Abstract

Lichens represent an important resource for common traditional medicines due to their numerous metabolites that can exert diverse pharmacological activities including anticancer effects. To find new anticancer compounds with fewer side effects and low tumor resistance, a bioprospective study of Usnea barbata (L.) F.H. Wigg. (U. barbata), a lichen from the Călimani Mountains (Suceava county, Romania) was performed. The aim of this research was to investigate the anticancer potential, morphologic changes, wound healing property, clonogenesis, and oxidative stress biomarker status of four extracts of U. barbata in different solvents (methanol, ethanol, acetone, and ethyl acetate), and also of usnic acid (UA) as a positive control on the CAL-27 (ATCC® CRL-2095™) oral squamous carcinoma (OSCC) cell line and V79 (ATCC® CCL-93™) lung fibroblasts as normal cells. Using the MTT assay and according to IC50 values, it was found that the most potent anticancer property was displayed by acetone and ethyl acetate extracts. All U. barbata extracts determined morphological modifications (losing adhesion capacity, membrane shrinkage, formation of abnormal cellular wrinkles, and vacuolization) with higher intensity in tumor cells than in normal ones. The most intense anti-migration effect was established in the acetone extract treatment. The clonogenic assay showed that some U. barbata extracts decreased the ability of cancer cells to form colonies compared to untreated cells, suggesting a potential anti-tumorigenic property of the tested extracts. Therefore, all the U. barbata extracts manifest anticancer activity of different intensity, based, at least partially, on an imbalance in antioxidant defense mechanisms, causing oxidative stress.

Highlights

  • Nowadays, cancer still remains one of the most important causes of death, representing a challenge for the scientific community to search for new bioactive molecules that are effective and safe in the fight against this implacable disease of the contemporary world [1,2]

  • The novelty of our study consists in the evaluation anticancer properties evaluation of four autochthonous U. barbata dry extracts in various solvents and comparative analysis of the obtained results

  • Their activities were examined on the CAL-27 tongue squamous carcinoma cell line and V79 normal cells, noting the differentiated cytotoxicity, higher in tumor cells than in normal ones

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Summary

Introduction

Cancer still remains one of the most important causes of death, representing a challenge for the scientific community to search for new bioactive molecules that are effective and safe in the fight against this implacable disease of the contemporary world [1,2]. OSCC represents more than 90% of all oral neoplasms, which have as common sites of development the tongue, lips, and floor of the mouth. This type of neoplasm has a high mortality rate (5-year survival rate of around 50%) because numerous cases are diagnosed at a late stage of the disease [3]. The major purpose of current cancer therapy is to perturb or kill the malignant cells, from early stages neoplasms, or those remaining after surgery, without affecting the normal cytophysiological processes, and to trigger the immunity defense against the residual tumor cells. Finding new pharmacological agents with anticancer activity constitutes an essential concern of oncological research and medical practice to improve antitumor therapy effectiveness

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