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).
Highlights
Skin cancer is a tumour formed from the uncontrolled growth of abnormal skin cells
Successful conjugation of Gallic acid (GA) with stearylamine was confirmed with FTIR spectra, as shown in Figure 2 (KBr pellet, cm−1): 3365 -NH stretching, 1708 -C=0 stretching
The cytotoxicity data for the test compounds (5-FU and GA–SA conjugate) in A431 cell line are shown in Table 1, Table 2 and Figure 5
Summary
Skin cancer is a tumour formed from the uncontrolled growth of abnormal skin cells. It has a multifactorial aetiology involving genetic alterations, environmental factors, and lifestyle factors. 5-Fluorouracil (5-FU) is an anticancer drug that suppresses the activity of thymidylate synthetase. The anticancer efficacy of the combination of the test compounds (5-FU and the GA–SA conjugate) was evaluated using A431 cell line and was determined based on the percentage cytotoxicity of the test compounds. The cytotoxic activities of the test compounds (5FU and the GA–SA conjugate) were evaluated against A431 human squamous carcinoma cell line. The effect of the test compounds on cell viability was determined by MTT assay. In this assay, 20 μL of 5 mg/mL MTT was added to each wells, and the wells were incubated at 37 °C for 3 h. The safety of the test compounds (5-FU and the GA–SA conjugate) was screened using HaCaT human immortalised keratinocyte cell line.
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