Abstract
Besides being traditionally used to relieve hepatobiliary disorders, Cynara cardunculus L. has evidenced anticancer potential on triple-negative breast cancer (TNBC). This study highlights the antiproliferative effects of lipophilic extracts from C. cardunculus L. var. altilis (DC) leaves and florets, and of their major compounds, namely cynaropicrin and taraxasteryl acetate, against MDA-MB-231 cells. Our results demonstrated that MDA-MB-231 cells were much less resistant to leaves extract (IC50 10.39 µg/mL) than to florets extract (IC50 315.22 µg/mL), during 48 h. Moreover, leaves extract and cynaropicrin (IC50 6.19 µg/mL) suppressed MDA-MB-231 cells colonies formation, via an anchorage-independent growth assay. Leaves extract and cynaropicrin were also assessed regarding their regulation on caspase-3 activity, by using a spectrophotometric assay, and expression levels of G2/mitosis checkpoint and Akt signaling pathway proteins, by Western blotting. Leaves extract increased caspase-3 activity, while cynaropicrin did not affect it. Additionally, they caused p21Waf1/Cip1 upregulation, as well as cyclin B1 and phospho(Tyr15)-CDK1 accumulation, which may be related to G2 cell cycle arrest. They also downregulated phospho(Ser473)-Akt, without changing total Akt1 level. Cynaropicrin probably contributed to leaves extract antiproliferative action. These promising insights suggest that cultivated cardoon leaves lipophilic extract and cynaropicrin may be considered toward a natural-based therapeutic approach on TNBC.
Highlights
Breast cancer represents the most prevalent cancer among women, and one of the most frequent causes of female cancer death [1]
Considering the preliminary insights of Triple-negative breast cancer (TNBC) antiproliferative potential exhibited by cultivated cardoon extracts [15,22], we determined the IC50 values of cultivated cardoon leaves and florets lipophilic extracts, upon MDA-MB-231 cellular viability after 48 h, via MTT assay (Table 1)
The present study demonstrates important data about the in vitro antiproliferative potential of
Summary
Breast cancer represents the most prevalent cancer among women, and one of the most frequent causes of female cancer death [1]. Triple-negative breast cancer (TNBC) is characterized by estrogen receptor (ER) and progesterone receptor (PR) negative, and lack of human epidermal growth factor receptor type 2 overexpression, accounting for 10%–20% of breast cancer cases. Targeted therapy was not found for TNBC [2]. The most common chemotherapy lies on primary anthracycline and anthracycline/taxane derivatives, which generally is not efficient since it carries high relapse risk during the first three years after treatment, and high incidence of metastases in the liver, central nervous system, and lungs [3]. The development of new TNBC therapeutic strategies, as preventive.
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