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基于20(S)-人参皂苷Rg3的多肽纳米颗粒靶向递送治疗结肠癌。

Targeted delivery of 20(S)-ginsenoside Rg3-based polypeptide nanoparticles to treat colon cancer.

作者信息

Qiu Renna, Qian Feng, Wang Xiaofeng, Li Hongjun, Wang Lizhe

机构信息

China-Japan Union Hospital of Jilin University, No. 126 Xiantai Street, Changchun, 130033, Jilin, China.

The First Hospital of Jilin University, No.71, Xinmin Street, Changchun, 130021, Jilin, China.

出版信息

Biomed Microdevices. 2019 Feb 20;21(1):18. doi: 10.1007/s10544-019-0374-0.

DOI:10.1007/s10544-019-0374-0
PMID:30783757
Abstract

Colorectal cancer (CRC) is a major malignancy characterized by a high metastasis rate. Systematic chemotherapy is important for patients with advanced CRC. However, many limitations (e.g., side effects to normal organs, shorter circulation time, and unsatisfactory tumor inhibition results) of traditional chemotherapy restrict its further application. Thus, it is necessary to find a method to overcome these challenges and improve the efficacy of CRC treatment. In this study, 20(S)-ginsenoside (Rg3) co-loaded poly(ethylene glycol)-block-poly(L-glutamic acid-co-L-phenylalanine) (mPEG-b-P(Glu-co-Phe)) nanoparticles (Rg3-NPs) were prepared. mPEG-b-P(Glu-co-Phe)-based drug delivery systems are pH sensitive that can target cancer cells and circulate for longer in blood. Rg3 could be released rapidly from the nanoparticles within tumor cells. A subcutaneous colon cancer mouse model was developed to evaluate the anticancer efficiency of the Rg3-NPs. The in vivo study indicated that the Rg3-NPs could significantly inhibit tumor proliferation by decreasing the expressions of proliferating cell nuclear antigen, resulting in tumor apoptosis through the increased expressions of caspase-3. Our study demonstrated the marked potential of the Rg3-NPs to treat CRC.

摘要

结直肠癌(CRC)是一种以高转移率为特征的主要恶性肿瘤。系统化疗对晚期CRC患者很重要。然而,传统化疗的许多局限性(如对正常器官的副作用、较短的循环时间以及不理想的肿瘤抑制结果)限制了其进一步应用。因此,有必要找到一种方法来克服这些挑战并提高CRC治疗的疗效。在本研究中,制备了共负载20(S)-人参皂苷(Rg3)的聚(乙二醇)-嵌段-聚(L-谷氨酸-co-L-苯丙氨酸)(mPEG-b-P(Glu-co-Phe))纳米颗粒(Rg3-NPs)。基于mPEG-b-P(Glu-co-Phe)的药物递送系统对pH敏感,能够靶向癌细胞并在血液中循环更长时间。Rg3可以在肿瘤细胞内从纳米颗粒中快速释放。建立了皮下结肠癌小鼠模型以评估Rg3-NPs的抗癌效率。体内研究表明,Rg3-NPs可通过降低增殖细胞核抗原的表达显著抑制肿瘤增殖,并通过增加caspase-3的表达导致肿瘤凋亡。我们的研究证明了Rg3-NPs治疗CRC的显著潜力。

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