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Published on: June 13, 2014
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.
Abstract:
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.
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.

