scholarly journals Synergistic anti-cancer activity of combined 5-fuorouracil and gallic acid-stearylamine conjugate in A431 human squamous carcinoma cell line

2021 ◽  
Vol 18 (3) ◽  
pp. 471-477
Author(s):  
R. Rajagopalan ◽  
Sanjay K. Jain ◽  
Piyush Trivedi

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).

1991 ◽  
Vol 16 ◽  
pp. 82
Author(s):  
Hidehiko Yoshida ◽  
Shuji Hasegawa ◽  
Hiroshi Kuromi ◽  
Hideki Tanzawa ◽  
Kikuo Takahashi ◽  
...  

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Piyawat Tangsuksan ◽  
Jureeporn Chuerduangphui ◽  
Chutha Takahashi Yupanqui ◽  
Teerapol Srichana ◽  
Ekarat Hitakomate ◽  
...  

Abstract Background Oral cancer is often preceded by a mucosal lesion called an oral potentially malignant disorder (OPMD). Many plant-derived compounds are of value in medicine. The objectives of this study were to develop a soluble mucoadhesive film containing α-mangostin (α-MG), a compound extracted from the peel of mangosteen fruit, and determine its activities against oral cancer cells, against human papillomavirus type 16 (HPV-16) pseudovirus, and its anti-inflammatory properties. Methods A soluble mucoadhesive film containing α-MG was prepared. Oral squamous carcinoma cell line (SCC25), murine macrophage cells (RAW264.7), and human gingival fibroblast cell line were cultured. Anticancer activity and viability of SCC25 cells in response to α-MG film solution were determined by MTT assay. HPV-16 pseudovirus was constructed and effects of the film solution on attachment and post-attachment steps of the infection were investigated. Anti-inflammatory activity was assessed by nitric oxide (NO) inhibition. Fibroblast cell migration was determined by in vitro scratch assay. Results The soluble α-MG film showed cytotoxic effects on SCC25 cells in concentration > 125 µg/ml with IC50 of 152.5 µg/ml. Antiviral activity against HPV-16 pseudovirus was observed at attachment step, but not at post-attachment step. The film also possessed a strong anti-inflammatory effect and promoted wound healing without cytotoxicity. Conclusions Mucoadhesive film containing α-MG has a cytotoxic effect on oral squamous carcinoma cell line and an inhibitory effect on HPV-16 pseudovirus at attachment step. The α-MG film also shows a potent anti-inflammatory activity and enhances wound healing. Thus, the soluble α-MG film may have a potential role in treating oral cancer.


INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (06) ◽  
pp. 49-59
Author(s):  
Priyambada Kshiroda Nandini Sarangi ◽  
Jyotirmaya Sahoo ◽  
Chita Ranjan Sahoo ◽  
Sudhir Kumar Paidesetty ◽  
Guru Prasad Mohanta

A series of eight quinoline-thiazole hybrid-bearing diazenylsulfonamides, 4a-4h, were synthesized and characterized by UV-Vis, FT/IR, 1H NMR and lC-MS. These compounds were formed when two prepared intermediate precursors of Schiff-base compounds, (E)-N-((2-chloroquinolin-3-yl)methylene)-4phenylthiazol-2-amine (3a) and (E)-N-((2-chloroquinolin-3-yl)methylene)-4-chlorophenylthiazol-2-amine (3b) were converted to the corresponding diazenyl compounds 4a-4h by treating and coupling with the individual diazonium salts of sulfa-drugs. The results of in vitro cytotoxic activity of the synthesized compounds in two cancer cell lines MCF 7 (human breast cancer cell line) and K562 (myelogenousleukemia cell line) have shown the IC50 values as given: 4b against MCF 7 19.52 and against K562 20.55µM; 4d against MCF 7 15.96 and against K562 13.05µM. Moreover, the compound 4-(((Z)-(2-chloroquinolin-3yl)(4-phenylthiazol-2-ylimino)methyl)diazenyl)benzenesulfonic acid (4d) induced maximum percentage of apoptosis. Furthermore, the in vitro antioxidant activity study revealed that among all the synthesized compounds, compound 4d has an excellent radical scavenging effect. Molecular docking was additionally performed to investigate the binding affinity of H-bonding interaction of synthesized compounds with a targeted enzyme and to compare it with the anticancer drugs, dasatinib, bosutinib and dacarbazine.


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