Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036, Rende, CS, Italy.
Department of Agraria, University "Mediterranea" of Reggio Calabria, Località Feo di Vito, 89122, Reggio Calabria, Italy.
Biomed Pharmacother. 2018 Nov;107:967-978. doi: 10.1016/j.biopha.2018.08.090. Epub 2018 Aug 23.
The bioactivities of Santolina corsica Jord. & Fourr. n-hexane (EHS) and methanol (EMS) extracts were evaluated in relation to their chemical profile.
EHS and EMS were analysed by gas chromatography-mass spectrometry () and high performance liquid chromatography-diode array detection (HPLC-DAD), respectively. Antioxidant activity was determined by β-carotene bleaching, Ferric Reducing Activity Power (FRAP), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) tests. Nitric oxide (NO) production was assessed in LPS-stimulated RAW 264.7 cells. Anti-proliferative activity was evaluated by MTT assay on A549, HeLa, PC3, MCF-7, MDA-MB-231 cancer cells, and non-tumorigenic MCF10 A cells. Cell motility, migration and invasion were assessed by wound-healing scratch, migration and invasion assays, respectively. DNA fragmentation was tested by TUNEL assay. Cells morphology was studied by phase-contrast microscopy. Procaspase-8, -9, poly (ADP-ribose) polymerase and COX-2 expression levels were evaluated by immunoblotting analysis.
Kaempferol-3-O-glucoside (5878.67 mg/100 g of extract), chlorogenic acid (746.11 mg/100 g), and rosmarinic acid (550.16 mg/100 g) were the dominant EMS constituents. EHS showed myrcene (18.86%) as the main compound, followed by palmitic acid methyl and ethyl esters (9.35 and 9.16%, respectively), β-phellandrene (8.48%), and ar-curcumene (5.63%). Both extracts showed promising anti-proliferative activity on all tested cancer cells, without inducing cytotoxicity in non-tumorigenic cells MCF-10 A. Moreover, extracts inhibited motility, migration, and invasion of MDA-MB-231 cells, inducing apoptosis. EHS decreased NO production, showing anti-inflammatory activity.
S. corsica extracts might be potentially useful in cancer treatment, since reduce invasive and migratory potential of MDA-MB-231 cells triggering apoptosis.
评估 Santolina corsica Jord. & Fourr. 正己烷（EHS）和甲醇（EMS）提取物的生物活性与其化学特征的关系。
通过气相色谱-质谱联用仪（GC-MS）和高效液相色谱-二极管阵列检测（HPLC-DAD）分别对 EHS 和 EMS 进行分析。通过β-胡萝卜素漂白、铁还原能力（FRAP）、2,2-二苯基-1-苦基肼（DPPH）和 2,2'-联氮-双-3-乙基苯并噻唑啉-6-磺酸（ABTS）试验测定抗氧化活性。通过 LPS 刺激的 RAW 264.7 细胞测定一氧化氮（NO）的产生。通过 MTT 试验评估对 A549、HeLa、PC3、MCF-7、MDA-MB-231 癌细胞和非致瘤性 MCF10A 细胞的抗增殖活性。通过划痕愈合试验、迁移和侵袭试验分别评估细胞迁移、迁移和侵袭能力。通过 TUNEL 试验检测 DNA 片段化。通过相差显微镜观察细胞形态。通过免疫印迹分析评估 procaspase-8、-9、多聚（ADP-核糖）聚合酶和 COX-2 的表达水平。
芹糖苷-3-O-葡萄糖苷（5878.67mg/100g 提取物）、绿原酸（746.11mg/100g）和迷迭香酸（550.16mg/100g）是 EMS 的主要成分。EHS 以薄荷烯（18.86%）为主要化合物，其次是棕榈酸甲酯和乙酯（9.35%和 9.16%）、β-水芹烯（8.48%）和α-姜黄烯（5.63%）。两种提取物均对所有测试的癌细胞表现出有希望的抗增殖活性，而对非致瘤性 MCF10A 细胞没有诱导细胞毒性。此外，提取物抑制 MDA-MB-231 细胞的运动、迁移和侵袭，诱导细胞凋亡。EHS 降低了 NO 的产生，具有抗炎活性。
S. corsica 提取物可能在癌症治疗中具有潜在的用途，因为它降低了 MDA-MB-231 细胞的侵袭和迁移潜力，从而触发细胞凋亡。
