Related Experiment Video
Updated: Nov 22, 2025
Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
Published on: June 13, 2014
Anticancer evaluation of N-benzoyl-3-allylthiourea as potential antibreast cancer agent through enhances HER-2
Tri Widiandani1, Siswandono1, Edy Meiyanto2,3
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Universitas Airlangga, Surabaya 60155, Indonesia.
Abstract:
Breast cancer with HER-2 overexpression is sensitive to drugs which target the receptor or its kinase activity. Although the anti-HER-2 therapies commonly used have improved patient outcome, resistance usually occurs. In this present study, we investigated a modification of the chemical structure of allylthiourea derivatives in order to enhance the cytotoxicity effect on breast cancer cells with HER-2 overexpression. The aim of this research was to predict the absorption, distribution, metabolism, excretion, and toxicity by in silico study and to explore the effect N-benzoyl-3-allylthiourea (BATU) on MCF-7 cell line with overexpressing of HER-2 using MTT assay and western blot. The result showed that the cytotoxicity effects of BATU on MCF-7/HER-2 cell line (IC50 value 0.64 mM) were higher than on MCF-7 cell lines (IC50 value 1.47 mM). In addition, the cytotoxic effects of BATU on MCF-7 and MCF-7/HER-2 were higher than allylthiourea as a lead compound (IC50 value 5.22 and 3.17 mM). The results also confirmed that the BATU compound has the ability to effectively enhance its cytotoxicity against MCF-7/HER-2 through enhanced HER-2 expression and inhibition of nuclear factor kappa B (NF-kB) activation. Above all, the BATU compound is effective in increasing HER-2 expression and inactivating NF-kB transcription factors, thereby resulting in inhibition of protein expression which works a significant part in cell proliferation. Therefore, the BATU compound has the potential to be developed as a complementary drug in breast cancer therapy with HER-2 positive.
Insights
N-benzoyl-3-allylthiourea (BATU) enhances cytotoxicity in HER-2 positive breast cancer cells by increasing HER-2 expression and inhibiting NF-kB activation. This compound shows potential as a complementary therapy for HER-2 positive breast cancer.
Area of Science:
- Oncology
- Medicinal Chemistry
- Molecular Biology
Background:
- HER-2 overexpressing breast cancer is sensitive to targeted therapies, but resistance is common.
- Existing anti-HER-2 therapies improve outcomes but face limitations due to resistance.
- Allylthiourea derivatives are explored for enhanced anti-cancer effects.
Purpose of the Study:
- To investigate modified allylthiourea derivatives for enhanced cytotoxicity against HER-2 overexpressing breast cancer.
- To predict the pharmacokinetic and toxicity profiles of BATU using in silico methods.
- To evaluate the effect of N-benzoyl-3-allylthiourea (BATU) on MCF-7/HER-2 cells.
Main Methods:
- In silico prediction of absorption, distribution, metabolism, excretion, and toxicity (ADMET).
- In vitro evaluation of BATU cytotoxicity on MCF-7 and MCF-7/HER-2 cell lines using MTT assay.
- Western blot analysis to assess HER-2 expression and NF-kB activation.
Main Results:
- BATU demonstrated significantly higher cytotoxicity against MCF-7/HER-2 cells (IC50 0.64 mM) compared to MCF-7 cells (IC50 1.47 mM).
- BATU's cytotoxic effects were superior to the lead compound, allylthiourea, on both cell lines.
- BATU enhanced HER-2 expression and inhibited nuclear factor kappa B (NF-kB) activation in MCF-7/HER-2 cells.
Conclusions:
- N-benzoyl-3-allylthiourea (BATU) exhibits potent cytotoxicity against HER-2 overexpressing breast cancer cells.
- BATU's mechanism involves enhancing HER-2 expression and suppressing NF-kB signaling pathways.
- BATU holds promise as a potential complementary therapeutic agent for HER-2 positive breast cancer.
