Antiproliferative Effects of Cynara cardunculus L. var. altilis (DC) Lipophilic Extracts
authors Ramos, PAB; Guerra, AR; Guerreiro, O; Santos, SAO; Oliveira, H; Freire, CSR; Silvestre, AJD; Duarte, MF
nationality International
journal INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
author keywords Cynara cardunculus L. var. altilis (DC); lipophilic extracts; cynaropicrin; taraxasteryl acetate; triple-negative breast cancer MDA-MB-231 cell line; p21(Waf1/Cip1) upregulation; phospho(Tyr15)-CDK1 protein accumulation; phospho(Ser473)-Akt downregulation
keywords NEGATIVE BREAST-CANCER; SESQUITERPENE LACTONE; CELL-LINES; LEAF EXTRACT; SCOLYMUS L.; IN-VITRO; APOPTOSIS; INDUCTION; RISK; PARTHENOLIDE
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 mu g/mL) than to florets extract (IC50 315.22 mu g/mL), during 48 h. Moreover, leaves extract and cynaropicrin (IC50 6.19 mu g/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.
publisher MDPI AG
issn 1422-0067
year published 2017
volume 18
issue 1
digital object identifier (doi) 10.3390/ijms18010063
web of science category Biochemistry & Molecular Biology; Chemistry, Multidisciplinary
subject category Biochemistry & Molecular Biology; Chemistry
unique article identifier WOS:000393030600063
  ciceco authors
  impact metrics
times cited (wos core): 1
journal impact factor (jcr 2016): 3.226
5 year journal impact factor (jcr 2016): 3.482
category normalized journal impact factor percentile (jcr 2016): 63.693
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