Unleashing the anti-tumor angiogenic potential of nano-formulated orientin: In Silico, In Vitro, and In Ovo studies

Yashwanth Elumalai1, Kathiresan Nachammai2, Kirubhanand Chandrasekaran3

  • 1Faculty of Allied Health Science, Chettinad Hospital and Research Institute, Chettinad Academy of Research and Education, Kelambakkam, Tamil Nadu, India.

Plos One
|July 18, 2025
PubMed

Insights

Nano-formulated orientin (NF-O) shows promise in cancer therapy by inhibiting angiogenesis. NF-O effectively reduced cancer cell growth and blood vessel formation in preclinical models, suggesting its potential as a novel anti-angiogenic agent.

Area of Science:

  • Biochemistry
  • Nanotechnology
  • Oncology

Background:

  • Orientin, a flavonoid, possesses anti-inflammatory, anti-oxidant, and anti-arrhythmia properties.
  • Nano-formulation of orientin (NF-O) was explored to enhance its therapeutic efficacy and overcome limitations.
  • Key oncogenic targets including EGFR, ALK, KRAS, and NTRK were identified for orientin binding via in silico docking.

Purpose of the Study:

  • To investigate the anti-angiogenic potential of nano-formulated orientin (NF-O) for cancer therapy.
  • To evaluate the efficacy of NF-O in inhibiting cancer cell growth, migration, and angiogenesis.

Main Methods:

  • In silico docking studies to identify orientin's binding with oncogenic targets.
  • Characterization of NF-O using UV spectroscopy, dynamic light scattering, and Fourier Transform infrared spectroscopy.
  • In vitro studies on MCF-7 breast cancer cells and in ovo chick chorioallantoic membrane (CAM) assay to assess anti-angiogenic and anti-cancer effects.

Main Results:

  • Nano-formulation significantly reduced particle size (559 nm to 220 nm) and improved polydispersity index (0.863 to 0.173) without altering orientin's chemical structure.
  • NF-O demonstrated dose-dependent inhibition of MCF-7 breast cancer cell growth and viability.
  • NF-O significantly inhibited cell migration, angiogenesis (blood vessel density, branching, length, and network formation) in wound healing and CAM assays, outperforming native orientin.

Conclusions:

  • Nano-formulated orientin (NF-O) is a stable and effective formulation with enhanced therapeutic potential.
  • NF-O exhibits significant anti-angiogenic and anti-cancer properties, inhibiting tumor growth and metastasis.
  • NF-O represents a promising novel therapeutic agent for anti-angiogenic cancer treatment.