体。LyP-1修饰及未修饰的DiR脂质体分别尾静脉注射给予荷瘤裸鼠后,可见LyP-1修饰组肿瘤组织的荧光强度较高,提示DiR脂质体经LyP-1修饰后体内靶向性提高。LyP-1修饰及未修饰的1脂质体在体外对SCI 375细胞的IC50分别为3.4×10-6和8.0×10-6mol/L;修饰组在荷瘤裸鼠体内的抑瘤效果也显著高于未修饰组(P<0.05)。 展开更多
关键词 lyp-1 脂质体 多柔比星 肿瘤靶向 肿瘤治疗
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LyP-1 peptide-functionalized gold nanoprisms for SERRS imaging and tumor growth suppressing by PTT induced-hyperthermia 被引量:3
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作者 Xi Huang Yanlong Yin +2 位作者 Min Wu Wang Zan Qian Yang 《Chinese Chemical Letters》 SCIE CAS CSCD 2019年第6期1335-1340,共6页
Gold-based nanomaterials with plasmonic properties exhibit various potentials for biomedical applications. In this work, gold nanoprisms (GNPs) was synthesized and then modified with LyP-1, a tumor-homing peptide, to ... Gold-based nanomaterials with plasmonic properties exhibit various potentials for biomedical applications. In this work, gold nanoprisms (GNPs) was synthesized and then modified with LyP-1, a tumor-homing peptide, to improve the affinity of the GNPs to tumor cells, thus, to improve the efficacy of tumor-targeted photothermal therapy. The introduction of NIR dye IR780 not only enabled the GNPs-based nanosystem with the surface-enhanced resonant Raman scattering (SERRS) property, but also enhanced the plasmonic photothermal property which delivering therapeutic heating by 660 nm laser irradiation. The obtained GNPs/IR780-LyP-1 presented significantly increased of photothermal conversion in vitro and in vivo, which resulted in enhanced tumor-targeting photothermal therapeutic efficacy after laser irradiation. Hence, the GNPs/IR780-LyP-1 prepared in this study can be served as a Raman-encoded molecular imaging candidate and photothermal therapy agents for future cancer treatment. 展开更多
关键词 GOLD NANOPRISMS SERRS IMAGING lyp-1 PEPTIDE Tumor targeting Photothermal therapy
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Radiolabeling LyP-1 peptide and preliminary biodistribution evaluation in mice bearing MDA-MB-435 xenografts
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作者 YU Ming-ming WANG Rong-fu +2 位作者 CHEN Yue-hua ZHOU Hai-zhong DENG Xiao-hu 《Chinese Medical Journal》 SCIE CAS CSCD 2013年第3期471-475,共5页
Background Recent studies have shown the LyP-1 peptide can home to either tumor lymphatics or the tumor cells and be internalized by targeted cells. This study aimed to investigate the possibility of using Na1311 labe... Background Recent studies have shown the LyP-1 peptide can home to either tumor lymphatics or the tumor cells and be internalized by targeted cells. This study aimed to investigate the possibility of using Na1311 labeled LyP-1 peptide as an imaging agent or a therapeutic radiopharmaceutical in breast carcinoma and its metastasis. Methods The 10-mer cyclic peptide contained the LyP-1 sequence (YCGNKRTRGC) was synthesized by the solid phase method. Disulfide bonds between the cysteines maintain the cyclic structure. The LyP-1 peptide was labeled with Na1311 using the chloramine-T method. The [1311] LyP-1 peptide and a [1311] control peptide were injected via tail vein into nude mice bearing MDA-MB-435 tumor xenografts. Biodistribution and imaging results in vivo were obtained. Results The labeling efficiencies of LyP-1 peptide reached 80%+5% (n=5). The radiochemical purity was about 96%. The radiochemical purity of the labeled compound remains 92% at 24 hours in human serum at 37~C. In the biodistribution studies, the [1311] LyP-1 peptide accumulated in the tumor to a higher level than in other organs. The [1311] LyP-1 peptide can successfully image the tumor in nude mice bearing MDA-MB-435 tumor xenografts. Conclusions The LyP-1 peptide could be effectively labeled with Na1311 and the labeled compound is stable in human serum at 37℃ for 24 hours. The high specificity of [1311] LyP-1 peptide suggests it may be a promising new radiotracer for identifying tumors. 展开更多
关键词 lyp-1 peptide MDA-MB-435 xenografts BIODISTRIBUTION imaging
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细胞靶向肽在多肽偶联药物中的研究进展
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作者 任文杰 周昊 +3 位作者 刘梦瑶 李帅 史潇瑀 刘文涛 《精细化工中间体》 CAS 2023年第2期1-7,39,共8页
靶向治疗利于提高治疗效率,减少不良反应,克服耐药性,特别在癌症治疗领域被广泛运用。多肽偶联药物(PDC)由归巢肽、连接臂和具有药理作用的有效载荷构成。其中归巢肽包括细胞穿透肽(CPP)及细胞靶向肽(CTP),在整个分子中作用重要,决定了... 靶向治疗利于提高治疗效率,减少不良反应,克服耐药性,特别在癌症治疗领域被广泛运用。多肽偶联药物(PDC)由归巢肽、连接臂和具有药理作用的有效载荷构成。其中归巢肽包括细胞穿透肽(CPP)及细胞靶向肽(CTP),在整个分子中作用重要,决定了分子穿透生物膜并靶向特定靶标的能力。介绍了PDC中CTP的种类、递送药物的应用等,为CTP及其用于新型PDC研发提供指导,推进新型PDC的研发进程。 展开更多
关键词 多肽偶联药物 细胞靶向肽 RGD肽 NGR肽 促黄体激素释放激素 lyp-1
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