TY - JOUR A2 - Choi, song - hwan AU - Rachakhom, Wasitta AU - Banjerdpongchai, Ratana PY - 2020 DA - 2020/12/21 TI - effects of Calomelanone, a Dihydrochalcone Analogue, on Human Cancer Apoptosis/Regulated Cell Death in an Cancer在体外SP - 4926821 VL - 2020 AB - Calomelanone, 2 ,6 -dihydroxy-4 4 -二甲氧基二氢查尔酮,具有抗癌活性。本研究旨在探讨二氢查尔酮类似物卡美黑酮对人癌细胞的细胞毒性作用及其相关机制。采用MTT法测定甘美黑酮的细胞毒作用。Annexin V-FITC/碘化丙啶和DiOC6流式细胞术染色分别测定细胞死亡模式和线粒体跨膜电位(MTP)降低模式。用特定底物和比色法测定Caspase活性。免疫印迹法检测Bcl-2家族蛋白表达水平。用2 ,7 -二氢二氯荧光素二乙酸酯和二氢乙锭(荧光染料)。研究发现,calomelone对各种人类癌细胞有毒性,包括急性早幼粒细胞HL-60和单核细胞白血病U937细胞,在24 h时呈剂量依赖性,在48 h时对人肝细胞HepG2细胞有毒性。而HepG2细胞在24 h后增殖增加。Calomelanone通过诱导MTP破坏的内在途径诱导HL-60和U937细胞在24 h和HepG2细胞在48 h时凋亡。该化合物还能诱导caspase-3、caspase-8和caspase-9活性。Calomelanone上调HepG2细胞促凋亡蛋白Bax和Bak,下调抗凋亡蛋白Bcl-xL。此外,在HepG2细胞中,信号转导也与氧化应激有关。Calomelanone在处理24 h后诱导自噬,用单单尸胺(MDC)染色来代表自噬通量。这与Akt(生存途径)的减少和Atg5(自噬的标记物)的上调有关。因此,calomelanone诱导HL-60、U937和HepG2细胞凋亡/调控细胞死亡。 However, it also induced autophagy in HepG2 depending on duration, dose, and type of cells. Thus, calomelanone could be used as a potential anticancer agent for cancer treatment. Nevertheless, acute and chronic toxicity should be further investigated in animals before conducting investigations in human patients. SN - 2314-6133 UR - https://doi.org/10.1155/2020/4926821 DO - 10.1155/2020/4926821 JF - BioMed Research International PB - Hindawi KW - ER -