新型酚类化合物对 MCF-7 乳腺癌细胞系的体外和体内抗癌活性研究。
Effectiveness and Anticancer Activity of a Novel Phenolic Compound from Against the MCF-7 Breast Cancer Cell Line in vitro and in silico.
机构信息
Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Padjadjaran, Jatinangor, 45363, West Java, Indonesia.
出版信息
Drug Des Devel Ther. 2021 Aug 12;15:3523-3533. doi: 10.2147/DDDT.S321824. eCollection 2021.
BACKGROUND
Cancer is a leading cause of death worldwide, with breast cancer being the most common invasive cancer type in women. Several therapeutic strategies have been explored to reduce the mortality rates of breast cancer. Chemotherapy is the most commonly used systemic treatment, but associated with numerous side-effects. Development of anticancer agents with high efficacy and minimal negative effects is therefore an important focus of research. Natural materials provide an excellent source of bioactive compounds. For instance, from the Clusiaceae family has multiple pharmacological activities, including antioxidant, anti-inflammatory, antibacterial, antiviral, anti-HIV, antidepressant, and anticancer properties.
PURPOSE
The main objective of this study was to investigate the potential anticancer effects of compounds extracted from the bark of .
MATERIALS AND METHODS
Our experiments were divided into three steps: (1) chromatographic isolation of compounds using various separation techniques, such as extraction, separation and purification, (2) characterization via infrared (IR), nuclear magnetic resonance (NMR) and mass spectroscopy, and (3) evaluation of anticancer activity in vitro (MTT assay) and in silico (via analysis of molecular docking against caspase-9, tumor necrosis factor alpha (TNF-α), estrogen receptor alpha (ER-α), and human epidermal growth factor receptor 2 (HER-2)).
RESULTS
Depsidone () and benzophenone () from the ethyl acetate extract of bark of were identified as bioactive components. Examination of the activities of these compounds against MCF-7 cells revealed an IC value of 119.3 µg/mL for benzophenone, whereas IC for depsidone could not be estimated. Benzophenone activity was lower than that of the positive control doxorubicin (6.9 µg/mL). Depsidone showed the highest binding affinity for HER-2 (-9.2 kcal.mol-1) and benzophenone for ER-α (-8.0 kcal.mol-1).
CONCLUSION
Benzophenone displays potency as an anticancer agent through blocking ER-α.
背景
癌症是全球主要的死亡原因，乳腺癌是女性最常见的侵袭性癌症类型。已经探索了几种治疗策略来降低乳腺癌的死亡率。化疗是最常用的全身性治疗方法，但伴随着许多副作用。因此，开发具有高疗效和最小副作用的抗癌药物是研究的重点。天然材料为生物活性化合物提供了极好的来源。例如，桃金娘科植物的叶子具有多种药理活性，包括抗氧化、抗炎、抗菌、抗病毒、抗 HIV、抗抑郁和抗癌作用。
目的
本研究的主要目的是研究从桃金娘科植物树皮中提取的化合物的潜在抗癌作用。
材料和方法
我们的实验分为三个步骤：（1）使用各种分离技术，如提取、分离和纯化，对化合物进行色谱分离；（2）通过红外（IR）、核磁共振（NMR）和质谱对其进行表征；（3）体外（通过 MTT 测定法）和体内（通过分析与 caspase-9、肿瘤坏死因子-α（TNF-α）、雌激素受体-α（ER-α）和人表皮生长因子受体 2（HER-2）的分子对接）评估抗癌活性。
结果
从桃金娘科植物树皮的乙酸乙酯提取物中鉴定出了漆酚（）和苯并二酮（）为生物活性成分。研究这些化合物对 MCF-7 细胞的活性发现，苯并二酮的 IC 值为 119.3 µg/mL，而漆酚的 IC 值无法估算。苯并二酮的活性低于阳性对照阿霉素（6.9 µg/mL）。漆酚对 HER-2 的结合亲和力最高（-9.2 kcal.mol-1），而苯并二酮对 ER-α 的结合亲和力最高（-8.0 kcal.mol-1）。
结论
苯并二酮通过阻断 ER-α显示出作为抗癌剂的潜力。
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