School of Dentistry, Chung Shang Medical University, Taichung, Taiwan, ROC.
Anticancer Res. 2012 Jul;32(7):2735-45.
The study of the anticancer effects of destruxin B (DB) is rare and its anticancer mechanism remains unknown. The aim of this study was to test the in vitro and in vivo anticancer effects of DB, on human HT-29 colorectal cancer (CRC).
DB was isolated and characterized by high pressure liquid chromatography, electrospray ionization mass spectrometry and (1)H-nuclear magnetic resonance spectroscopy. (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to assess the effects of DB on HT-29 cells in vitro. The anticancer effects of DB were investigated in a murine xenograft model of human colon cancer.
A significant inhibition of cell viability was observed with DB treatment in time- and dose-dependent manners. DB administered subcutaneously daily at 0.6-15 mg/kg was proven to be safe and effective in inhibiting the growth of CRC cells. Expression of Bax, cleaved poly (ADP-ribose) polymerase and active caspase-3 were observed with DB treatment and the increase in tumor volumes of treated groups were significantly (p<0.05) lower than those of the mock-treated group.
DB has potential as a new therapeutic agent against human CRC.
关于破坏素 B（DB）的抗癌作用的研究很少，其抗癌机制尚不清楚。本研究旨在测试 DB 对人 HT-29 结肠直肠癌（CRC）的体外和体内抗癌作用。
通过高压液相色谱、电喷雾电离质谱和（1）H-核磁共振波谱对 DB 进行分离和表征。（3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四唑溴化盐（MTT）测定法用于评估 DB 对 HT-29 细胞的体外影响。在人结肠癌的小鼠异种移植模型中研究了 DB 的抗癌作用。
DB 处理呈时间和剂量依赖性显著抑制细胞活力。证明 DB 以 0.6-15mg/kg 的剂量每天皮下给药可安全有效地抑制 CRC 细胞的生长。用 DB 处理后观察到 Bax、切割的多聚（ADP-核糖）聚合酶和活性半胱天冬酶-3 的表达，并且治疗组的肿瘤体积增加明显低于（p<0.05）模拟处理组。
DB 具有作为治疗人类 CRC 的新治疗剂的潜力。
