Antitumor agent-78 具有抗肿瘤活性，能抑制癌细胞的生长和迁移。Antitumor agent-78 通过抑制 GPX-4 和升高 COX2 引发铁下垂 (Ferroptosis)。Antitumor agent-78 还能激活肿瘤细胞固有凋亡通路 (Bax-BCL-2-Caspase-3)，阻碍肿瘤细胞上皮间质转化 (EMT) 过程。

Antitumor agent-78 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-78 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-78 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells [1].

Antitumor agent-78 (compound 2b) (30 μM; 4 h) exhibits good liposoluble and improved cellular uptake in A549 cancer cells [1]. Antitumor agent-78 (20 μM; 36 h) produces cytotoxicity by inducing apoptosis of A549 cancer cells [1]. Antitumor agent-78 (20 μM; 24 h) results in significant down-regulation of Bcl-2 and upregulation of Bax, also leads to E-cadherin increase, Vimentin decrease [1]. Antitumor agent-78 (20 μM; 24 h) arrests cell cycle at S phase and G2/M phase [1]. Antitumor agent-78 (10 μM; 12 h) inhibits cells migration with inhibition rate of 53% [1]. Apoptosis Analysis [1] Cell Line: A549 cells Concentration: 20 μM Incubation Time: 36 hours Result: Resulte cell apopsotsis with average apoptotic values (including both early and late apoptotic states which were displayed in Q1-LR and Q1-UR, respectively) of 35.86%. Western Blot Analysis [1] Cell Line: A549 cells Concentration: 20 μM Incubation Time: 24 hours Result: Elevated the level of cleaved caspase-3 and reduced the level of caspase-3 in A549 cells. Decreased anti-apoptotic protein Bcl-2 and increased pro-apoptotic protein Bax. Elevated the expression of E-cadherin and on the other hand, lowered the protein level of Vimentin. Cell Cycle Analysis [1] Cell Line: A549 cells Concentration: 20 μM Incubation Time: 24 hours Result: Blocked cell cycle progression in S and G2/M phase with the values of 24.91% and 22.21%, respectively.

Antitumor agent-78 (compound 2b) (6 μg/kg; i.v.; injected on day 8, 10, 12) displays better potential antitumor activity than Oxaliplatin, without significant damage to kidney and liver as well as weight loss [1]. Animal Model: A549 xenograft models in mouse [1] Dosage: 6 μg/kg Administration: Intravenous injection; administration on day 8, 10, 12 after establishing xenograft models (A549 cells; s.c.) Result: Significantly repressed tumor growth, and maintained normal kidney and liver architecture in mice.

T63768

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