Anti-cancer effects of baicalein in non-small cell lung cancer in-vitro and in-vivo

Cathcart, Mary-Clare, Useckaite, Zivile, Drakeford, Clive, Semik, Vikki, Lysaght, Joanne, Gately, Kathy, O’Byrne, Kenneth J., & Pidgeon, Graham P. (2016) Anti-cancer effects of baicalein in non-small cell lung cancer in-vitro and in-vivo. BMC Cancer, 16, Article Number-707.

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  • Baicalein is a widely used Chinese herbal medicine derived from Scutellaria baicalenesis, which has been traditionally used as anti-inflammatory and anti-cancer therapy. In this study we examined the anti-tumour pathways activated following baicalein treatment in non-small cell lung cancer (NSCLC), both in-vitro and in-vivo.


  • The effect of baicalein treatment on H-460 cells in-vitro was assessed using both BrdU assay (cell proliferation) and High Content Screening (multi-parameter apoptosis assay). A xenograft nude mouse model was subsequently established using these cells and the effect of baicalein on tumour growth and survival assessed in-vivo. Tumours were harvested from these mice and histological tissue analysis carried out. VEGF, 12-lipoxygenase and microvessel density (CD-31) were assessed by immunohistochemistry (IHC), while H and E staining was carried out to assess mitotic index. Gene expression profiling was carried out on corresponding RNA samples using Human Cancer Pathway Finder Arrays and qRT-PCR, with further gene expression analysis carried out using qRT-PCR.


  • Baicalein significantly decreased lung cancer proliferation in H-460 cells in a dose dependent manner. At the functional level, a dose-dependent induction in apoptosis associated with decreased cellular f-actin content, an increase in nuclear condensation and an increase in mitochondrial mass potential was observed. Orthotopic treatment of experimental H-460 tumours in athymic nude mice with baicalein significantly (p < 0.05) reduced tumour growth and prolonged survival. Histological analysis of resulting tumour xenografts demonstrated reduced expression of both 12-lipoxygenase and VEGF proteins in baicalein-treated tumours, relative to untreated. A significant (p < 0.01) reduction in both mitotic index and micro-vessel density was observed following baicalein treatment. Gene expression profiling revealed a reduction (p < 0.01) in both VEGF and FGFR-2 following baicalein treatment, with a corresponding increase (p < 0.001) in RB-1.


  • This study is the first to demonstrate efficacy of baicalein both in-vitro and in-vivo in NSCLC. These effects may be mediated in part through a reduction in both cell cycle progression and angiogenesis. At the molecular level, alterations in expression of VEGF, FGFR-2, and RB-1 have been implicated, suggesting a molecular mechanism underlying this in-vivo effect.

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ID Code: 98793
Item Type: Journal Article
Refereed: Yes
Keywords: Scutellaria baicalenesis, Baicalein, Traditional Chinese herbal medicine, Anti-inflammatory, non-small-cell lung cancer, cancer therapeutics, treatment, anti-cancer therapy, anti-tumour pathways, apoptosis, angiogenesis, in vivo, in vitro, survival
DOI: 10.1186/s12885-016-2740-0
ISSN: 1471-2407
Subjects: Australian and New Zealand Standard Research Classification > MEDICAL AND HEALTH SCIENCES (110000) > COMPLEMENTARY AND ALTERNATIVE MEDICINE (110400) > Naturopathy (110402)
Australian and New Zealand Standard Research Classification > MEDICAL AND HEALTH SCIENCES (110000) > COMPLEMENTARY AND ALTERNATIVE MEDICINE (110400) > Traditional Chinese Medicine and Treatments (110404)
Australian and New Zealand Standard Research Classification > MEDICAL AND HEALTH SCIENCES (110000) > ONCOLOGY AND CARCINOGENESIS (111200) > Cancer Therapy (excl. Chemotherapy and Radiation Therapy) (111204)
Divisions: Current > Schools > School of Biomedical Sciences
Current > QUT Faculties and Divisions > Faculty of Health
Current > Institutes > Institute of Health and Biomedical Innovation
Copyright Owner: Copyright 2016 The Author(s)
Copyright Statement: This article is distributed under the terms of the Creative Commons Attribution 4.0 International License (, which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver ( applies to the data made available in this article, unless otherwise stated.
Deposited On: 12 Sep 2016 22:27
Last Modified: 13 Sep 2016 23:28

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