Abstract
Afzelin demonstrates anti-inflammatory and anti-cancer properties. Our purpose was to assess its influence on apoptosis, Bax, caspases, MUC1, cancer-related carbohydrate antigens, enzymes participating in their formation, and galectin-3 in AGS gastric cancer cells. A total of 60 and 120 μM afzelin was used in all experiments. Flow cytometry was applied to determine apoptotic response. Western blotting and RT PCR were used to detect the expression of mentioned factors. Flavonoid at higher concentration revealed slight apoptotic respond. Bax, caspase-3, -8, -9 increased upon afzelin action. Stimulatory effect of the flavonoid on MUC1 cytoplasmic tail and extracellular domain in cell lysates and on MUC1 gene was revealed. MUC1 release into the culture medium was inhibited by the flavonoid. The 60 μM afzelin dose stimulated GalNAcTL5 protein expression and inhibited C1GalT1. ST6GalNAcT mRNA was inhibited by both flavonoid doses. ST3GalT was inhibited by 120 μM afzelin on protein and mRNA level. Lewisa/b protein was reduced by both afzelin concentrations. FUT3 and FUT4 mRNA was inhibited by 120 μM dose of afzelin. Galectin-3 protein increased in cell lysates and decreased in culture supernatant by 60 and 120 μM flavonoid. Galectin-3 gene expression was stimulated by two used concentrations of afzelin in comparison to control. We conclude that afzelin can be considered as the potential anti-cancer agent, supporting conventional cancer treatment.
Highlights
Gastric cancer (GC) is one of the most common malignancies and leading cause of cancer-related death worldwide
Viability of the cells was 70–100% compared with the control cells without afzelin cells
After 24 h of incubation with afzelin, we revealed significant induction of apoptosis upon 120 μM concentration of the flavonoid, 8% of early apoptotic cells versus 4.3% in upon 120 μM concentration of the flavonoid, 8% of early apoptotic cells versus 4.3% in untreated control (Figure 3)
Summary
Gastric cancer (GC) is one of the most common malignancies and leading cause of cancer-related death worldwide. Due to a lack of specific signs of early gastric cancer, most patients are diagnosed too late and at advanced stages, with overall poor prognosis [1]. Looking for new therapeutic strategies, e.g., utilizing anti-tumour products with natural compounds with low by-effects, seems to be very reasonable. Medicinal plants are a major origin of potentially therapeutic molecules. Afzelin (kaempherol-3-rhamnoside), a flavonoid found, e.g., in Nymphaea odorata, is one of such compounds (Figure 1). It was reported to inhibit the growth of breast cancer cells by stimulating apoptosis [2], suppress cell proliferation in prostate cell lines [3], and demonstrated anti-inflammatory properties [4]
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