匙叶甘松根茎提取物对胶质母细胞瘤的强抗肿瘤的潜力及其分子药物靶点的硅分析

Title:Strong Anti-tumorous Potential of Nardostachys jatamansi Rhizome Extract on Glioblastoma and In Silico Analysis of its Molecular Drug Targets

Volume: 17 Issue: 1

Author(s): Himanshi Kapoor, Nalini Yadav, Madhu Chopra, Sushil Chandra Mahapatra, Veena Agrawal

Affiliation:

关键词: 胶质母细胞瘤、匙叶甘松，抗增殖效应，替代医学研究，分子对接，药物动力学。

摘要: Background: Glioblastoma has been reckoned as the prime cause of death due to brain tumours, being the most invasive and lethal. Available treatment options, i.e. surgery, radiotherapy, chemotherapy and targeted therapies are not effective in improving prognosis, so an alternate therapy is insistent. Plant based drugs are efficient due to their synergistic action, multi-targeted approach and least side effects.

Methods: The anti-tumorous potential of Nardostachys jatamansi rhizome extract (NJRE) on U87 MG cell line was evaluated through various in vitro and in silico bio-analytical tools.

Results: NJRE had a strong anti-proliferative effect on U87 MG cells, Its IC₅₀ was 33.73±3.5, 30.59±3.4 and 28.39±2.9 μg/mL, respectively after 24, 48 and 72 h. NJRE at 30 μg/mL induced DNA fragmentation, indicating apoptosis, early apoptosis began in the cells at 20 μg/mL, whereas higher doses exhibited late apoptosis as revealed by dual fluorescence staining. NJRE at 60 and 80 μg /mL caused a G₀/G₁ arrest and at 20 and 40 μg/mL showed excessive nucleation and mitotic catastrophe in the cells. Immuno-blotting validated the apoptotic mode of cell death through intrinsic pathway. NJRE was harmless to normal cells. In silico docking of NJRE marker compounds: oroselol, jatamansinol, nardostachysin, jatamansinone and nardosinone have revealed their synergistic and multi-targeted interactions with Vestigial endothelial growth factor receptor 2 (VEGFR2), Cyclin dependent kinase 2 (CDK2), B-cell lymphoma 2 (BCL2) and Epidermal growth factor receptor (EGFR).

Conclusion: A strong dose specific and time dependent anti-tumorous potential of NJRE on U87 MG cells was seen. The extract can be used for the development of safe and multi-targeted therapy to manage glioblastoma, which has not been reported earlier.

Cite this article as:

Himanshi Kapoor, Nalini Yadav, Madhu Chopra, Sushil Chandra Mahapatra, Veena Agrawal , Strong Anti-tumorous Potential of Nardostachys jatamansi Rhizome Extract on Glioblastoma and In Silico Analysis of its Molecular Drug Targets, Current Cancer Drug Targets 2017; 17 (1) . https://dx.doi.org/10.2174/1570163813666161019143740

DOI https://dx.doi.org/10.2174/1570163813666161019143740	Print ISSN 1568-0096
Publisher Name Bentham Science Publisher	Online ISSN 1873-5576