R Rajagopalan1
,
Sanjay K Jain2,
Piyush Trivedi1
1Department of Pharmaceutics, School of Pharmaceutical Sciences, Rajiv Gandhi Technological University, Bhopal (M.P.);
2Department of Pharmaceutics, Dr. Harisingh Gour University, Sagar (M.P.), India.
For correspondence:- R Rajagopalan
Email: rajagopalan10@gmail.com Tel:+919179626663
Accepted: 20 February 2019
Published: 31 March 2019
Citation:
Rajagopalan R, Jain SK, Trivedi P.
Synergistic anti-cancer activity of combined 5-fuorouracil and gallic acid-stearylamine conjugate in A431 human squamous carcinoma cell line. Trop J Pharm Res 2019; 18(3):471-477
doi:
10.4314/tjpr.v18i3.4
© 2019 The authors.
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Abstract
Purpose: To evaluate the individual and synergistic anti-cancer effects of 5-fuorouracil (5-FU) and synthesized gallic acid-stearylamine (GA-SA) conjugate in A431 human squamous cancer cell line.
Methods: Characterisation of the synthesised conjugate was performed using Fourier transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR), and mass spectrometry (MS). The synergistic effect of the combination therapy (5-FU/GA-SA) was assessed by determining their inhibitory concentration (IC30) whereby A431 cells were treated with 5-FU:GA–SA conjugate at various ratios ranging from 5:1 to 1:5.
Results: The cytotoxicity of 5-FU was 29 %, while that of the combination of 5-FU with GA–SA conjugate was as high as 60 %. Thus, this combination showed significant synergistic enhancement in cytotoxicity (p < 0.05). The results obtained also revealed that the IC30 values of 5-FU and the GA–SA conjugate were 1 and 10 µg/mL, respectively. The IC30 values of the combination ratios indicated that the dosages used in the study were safe in HaCaT normal cell line.
Conclusion: These results indicate that 5-FU/GA–SA conjugate at a ratio of 1:1 is effective against A431 cell line (cancer cells)) but safe in HaCaT cell lines (normal cells).
Keywords: 5-Flurouracil, Gallic acid, Stearylamine, Skin cancer, Cytotoxicity, Synergism