Jiramitmongkon Kanpitcha, Rotkrua Pichayanoot, Khanchaitit Paisan, Arunpanichlert Jiraporn, Soontornworajit Boonchoy
Faculty of Science and Technology, Department of Chemistry, Thammasat University, Pathumthani, Thailand.
National Nanotechnology Center, National Science and Technology Development Agency, Thailand Science Park, Pathumthani, Thailand.
PLoS One. 2025 Feb 13;20(2):e0317559. doi: 10.1371/journal.pone.0317559. eCollection 2025.
Colorectal cancer (CRC) poses a global health challenge, with current treatments often harming both cancerous and normal cells. To improve efficacy, a multifunctional drug delivery platform has been developed, integrating bioactive materials, anticancer agents, and targeted recognition ligands into a single molecule. This study aimed to create a molecular hybrid (MH) containing doxorubicin, AS1411 aptamer, and T9/U4 ASO to regulate SW480 cell proliferation. The AS1411 aptamer targets nucleolin, overexpressed on cancer cell membranes, while T9/U4 ASO inhibits human telomerase RNA activity, further hindering cancer cell proliferation. AS-T9/U4_MH was synthesized via oligonucleotide hybridization, followed by doxorubicin loading and evaluation of its impact on cell proliferation. Binding capability of this MH was verified using fluorescence microscopy and flow cytometry, demonstrating specific recognition of SW480 cells due to nucleolin availability on the cell surface. These findings were corroborated by both microscopy and flow cytometry. AS-T9/U4_MH exhibited anti-proliferative effects, with the doxorubicin-loaded system demonstrating encapsulation and reduced toxicity. Moreover, the presence of Dox within AS-T9/U4_MH led to a notable reduction in hTERT and vimentin expression in SW480 cells. Additionally, examination of apoptotic pathways unveiled a marked decrease in Bcl-2 expression and a simultaneous increase in Bax expression in SW480 cells treated with Dox-loaded AS-T9/U4_MH, indicating its impact on promoting apoptosis. This molecular hybrid shows promise as a platform for integrating chemotherapeutic drugs with bioactive materials for cancer therapy.
结直肠癌(CRC)是一项全球性的健康挑战,目前的治疗方法常常对癌细胞和正常细胞都造成损害。为了提高疗效,已开发出一种多功能药物递送平台,将生物活性材料、抗癌剂和靶向识别配体整合到单个分子中。本研究旨在创建一种包含阿霉素、AS1411适配体和T9/U4反义寡核苷酸(ASO)的分子杂交体(MH),以调节SW480细胞的增殖。AS1411适配体靶向癌细胞膜上过度表达的核仁素,而T9/U4 ASO抑制人端粒酶RNA活性,进一步阻碍癌细胞增殖。通过寡核苷酸杂交合成AS-T9/U4_MH,随后加载阿霉素并评估其对细胞增殖的影响。使用荧光显微镜和流式细胞术验证了该MH的结合能力,证明由于细胞表面存在核仁素,其对SW480细胞具有特异性识别。显微镜和流式细胞术均证实了这些发现。AS-T9/U4_MH表现出抗增殖作用,加载阿霉素的系统显示出封装效果并降低了毒性。此外,AS-T9/U4_MH中阿霉素的存在导致SW480细胞中hTERT和波形蛋白的表达显著降低。此外,对凋亡途径的检测发现,在用加载阿霉素的AS-T9/U4_MH处理的SW480细胞中,Bcl-2表达显著降低,同时Bax表达增加,表明其对促进凋亡的影响。这种分子杂交体有望成为将化疗药物与生物活性材料整合用于癌症治疗的平台。
Asian Pac J Cancer Prev. 2021-7-1
Expert Opin Drug Deliv. 2018-10-5
Front Mol Biosci. 2023-9-21
Biomater Res. 2022-9-30
Front Bioeng Biotechnol. 2022-2-16
J Nanobiotechnology. 2022-1-31
Cancers (Basel). 2021-10-5
Asian Pac J Cancer Prev. 2021-7-1