Nishizaki Tomoyuki, Kanno Takeshi, Tsuchiya Ayako, Kaku Yoshiko, Shimizu Tadashi, Tanaka Akito
Division of Bioinformation, Department of Physiology, Hyogo College of Medicine, 1-1 Mukogawa-cho, Nishinomiya 663-8501, Japan.
Laboratory of Chemical Biology, Advanced Medicinal Research Center, Hyogo University of Health Sciences, 1-3-6 Minatojima, Chuo-ku, Kobe 650-8530, Japan.
Molecules. 2014 Dec 19;19(12):21462-72. doi: 10.3390/molecules191221462.
We have originally synthesized the naftopidil analogue 1-[2-(2-methoxyphenylamino)ethylamino]-3-(naphthalene-1-yloxy)propan-2-ol (HUHS 1015) as a new anticancer drug. HUHS1015 induces cell death in a wide variety of human cancer cell lines originated from malignant pleural mesothelioma, lung cancer, hepatoma, gastric cancer, colorectal cancer, bladder cancer, prostate cancer, and renal cancer. HUHS1015-induced cell death includes necrosis (necroptosis) and apoptosis, and the underlying mechanism differs depending upon cancer cell types. HUHS1015 effectively suppresses tumor growth in mice inoculated with NCI-H2052, MKN45, or CW2 cells, with a potential similar to or higher than that of currently used anticancer drugs. Here we show how HUHS1015 might offer brilliant hope for cancer therapy.
我们最初合成了萘哌地尔类似物1-[2-(2-甲氧基苯氨基)乙氨基]-3-(萘-1-基氧基)丙-2-醇(HUHS 1015)作为一种新型抗癌药物。HUHS1015可诱导多种源自恶性胸膜间皮瘤、肺癌、肝癌、胃癌、结直肠癌、膀胱癌、前列腺癌和肾癌的人类癌细胞系发生细胞死亡。HUHS1015诱导的细胞死亡包括坏死(坏死性凋亡)和凋亡,其潜在机制因癌细胞类型而异。HUHS1015能有效抑制接种NCI-H2052、MKN45或CW2细胞的小鼠体内肿瘤生长,其潜力与目前使用的抗癌药物相似或更高。在此我们展示了HUHS1015如何可能为癌症治疗带来巨大希望。