适配体C2min介导的可靶向2种前列腺癌基因的递送系统

张晶; 顾永卫; 武鑫

doi:10.3969/j.issn.1006-0111.201906038

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适配体C2min介导的可靶向2种前列腺癌基因的递送系统

张晶, 顾永卫, 武鑫

文章导航 > 药学实践与服务 > 2020 > 38(1): 47-51,66

张晶, 顾永卫, 武鑫. 适配体C2min介导的可靶向2种前列腺癌基因的递送系统[J]. 药学实践与服务, 2020, 38(1): 47-51,66. doi: 10.3969/j.issn.1006-0111.201906038

引用本文:

张晶, 顾永卫, 武鑫. 适配体C2min介导的可靶向2种前列腺癌基因的递送系统[J]. 药学实践与服务, 2020, 38(1): 47-51,66. doi: 10.3969/j.issn.1006-0111.201906038

ZHANG Jing, GU Yongwei, WU Xin. The C2min aptamer-modified gene delivery system for targeting ADPC/AIPC prostate cancer[J]. Journal of Pharmaceutical Practice and Service, 2020, 38(1): 47-51,66. doi: 10.3969/j.issn.1006-0111.201906038

Citation:

ZHANG Jing, GU Yongwei, WU Xin. The C2min aptamer-modified gene delivery system for targeting ADPC/AIPC prostate cancer[J]. Journal of Pharmaceutical Practice and Service, 2020, 38(1): 47-51,66. doi: 10.3969/j.issn.1006-0111.201906038

适配体C2min介导的可靶向2种前列腺癌基因的递送系统

doi: 10.3969/j.issn.1006-0111.201906038

1.
内蒙古医科大学附属医院药剂部, 内蒙古呼和浩特 010050
2.
上海维洱实验室, 上海 201712
3.
内蒙古医科大学附属医院药剂部, 内蒙古呼和浩特 010050;上海维洱实验室, 上海 201712

基金项目: 国家自然科学基金（81072100）；上海市青年科技启明星计划资助（18QB1400400）

The C2min aptamer-modified gene delivery system for targeting ADPC/AIPC prostate cancer

1.
Department of Pharmacy, Affiliated Hospital of Inner Mongolia Medical University, Hohhot 010050, China
2.
Shanghai Wei Er Laboratory, shanghai 201712, China
3.
Department of Pharmacy, Affiliated Hospital of Inner Mongolia Medical University, Hohhot 010050, China;Shanghai Wei Er Laboratory, shanghai 201712, China

摘要: 目的通过合成可靶向两种前列腺癌的基因载体PAMAM-PEG-C2min，以提高基因的转染效率和肿瘤靶向性。方法将双功能聚乙二醇的一端与聚酰胺-胺（PAMAM）相连，另一端与适配体（C2min）连接，并利用¹H NMR技术对合成的PAMAM-PEG-C2min基因载体进行结构鉴定。通过两种前列腺癌PC3和LNCaP细胞的体外摄取和基因转染实验（包载siR-M基因），考察纳米复合物的生物学特性。并利用动物活体成像技术考察合成的纳米复合物的体内分布特征。结果核磁共振结果表明，本研究成功合成了PAMAM-PEG-C2min。PC3和LNCaP细胞对PAMAM-PEG-C2min的摄取结果体现出浓度依赖性。且与不经C2min修饰的PAMA-PEGM相比，PAMAM-PEG-C2min递药系统的基因转染效率和肿瘤细胞靶向性明显提高。体内靶向性结果表明，PAMAM-PEG-C2min可实现同时靶向2种前列腺癌组织的作用。结论本研究合成的PAMAM-PEG-C2min递送载体具有良好的肿瘤靶向性，为前列腺癌的综合治疗和靶向治疗提供了新的技术平台。
- 适配体 /
- 靶向 /
- 雄激素依赖型前列腺癌 /
- 雄激素非依赖型前列腺癌 /
- 基因载体
Abstract: Objective To synthesize a novel prostate cancer targeting gene vector PAMAM-PEG-C2min and improve gene transfection efficiency targeting on prostate cancer. Methods The aptamer (C2min) and polyamide-amine (PAMAM) were ligated by polyethylene glycol (PEG). The structure of the synthesized PAMAM-PEG-C2min was identified by NMR. The biological characteristics of the nanoparticles were examined by the uptake experiments and gene transfection experiments (the loaded gene was siR-M) with the prostate cancer cells (PC3 and LNCaP). Besides, the in vivo targeting was investigated using in vivo image system. The in vivo targeting results indicated that PAMAM-PEG-C2min can achieve the simultaneous targeting of two prostate cancer tissues. Results The PAMAM-PEG-C2min synthesis was confirmed by NMR. Cell uptake experiments showed that the cell uptake efficiency of PAMAM-PEG-C2min was concentration dependent. In vitro experiments showed that the PC3 and LNCaP cells transfection efficiency and targeting of PAMAM-PEG modified with C2min were significantly improved compared with the PEG modified PAMAM. Conclusion PAMAM-PEG-C2min is a potential targeted drug delivery vehicle. It provides a new technology platform for comprehensive and specific targeting treatment of prostate cancer.
- adapter /
- targeting drug delivery /
- androgen-dependent prostate cancer /
- androgen-independent prostate cancer /
- gene vector

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适配体C2min介导的可靶向2种前列腺癌基因的递送系统

doi: 10.3969/j.issn.1006-0111.201906038

1. 内蒙古医科大学附属医院药剂部, 内蒙古呼和浩特 010050

2. 上海维洱实验室, 上海 201712

3. 内蒙古医科大学附属医院药剂部, 内蒙古呼和浩特 010050;上海维洱实验室, 上海 201712

基金项目: 国家自然科学基金（81072100）；上海市青年科技启明星计划资助（18QB1400400）

收稿日期: 2019-06-14
修回日期: 2019-07-26

关键词:

适配体 /

靶向 /

雄激素依赖型前列腺癌 /

雄激素非依赖型前列腺癌 /

基因载体

摘要: 目的通过合成可靶向两种前列腺癌的基因载体PAMAM-PEG-C2min，以提高基因的转染效率和肿瘤靶向性。方法将双功能聚乙二醇的一端与聚酰胺-胺（PAMAM）相连，另一端与适配体（C2min）连接，并利用¹H NMR技术对合成的PAMAM-PEG-C2min基因载体进行结构鉴定。通过两种前列腺癌PC3和LNCaP细胞的体外摄取和基因转染实验（包载siR-M基因），考察纳米复合物的生物学特性。并利用动物活体成像技术考察合成的纳米复合物的体内分布特征。结果核磁共振结果表明，本研究成功合成了PAMAM-PEG-C2min。PC3和LNCaP细胞对PAMAM-PEG-C2min的摄取结果体现出浓度依赖性。且与不经C2min修饰的PAMA-PEGM相比，PAMAM-PEG-C2min递药系统的基因转染效率和肿瘤细胞靶向性明显提高。体内靶向性结果表明，PAMAM-PEG-C2min可实现同时靶向2种前列腺癌组织的作用。结论本研究合成的PAMAM-PEG-C2min递送载体具有良好的肿瘤靶向性，为前列腺癌的综合治疗和靶向治疗提供了新的技术平台。

English Abstract

The C2min aptamer-modified gene delivery system for targeting ADPC/AIPC prostate cancer

1. Department of Pharmacy, Affiliated Hospital of Inner Mongolia Medical University, Hohhot 010050, China

2. Shanghai Wei Er Laboratory, shanghai 201712, China

3. Department of Pharmacy, Affiliated Hospital of Inner Mongolia Medical University, Hohhot 010050, China;Shanghai Wei Er Laboratory, shanghai 201712, China

Received Date: 2019-06-14
Rev Recd Date: 2019-07-26

Keywords:

Abstract: Objective To synthesize a novel prostate cancer targeting gene vector PAMAM-PEG-C2min and improve gene transfection efficiency targeting on prostate cancer. Methods The aptamer (C2min) and polyamide-amine (PAMAM) were ligated by polyethylene glycol (PEG). The structure of the synthesized PAMAM-PEG-C2min was identified by NMR. The biological characteristics of the nanoparticles were examined by the uptake experiments and gene transfection experiments (the loaded gene was siR-M) with the prostate cancer cells (PC3 and LNCaP). Besides, the in vivo targeting was investigated using in vivo image system. The in vivo targeting results indicated that PAMAM-PEG-C2min can achieve the simultaneous targeting of two prostate cancer tissues. Results The PAMAM-PEG-C2min synthesis was confirmed by NMR. Cell uptake experiments showed that the cell uptake efficiency of PAMAM-PEG-C2min was concentration dependent. In vitro experiments showed that the PC3 and LNCaP cells transfection efficiency and targeting of PAMAM-PEG modified with C2min were significantly improved compared with the PEG modified PAMAM. Conclusion PAMAM-PEG-C2min is a potential targeted drug delivery vehicle. It provides a new technology platform for comprehensive and specific targeting treatment of prostate cancer.

张晶, 顾永卫, 武鑫. 适配体C2min介导的可靶向2种前列腺癌基因的递送系统[J]. 药学实践与服务, 2020, 38(1): 47-51,66. doi: 10.3969/j.issn.1006-0111.201906038

引用本文:

张晶, 顾永卫, 武鑫. 适配体C2min介导的可靶向2种前列腺癌基因的递送系统[J]. 药学实践与服务, 2020, 38(1): 47-51,66. doi: 10.3969/j.issn.1006-0111.201906038

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适配体C2min介导的可靶向2种前列腺癌基因的递送系统

doi: 10.3969/j.issn.1006-0111.201906038

The C2min aptamer-modified gene delivery system for targeting ADPC/AIPC prostate cancer

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适配体C2min介导的可靶向2种前列腺癌基因的递送系统

doi: 10.3969/j.issn.1006-0111.201906038

1. 内蒙古医科大学附属医院药剂部, 内蒙古 呼和浩特 010050 2. 上海维洱实验室, 上海 201712 3. 内蒙古医科大学附属医院药剂部, 内蒙古 呼和浩特 010050;上海维洱实验室, 上海 201712

English Abstract

The C2min aptamer-modified gene delivery system for targeting ADPC/AIPC prostate cancer

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目录

1. 内蒙古医科大学附属医院药剂部, 内蒙古呼和浩特 010050

2. 上海维洱实验室, 上海 201712

3. 内蒙古医科大学附属医院药剂部, 内蒙古呼和浩特 010050;上海维洱实验室, 上海 201712