Elumalai Yashwanth, Nachammai Kathiresan, Chandrasekaran Kirubhanand, Kulanthaivel Langeswaran, Stephen Sharon Benita, Shil Kanu, Anandan Ram Kumar, Bima Abdulhadi Ibrahim, Khan Zeenath, Burzangi Abdulhadi S, Shaik Noor A, Al-Rayes Nuha, Subbaraj Gowtham Kumar
Faculty of Allied Health Science, Chettinad Hospital and Research Institute, Chettinad Academy of Research and Education, Kelambakkam, Tamil Nadu, India.
Department of Biotechnology, Alagappa University, Karaikudi, Tamil Nadu, India.
PLoS One. 2025 Jul 18;20(7):e0322564. doi: 10.1371/journal.pone.0322564. eCollection 2025.
The study investigated the potential of nano-formulated orientin (NF-O) in the anti-angiogenic cancer therapy. Orientin is a flavonoid that has a promising effect against anti-inflammatory, anti-oxidant, and anti-arrhythmia properties. Nano-formulation aimed to overcome this limitation and also served to enhance its therapeutic efficacy. In silico docking studies, the favorable binding of orientin was identified with the key oncogenic targets (EGFR, ALK, KRAS, NTRK). After nano-formulation, UV spectroscopy confirmed the integrity of orientin with no shift in the λmax (347 nm). Dynamic light scattering showed a significant reduction in the improved particle size (PDI decreased from 0.863 to 0.173) by nano-formulation from 559 nm to 220 nm. Fourier Transform infrared spectroscopy analysis confirmed that the nano-formulation process did not alter the chemical structure of orientin. In-vitro studies using MCF-7 breast cancer cells showed that NF-O inhibited cell growth and reduced viability in a dose-dependent manner. At 10 µM, NF-O significantly inhibited the cell growth and migration compared to the control and native orientin in wound healing assays (p < 0.01). In ova, using the chick chorioallantoic membrane (CAM) assay, NF-O (10 µg/ml) significantly inhibited angiogenesis by reducing blood vessel density, branching, length, and network formation compared to controls and native orientin. These findings suggest that NF-O holds significant promise as a novel anti-angiogenic agent for the cancer treatment.
该研究调查了纳米制剂异荭草素（NF-O）在抗血管生成癌症治疗中的潜力。异荭草素是一种黄酮类化合物，具有抗炎、抗氧化和抗心律失常的良好作用。纳米制剂旨在克服这一局限性，并提高其治疗效果。在计算机对接研究中，确定异荭草素与关键致癌靶点（表皮生长因子受体、间变性淋巴瘤激酶、 Kirsten大鼠肉瘤病毒癌基因、神经营养酪氨酸激酶受体）具有良好的结合。纳米制剂后，紫外光谱证实异荭草素的完整性，最大吸收波长（λmax）无位移（347nm）。动态光散射显示，纳米制剂使粒径显著减小（多分散指数从0.863降至0.173），从559nm降至220nm。傅里叶变换红外光谱分析证实，纳米制剂过程未改变异荭草素的化学结构。使用MCF-7乳腺癌细胞的体外研究表明，NF-O以剂量依赖性方式抑制细胞生长并降低活力。在10µM时，与对照组和天然异荭草素相比，NF-O在伤口愈合试验中显著抑制细胞生长和迁移（p＜0.01）。在鸡胚中，使用鸡胚绒毛尿囊膜（CAM）试验，与对照组和天然异荭草素相比，NF-O（10µg/ml）通过降低血管密度、分支、长度和网络形成，显著抑制血管生成。这些发现表明，NF-O作为一种新型抗血管生成剂在癌症治疗中具有巨大潜力。
