科学家制成具超强抗癌活性药剂

gexiaom

New anti-cancer drug found effective

University of Illinois researchers said the new agent belongs to a class of drugs called bisphosphonates -- compounds originally developed to treat osteoporosis and other bone diseases.
Wednesday, March 25, 2009


(UPI) - A U.S.-led team of scientists says it has developed an anti-cancer agent that's about 200 times more effective than similar drugs used in recent studies.
University of Illinois researchers said the new agent belongs to a class of drugs called bisphosphonates -- compounds originally developed to treat osteoporosis and other bone diseases.

Previous studies found the bisphosphonate drug zoledronate, significantly reduced the recurrence of breast cancer in pre-menopausal women with estrogen-receptor-positive breast cancer. Similar results were reported previously for hormone-refractory prostate cancer.

The scientists, however, said zoledronate quickly binds to bone, reducing its efficacy in other tissues.

"We're trying to develop bisphosphonates that will be very active but won't bind to the bone, because if they bind to the bone they're not going to go to breast, lung or other tissues," said University of Illinois Professor Eric Oldfield, who led the new study.

The team subsequently developed a new compound, BPH-715, that proved especially potent in cell culture and effectively inhibited tumor cell growth and invasiveness. BPH-715 was 200 times more effective than zoledronate, the research indicated.

The researchers -- Andrew Wang of Academia Sinica in Taipei, Illinois chemists Rong Cao and Yonghui Zhang, Tadahiko Kubo of Japan's Hiroshima University and Socrates Papapoulos of Leiden University in the Netherlands -- report their findings in the Journal of the American Chemical Society.

科学家制成具超强抗癌活性药剂
一个由美国、荷兰、台湾和日本科学家组成的研究小组，近日制成了一种新的抗肿瘤化学制剂，其杀灭癌细胞的活性是新近临床实验所用类似药物的200倍左右。相关论文3月23日发表在《美国化学会志》（JACS）上。

药物研发人员多年来一直不断努力，想要设计药物来阻止癌细胞的存活路径。研究的重点集中在Ras蛋白，因为大约三分之一的人类癌症都包含Ras基因的突变，其导致细胞信号出错。不过这些努力收效甚微。

此次发现的化合物名为BPH-715，它属于双膦酸盐（bisphosphonate）。双膦酸盐最初是用来治疗骨质疏松症和其它骨病，但最近科学家发现，它们也具有抗癌和提升免疫的性能。

研究人员发现，BPH-715能够有效抑制肿瘤细胞的生长和入侵。小鼠实验显示，它能够杀灭癌细胞，而且与类似的双膦酸盐药物唑来磷酸（Zoledronate）不同，它对骨的化学亲和性很低，从而不会降低对其它组织的功效。

在人体中，类似BPH-715和唑来磷酸的化合物还具有额外的抗癌好处——它们刺激免疫细胞γδ-T细胞的增殖，帮助杀灭癌细胞。

此次研究领导者、美国伊力诺依大学化学教授Eric Oldfield说：“新药剂的活性大约是新近临床使用药物的200倍，这些临床药物的目的是激活γδ-T细胞和杀灭癌细胞。此外，在阻止小鼠体内的肿瘤进程方面，这些新药剂也比现有的双膦酸盐药物效果好。”