Scholarlink

<p>Artemisinin, a bioactive compound from <i>Artemisia annua</i> with potent antioxidant, antimicrobial and anticancer properties, faces limited clinical utility due to poor solubility and low bioavailability. Given the rising prevalence of multidrug-resistant (MDR) <i>Pseudomonas aeruginosa</i> alternative therapeutic strategies are essential. This study synthesized and characterized artemisinin-loaded micelle/liposome nanoparticles (Art/PEG<sub>400</sub>-OA NPs) and evaluated their antibacterial, antibiofilm, and anticancer efficacy. Artemisinin was successfully encapsulated within PEG<sub>400</sub>-OA NPs and characterized via FT-IR, FE-SEM, TEM, TGA, and zeta potential measurements. The nanoparticles exhibited uniform morphology, particle sizes of 40.8&#xa0;nm (TEM) and 149.8&#xa0;nm (FE-SEM), high encapsulation efficiency (92.14%), and strong thermal and colloidal stability. Synergistic and partial synergistic interactions between Art/PEG<sub>400</sub>-OA NPs and ciprofloxacin were observed in MDR bacterial samples, significantly inhibiting biofilm formation. Quantitative RT-PCR analysis revealed the downregulation of efflux pump genes (<i>mexA</i>,<i> mexB</i>,<i> mexX</i>,<i> mexY</i>,<i> oprM</i>) and biofilm-associated genes (<i>algD</i>, <i>pelA</i>) following combination therapy. In AGS gastric cancer cells, Art/PEG<sub>400</sub>-OA NPs induced dose- and time-dependent cytotoxicity (IC₅₀: 67.75, 62.25 and 54.98&#xa0;µg/mL at 24, 48 and 72&#xa0;h), increased apoptosis (31.76% ± 4.2%), and reduced wound-healing migration (56.65% ± 4.26%). Expression analysis demonstrated upregulation of tumor-suppressive miR-34a, and downregulation of its targets (<i>CTNNB1</i>,<i> TGFB1</i>,<i> MMP2</i> and <i>MMP9</i>). Conversely, miR-181a was downregulated, leading to the upregulation of apoptotic target genes (<i>TP53</i>,<i> CASP8</i>,<i> CASP9</i>). Molecular docking supported strong artemisinin binding to key bacterial and oncogenic proteins. Overall, Art/PEG<sub>400</sub>-OA nanoparticles represent a potent dual-action nanotherapeutic platform against antibiotic-resistant infections and gastric cancer.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Dual antimicrobial and anticancer functions of artemisinin-loaded PEG400-oa nanoparticles: synergistic activity with ciprofloxacin and mechanistic insights from molecular docking

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2026年7月7日

查看全文
  • Asma Seyedan,
  • Mahdi Shahriarinour,
  • Somayeh Ataei Jaliseh,
  • Najmeh Ranji,
  • Hossein Zahmatkesh

摘要

Artemisinin, a bioactive compound from Artemisia annua with potent antioxidant, antimicrobial and anticancer properties, faces limited clinical utility due to poor solubility and low bioavailability. Given the rising prevalence of multidrug-resistant (MDR) Pseudomonas aeruginosa alternative therapeutic strategies are essential. This study synthesized and characterized artemisinin-loaded micelle/liposome nanoparticles (Art/PEG400-OA NPs) and evaluated their antibacterial, antibiofilm, and anticancer efficacy. Artemisinin was successfully encapsulated within PEG400-OA NPs and characterized via FT-IR, FE-SEM, TEM, TGA, and zeta potential measurements. The nanoparticles exhibited uniform morphology, particle sizes of 40.8 nm (TEM) and 149.8 nm (FE-SEM), high encapsulation efficiency (92.14%), and strong thermal and colloidal stability. Synergistic and partial synergistic interactions between Art/PEG400-OA NPs and ciprofloxacin were observed in MDR bacterial samples, significantly inhibiting biofilm formation. Quantitative RT-PCR analysis revealed the downregulation of efflux pump genes (mexA, mexB, mexX, mexY, oprM) and biofilm-associated genes (algD, pelA) following combination therapy. In AGS gastric cancer cells, Art/PEG400-OA NPs induced dose- and time-dependent cytotoxicity (IC₅₀: 67.75, 62.25 and 54.98 µg/mL at 24, 48 and 72 h), increased apoptosis (31.76% ± 4.2%), and reduced wound-healing migration (56.65% ± 4.26%). Expression analysis demonstrated upregulation of tumor-suppressive miR-34a, and downregulation of its targets (CTNNB1, TGFB1, MMP2 and MMP9). Conversely, miR-181a was downregulated, leading to the upregulation of apoptotic target genes (TP53, CASP8, CASP9). Molecular docking supported strong artemisinin binding to key bacterial and oncogenic proteins. Overall, Art/PEG400-OA nanoparticles represent a potent dual-action nanotherapeutic platform against antibiotic-resistant infections and gastric cancer.

Graphical Abstract