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Therapeutic Nanoparticles and Their Targeted Delivery Applications
Open AccessArticle

Antitumor Effects of N-Butylidenephthalide Encapsulated in Lipopolyplexs in Colorectal Cancer Cells

1
Institute of Medicine, Chung Shan Medical University, Taichung 40201, Taiwan
2
Department of Medical Laboratory and Biotechnology, Chung Shan Medical University, Taichung 40201, Taiwan
3
Agricultural Biotechnology Research Center, Academia Sinica, Taipei 11529, Taiwan
4
Department of Biological Science and Technology, National Chiao Tung University, Hsinchu 30068, Taiwan
5
Institute of Molecular Medicine and Bioengineering, National Chiao Tung University, Hsinchu 30068, Taiwan
6
Division of Gastroenterology, Department of Internal Medicine, Kaohsiung Armed Forces General Hospital, Kaohsiung 80284, Taiwan
7
Clinical Laboratory, Chung Shan Medical University Hospital, Taichung 40201, Taiwan
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Zacharias Suntres
Molecules 2020, 25(10), 2394; https://doi.org/10.3390/molecules25102394
Received: 1 May 2020 / Revised: 19 May 2020 / Accepted: 19 May 2020 / Published: 21 May 2020
(This article belongs to the Special Issue Nanotechnology-Drug Delivery Systems)
Colorectal cancer (CRC) is the third most common type of cancer and the second most common cause of cancer-related death in the world. N-Butylidenephthalide (BP), a natural compound, inhibits several cancers, such as hepatoma, brain tumor and colon cancer. However, due to the unstable structure, the activity of BP is quickly lost after dissolution in an aqueous solution. A polycationic liposomal polyethylenimine and polyethylene glycol complex (LPPC), a new drug carrier, encapsulates both hydrophobic and hydrophilic compounds, maintains the activity of the compound, and increases uptake of cancer cells. The purpose of this study is to investigate the antitumor effects and protection of BP encapsulated in LPPC in CRC cells. The LPPC encapsulation protected BP activity, increased the cytotoxicity of BP and enhanced cell uptake through clathrin-mediated endocytosis. Moreover, the BP/LPPC-regulated the expression of the p21 protein and cell cycle-related proteins (CDK4, Cyclin B1 and Cyclin D1), resulting in an increase in the population of cells in the G0/G1 and subG1 phases. BP/LPPC induced cell apoptosis by activating the extrinsic (Fas, Fas-L and Caspase-8) and intrinsic (Bax and Caspase-9) apoptosis pathways. Additionally, BP/LPPC combined with 5-FU synergistically inhibited the growth of HT-29 cells. In conclusion, LPPC enhanced the antitumor activity and cellular uptake of BP, and the BP/LPPC complex induced cell cycle arrest and apoptosis, thereby causing death. These findings suggest the putative use of BP/LPPC as an adjuvant cytotoxic agent for colorectal cancer. View Full-Text
Keywords: N-butylidenephthalide; LPPC nanoparticle; colorectal cancer; antitumor; cytotoxicity N-butylidenephthalide; LPPC nanoparticle; colorectal cancer; antitumor; cytotoxicity
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MDPI and ACS Style

Chang, K.-F.; Chang, J.T.; Huang, X.-F.; Lin, Y.-L.; Liao, K.-W.; Huang, C.-W.; Tsai, N.-M. Antitumor Effects of N-Butylidenephthalide Encapsulated in Lipopolyplexs in Colorectal Cancer Cells. Molecules 2020, 25, 2394.

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