Abstract
Colorectal cancer is a leading cause of death worldwide and occurs through the highly complex coordination of multiple cellular pathways, resulting in carcinogenesis. Recent studies have increasingly revealed that constituents of lichen extracts exhibit potent pharmaceutical activities, including anticancer activity against various cancer cells, making them promising candidates for new anticancer therapeutic drugs. The main objective of this study was to evaluate the anticancer capacities of ramalin, a secondary metabolite from the Antarctic lichen Ramalina terebrata, in the human colorectal cancer cell line HCT116. In this study, ramalin displayed concentration-dependent anticancer activity against HCT116 cells, significantly suppressing proliferation and inducing apoptosis. Furthermore, ramalin induced cell cycle arrest in the gap 2/mitosis (G2/M) phase through the modulation of hallmark genes involved in the G2/M phase transition, such as tumour protein p53 (TP53), cyclin-dependent kinase inhibitor 1A (CDKN1A), cyclin-dependent kinase 1 (CDK1) and cyclin B1 (CCNB1). At both the transcriptional and translational level, ramalin caused a gradual increase in the expression of TP53 and its downstream gene CDKN1A, while decreasing the expression of CDK1 and CCNB1 in a concentration-dependent manner. In addition, ramalin significantly inhibited the migration and invasion of colorectal cancer cells in a concentration-dependent manner. Taken together, these data suggest that ramalin may be a therapeutic candidate for the targeted therapy of colorectal cancer.
Highlights
Colon cancer is one of the leading causes of morbidity and mortality, and is the third most common cancer in both men and women worldwide
Recent studies have shown that ramalin, a secondary metabolite derived from the Antarctic lichen Ramalina terebrata (Figure 1), has significant antioxidant and anti-inflammatory activities [17,18]
To determine if ramalin colorectal cancer cells, wewe performed a cell proliferation assay in HCT116 cells, with different concentrations of ramalin (0, 12.5, 25, 50 and 100 μg/mL)
Summary
Colon cancer is one of the leading causes of morbidity and mortality, and is the third most common cancer in both men and women worldwide. One of the hallmarks of cancer is that abnormal cancer cells can penetrate into adjacent parts of the body and spread to other organs, in a process called metastasis [1]. In terms of patient survival, metastatic colorectal cancer has a very poor prognosis compared to other cancers. Approximately 20–25% of patients with colorectal cancer have progressed to metastasis at the time of diagnosis, and approximately 50% of all patients. Molecules 2017, 22, 1361 with colorectal cancer eventually develop metastatic cancers [2]. An urgent need exists for agents that can treat colon cancer and prevent its metastasis
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