Lima E Silva Magalli C B, Bogo Danielle, Alexandrino Caroline A F, Perdomo Renata T, Figueiredo Patrícia de O, do Prado Pamela R, Garcez Fernanda R, Kadri Monica C T, Ximenes Thalita V N, Guimarães Rita de Cassia A, Sarmento Ulana C, Macedo Maria Lígia R
1 Molecular Biology and Cell Culture Laboratory, School of Pharmaceutical Sciences, Foods and Nutrition (FACFAN), Federal University of Mato Grosso do Sul (UFMS) , Campo Grande, Brazil .
2 Laboratory of Pronabio (Bioactive Natural Products)-Chemistry Institute, Federal University of Mato Grosso do Sul , Campo Grande, Brazil .
J Med Food. 2018 Oct;21(10):1024-1034. doi: 10.1089/jmf.2018.0001. Epub 2018 May 1.
Campomanesia adamantium, a native species of the Brazilian Cerrado, is characterized as a natural source of phenolic compounds and has known potential anticancer activities. This study aimed to evaluate the chemical profile of dichloromethane extracts of pulp (DEGPU) and peel (DEGPE) from the fruits of C. adamantium and to identify compounds with antiproliferative effects in vitro against melanoma cells by sulforhodamine B (SRB) assay, apoptosis induction assay, caspase-3 activation assay, nitric oxide (NO) release in coculture of B16-F10 cells and murine peritoneal macrophages. The chemical profiles of DEGPU and DEGPE were analyzed by high performance liquid chromatography coupled to diode array detector and mass spectrometer using the electrospray ionization interface (HPLC-DAD-ESI-MS/MS). Thirteen compounds were identified in both extracts and the chromatographic study of the most active extract in SRB assay DEGPU (GI of 16.17 μg/mL) resulted in the isolation of seven compounds. The isolated compound dimethylchalcone (DMC) had the highest antiproliferative activity against B16-F10 with a GI of 7.11 μg/mL. DEGPU extract activated caspase-3 in 29% of cells at 25 μg/mL and caused a 50% decrease in NO release in coculture. DEGPU can be characterized as a source of bioactive compounds such as DMC, as seen from its antiproliferative effect in vitro by inducing B16-F10 cells to undergo apoptosis, essential feature in the search for new anticancer drugs.
金刚番樱桃是巴西塞拉多地区的本土物种，其特点是富含酚类化合物，具有潜在的抗癌活性。本研究旨在评估金刚番樱桃果实果肉二氯甲烷提取物（DEGPU）和果皮二氯甲烷提取物（DEGPE）的化学组成，并通过磺酰罗丹明B（SRB）法、凋亡诱导试验、半胱天冬酶-3激活试验、B16-F10细胞与小鼠腹腔巨噬细胞共培养体系中一氧化氮（NO）释放试验，鉴定体外对黑色素瘤细胞具有抗增殖作用的化合物。采用高效液相色谱-二极管阵列检测器-质谱联用仪（HPLC-DAD-ESI-MS/MS），以电喷雾电离接口分析DEGPU和DEGPE的化学组成。在两种提取物中均鉴定出13种化合物，对SRB试验中活性最高的提取物DEGPU（GI为16.17μg/mL）进行色谱研究，分离出7种化合物。分离得到的化合物二甲基查耳酮（DMC）对B16-F10细胞的抗增殖活性最高，GI为7.11μg/mL。DEGPU提取物在25μg/mL时可使29%的细胞激活半胱天冬酶-3，并使共培养体系中的NO释放量降低50%。从DEGPU通过诱导B16-F10细胞凋亡而产生的体外抗增殖作用可以看出，它可被视为生物活性化合物如DMC的来源，这是寻找新型抗癌药物的重要特征。
