Department of Pharmacognosy, "Victor Babeş" University of Medicine and Pharmacy, 2, Eftimie Murgu Square, 300041 Timişoara, Romania.
Pharmazentrum Frankfurt/ZAFES, Institute of General Pharmacology and Toxicology, Clinic of the Goethe University, D-60590 Frankfurt/Main, Germany.
Nutrients. 2019 Apr 16;11(4):858. doi: 10.3390/nu11040858.
Apigenin (4',5,7-trihydroxyflavone) (Api) is an important component of the human diet, being distributed in a wide number of fruits, vegetables and herbs with the most important sources being represented by chamomile, celery, celeriac and parsley. This study was designed for a comprehensive evaluation of Api as an antiproliferative, proapoptotic, antiangiogenic and immunomodulatory phytocompound. In the set experimental conditions, Api presents antiproliferative activity against the A375 human melanoma cell line, a G2/M arrest of the cell cycle and cytotoxic events as revealed by the lactate dehydrogenase release. Caspase 3 activity was inversely proportional to the Api tested doses, namely 30 μM and 60 μM. Phenomena of early apoptosis, late apoptosis and necrosis following incubation with Api were detected by Annexin V-PI double staining. The flavone interfered with the mitochondrial respiration by modulating both glycolytic and mitochondrial pathways for ATP production. The metabolic activity of human dendritic cells (DCs) under LPS-activation was clearly attenuated by stimulation with high concentrations of Api. Il-6 and IL-10 secretion was almost completely blocked while TNF alpha secretion was reduced by about 60%. Api elicited antiangiogenic properties in a dose-dependent manner. Both concentrations of Api influenced tumour cell growth and migration, inducing a limited tumour area inside the application ring, associated with a low number of capillaries.
芹菜素（4'，5，7-三羟基黄酮）（Api）是人类饮食中的重要组成部分，分布在许多水果、蔬菜和草药中，最重要的来源是甘菊、芹菜、块根芹和欧芹。本研究旨在全面评估 Api 作为一种抗增殖、促凋亡、抗血管生成和免疫调节植物化合物的作用。在设定的实验条件下，Api 对 A375 人黑色素瘤细胞系表现出抗增殖活性，导致细胞周期 G2/M 期阻滞和细胞毒性事件，如乳酸脱氢酶释放所揭示的那样。Caspase 3 活性与测试的 Api 剂量呈反比，即 30 μM 和 60 μM。用 Annexin V-PI 双重染色检测到 Api 孵育后早期凋亡、晚期凋亡和坏死现象。该黄酮通过调节糖酵解和线粒体途径来干扰线粒体呼吸以产生 ATP。高浓度 Api 刺激可明显减弱脂多糖激活下人树突状细胞（DC）的代谢活性。IL-6 和 IL-10 分泌几乎完全被阻断，而 TNF alpha 分泌减少约 60%。Api 以剂量依赖的方式表现出抗血管生成特性。两种浓度的 Api 均影响肿瘤细胞的生长和迁移，在应用环内诱导有限的肿瘤区域，与毛细血管数量少有关。
