Institute of Biomedical and Pharmaceutical Technology, Fuzhou University, Fuzhou, China.
Fujian Provincial Key Laboratory of Tumor Biotherapy, Fujian Cancer Hospital and Fujian Medical University Cancer Hospital, Fuzhou, China.
J Antibiot (Tokyo). 2019 Jan;72(1):34-44. doi: 10.1038/s41429-018-0104-5. Epub 2018 Sep 27.
4,4'-bond secalonic acid D (4,4'-SAD) is a known compound isolated from the marine-derived fungus Penicillium oxalicum. No study about the antitumor effect of this compound has been reported, except for a few focusing on its bactericidal properties. Herein, we performed an in vitro biology test and found that 4,4'-SAD stimulated the apoptosis of tumor cells in the human hepatocellular carcinoma cell lines PLC/PRF/5 and HuH-7 by activating caspase-3, caspase-8, caspase-9, PARP, p53, and cyclin B1, as well as by regulating the Bax/Bcl-2 ratio. In vivo studies showed that 4,4'-SAD had antitumor efficacy in H22 cell xenograft model. Immunohistochemical analysis revealed that 4,4'-SAD could regulate Bax expression, which is a biomarker of tumor growth. In summary, 4,4'-SAD significantly inhibited tumor growth both in vivo and in vitro.
4,4'-联噻唑酸 D（4,4'-SAD）是一种从海洋来源的青霉属真菌Penicillium oxalicum 中分离得到的已知化合物。除了少数关注其杀菌特性的研究外，尚未有关于该化合物抗肿瘤作用的报道。在此，我们进行了体外生物学试验，发现 4,4'-SAD 通过激活 caspase-3、caspase-8、caspase-9、PARP、p53 和 cyclin B1，以及调节 Bax/Bcl-2 比值，刺激人肝癌细胞系 PLC/PRF/5 和 HuH-7 中的肿瘤细胞凋亡。体内研究表明，4,4'-SAD 在 H22 细胞移植瘤模型中具有抗肿瘤功效。免疫组织化学分析显示，4,4'-SAD 可以调节 Bax 表达，Bax 是肿瘤生长的生物标志物。总之，4,4'-SAD 显著抑制了体内和体外的肿瘤生长。
