Lomovsky A I, Baburina Y L, Fadeev R S, Kobyakova M I, Lomovskaya Ya V, Krestinin R R, Sotnikova L D, Krestinina O V
Institute of Theoretical and Experimental Biophysics, Pushchino, Moscow oblast, 142290 Russia.
Research Institute of Clinical and Experimental Lymphology-Branch of Institute of Cytology and Genetics, Siberian Branch, Russian Academy of Sciences, Novosibirsk, 630117 Russia.
Mol Biol (Mosk). 2024 Jan-Feb;58(1):141-153. doi: 10.31857/S0026898424010136.
Melatonin (N-acetyl-5-methoxytryptamine, MEL) is a hormone synthesized by the pineal gland. Due to its oncostatic effect, it can be considered as an antitumor agent and used for combination therapy. ABT-737, a Bcl-2 inhibitor, promotes cell death after treatment with agents that induce pro-apoptotic signals. In the present study, the combined effect of MEL and ABT-737 on changes in proliferative and mitotic activity, mitochondrial membrane potential, intracellular production of reactive oxygen species (ROS), and cytosolic Ca^(2+) was studied. Moreover, changes in the expression of anti- and pro-apoptotic proteins (Bcl-2 and Bax), autophagy markers (LC3A/B (I, II)), endoplasmic reticulum stress markers (chaperones BIP and PDI, CHOP) were studied under these conditions. The effect of MEL together with ABT-737 led to an increase in the level of cytosolic Ca^(2+), intracellular production of ROS and a decrease in the membrane potential of mitochondria. The content of Bcl-2 increased, while the level of Bax decreased. Activation of CHOP stimulated autophagy and led to a decrease in the synthesis of chaperones BIP and PDI. It is assumed that melatonin can enhance the effect of other chemotherapeutic agents and can be used in the treatment of tumors.
褪黑素(N-乙酰基-5-甲氧基色胺,MEL)是一种由松果体合成的激素。由于其抑癌作用,它可被视为一种抗肿瘤药物并用于联合治疗。ABT-737是一种Bcl-2抑制剂,在用诱导促凋亡信号的药物处理后可促进细胞死亡。在本研究中,研究了MEL和ABT-737联合对增殖和有丝分裂活性、线粒体膜电位、细胞内活性氧(ROS)产生以及胞质Ca^(2+)变化的影响。此外,还研究了在这些条件下抗凋亡和促凋亡蛋白(Bcl-2和Bax)、自噬标志物(LC3A/B(I、II))、内质网应激标志物(伴侣蛋白BIP和PDI、CHOP)表达的变化。MEL与ABT-737共同作用导致胞质Ca^(2+)水平升高、细胞内ROS产生增加以及线粒体膜电位降低。Bcl-2含量增加,而Bax水平降低。CHOP的激活刺激了自噬并导致伴侣蛋白BIP和PDI的合成减少。推测褪黑素可增强其他化疗药物的作用,并可用于肿瘤治疗。